TW202120487A - Fused heterocyclic compounds and their use as pest control agents - Google Patents

Fused heterocyclic compounds and their use as pest control agents Download PDF

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TW202120487A
TW202120487A TW109128488A TW109128488A TW202120487A TW 202120487 A TW202120487 A TW 202120487A TW 109128488 A TW109128488 A TW 109128488A TW 109128488 A TW109128488 A TW 109128488A TW 202120487 A TW202120487 A TW 202120487A
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trifluoromethyl
ethylsulfonyl
pyridin
phthalazine
oxo
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TW109128488A
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加甘 庫克雷賈
拉利特 庫瑪 吉納
蘇芮許 庫瑪 蘇薩
桑迪 亞修克 卡佩
維拉 辛
羅希特 薩克斯納
維什瓦納斯 加迪
瓊妮 庫瑪
拉維庫瑪 蘇雅娜拉雅娜 薩拉古爾
亞歷山大Gm 克勞森納
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印度商皮埃企業有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Abstract

The present invention discloses a fused heterocyclic compound of formula (I),
Figure 109128488-A0101-11-0001-2
wherein, R1 , G1 , G2 , G3 , G4 , A1 , A2 , Q, n and Z are as defined in the detailed description. The present invention further discloses methods for their preparation and use of the compounds of formula (I) as a pest control agent.

Description

稠合雜環化合物及其作為害蟲防治劑的用途Condensed heterocyclic compound and its use as pest control agent

本發明涉及稠合的雜環化合物。更具體地,本發明涉及式(I)的稠合雜環化合物及其製備方法。本發明進一步涉及式(I)的稠合雜環化合物作為害蟲防治劑的用途。The present invention relates to fused heterocyclic compounds. More specifically, the present invention relates to a fused heterocyclic compound of formula (I) and a preparation method thereof. The present invention further relates to the use of the fused heterocyclic compound of formula (I) as a pest control agent.

當前可獲得的現代殺蟲劑和殺蟎劑必須滿足在有效量、殘留活性、活性譜和效果以及它們的可能用途等諸多方面的要求。在過去的幾十年裡,人們努力開發能發揮生物化學作用模式(目前只在昆蟲或蟎蟲體內出現)的,而且還顯示出比已知殺蟲劑更優越的特性的針對性的殺蟲劑。The currently available modern insecticides and acaricides must meet the requirements of many aspects such as effective amount, residual activity, activity spectrum and effect, and their possible uses. In the past few decades, people have worked hard to develop targeted insecticides that can exert a biochemical mode of action (currently only present in insects or mites) and also show superior properties than known insecticides. .

具有殺蟲活性的雜環化合物是已知的,例如在WO2019131575、WO2019131587、WO201913273、WO201908115、WO2018206348、WO2018202494、WO2018197315、WO2018141954、WO2018008727、WO2017055185和WO2016125621中有所描述。Heterocyclic compounds with insecticidal activity are known, for example, described in WO2019131575, WO2019131587, WO201913273, WO201908115, WO2018206348, WO2018202494, WO2018197315, WO2018141954, WO2018008727, WO2017055185 and WO2016125621.

但是,通過長期使用這種殺蟲劑,許多害蟲獲得了抗藥性,所以通過已經多年使用的現有殺蟲劑和殺菌劑進行有效控制變得越來越困難,並且這種現像在最近幾年越來越嚴重。此外,這些現有殺蟲劑中的某些具有高毒性,或由於其殘留特性而在環境中保留很長時間,這可能會造成生態系統的破壞,成為一個日益嚴重的問題。However, through long-term use of this insecticide, many pests have acquired resistance, so effective control by existing insecticides and fungicides that have been used for many years has become more and more difficult, and this phenomenon has become increasingly It's getting worse. In addition, some of these existing pesticides are highly toxic or remain in the environment for a long time due to their residual characteristics, which may cause damage to the ecosystem and become an increasingly serious problem.

因此,持續需要更有效、毒性更低、對環境更安全和/或具有不同作用方式的新化合物。Therefore, there is a continuing need for new compounds that are more effective, less toxic, safer to the environment, and/or have different modes of action.

鑑於上述情況,本發明設想了滿足或克服與現有技術有關的缺點的此類化合物。In view of the foregoing, the present invention contemplates such compounds that meet or overcome the disadvantages related to the prior art.

令人驚訝的是,現已發現某些含硫取代基的新型殺蟲活性稠合雜環化合物具有理想的殺蟲性能。Surprisingly, it has been discovered that certain new insecticidal active fused heterocyclic compounds with sulfur-containing substituents have ideal insecticidal properties.

因此,本發明提供了式(I)的稠合雜環化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物。

Figure 02_image001
式(I) 其中,R1 、G1 、G2 、G3 、G4 、A1 、A2 、Q、n和Z如詳細描述中所定義。Therefore, the present invention provides the fused heterocyclic compound of formula (I) or its agriculturally acceptable salt, isomer/structural isomer, stereoisomer, diastereomer, enantiomer Forms, tautomers, metal complexes, polymorphs or N-oxides.
Figure 02_image001
Formula (I) wherein R 1 , G 1 , G 2 , G 3 , G 4 , A 1 , A 2 , Q, n, and Z are as defined in the detailed description.

在一個實施方案中,本發明提供了一種製備式(I)化合物或其農業上可接受的鹽的方法。In one embodiment, the present invention provides a method for preparing a compound of formula (I) or an agriculturally acceptable salt thereof.

在另一個實施方案中,本發明提供了用於控製或預防無脊椎動物害蟲的組合物,其包含生物學有效量的式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物以及至少一種選自表面活性劑和助劑的其他組分。In another embodiment, the present invention provides a composition for controlling or preventing invertebrate pests, which comprises a biologically effective amount of a compound of formula (I) or an agriculturally acceptable salt, isomer/structure thereof Isomers, stereoisomers, diastereomers, enantiomers, tautomers, metal complexes, polymorphs or N-oxides and at least one selected from surfactants and Other components of the adjuvant.

在另一個實施方案中,組合物還包含至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物農藥、除草劑、植物生長調節劑、抗生素、肥料或營養素的至少一種生物活性和相容性化合物。In another embodiment, the composition further comprises at least one biological agent selected from the group consisting of suicide fungicides, insecticides, nematicides, acaricides, biological pesticides, herbicides, plant growth regulators, antibiotics, fertilizers or nutrients. Active and compatible compounds.

在另一實施方案中,本發明提供了式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映體、對映體、互變異構體、金屬絡合物、多晶型物或N-氧化物、其組合物或組合用於防治農作物和/或園藝作物中的無脊椎動物害蟲或動物寄生蟲的用途。In another embodiment, the present invention provides compounds of formula (I) or agriculturally acceptable salts, isomers/structural isomers, stereoisomers, diastereomers, enantiomers, tautomers Structures, metal complexes, polymorphs or N-oxides, combinations or combinations thereof are used to control invertebrate pests or animal parasites in crops and/or horticultural crops.

在又一實施方案中,本發明提供了一種防治無脊椎動物害蟲的方法,包括使用生物有效量的式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映體、對映體、互變異構體、金屬絡合物、多晶型物或N-氧化物、其組合物或組合接觸無脊椎動物害蟲、其棲息地、繁殖地、食物、植物、種子、土壤、無脊椎動物害蟲生長或可能生長的區域、材料或環境,或希望免受蟲害或侵擾的材料、植物、種子、土壤、表面或空間。In yet another embodiment, the present invention provides a method for controlling invertebrate pests, comprising using a biologically effective amount of a compound of formula (I) or an agriculturally acceptable salt, isomer/structural isomer, stereo Isomers, diastereomers, enantiomers, tautomers, metal complexes, polymorphs or N-oxides, their compositions or combinations contact invertebrate pests, their habitats, and breeding grounds , Food, plant, seed, soil, area, material or environment where invertebrate pests grow or may grow, or material, plant, seed, soil, surface or space where it is desired to be protected from pests or infestations.

本發明詳細描述 定義Detailed description of the invention definition

本發明中所提供的術語定義僅用於說明目的,絕不限制本發明公開的本發明的範圍。The term definitions provided in the present invention are only for illustrative purposes, and in no way limit the scope of the present invention disclosed by the present invention.

本文所用的“包含”、“包括”、“具有”、“擁有”、“以...為特徵”或其任何其他變體旨在涵蓋非排他性包含,但須受明確指明的除外。例如,組合、混合、過程或方法包含的要素表的不一定局限於這些要素,但可以包括沒有明確列出的該組合、混合、步驟或方法固有的其他要素。As used herein, "include", "include", "have", "have", "characterized by" or any other variations thereof are intended to cover non-exclusive inclusions, unless explicitly indicated. For example, the element table included in the combination, mixture, process, or method is not necessarily limited to these elements, but may include other elements inherent to the combination, mixture, step, or method that are not explicitly listed.

過渡詞“由...組成”排除任何未指定的元素、步驟或成分。如果在請求項中(除了通常與之相關的雜項之外),這樣的請求項將包含除所述材料之外的材料。當“由…組成”一詞出現在請求項正文的一個條款中,而不是緊接在序言之後時,它只限制該條款所規定的要素;其他因素也未從整個請求項中排除。The transition word "consisting of" excludes any unspecified elements, steps or ingredients. If it is in a request (in addition to the miscellaneous items normally associated with it), such a request will contain materials other than those mentioned. When the word "consisting of" appears in a clause in the body of the claim, rather than immediately after the preamble, it only restricts the elements specified in the clause; other factors are not excluded from the entire claim.

過渡詞“基本上由...組成”用於定義包括材料、步驟、特徵、成分或要素的組合物或方法,條件是這些附加材料、步驟、特徵、成分或要素不實質上影響請求項保護的發明的基本要素和新穎特徵。術語“基本上由......組成”佔據“包含”和“由......組成”之間的中間地帶。The transition term "consisting essentially of" is used to define a composition or method that includes materials, steps, features, ingredients or elements, provided that these additional materials, steps, features, ingredients or elements do not materially affect the protection of the claim The basic elements and novel features of the invention. The term "consisting essentially of" occupies the middle ground between "comprising" and "consisting of".

此外,除非有相反的明確說明,否則“或”是指包含性的“或”而不是排他性的“或”。例如,條件A“或”B滿足以下任何一個:A為真(或存在)且B為假(或不存在),A為假(或不存在)且B為真(或現在),A和B都為真(或存在)。In addition, unless expressly stated to the contrary, "or" refers to an inclusive "or" rather than an exclusive "or". For example, the condition A "or" B satisfies any one of the following: A is true (or exists) and B is false (or does not exist), A is false (or does not exist) and B is true (or present), A and B All are true (or exist).

此外,在本發明的要素或成分之前的不定冠詞“a”和“an”不限制該要素或成分的實例(即出現次數)的數量。因此,“a”或“an”應該被理解為包括一個或至少一個,並且要素或成分的單數單詞形式也包括複數,除非該數明顯是單數的。In addition, the indefinite articles "a" and "an" before an element or ingredient of the present invention do not limit the number of instances (ie, the number of occurrences) of the element or ingredient. Therefore, "a" or "an" should be understood to include one or at least one, and the singular word form of an element or component also includes the plural unless the number is clearly singular.

如本發明所述,術語“無脊椎動物害蟲”包括作為具有經濟重要性害蟲的節肢動物、腹足動物和線蟲。術語“節肢動物”包括昆蟲、蟎蟲、蜘蛛、蠍子、蜈蚣、千足蟲、藥蟲和甲蟲。術語“腹足類”一詞包括蝸牛、蛞蝓和其他莖突蟲。“線蟲”一詞是指線蟲門的活生物體。術語“蠕蟲”包括蛔蟲、犬絲蟲、植食性線蟲、吸蟲、棘頭蟲和絛蟲。As described in the present invention, the term "invertebrate pests" includes arthropods, gastropods, and nematodes that are economically important pests. The term "arthropod" includes insects, mites, spiders, scorpions, centipedes, millipedes, medicinal insects, and beetles. The term "gastropod" includes snails, slugs and other styloid worms. The term "nematode" refers to living organisms of the phylum Nematode. The term "worm" includes roundworms, canine filarials, phytophagous nematodes, trematodes, acanthocephalans, and tapeworms.

術語“農業學的”一詞是指農作物如食物和纖維的生產,包括種植玉米、大豆和其他豆類、大米、穀物(如小麥、燕麥、大麥、黑麥、水稻、玉米)、綠葉蔬菜(如生菜、捲心菜和其他油菜作物)、果實蔬菜(如番茄、胡椒、茄子、十字花科植物和葫蘆)、土豆、紅薯、葡萄、棉花、樹木果實(如梨果和柑橘),小水果(草莓、櫻桃)和其他特種作物(如油菜、向日葵、橄欖)。The term "agricultural" refers to the production of crops such as food and fiber, including the cultivation of corn, soybeans and other legumes, rice, grains (such as wheat, oats, barley, rye, rice, corn), green leafy vegetables (such as Lettuce, cabbage and other rape crops), fruit vegetables (such as tomatoes, peppers, eggplants, cruciferous plants and gourds), potatoes, sweet potatoes, grapes, cotton, tree fruits (such as pears and citrus), small fruits (strawberries, Cherries) and other special crops (such as rape, sunflower, olives).

術語“非農學的”一詞指的非農作物,例如園藝作物(例如,花房、苗圃或不在田間生長的觀賞植物)、住宅、農業、商業和工業結構、草皮(例如,草皮農場、牧場、高爾夫球場、草坪、運動場等)、木製品、儲藏物、農林業和植被管理、公共衛生(即人類)和動物健康(例如寵物、牲畜和家禽等馴養動物,野生動物等非馴養動物)應用。The term "non-agricultural" refers to non-agricultural crops, such as horticultural crops (for example, flower houses, nurseries or ornamental plants that do not grow in the field), residential, agricultural, commercial and industrial structures, turf (for example, turf farms, pastures, golf Fields, lawns, sports fields, etc.), wood products, storage, agroforestry and vegetation management, public health (ie humans) and animal health (such as pets, livestock and poultry and other domesticated animals, wild animals and other non-domesticated animals) applications.

非農學應用包括通過向要保護的動物施用殺寄生蟲有效量(即生物學上有效)的本發明化合物(通常以配製用於獸醫用途的組合物形式)來保護動物免受無脊椎寄生蟲的侵害。本公開和請求項中所提及的術語“殺寄生蟲的”和“寄生殺蟲地”是指為保護動物免受害蟲的侵害對無脊椎寄生蟲害的可觀察到的效果。寄生殺蟲效果通常與減少目標無脊椎動物寄生蟲的出現或活動有關。對害蟲的這種效果包括壞死、死亡、生長遲緩、活動性降低或在宿主動物身體或身上的寄宿能力降低、進食減少和對繁殖的抑制。這些對無脊椎動物寄生蟲的影響可防治(包括預防、減少或消除)動物免受寄生蟲的侵擾或感染。Non-agricultural applications include the protection of animals from invertebrate parasites by administering to the animal to be protected a parasiticidal effective amount (ie, biologically effective) of the compound of the invention (usually in the form of a composition formulated for veterinary use) Infringe. The terms "parasite-killing" and "parasitic pesticidal site" mentioned in the present disclosure and claims refer to the observable effects on invertebrate parasites in order to protect animals from pests. The parasitic insecticidal effect is usually related to reducing the appearance or activity of target invertebrate parasites. This effect on pests includes necrosis, death, growth retardation, reduced mobility or reduced lodging ability on the host animal's body or body, reduced feeding, and inhibition of reproduction. These effects on invertebrate parasites can prevent (including preventing, reducing or eliminating) animals from infestation or infection by parasites.

本發明的化合物可以以純的形式或作為不同可能的異構形式的混合物存在,例如立體異構體或結構異構體。 各種立體異構體包括對映異構體、非對映異構體、手性異構體、阻轉異構體、構象異構體、旋轉異構體、互變異構體、光學異構體、多晶型物和幾何異構體。這些異構體的任何所需混合物都屬於本發明的請求項的範圍。本領域技術人員將理解,當相對於其他異構體富集時或當與其他異構體分離時,一種立體異構體可以更具活性和/或可以表現出有益效果。另外,本領域技術人員知道分離、富集和/或選擇性製備所述異構體的過程或方法或技術。The compounds of the invention may exist in pure form or as a mixture of different possible isomeric forms, such as stereoisomers or structural isomers. Various stereoisomers including enantiomers, diastereomers, chiral isomers, atropisomers, conformational isomers, rotamers, tautomers, optical isomers , Polymorphs and geometric isomers. Any desired mixtures of these isomers fall within the scope of the claims of the present invention. Those skilled in the art will understand that one stereoisomer may be more active and/or may exhibit beneficial effects when enriched relative to other isomers or when separated from other isomers. In addition, those skilled in the art know processes or methods or techniques for separating, enriching and/or selectively preparing the isomers.

現就本說明中使用的各種術語的含義給予說明。The meanings of various terms used in this description are now explained.

本文中使用的術語“脂肪族化合物”或“脂肪族基團”是其碳原子以直鏈、支鏈或非芳香環連接的有機化合物。The term "aliphatic compound" or "aliphatic group" as used herein is an organic compound whose carbon atoms are connected in a straight chain, a branched chain, or a non-aromatic ring.

術語“烷基”(獨立使用或在“烷基硫”或“鹵代烷基”或-N(烷基)或烷基羰基烷基或烷基磺醯胺基等複合詞中使用),包括直鏈或支鏈C1 到C24 烷基,優選C1 到C15 烷基,優選C1 到C10 烷基,更優選C1 到C6 烷基。烷基的非限制性例子包括甲基、乙基、丙基、1-甲基乙基、1-甲基乙基、戊基、1-甲基丁基、1-甲基丁基、2-甲基丁基、2-甲基丙基、1-甲基戊基、1-甲基戊基、1-甲基戊基、2-甲基戊基、3-甲基戊基、4-甲基戊基、1,1-二甲基丁基、1,2-二甲基丁基、2,3-二甲基丁基、3,3-二甲基丁基、1-乙基丁基、2-乙基丁基、1,1,2-三甲基丙基、1,2,2-三甲基丙基,1-乙基1-甲基丙基和l-乙基2-甲基丙基或不同異構體。如果烷基在複合取代基的末端,例如,在烷基環烷基中,起始的複合取代基的部分,例如環烷基,可以以相同或不同方式且獨立地被烷基單取代或多取代。這同樣適用於其他自由基如烯基、烷基、羥基、鹵素、羰基、羰基氧基等位於末端的複合取代基。The term "alkyl" (used independently or in compound words such as "alkylsulfide" or "haloalkyl" or -N (alkyl) or alkylcarbonylalkyl or alkylsulfonamide) includes straight chain or Branched C 1 to C 24 alkyl, preferably C 1 to C 15 alkyl, preferably C 1 to C 10 alkyl, more preferably C 1 to C 6 alkyl. Non-limiting examples of alkyl groups include methyl, ethyl, propyl, 1-methylethyl, 1-methylethyl, pentyl, 1-methylbutyl, 1-methylbutyl, 2- Methylbutyl, 2-methylpropyl, 1-methylpentyl, 1-methylpentyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methyl Pentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl , 2-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl and 1-ethyl-2-methyl Group propyl or different isomers. If the alkyl group is at the end of a compound substituent, for example, in an alkylcycloalkyl group, the part of the initial compound substituent, such as a cycloalkyl group, may be mono- or multiple-substituted by the alkyl group in the same or different ways and independently replace. The same applies to other radicals such as alkenyl, alkyl, hydroxyl, halogen, carbonyl, carbonyloxy and other compound substituents at the end.

術語“烯基”(獨立使用或在複合詞中使用),包括直鏈或C2 到C24 烯烴、優選C2 到C15 烯烴、更優選C2 到C10 烯烴、更優選C2 到C6 烯烴的支鏈。烯烴的非限制性例子包括乙烯基、1-丙烯基、2-丙烯基、1-丁烯基、2-丁烯基、1-甲基-1-丙烯基、2-甲基-2-丙烯基、2-甲基-1-丁烯基、1-甲基-1-丁烯基、2-甲基-1-丁烯基、3-甲基-2-丁烯基、3-甲基-3-丁烯基、2-甲基-3-丁烯基、3-甲基-3-丁烯基、1-1-二甲-2-丁烯基、1,2-二甲基-2-丙烯、1-乙基-1-丙烯、1-乙基-2-丙烯、1-乙基-2-戊烯、3-甲基-1-戊烯、2-甲基-1-戊烯、3-甲基-2-戊烯、3-甲基-2-戊烯、3-甲基-3-戊烯、3-甲基-3-戊烯、4-甲基-4-戊烯、3-甲基-4-戊烯、3-甲基-4-戊烯、1,1-二甲基-2-丁烯基、l,l-二甲基-3-丁烯基、1,2-二甲基-2-丁烯基、1,2-二甲基-3-丁烯基、1,3-二甲基-3-丁烯基、2,3-二甲基-3-丁烯基、2,3-二甲基-3-丁烯基、2,3-二甲基-3-丁烯基、3,3-二甲基-3-丁烯基、1-乙基-1-丁烯基、1-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、2-乙基-2-丁烯基、1-乙基-2-丁烯基、l-乙基-2-甲基-l-丙烯和l-乙基-2-甲基-2-丙烯及其異構體。烯烴也包括多烯,如1,2-丙二烯和2,4-己二烯。除非在其他地方有明確的定義,這個定義也適用於烯烴作為複合取代基的一部分,例如鹵代烯烴等。The term "alkenyl" (used independently or in compound words) includes linear or C 2 to C 24 olefins, preferably C 2 to C 15 olefins, more preferably C 2 to C 10 olefins, more preferably C 2 to C 6 Alkene branching. Non-limiting examples of olefins include vinyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 1-methyl-1-propenyl, 2-methyl-2-propene Group, 2-methyl-1-butenyl, 1-methyl-1-butenyl, 2-methyl-1-butenyl, 3-methyl-2-butenyl, 3-methyl -3-butenyl, 2-methyl-3-butenyl, 3-methyl-3-butenyl, 1-1-dimethyl-2-butenyl, 1,2-dimethyl- 2-propene, 1-ethyl-1-propene, 1-ethyl-2-propene, 1-ethyl-2-pentene, 3-methyl-1-pentene, 2-methyl-1-pentene Ene, 3-methyl-2-pentene, 3-methyl-2-pentene, 3-methyl-3-pentene, 3-methyl-3-pentene, 4-methyl-4-pentene Ene, 3-methyl-4-pentene, 3-methyl-4-pentene, 1,1-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-Dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl-3-butenyl, 2,3-dimethyl- 3-butenyl, 2,3-dimethyl-3-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-3-butenyl, 1- Ethyl-1-butenyl, 1-ethyl-2-butenyl, 2-ethyl-2-butenyl, 2-ethyl-2-butenyl, 2-ethyl-2-butenyl Alkenyl, 2-ethyl-2-butenyl, 2-ethyl-2-butenyl, 1-ethyl-2-butenyl, 1-ethyl-2-methyl-1-propene and l-Ethyl-2-methyl-2-propene and its isomers. Olefins also include polyenes such as 1,2-propadiene and 2,4-hexadiene. Unless there is a clear definition elsewhere, this definition also applies to olefins as part of a composite substituent, such as halogenated olefins.

術語“炔基”(單獨使用或在複合詞中使用)包括支鏈或直鏈C2 到C24 炔烴、優選C2 到C15 炔烴、更優選C2 到C10 炔烴、最優選C2 到C6 炔烴。炔的非限制性例子包括乙炔基、1-丙炔基、2-丙炔基、1-丁炔基、2-丁炔基、3-丁炔基、1-甲基-2-丙炔基、1-戊炔基、2-戊炔基、3-戊炔基,4-戊炔基、1-甲基-2-丁炔基、1-甲基-3-丁炔基、2-甲基-3-丁炔基、3-甲基-1-丁炔基、1,1-二甲基-2-丙炔基、1-乙基-2-丙炔基、1-己炔基、2-己炔基、3-己炔基、4-己炔基、5-己炔基、1-甲基-2-戊炔基、1-甲基-3-戊炔基、1-甲基-4-戊炔基、2-甲基-3-戊炔基、2-甲基-4-戊炔基、3-甲基-1-戊炔基、3-甲基-4-戊炔基、4-甲基-1-戊炔基、4-甲基-2-戊炔基、1,1-二甲基-2-丁炔基、1,1-二甲基-3-丁炔基、1,2-二甲基-3-丁炔基、2,2-二甲基-3-丁炔基、3,3-二甲基-1-丁炔基、1-乙基-2-丁炔基、1-乙基-3-丁炔基、2-乙基-3-丁炔基和1-乙基-1-甲基-2-丙炔基和不同的異構體。除非在別處具體限定,否則定義也適用於作為複合取代基的一部分的炔基,例如鹵代炔基等。術語“炔基”還可包括由多個三鍵組成的部分,例如2,5-己二炔基。The term "alkynyl" (used alone or in compound words) includes branched or straight chain C 2 to C 24 alkynes, preferably C 2 to C 15 alkynes, more preferably C 2 to C 10 alkynes, most preferably C 2 to C 6 alkynes. Non-limiting examples of alkynes include ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1-methyl-2-propynyl , 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-methyl-2-butynyl, 1-methyl-3-butynyl, 2-methyl 3-butynyl, 3-methyl-1-butynyl, 1,1-dimethyl-2-propynyl, 1-ethyl-2-propynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 1-methyl -4-pentynyl, 2-methyl-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-1-pentynyl, 3-methyl-4-pentynyl , 4-methyl-1-pentynyl, 4-methyl-2-pentynyl, 1,1-dimethyl-2-butynyl, 1,1-dimethyl-3-butynyl , 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 3,3-dimethyl-1-butynyl, 1-ethyl-2- Butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl and 1-ethyl-1-methyl-2-propynyl and different isomers. Unless specifically defined elsewhere, the definition also applies to alkynyl groups that are part of a composite substituent, such as haloalkynyl groups and the like. The term "alkynyl" may also include moieties composed of multiple triple bonds, such as 2,5-hexadiynyl.

“環烷基”是指閉合形成環的烷基。非限制性實例包括但不限於環丙基、環丁基、環戊基和環己基。除非在別處明確限定,否則該定義也適用於作為複合取代基的一部分的環烷基,例如環烷基烷基等。"Cycloalkyl" refers to an alkyl group that is closed to form a ring. Non-limiting examples include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. Unless specifically defined elsewhere, this definition also applies to cycloalkyl groups that are part of a composite substituent, such as cycloalkylalkyl groups and the like.

“環烯基”是指烯基封閉形成環,包括單環、部分不飽和的烴基。非限制性實例包括但不限於環戊烯基和環己烯基。除非在別處明確限定,否則該定義也適用於作為複合取代基的一部分的環烯基,例如環烯基烷基等。"Cycloalkenyl" means an alkenyl group is closed to form a ring, including monocyclic, partially unsaturated hydrocarbon groups. Non-limiting examples include, but are not limited to, cyclopentenyl and cyclohexenyl. Unless specifically defined elsewhere, this definition also applies to cycloalkenyl groups that are part of a composite substituent, such as cycloalkenylalkyl and the like.

“環炔基”是指炔基封閉形成環,包括單環、部分不飽和的基團。除非在別處具體限定,否則該定義也適用於作為複合取代基的一部分的環炔基,例如環炔基烷基等。"Cycloalkynyl" refers to an alkynyl group closed to form a ring, including monocyclic, partially unsaturated groups. Unless specifically defined elsewhere, this definition also applies to cycloalkynyl groups that are part of a composite substituent, such as cycloalkynylalkyl and the like.

“環烷氧基”、“環烯氧基”等類似詞具有類似的定義。環烷氧基的非限制性實例包括環丙氧基,環戊氧基和環己氧基。除非在別處明確限定,否則該定義也適用於環烷氧基作為複合取代基的一部分,例如環烷氧基烷基等。Similar words such as "cycloalkoxy" and "cycloalkenyloxy" have similar definitions. Non-limiting examples of cycloalkoxy groups include cyclopropoxy, cyclopentyloxy and cyclohexyloxy. Unless specifically defined elsewhere, this definition also applies to cycloalkoxy as part of a composite substituent, such as cycloalkoxyalkyl and the like.

“鹵素”(獨立或以複合詞如“鹵代烷基”)包括氟、氯、溴或碘。此外,當用於諸如“鹵代烷基”的複合詞時,所述烷基可以部分或完全被鹵素原子取代,所述鹵素原子可以相同或不同。“鹵代烷基”的非限制性實例包括氯甲基、溴甲基、二氯甲基、三氯甲基、氟甲基、二氟甲基、三氟甲基、氯氟甲基、二氯氟甲基、氯二氟甲基、1-氯乙基、1-溴乙基、1-氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氯-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯-2-氟乙基、2,2,2-三氯乙基、五氟乙基、1,1,2-二氟乙基-二氯-2,2,2-三氟乙基和1,1,1-三氟丙-2-基。除非在別處明確限定,否則這個定義也適用於鹵代烷基作為複合取代基的一部分,例如鹵代烷基氨基烷基等。"Halogen" (independently or in compound words such as "haloalkyl") includes fluorine, chlorine, bromine or iodine. In addition, when used in compound words such as "haloalkyl", the alkyl group may be partially or completely substituted with halogen atoms, and the halogen atoms may be the same or different. Non-limiting examples of "haloalkyl" include chloromethyl, bromomethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl, trifluoromethyl, chlorofluoromethyl, dichlorofluoromethyl Methyl, chlorodifluoromethyl, 1-chloroethyl, 1-bromoethyl, 1-fluoroethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoro Ethyl, 2-chloro-2-fluoroethyl, 2-chloro-2,2-difluoroethyl, 2,2-dichloro-2-fluoroethyl, 2,2,2-trichloroethyl, Pentafluoroethyl, 1,1,2-difluoroethyl-dichloro-2,2,2-trifluoroethyl and 1,1,1-trifluoroprop-2-yl. Unless specifically defined elsewhere, this definition also applies to haloalkyl as part of a composite substituent, such as haloalkylaminoalkyl and the like.

“鹵代烯基”和“鹵代炔基”的定義類似,不同的是烯基和炔基代替烷基作為取代基的一部分存在。The definitions of "haloalkenyl" and "haloalkynyl" are similar, except that alkenyl and alkynyl are present as part of the substituent instead of alkyl.

“鹵代烷氧基”是指直鏈或支鏈烷氧基,其中這些基團中的一些或所有氫原子可以被如上所述的鹵素原子取代。鹵代烷氧基的非限制性實例包括氯甲氧基、溴甲氧基、二氯甲氧基、三氯甲氧基、氟甲氧基、二氟甲氧基、三氟甲氧基、氯氟甲氧基、二氯氟甲氧基、氯二氟甲氧基、1-氯乙氧基、1-溴乙氧基、1-氟乙氧基、2-氟乙氧基、2,2-二氟乙氧基、2,2,2-三氟乙氧基、2-氯-2-氟乙氧基、2-氯-2,2-二氟乙氧基、2,2-二氯-2-氟乙氧基、2,2,2-三氯乙氧基、五氟乙氧基和1,1,1-三氟丙-2-氧基。除非在別處明確限定,否則該定義也適用於鹵代烷氧基作為複合取代基的一部分的基團,例如鹵代烷氧基烷基等。"Haloalkoxy" refers to a straight or branched chain alkoxy group in which some or all of the hydrogen atoms in these groups may be replaced by halogen atoms as described above. Non-limiting examples of halogenated alkoxy groups include chloromethoxy, bromomethoxy, dichloromethoxy, trichloromethoxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, chlorofluoro Methoxy, dichlorofluoromethoxy, chlorodifluoromethoxy, 1-chloroethoxy, 1-bromoethoxy, 1-fluoroethoxy, 2-fluoroethoxy, 2,2- Difluoroethoxy, 2,2,2-trifluoroethoxy, 2-chloro-2-fluoroethoxy, 2-chloro-2,2-difluoroethoxy, 2,2-dichloro- 2-fluoroethoxy, 2,2,2-trichloroethoxy, pentafluoroethoxy and 1,1,1-trifluoroprop-2-oxy. Unless specifically defined elsewhere, this definition also applies to groups with haloalkoxy as part of a composite substituent, such as haloalkoxyalkyl and the like.

術語“鹵代烷硫基”是指直鏈或支鏈烷硫基團,其中這些基團中至少一個至多所有氫原子可被如上所述的鹵素原子取代。鹵代烷硫基的非限制性實例包括氯甲硫基、碘甲硫基、溴甲硫基、二氯甲硫基、三氯甲硫基、氟甲硫基、二氟甲硫基、三氟甲硫基、氯氟甲硫基、二氯氟甲硫基、氯二氟甲硫基、1-氯乙硫基、1-溴乙硫基、1-氟乙硫基、2-氟乙硫基、2,2-二氟乙硫基、2,2,2-三氟乙硫基、2-氯-2-氟乙硫基、2-氯-2,2-二氟乙硫基、2,2-二氯-2-氟乙硫基、2,2,2-三氯乙硫基、五氟乙硫基和1,1,1-三氟-2-基硫基。除非在別處明確限定、否則該定義也適用於鹵代烷硫基作為複合取代基的一部分的基團,例如鹵代烷硫基烷基等。The term "haloalkylthio" refers to straight-chain or branched alkylthio groups in which at least one and at most all hydrogen atoms in these groups can be replaced by halogen atoms as described above. Non-limiting examples of haloalkylthio groups include chloromethylthio, iodomethylthio, bromomethylthio, dichloromethylthio, trichloromethylthio, fluoromethylthio, difluoromethylthio, trifluoromethyl Sulfuryl, chlorofluoromethylthio, dichlorofluoromethylthio, chlorodifluoromethylthio, 1-chloroethylthio, 1-bromoethylthio, 1-fluoroethylthio, 2-fluoroethylthio , 2,2-Difluoroethylthio, 2,2,2-trifluoroethylthio, 2-chloro-2-fluoroethylthio, 2-chloro-2,2-difluoroethylthio, 2, 2-Dichloro-2-fluoroethylthio, 2,2,2-trichloroethylthio, pentafluoroethylthio and 1,1,1-trifluoro-2-ylthio. Unless specifically defined elsewhere, this definition also applies to groups with haloalkylthio as part of a composite substituent, such as haloalkylthioalkyl and the like.

“鹵代烷基亞磺醯基”的實例包括CF3 S(O)、CCl3 S(O)、CF3 CH2 S(O)。“鹵代烷基磺醯基”的非限制性實例包括CF3 S(O)2 、CCl3 S(O)2 、CF3 CH2 S(O)2 和CF3 CF2 S(O)2Examples of "haloalkylsulfinyl" include CF 3 S(O), CCl 3 S(O), CF 3 CH 2 S(O). Non-limiting examples of "haloalkylsulfonyl" include CF 3 S(O) 2 , CCl 3 S(O) 2 , CF 3 CH 2 S(O) 2 and CF 3 CF 2 S(O) 2 .

術語“羥基”表示-OH,氨基表示-NRR,其中R可以是H或任何可能的取代基,例如烷基。羰基表示-C(O)-,羰基氧基表示-OC(O)-,亞磺醯基表示SO,磺醯基表示S(O)2The term "hydroxy" means -OH, and amino means -NRR, where R can be H or any possible substituent, such as an alkyl group. The carbonyl group represents -C(O)-, the carbonyloxy group represents -OC(O)-, the sulfinyl group represents SO, and the sulfonyl group represents S(O) 2 .

術語“烷氧基”(單獨使用或以複合詞的形式使用)包括C1 至C24 烷氧基,優選C1 至C15 烷氧基,更優選C1 至C10 烷氧基,最優選C1 至C6 烷氧基。烷氧基的實例包括甲氧基、乙氧基、丙氧基、1-甲基乙氧基、丁氧基、1-甲基丙氧基、2-甲基丙氧基、1,1-二甲基乙氧基、戊氧基、1-甲基丁氧基、2-甲基丁氧基、3-甲基丁氧基、2,2-二甲基丙氧基、1-乙基丙氧基、己氧基、1,1-二甲基丙氧基、1,2-二甲基丙氧基、1-甲基戊氧基、2-甲基戊氧基、3-甲基戊氧基、4-甲基戊氧基、1,1-二甲基丁氧基、1,2-二甲基丁氧基、1,3-二甲基丁氧基、2,2-二甲基丁氧基、2,3-二甲基丁氧基、3,3-二甲基丁氧基、1-乙基丁氧基、2-乙基丁氧基、1,1,2-三甲基丙氧基、1,2,2-三甲基丙氧基、1-乙基-1-甲基丙氧基和1-乙基-2-甲基丙氧基和不同的異構體。除非在別處具體限定,否則該定義也適用於烷氧基作為複合取代基的一部分,例如鹵代烷氧基、炔基烷氧基等。The term "alkoxy" (used alone or as a compound word) includes C 1 to C 24 alkoxy, preferably C 1 to C 15 alkoxy, more preferably C 1 to C 10 alkoxy, most preferably C 1 to C 6 alkoxy. Examples of alkoxy groups include methoxy, ethoxy, propoxy, 1-methylethoxy, butoxy, 1-methylpropoxy, 2-methylpropoxy, 1,1- Dimethylethoxy, pentoxy, 1-methylbutoxy, 2-methylbutoxy, 3-methylbutoxy, 2,2-dimethylpropoxy, 1-ethyl Propoxy, hexyloxy, 1,1-dimethylpropoxy, 1,2-dimethylpropoxy, 1-methylpentyloxy, 2-methylpentyloxy, 3-methyl Pentyloxy, 4-methylpentyloxy, 1,1-dimethylbutoxy, 1,2-dimethylbutoxy, 1,3-dimethylbutoxy, 2,2-di Methylbutoxy, 2,3-dimethylbutoxy, 3,3-dimethylbutoxy, 1-ethylbutoxy, 2-ethylbutoxy, 1,1,2- Trimethylpropoxy, 1,2,2-trimethylpropoxy, 1-ethyl-1-methylpropoxy and 1-ethyl-2-methylpropoxy and different isomers body. Unless specifically defined elsewhere, this definition also applies to alkoxy groups as part of a composite substituent, such as halogenated alkoxy groups, alkynyl alkoxy groups, and the like.

術語“烷氧基烷基”表示烷基被烷氧基取代。“烷氧基烷基”的非限制性實例包括CH3 OCH2 、CH3 OCH2 CH2 、CH3 CH2 OCH2 、CH3 CH2 CH2 CH2 OCH2 和CH3 CH2 OCH2 CH2The term "alkoxyalkyl" means that an alkyl group is substituted by an alkoxy group. Non-limiting examples of "alkoxyalkyl" include CH 3 OCH 2 , CH 3 OCH 2 CH 2 , CH 3 CH 2 OCH 2 , CH 3 CH 2 CH 2 CH 2 OCH 2 and CH 3 CH 2 OCH 2 CH 2 .

術語“烷氧基烷氧基”表示烷氧基被烷氧基取代。The term "alkoxyalkoxy" means that an alkoxy group is substituted by an alkoxy group.

術語“烷硫基”包括支鏈或直鏈烷硫基基團,例如甲硫基、乙硫基、丙硫基、1-甲硫基硫基、丁硫基、1-甲基丙硫基、2-甲基丙硫基、1,1-二甲基乙硫基、戊硫基、1-甲基丁硫基、2-甲基丁硫基、3-甲基丁硫基、2,2-二甲基丙硫基、1-乙基丙硫基、己硫基、1,1-二甲基丙硫基、1,2-二甲基丙硫基、1-甲基戊硫基、2-甲基戊硫基、3-甲基戊硫基、4-甲基戊硫基、1,1-二甲基丁硫基 1,2-二甲基丁硫基、1,3-二甲基丁硫基、2,2-二甲基丁硫基、2,3-二甲基丁硫基、3,3-二甲基丁硫基、1-乙基丁硫基、2-乙基丁硫基、1,1,2-三甲基丙硫基、1,2,2-二甲基丁硫基、2-三甲基丙硫基、1-乙基-1-甲基丙硫基和1-乙基-2-甲基丙硫基以及不同的異構體。The term "alkylthio" includes branched or straight chain alkylthio groups, such as methylthio, ethylthio, propylthio, 1-methylthio, butylthio, 1-methylpropylthio , 2-methylpropylthio, 1,1-dimethylethylthio, pentylthio, 1-methylbutylthio, 2-methylbutylthio, 3-methylbutylthio, 2, 2-Dimethylpropylthio, 1-ethylpropylthio, hexylthio, 1,1-dimethylpropylthio, 1,2-dimethylpropylthio, 1-methylpentylthio , 2-Methylpentylthio, 3-methylpentylthio, 4-methylpentylthio, 1,1-dimethylbutylthio, 1,2-dimethylbutylthio, 1,3- Dimethylbutylthio, 2,2-dimethylbutylthio, 2,3-dimethylbutylthio, 3,3-dimethylbutylthio, 1-ethylbutylthio, 2- Ethylbutylthio, 1,1,2-trimethylpropylthio, 1,2,2-dimethylbutylthio, 2-trimethylpropylthio, 1-ethyl-1-methyl Propylthio and 1-ethyl-2-methylpropylthio and different isomers.

鹵代環烷基、鹵代環烯基、烷基環烷基、環烷基烷基、環烷氧基烷基、烷基亞磺醯基烷基、烷基磺醯基烷基、鹵代烷基羰基、環烷基羰基、鹵代烷氧基烷基等的定義與上述例子類似。Halocycloalkyl, halocycloalkenyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkoxyalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, haloalkyl The definitions of carbonyl, cycloalkylcarbonyl, haloalkoxyalkyl, etc. are similar to the above examples.

術語“烷基硫代烷基”表示烷基被烷硫基取代。“烷基硫代烷基”的非限制性實例包括-CH2 SCH2 、-CH2 SCH2 CH2 、CH3 CH2 SCH2 、CH3 CH2 CH2 CH2 SCH2 和CH3 CH2 SCH2 CH2 。“烷基硫代烷氧基”表示烷氧基被烷硫基取代。“環烷基代烷基氨基”表示烷基氨基被環烷基取代。The term "alkylthioalkyl" means that an alkyl group is substituted with an alkylthio group. Non-limiting examples of "alkylthioalkyl" include -CH 2 SCH 2 , -CH 2 SCH 2 CH 2 , CH 3 CH 2 SCH 2 , CH 3 CH 2 CH 2 CH 2 SCH 2 and CH 3 CH 2 SCH 2 CH 2 . "Alkylthioalkoxy" means that the alkoxy group is substituted with an alkylthio group. "Cycloalkylalkylamino" means that the alkylamino group is substituted with a cycloalkyl group.

術語烷氧基烷氧基烷基、烷基氨基烷基、二烷基氨基烷基、環烷基氨基烷基、環烷基氨基羰基等的定義與“烷基硫代烷基”或“環烷基代烷基氨基”類似。The terms alkoxyalkoxyalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkylaminoalkyl, cycloalkylaminocarbonyl, etc. are defined in the same way as "alkylthioalkyl" or "cyclic "Alkylalkylamino" is similar.

術語“烷氧基羰基”是通過羰基(-CO-)與骨架鍵合的烷氧基。除非在別處具體限定,否則該定義也適用於烷氧基羰基作為複合取代基的一部分,例如環烷基烷氧基羰基等。The term "alkoxycarbonyl" is an alkoxy group bonded to the backbone through a carbonyl group (-CO-). Unless specifically defined elsewhere, this definition also applies to alkoxycarbonyl groups as part of composite substituents, such as cycloalkylalkoxycarbonyl groups and the like.

術語“烷氧基羰基烷基氨基”表示烷基氨基被烷氧基羰基取代。“烷基羰基烷基氨基”表示烷基氨基被烷基羰基取代。術語烷硫基烷氧基羰基、環烷基烷基氨基烷基等的定義與此類似。The term "alkoxycarbonylalkylamino" means that the alkylamino group is substituted by an alkoxycarbonyl group. "Alkylcarbonylalkylamino" means that an alkylamino group is substituted with an alkylcarbonyl group. The definitions of the terms alkylthioalkoxycarbonyl, cycloalkylalkylaminoalkyl, etc. are similar to this.

“烷基亞磺醯基”的非限制性例子包括但不限於甲基亞磺醯基、乙基亞磺醯基、丙基亞磺醯基、1-甲基乙基亞磺醯基、丁基亞磺醯基、1-甲基丙基亞磺醯基、2-甲基丁基亞磺醯基、1-甲基丁基亞磺醯基、2-甲基丁基亞磺醯基、2-甲基丁基亞磺醯基、1-乙基丙基亞磺醯基、1-乙基丙基亞磺醯基、1-2-二甲基丙基亞磺醯基、2-甲基戊基磺醯、3-甲基戊基磺醯、4-甲基戊基磺醯、1,1-二甲基丁基磺醯、1,3-二甲基丁基磺醯、2,3-二甲基丁基磺醯、3,3-二甲基丁基磺醯、1-乙基丁基磺醯、1,1,2-三甲基丙基磺醯、1-乙基1-甲基丙基磺醯和1-乙基2-甲基丙基磺醯及其異構體。“芳基亞磺醯基”一詞包括Ar-S(O),其中Ar可以是任何羧基或雜環。除非另有專門定義,否則這一定義也適用於烷基亞磺醯基作為複合取代基的一部分,例如鹵代烷基亞磺醯基等。Non-limiting examples of "alkylsulfinyl" include, but are not limited to, methylsulfinyl, ethylsulfinyl, propylsulfinyl, 1-methylethylsulfinyl, butyl Sulfinyl, 1-methylpropylsulfinyl, 2-methylbutylsulfinyl, 1-methylbutylsulfinyl, 2-methylbutylsulfinyl, 2-Methylbutylsulfinyl, 1-ethylpropylsulfinyl, 1-ethylpropylsulfinyl, 1-2-dimethylpropylsulfinyl, 2-methyl Butyl sulfonate, 3-methyl pentyl sulfonate, 4-methyl pentyl sulfonate, 1,1-dimethyl butyl sulfonate, 1,3-dimethyl butyl sulfonate, 2, 3-dimethyl butyl sulfonate, 3,3-dimethyl butyl sulfonate, 1-ethyl butyl sulfonate, 1,1,2-trimethyl propyl sulfonate, 1-ethyl 1 -Methyl propyl sulfonate and 1-ethyl 2-methyl propyl sulfonate and their isomers. The term "arylsulfinyl" includes Ar-S(O), where Ar can be any carboxyl or heterocyclic ring. Unless specifically defined otherwise, this definition also applies to alkylsulfinyl groups as part of a composite substituent, such as halogenated alkylsulfinyl groups and the like.

“烷基磺醯基”的非限制性例子包括但不限於甲基磺醯基、乙基磺醯基、丙基磺醯基、1-甲基乙基磺醯基、丁基磺醯基、1-甲基丙基磺醯基、2-甲基丁基磺醯基、1-甲基丁基磺醯基、2-甲基丁基磺醯基、3-甲基丁基磺醯基、2,2-甲基丙基磺醯基、1-乙基丙基磺醯基、1-乙基丙基磺醯基、1,2-二甲基丙基磺醯基、1-甲基磺醯基、2-甲基戊基磺基、3-甲基戊基磺基、4-甲基戊基磺基、1,1-二甲基丁基磺基、1,2-二甲基丁基磺基、2,2-二甲基丁基磺基、2,3-二甲基丁基磺基、3,3-二甲基丁基磺基、1-乙基丁基磺基、1,1,2-三甲基丙基磺基、1-乙基1-甲基丙基磺基、l-乙基2-甲基丙基磺基及其異構體。“芳基磺醯基”一詞包括Ar-S(O)2 ,其中Ar可以是任何羧基或雜環。除非另有定義,這個定義也適用於烷基磺醯基作為複合取代基的一部分,例如烷基磺基烷基等。Non-limiting examples of "alkylsulfonyl" include, but are not limited to, methylsulfonyl, ethylsulfonyl, propylsulfonyl, 1-methylethylsulfonyl, butylsulfonyl, 1-methylpropylsulfonyl, 2-methylbutylsulfonyl, 1-methylbutylsulfonyl, 2-methylbutylsulfonyl, 3-methylbutylsulfonyl, 2,2-Methylpropylsulfonyl, 1-ethylpropylsulfonyl, 1-ethylpropylsulfonyl, 1,2-dimethylpropylsulfonyl, 1-methylsulfonyl Acetyl, 2-methylpentylsulfonyl, 3-methylpentylsulfonyl, 4-methylpentylsulfonyl, 1,1-dimethylbutylsulfonyl, 1,2-dimethylbutyl Base sulfo, 2,2-dimethylbutylsulfonyl, 2,3-dimethylbutylsulfonyl, 3,3-dimethylbutylsulfonyl, 1-ethylbutylsulfonyl, 1 , 1,2-Trimethylpropylsulfonyl, 1-ethyl 1-methylpropylsulfonyl, 1-ethyl 2-methylpropylsulfonyl and their isomers. The term "arylsulfonyl" includes Ar-S(O) 2 , where Ar can be any carboxyl or heterocyclic ring. Unless otherwise defined, this definition also applies to alkylsulfonyl groups as part of a composite substituent, such as alkylsulfonylalkyl groups and the like.

“烷基胺基”、“二烷基胺基”等術語的定義與上述示例類似。The definitions of terms such as "alkylamino" and "dialkylamino" are similar to the above examples.

術語“碳環”或“碳環的”或“碳環基的”包括“芳族碳環系”和“非芳族碳環系”或多環或雙環(螺環、稠合、橋連、非稠合)環化合物,其中環可以是芳族的或非芳香族(其中芳香族表示符合休克爾規則,非芳香族表示不滿足休克爾規則)。The term "carbocyclic" or "carbocyclic" or "carbocyclic" includes "aromatic carbocyclic ring system" and "non-aromatic carbocyclic ring system" or polycyclic or bicyclic (spirocyclic, fused, bridged, Non-fused) ring compounds, where the ring can be aromatic or non-aromatic (where aromatic means conforming to Huckel’s rule, non-aromatic means not meeting Huckel’s rule).

與環相關的術語“雜”是指至少一個環原子不是碳原子的環,其可以包含1至4個獨立地選自氮、氧和硫的雜原子,條件是每個環裏面不超過4個氮、2個氧和2個硫。The term "hetero" in connection with the ring refers to a ring in which at least one ring atom is not a carbon atom, which may contain 1 to 4 heteroatoms independently selected from nitrogen, oxygen and sulfur, provided that there are no more than 4 in each ring Nitrogen, 2 oxygen and 2 sulfur.

術語“芳香族”表示符合休克爾規則,“非芳香族”表示不滿足休克爾規則。The term "aromatic" means that the Huckel rule is met, and "non-aromatic" means that the Huckel rule is not met.

術語“雜環”或“雜環的”包括“芳香雜環”或“雜芳基環系”和“非芳香雜環系”或多環或雙環(螺環,稠合,橋連,非稠合)環化合物,環可以是芳香族的或非芳香族,其中雜環含有至少一個選自N、O、S(O)0-2 的雜原子,和/或雜環的C環成員可以被C(=O)、C(=S)、C(=CR*R*)和C=NR*取代(*表示整數)。The term "heterocyclic ring" or "heterocyclic ring" includes "aromatic heterocyclic ring" or "heteroaryl ring system" and "non-aromatic heterocyclic ring system" or polycyclic or bicyclic (spiro, fused, bridged, non-fused Con) cyclic compound, the ring can be aromatic or non-aromatic, wherein the heterocyclic ring contains at least one heteroatom selected from N, O, S(O) 0-2 , and/or the C ring member of the heterocyclic ring can be Replace with C(=O), C(=S), C(=CR*R*) and C=NR* (* represents an integer).

術語“非芳族雜環”或“非芳族雜環”是指含有1至4個選自氧、氮和硫的雜原子的三至十五元(優選三至十二元)飽和或部分不飽和的雜環:單環,雙環或三環雜環,除碳環成員外,還含有1-3個氮原子和/或一個氧或硫原子或一個或兩個氧和/或硫原子;如果環含有多個氧原子,則它們不直接相鄰;例如(但不限於)環氧乙烷,疊氮基,氧雜環丁烷基,氮雜環丁烷基,硫雜環丁烷基,2-四氫呋喃基,3-四氫呋喃基、2-四氫噻吩基、3-四氫噻吩基、1-吡咯烷基、2-吡咯烷基、3-吡咯烷基、3-異惡唑烷基、4-異惡唑烷基、5-異惡唑烷基、3-異噻唑烷基、4-異噻唑烷基、5-異噻唑烷基、1-吡唑烷基、3-吡唑烷基、4-吡唑烷基、5-吡唑烷基、2-惡唑烷基、4-惡唑烷基、5-惡唑烷基、2-噻唑烷基、4-噻唑烷基、5-噻唑烷基、1-咪唑烷基、2-咪唑烷基、4-咪唑烷基、1,2,4-惡二唑烷-3-基、1,2,4-惡二唑烷-5-基、1,2,4-噻二唑烷-3-基、1,2,4-噻二唑烷-5-基、1,2,4-三唑烷-1-基、1,2,4-三唑烷-3-基、1,3,4-惡二唑烷-2-基、1,3,4-噻二唑烷-2-基、1,3,4-三唑烷-1-基、1,3,4-三唑烷-2-基、2,3-二氫呋喃-2-基、2,3-二氫呋喃-3-基、2,4-二氫呋喃-2-基、2,4-二氫呋喃-3-基、2,3-二氫噻吩-2-基、2,3-二氫噻吩-3-基、2,4-二氫噻吩-2-基、2,4-二氫噻吩-3-基、吡咯啉基、2-吡咯啉-2-基、2-吡咯-3-基、3-吡咯-2-基、3-吡咯-3-基、2-異惡唑啉-3-基、3-異惡唑啉-3-基、4-異惡唑啉-3-基、2-異惡唑啉-4-基、3-異惡唑啉-4-基、4-異惡唑啉-4-基、2-異惡唑啉-5-基、3-異惡唑啉-5-基、4-異惡唑啉-5-基、2-異噻唑啉-3-基、3-異噻唑啉-3-、4-異噻唑啉-3-基、2-異噻唑啉-4-基、3-異噻唑啉-4-基、4-異噻唑啉-4-基、2-異噻唑啉-5-基、3-異噻唑啉-5-基、4-異噻唑啉-5-基、2,3-二氫吡唑-1-基、2,3-二氫吡唑-2-基、2,3-二氫吡唑-3-基、2,3-二氫吡唑-4-基、2,3-二氫吡唑-5-基、3,4-二氫吡唑-1-基、3,4-二氫吡唑-3-基、3,4-二氫吡唑-4-基、3,4-二氫吡唑-5-基、4,5-二氫吡唑-1-基、4,5-二氫吡唑-3-基、4,5-二氫吡唑-4-基、4,5-二氫吡唑-5-基、2,3-二氫惡唑-2-基、2,3-二氫惡唑-3-基、2,3-二氫惡唑-4-基、2,3-二氫惡唑-5-基、3,4-二氫惡唑-2-基、3,4-二氫惡唑-3-基、3,4-二氫惡唑-4-基、3,4-二氫惡唑-5-基、3,4-二氫惡唑-2-基、3,4-二氫惡唑-3-基、3,4-二氫惡唑-4-基、呱啶基、2點二乙烯基、3-呱啶基、4-呱啶基、吡嗪基、嗎啉基、硫代嗎啉基、1,3-二惡烷-5-基、2-四氫吡喃基、4-四氫吡喃基、2-四氫噻吩基、3-六氫噠嗪基、4-六氫噠嗪基、2-六氫嘧啶基、 4-六氫嘧啶基、5-六氫嘧啶基、2-呱嗪基、1,3,5-六氫三嗪-2-基、1,2,4-六氫三嗪-3-基、環絲氨酸、2,3,4,5-四氫[1H] 氮雜卓-1-或-2-或-3-或-4-或-5-或-6-或-7-基、3,4,5,6-四氫[2H] 氮雜卓-2-或-3-或-4-或-5-或-6-或-7-基、2,3,4,7-四氫[1H]氮雜卓-1-或-2-或-3-或-4-或-5-或-6-或-7-基、2,3,6,7-四氫[1H]氮雜卓-1-或-2-或-3-或-4-或-5-或-6-或-7-基、六氫氮雜-1-或-2-或-3-或-4-基、四-和六氫氧雜環庚烯基、如2,3,4,5-四氫[1H]氧雜環庚烷-2-或-3-或-4-或-5-或-6-或-7-基、2,3,4,7-四氫[1H]氧雜-2-酮或-3-或-4-或-5-或-6-或-7-基、2,3,6,7-四氫[1H]氧雜-2-酮或-3-或-4-或-5-或-6-或-7-基、六氫氮雜-1-或-2--或-3-或-4-基、四-和六氫-1,3-二氮雜基、四-和六氫-1,4-二氮雜基、四-和六氫-1,3-氧氮雜基、四-和六氫-1,4-氧氮雜基、四-和六氫-1,3-二氧雜環庚烯基、四氫和六氫-1,4-二氧雜環庚烯基。除非在別處具體限定,否則該定義也適用於雜環烷基作為複合取代基的一部分,例如雜環基烷基等。The term "non-aromatic heterocyclic ring" or "non-aromatic heterocyclic ring" refers to a three to fifteen membered (preferably three to twelve membered) saturated or partially saturated or partially containing 1 to 4 heteroatoms selected from oxygen, nitrogen and sulfur Unsaturated heterocycles: monocyclic, bicyclic or tricyclic heterocycles, in addition to carbocyclic members, also contain 1-3 nitrogen atoms and/or one oxygen or sulfur atom or one or two oxygen and/or sulfur atoms; If the ring contains multiple oxygen atoms, they are not directly adjacent; for example (but not limited to) ethylene oxide, azido, oxetanyl, azetidinyl, thietane , 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydrothienyl, 3-tetrahydrothienyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 3-isoxazolidinyl , 4-isoxazolidinyl, 5-isoxazolidinyl, 3-isothiazolidinyl, 4-isothiazolidinyl, 5-isothiazolidinyl, 1-pyrazolidinyl, 3-pyrazolidine Group, 4-pyrazolidinyl, 5-pyrazolidinyl, 2-oxazolidinyl, 4-oxazolidinyl, 5-oxazolidinyl, 2-thiazolidinyl, 4-thiazolidinyl, 5 -Thiazolidinyl, 1-imidazolidinyl, 2-imidazolidinyl, 4-imidazolidinyl, 1,2,4-oxadiazolidine-3-yl, 1,2,4-oxadiazolidine-5 -Yl, 1,2,4-thiadiazolidine-3-yl, 1,2,4-thiadiazolidine-5-yl, 1,2,4-triazolidine-1-yl, 1,2 ,4-Triazolidine-3-yl, 1,3,4-oxadiazolidine-2-yl, 1,3,4-thiadiazolidine-2-yl, 1,3,4-triazolidine -1-yl, 1,3,4-triazolidine-2-yl, 2,3-dihydrofuran-2-yl, 2,3-dihydrofuran-3-yl, 2,4-dihydrofuran -2-yl, 2,4-dihydrofuran-3-yl, 2,3-dihydrothiophen-2-yl, 2,3-dihydrothiophen-3-yl, 2,4-dihydrothiophen-2 -Yl, 2,4-dihydrothiophen-3-yl, pyrrolinyl, 2-pyrrolin-2-yl, 2-pyrrol-3-yl, 3-pyrrol-2-yl, 3-pyrrol-3-yl Yl, 2-isoxazolin-3-yl, 3-isoxazolin-3-yl, 4-isoxazolin-3-yl, 2-isoxazolin-4-yl, 3-isoxazolin-3-yl Azolin-4-yl, 4-isoxazolin-4-yl, 2-isoxazolin-5-yl, 3-isoxazolin-5-yl, 4-isoxazolin-5-yl , 2-isothiazolin-3-yl, 3-isothiazolin-3-yl, 4-isothiazolin-3-yl, 2-isothiazolin-4-yl, 3-isothiazolin-4-yl, 4-isothiazolin-4-yl, 2-isothiazolin-5-yl, 3-isothiazolin-5-yl, 4-isothiazolin-5-yl, 2,3-dihydropyrazole-1 -Yl, 2,3-dihydropyrazol-2-yl, 2,3-dihydropyrazol-3-yl, 2,3-dihydropyrazol-4-yl, 2,3-dihydropyrazole -5-yl, 3,4-dihydropyrazol-1-yl, 3,4-dihydropyrazol-3-yl, 3,4-dihydropyrazol-4-yl, 3,4-dihydro Pyrazol-5-yl, 4,5-dihydropyrazol-1-yl, 4,5-dihydropyrazol-3-yl, 4,5 -Dihydropyrazol-4-yl, 4,5-dihydropyrazol-5-yl, 2,3-dihydrooxazol-2-yl, 2,3-dihydrooxazol-3-yl, 2 ,3-Dihydrooxazol-4-yl, 2,3-dihydrooxazol-5-yl, 3,4-dihydrooxazol-2-yl, 3,4-dihydrooxazol-3-yl , 3,4-dihydrooxazol-4-yl, 3,4-dihydrooxazol-5-yl, 3,4-dihydrooxazol-2-yl, 3,4-dihydrooxazole-3 -Base, 3,4-dihydrooxazol-4-yl, pyridinyl, 2-point divinyl, 3-pyridinyl, 4-pyridinyl, pyrazinyl, morpholinyl, thiomorpholine Group, 1,3-dioxan-5-yl, 2-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, 3-hexahydropyridazinyl, 4-hexahydropyranyl Azinyl, 2-hexahydropyrimidinyl, 4-hexahydropyrimidinyl, 5-hexahydropyrimidinyl, 2-piperazinyl, 1,3,5-hexahydrotriazin-2-yl, 1,2,4 -Hexahydrotriazin-3-yl, cycloserine, 2,3,4,5-tetrahydro[1H] azepine-1- or -2- or -3- or -4- or -5- or- 6- or -7-yl, 3,4,5,6-tetrahydro[2H] azepine-2- or -3- or -4- or -5- or -6- or -7-yl, 2 ,3,4,7-Tetrahydro[1H]azepine-1- or -2- or -3- or -4- or -5- or -6- or -7-yl, 2,3,6, 7-Tetrahydro[1H]azepine-1- or -2- or -3- or -4- or -5- or -6- or -7-yl, hexahydroazepine-1- or -2- Or -3- or -4-yl, tetra- and hexahydrooxepenyl, such as 2,3,4,5-tetrahydro[1H]oxepane-2- or -3- or- 4- or -5- or -6- or -7-yl, 2,3,4,7-tetrahydro[1H]oxa-2-one or -3- or -4- or -5- or -6 -Or-7-yl, 2,3,6,7-tetrahydro[1H]oxetan-2-one or -3- or -4- or -5- or -6-or-7-yl, hexahydro Aza-1- or -2-- or -3- or -4-yl, tetra- and hexahydro-1,3-diazepine, tetra- and hexahydro-1,4-diazepine, Tetra- and hexahydro-1,3-oxazepine, tetra- and hexahydro-1,4-oxazepine, tetra- and hexahydro-1,3-dioxepenyl, tetrahydro And hexahydro-1,4-dioxepenyl. Unless specifically defined elsewhere, this definition also applies to heterocycloalkyl as part of a composite substituent, such as heterocyclylalkyl and the like.

術語“雜芳基”是指包含氧、氮和硫族中的一至四個雜原子的5或6元全不飽和單環系;如果該環含有一個以上的氧原子,它們並不直接相鄰;5元雜芳基包含一至四個氮原子或一至三個氮原子及一個硫或氧原子:除了碳原子外,五元雜芳基還可含有一至四個氮原子或一至三個氮原子及一個硫或氧原子作為環成員,例如(但不限於)呋喃基、噻吩基、吡咯基、異惡唑基、異噻唑基、吡唑基、惡唑基、噻唑基、咪唑基、1,2,4-惡二唑基、1,2,4-噻二唑基1,2,4,4-三唑基、1,3,4-惡二唑基、1,3,4-噻二唑基、1,3,4-三唑基、四唑基;含有一至四個氮原子的氮鍵合的5-元雜芳基,或含有一至三個氮原子的苯並稠合的氮鍵合的5-元雜芳基:除碳原子外,可含有一至四個氮原子的五元雜芳基或者一至三個氮原子作為環成員並且其中兩個相鄰的碳環成員或一個氮和一個相鄰的碳環成員可以通過丁-1,3-二烯-1,4-二基橋接,其中一個或兩個碳原子可被氮原子取代,其中這些環通過一個氮環成員與骨架連接,例如(但不限於)1-吡咯基、1-吡唑基、1,2,4-三唑-1-基、1-咪唑基、1,2,3-三唑-1-基和1,3,4-三唑-1-基。The term "heteroaryl" refers to a 5- or 6-membered fully unsaturated monocyclic ring system containing one to four heteroatoms from oxygen, nitrogen and chalcogenide; if the ring contains more than one oxygen atom, they are not directly adjacent ; 5-membered heteroaryl contains one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom: in addition to carbon atoms, five-membered heteroaryl groups can also contain one to four nitrogen atoms or one to three nitrogen atoms and A sulfur or oxygen atom as a ring member, such as (but not limited to) furyl, thienyl, pyrrolyl, isoxazolyl, isothiazolyl, pyrazolyl, oxazolyl, thiazolyl, imidazolyl, 1, 2 ,4-oxadiazolyl, 1,2,4-thiadiazolyl, 1,2,4,4-triazolyl, 1,3,4-oxadiazolyl, 1,3,4-thiadiazole Group, 1,3,4-triazolyl, tetrazolyl; nitrogen-bonded 5-membered heteroaryl containing one to four nitrogen atoms, or benzo-fused nitrogen-bonded containing one to three nitrogen atoms 5-membered heteroaryl group: in addition to carbon atoms, a five-membered heteroaryl group that can contain one to four nitrogen atoms or one to three nitrogen atoms as ring members and two adjacent carbocyclic members or one nitrogen and one Adjacent carbocyclic members can be bridged by a but-1,3-diene-1,4-diyl group, one or two of the carbon atoms can be replaced by nitrogen atoms, and these rings are connected to the backbone through a nitrogen ring member, For example (but not limited to) 1-pyrrolyl, 1-pyrazolyl, 1,2,4-triazol-1-yl, 1-imidazolyl, 1,2,3-triazol-1-yl and 1, 3,4-Triazol-1-yl.

含有1-4個氮原子的6-元雜芳基:6-元雜芳基,其除碳原子外,還可分別含有1-3個和1-4個氮原子作為環成員,例如(但不限於)2-吡啶基、3-吡啶基、4-吡啶基、3-噠嗪基、4-噠嗪基、2-嘧啶基、4-嘧啶基、5-嘧啶基、2-吡嗪基、1,3,5-三嗪-2-基、1,2,4-三嗪-3-基和1,2,4,5-四嗪-3-基;含有一至三個氮原子或一個氮原子和一個氧或硫原子的苯並稠合的5-元雜芳基:例如(但不限於)吲哚-1-基、吲哚-2-基、吲哚-3-基、吲哚-4-基、吲哚-5-基、吲哚-6-基、吲哚-7-基、苯並咪唑-1-基、苯並咪唑-2-基、苯並咪唑-4-基、苯並咪唑-5-基、吲唑-l-基、吲唑-3-基、吲唑-4-基、吲唑-5-基、吲唑-6-基、吲唑-7-基、吲唑-2-基、1-苯並呋喃-2-基、1-苯並呋喃-3-基、1-苯並呋喃-4-基、1-苯並呋喃-5-基、1-苯並呋喃-6-基、1-苯並呋喃-7-基、1-苯並噻吩-2-基、1-苯並噻吩-3-基基團、1-苯並噻吩-4-基、1-苯並噻吩-5-基、1-苯並噻吩-6-基、1-苯並噻吩-7-基、1,3-苯並噻唑-2-基、1,3-苯並噻唑-4-基、1,3-苯並噻唑-5-基、1,3-苯並噻唑-6-基、1,3-苯並噻唑-7-基、1,3-苯並惡唑-2-基、1,3-苯並惡唑-4-基、1,3-苯並惡唑-5-基、1,3-苯並惡唑-6-基和1,3-苯並惡唑-7-基;含有一至三個氮原子的苯並稠合的6-元雜芳基:例如(但不限於)喹啉-2-基、喹啉-3-基、喹啉-4-基、喹啉-5-基、喹啉-6-基、喹啉-7-基、喹啉-8-基、異喹啉-1-基、異喹啉-3-基、異喹啉-4-基、異喹啉-5-基、異喹啉-6-基、異喹啉-7-基和異喹啉啉-8-基。除非在其他地方特別定義,該定義也適用於雜芳基作為複合取代基的一部分,例如雜芳基烷基等。6-membered heteroaryl groups containing 1-4 nitrogen atoms: 6-membered heteroaryl groups, in addition to carbon atoms, can also contain 1-3 and 1-4 nitrogen atoms as ring members, for example (but Not limited to) 2-pyridyl, 3-pyridyl, 4-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 2-pyrazinyl , 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl and 1,2,4,5-tetrazin-3-yl; containing one to three nitrogen atoms or one A benzo-fused 5-membered heteroaryl group containing a nitrogen atom and an oxygen or sulfur atom: for example (but not limited to) indol-1-yl, indol-2-yl, indol-3-yl, indole -4-yl, indol-5-yl, indol-6-yl, indol-7-yl, benzimidazol-1-yl, benzimidazol-2-yl, benzimidazol-4-yl, Benzimidazol-5-yl, indazol-1-yl, indazol-3-yl, indazol-4-yl, indazol-5-yl, indazol-6-yl, indazol-7-yl, Indazol-2-yl, 1-benzofuran-2-yl, 1-benzofuran-3-yl, 1-benzofuran-4-yl, 1-benzofuran-5-yl, 1-benzene And furan-6-yl, 1-benzofuran-7-yl, 1-benzothiophen-2-yl, 1-benzothiophen-3-yl group, 1-benzothiophen-4-yl, 1 -Benzothiophen-5-yl, 1-benzothiophen-6-yl, 1-benzothiophen-7-yl, 1,3-benzothiazol-2-yl, 1,3-benzothiazole-4 -Yl, 1,3-benzothiazol-5-yl, 1,3-benzothiazol-6-yl, 1,3-benzothiazol-7-yl, 1,3-benzoxazole-2- Yl, 1,3-benzoxazol-4-yl, 1,3-benzoxazol-5-yl, 1,3-benzoxazol-6-yl and 1,3-benzoxazole- 7-yl; benzo-fused 6-membered heteroaryl containing one to three nitrogen atoms: for example (but not limited to) quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, Quinolin-5-yl, quinolin-6-yl, quinolin-7-yl, quinolin-8-yl, isoquinolin-1-yl, isoquinolin-3-yl, isoquinolin-4- Group, isoquinolin-5-yl, isoquinolin-6-yl, isoquinolin-7-yl and isoquinolin-8-yl. Unless specifically defined elsewhere, this definition also applies to heteroaryl groups as part of a composite substituent, such as heteroarylalkyl groups.

術語“三烷基甲矽烷基”包括3個支鏈和/或直鏈烷基自由基,它們附屬於並連接在矽原子上,例如三甲基甲矽烷基,三乙基甲矽烷基和叔丁基二甲基甲矽烷基。“鹵代烷基甲矽烷基”表示三個烷基中的至少一個被鹵素原子部分或完全取代,所述鹵素原子可以相同或不同。“烷氧基三烷基甲矽烷基”表示三個烷基中的至少一個被一個或多個可以相同或不同的烷氧基取代。“三烷基甲矽烷氧基”表示通過氧連接的三烷基甲矽烷基部分。The term "trialkylsilyl" includes 3 branched and/or linear alkyl radicals attached to and attached to a silicon atom, such as trimethylsilyl, triethylsilyl and tertiary Butyldimethylsilyl. The "haloalkylsilyl group" means that at least one of the three alkyl groups is partially or completely substituted with a halogen atom, which may be the same or different. "Alkoxytrialkylsilyl" means that at least one of the three alkyl groups is substituted with one or more alkoxy groups which may be the same or different. "Trialkylsilyloxy" means a trialkylsilyl moiety linked by oxygen.

“烷基羰基”的非限制性實例包括C(O)CH3 、C(O)CH2 CH2 CH3 和C(O)CH(CH3 )2 。“烷氧基羰基”的實例包括CH3 OC(=O)、CH3 CH2 OC(=O)、CH3 CH2 CH2 OC(=O)、(CH3 )2 CHOC(=O)和不同的丁氧基或戊氧基羰基異構體。“烷基氨基羰基”的實例包括CH3 NHC(=O)、CH3 CH2 NHC(=O)、CH3 CH2 CH2 NHC(=O)、(CH3 )2 CHNHC(=O)和不同的丁氨基-或戊基氨基羰基異構體。“二烷基氨基羰基”的實例包括(CH3 )2 NC(=O)、(CH3 CH2 )2 NC(=O)、CH3 CH2 (CH3 )NC(=O)、CH3 CH2 CH2 (CH3 )NC(=O)和(CH3 )2 CHN(CH3 )C(=O)“烷氧基烷基羰基”的實例包括CH3 OCH2 C(=O)、CH3 OCH2 CH2 C(=O)、CH3 CH2 OCH2 C(=O)、CH3 CH2 CH2 CH2 OCH2 C(=O)和CH3 CH2 OCH2 CH2 C(=O)。“烷基硫代烷基羰基”的實例包括CH3 SCH2 C(=O)、CH3 SCH2 CH2 C(=O)、CH3 CH2 SCH2 C(=O)、CH3 CH2 CH2 CH2 SCH2 C(=O)和CH3 CH2 SCH2 CH2 C(=O)。鹵代烷基磺醯基羰基、烷基磺醯基氨基羰基、烷基硫代烷氧基羰基、烷氧基羰基烷基氨基等的定義與此類似。Non-limiting examples of "alkylcarbonyl" include C (O) CH 3, C (O) CH 2 CH 2 CH 3 and C (O) CH (CH 3 ) 2. Examples of "alkoxycarbonyl" include CH 3 OC (=O), CH 3 CH 2 OC (=O), CH 3 CH 2 CH 2 OC (=O), (CH 3 ) 2 CHOC (=O), and Different butoxy or pentoxycarbonyl isomers. Examples of "alkylaminocarbonyl" include CH 3 NHC (=O), CH 3 CH 2 NHC (=O), CH 3 CH 2 CH 2 NHC (=O), (CH 3 ) 2 CHNHC (=O), and Different butylamino- or pentylaminocarbonyl isomers. Examples of "dialkylaminocarbonyl" include (CH 3 ) 2 NC(=O), (CH 3 CH 2 ) 2 NC(=O), CH 3 CH 2 (CH 3 )NC(=O), CH 3 Examples of CH 2 CH 2 (CH 3 )NC(=O) and (CH 3 ) 2 CHN(CH 3 )C(=O) "alkoxyalkylcarbonyl" include CH 3 OCH 2 C(=O), CH 3 OCH 2 CH 2 C(=O), CH 3 CH 2 OCH 2 C(=O), CH 3 CH 2 CH 2 CH 2 OCH 2 C(=O) and CH 3 CH 2 OCH 2 CH 2 C( =O). Examples of "alkylthioalkylcarbonyl" include CH 3 SCH 2 C(=O), CH 3 SCH 2 CH 2 C(=O), CH 3 CH 2 SCH 2 C(=O), CH 3 CH 2 CH 2 CH 2 SCH 2 C(=O) and CH 3 CH 2 SCH 2 CH 2 C(=O). The definitions of haloalkylsulfonylcarbonyl, alkylsulfonylaminocarbonyl, alkylthioalkoxycarbonyl, alkoxycarbonylalkylamino, etc. are similar to this.

“烷基氨基烷基羰基”的非限制性實例包括CH3 NHCH2 C(=O)、CH3 NHCH2 CH2 C(=O)、CH3 CH2 NHCH2 C(=O)、CH3 CH2 CH2 CH2 NHCH2 C(=O)和CH3 CH2 NHCH2 CH2 C(=O)。Non-limiting examples of "alkylaminoalkylcarbonyl" include CH 3 NHCH 2 C(=O), CH 3 NHCH 2 CH 2 C(=O), CH 3 CH 2 NHCH 2 C(=O), CH 3 CH 2 CH 2 CH 2 NHCH 2 C(=O) and CH 3 CH 2 NHCH 2 CH 2 C(=O).

“醯胺”指的是A-R'C = ONR''-B,其中R'和R''表示取代基,A和B表示任何基團。"Amine" refers to A-R'C = ONR"-B, where R'and R" represent substituents, and A and B represent any group.

“硫代醯胺”是指A-R'C=SNR''-B,其中R'和R''表示取代基,A和B表示任何基團。"Thioamide" means A-R'C=SNR"-B, where R'and R" represent substituents, and A and B represent any groups.

取代基中的碳原子總數由“Ci -Cj ”首碼表示,其中i和j是數字1至21。例如,C1 -C3 烷基磺醯基表示甲基磺醯基至丙基磺醯基;C2 烷氧基烷基表示CH3 OCH2 ;C3 烷氧基烷基表示例如CH3CH(OCH3)、CH3OCH2 CH2 或CH3 CH2 OCH2 ;C4 烷氧基烷基表示被含有總共四個碳原子的烷氧基取代的烷基的各種異構體,實例包括CH3 CH2 CH2 OCH2 和CH3 CH2 OCH2 CH2 。在上述敘述中,當式(I)化合物由一個或多個雜環組成時,所有取代基通過任何可用的碳或氮通過取代所述碳或氮上的氫而連接到這些環上。The total number of carbon atoms in the substituent is represented by the prefix "C i -C j ", where i and j are the numbers 1-21. For example, C 1 -C 3 alkylsulfonyl represents methylsulfonyl to propylsulfonyl; C 2 alkoxyalkyl represents CH 3 OCH 2 ; C 3 alkoxyalkyl represents, for example, CH3CH(OCH3 ), CH3OCH 2 CH 2 or CH 3 CH 2 OCH 2 ; C 4 alkoxyalkyl means various isomers of alkyl groups substituted with alkoxy groups containing a total of four carbon atoms, examples include CH 3 CH 2 CH 2 OCH 2 and CH 3 CH 2 OCH 2 CH 2 . In the above description, when the compound of formula (I) consists of one or more heterocyclic rings, all substituents are connected to these rings through any available carbon or nitrogen by replacing the hydrogen on the carbon or nitrogen.

當化合物被帶有下標的取代基取代時,所述取代基表示所述取代基的數目可以超過1,所述取代基(當它們超過1時)獨立地選自所定義的取代基。 此外,當(R)m 中的下標m表示範圍從例如0到4的整數時,則取代基的數目可以從0和4之間的整數中選擇。When a compound is substituted by a substituent with a subscript, the substituent means that the number of the substituent may exceed 1, and the substituent (when they exceed 1) are independently selected from the defined substituents. In addition, when the subscript m in (R) m represents an integer ranging from, for example, 0 to 4, the number of substituents can be selected from an integer between 0 and 4.

當基團含有可以是氫的取代基時,則當該取代基被認為是氫時,可以認為所述基團未被取代。When a group contains a substituent that may be hydrogen, then when the substituent is considered to be hydrogen, the group can be considered unsubstituted.

本文中的實施方案及其各種特徵和有利的細節將參照描述中的非限制性實施方案進行說明。為避免不必要地模糊本文實施方案,省略了對已知成分和處理技術的描述。這裏使用的示例僅旨在便於理解可以實踐本文的實施方案的方式,並且進一步使本領域技術人員能夠實踐本文的實施方案。因此,這些實施方案不應被解釋為限制本發明實施方案的範圍。The embodiments herein and their various features and advantageous details will be described with reference to the non-limiting embodiments in the description. To avoid unnecessarily obscuring the embodiments herein, descriptions of known components and processing techniques are omitted. The examples used here are only intended to facilitate understanding of the ways in which the embodiments herein can be practiced, and to further enable those skilled in the art to practice the embodiments herein. Therefore, these embodiments should not be construed as limiting the scope of the embodiments of the present invention.

具體實施方案的描述將充分地揭示本文實施方案的大致性質,使其他人可以通過應用當前知識,能夠修改和/或適應應用這些具體實施方式而不脫離一般概念,因此,這種適應和修改,應被理解為具有本發明同樣地意義和範圍。需要理解的是,這裏使用的片語或術語是為了描述目的,不對本發明施加限制。因此,雖然這裏的實施方案是以首選實施方案的形式描述的,但那些精通該技術的人將認識到,在這裏描述的實施方案的精神和範圍內,通過修改可以實踐這裏的實施方案。The description of the specific embodiments will fully reveal the general nature of the embodiments herein, so that others can modify and/or adapt these specific embodiments by applying current knowledge without departing from the general concept. Therefore, this adaptation and modification, It should be understood to have the same meaning and scope as the present invention. It should be understood that the phrases or terms used here are for descriptive purposes and do not impose limitations on the present invention. Therefore, although the embodiments herein are described in the form of preferred embodiments, those skilled in the technology will recognize that the embodiments herein can be practiced with modifications within the spirit and scope of the embodiments described herein.

在本詳述中包含的對文檔、步驟、材料、裝置、物品等的任何討論僅僅是為了提供本發明的背景,不應視為承認這些事項構成現有技術基礎的一部分,或是本申請的最先日期之前存在的本領域的一般常識。Any discussion of documents, procedures, materials, devices, articles, etc. contained in this detailed description is only for the purpose of providing the background of the present invention, and should not be regarded as an admission that these matters form part of the prior art basis or are the most important part of this application. General common sense in the field that existed before the previous date.

儘管在描述和描述/請求項中提到的數值可能構成本發明的本發明的關鍵部分,但是如果該偏差遵循相同的科學,則與這些數值的任何偏差仍然是本發明的範圍內。如果合適,本發明的發明化合物可以作為不同可能的異構形式的混合物存在,尤其是立體異構體的混合物,例如E和Z、蘇式和赤型、光學異構體,還有互變異構體(如果合適)。E和Z異構體以及蘇型和赤型異構體和光學異構體的任何所需混合物和可能的互變異構形式都被是本公開和請求項的範圍。Although the numerical values mentioned in the description and description/requests may constitute a key part of the present invention, if the deviation follows the same science, any deviation from these numerical values is still within the scope of the present invention. If appropriate, the inventive compounds of the present invention may exist as mixtures of different possible isomeric forms, especially mixtures of stereoisomers, such as E and Z, threo and erythro forms, optical isomers, and tautomers. Body (if appropriate). Any desired mixtures and possible tautomeric forms of E and Z isomers and threo and erythro isomers and optical isomers are within the scope of the present disclosure and claims.

用於本發明目的的術語“害蟲”包括但不限於真菌、原生藻菌(卵菌綱)、細菌、線蟲、蟎蟲、蜱蟲、昆蟲和齧齒動物。The term "pest" for the purposes of the present invention includes but is not limited to fungi, stramenopiles (Oomycetes), bacteria, nematodes, mites, ticks, insects and rodents.

術語“植物”在此應理解為意指所有植物和植物種群,例如需要的和不需要的野生植物或作物植物(包括天然存在的作物植物)。作物植物可以是通過常規育種和優化方法或通過生物技術和基因工程方法或這些方法的組合獲得的植物,包括轉基因植物和植物育種者權利受保護和不受保護的植物栽培種。The term "plant" should be understood here to mean all plants and plant populations, such as desired and undesired wild plants or crop plants (including naturally occurring crop plants). Crop plants can be plants obtained through conventional breeding and optimization methods or through biotechnology and genetic engineering methods or a combination of these methods, including transgenic plants and plant breeders' rights protected and unprotected plant cultivars.

用於本發明的目的的術語“植物”包括以樹木、灌木、草本植物、草、蕨類植物和苔蘚這些通常在田間生長,通過其根部吸收水和所需物質,以及通過光合作用合成葉片中的營養成分的活生物體。The term "plants" used for the purpose of the present invention includes trees, shrubs, herbs, grasses, ferns and mosses, which usually grow in the field, absorb water and required substances through their roots, and synthesize the leaves through photosynthesis. The nutrients of living organisms.

用於本發明目的的“植物”的實例包括但不限於農作物,例如小麥、黑麥、大麥、黑小麥、燕麥或大米;甜菜;水果和果樹,例如梨果、核果或軟果,例如蘋果、梨、李子、桃子、杏仁、櫻桃、草莓、覆盆子、黑莓或醋栗;豆科植物,如扁豆、豌豆、苜蓿或大豆;油菜、芥菜、橄欖、向日葵、椰子、可哥豆、蓖麻油植物、油棕櫚、花生或大豆等油料植物;葫蘆,如南瓜、黃瓜或甜瓜;纖維植物,如棉花、亞麻、大麻或黃麻;柑橘類水果和柑橘樹,如柳丁、檸檬、葡萄柚或柑橘;任何園藝植物、蔬菜,如菠菜、生菜、蘆筍、捲心菜、胡蘿蔔、洋蔥、番茄、土豆、葫蘆或辣椒粉;月桂科屬植物,如鱷梨、肉桂或樟腦;葫蘆科植物;含油植物;能源和原料植物,如穀物、玉米、大豆、其他豆科植物、油菜、甘蔗或油棕;煙草;堅果;咖啡;茶;可哥;香蕉;胡椒;葡萄藤(鮮食葡萄和葡萄汁、葡萄藤);跳;草皮;甜葉(也稱甜葉菊);天然橡膠植物或觀賞植物和林業植物,例如花、灌木、闊葉樹或常綠植物,例如針葉樹;以及植物繁殖材料,例如種子,以及這些植物的作物材料。Examples of "plants" used for the purpose of the present invention include, but are not limited to, crops such as wheat, rye, barley, triticale, oats or rice; sugar beets; fruits and fruit trees such as pome, stone fruit or soft fruit such as apples, Pears, plums, peaches, almonds, cherries, strawberries, raspberries, blackberries or gooseberries; legumes, such as lentils, peas, alfalfa or soybeans; rape, mustard, olives, sunflowers, coconuts, cocoa beans, castor oil plants , Oil palm, peanuts or soybeans and other oil plants; gourds, such as pumpkin, cucumber or melon; fiber plants, such as cotton, flax, hemp or jute; citrus fruits and citrus trees, such as oranges, lemons, grapefruit or citrus; Any horticultural plant, vegetable, such as spinach, lettuce, asparagus, cabbage, carrot, onion, tomato, potato, gourd or paprika; Laurel plants, such as avocado, cinnamon or camphor; Cucurbitaceae; oily plants; energy and Raw material plants, such as grains, corn, soybeans, other legumes, rapeseed, sugarcane or oil palm; tobacco; nuts; coffee; tea; cocoa; bananas; peppers; grapevines (table grapes and grape juice, grapevines); Hops; turf; sweet leaves (also called stevia); natural rubber plants or ornamental plants and forestry plants, such as flowers, shrubs, broad-leaved trees, or evergreen plants, such as conifers; and plant propagation materials, such as seeds, and crop materials of these plants .

優選地,用於本發明目的的植物包括但不限於穀類、玉米、大米、大豆和其他豆科植物、水果和果樹、葡萄、堅果和堅果樹、柑橘和柑橘樹、任何園藝植物、 葫蘆科、含油植物、煙草、咖啡、茶、可哥、甜菜、甘蔗、棉花、馬鈴薯、番茄、洋蔥、辣椒和蔬菜、觀賞植物、任何供人類和動物使用的花卉植物和其他植物。Preferably, plants used for the purpose of the present invention include, but are not limited to, cereals, corn, rice, soybeans and other legumes, fruits and fruit trees, grapes, nuts and nut trees, citrus and citrus trees, any horticultural plants, Cucurbitaceae, Oily plants, tobacco, coffee, tea, cocoa, beets, sugar cane, cotton, potatoes, tomatoes, onions, peppers and vegetables, ornamental plants, any floral plants and other plants for human and animal use.

術語“植物部分”應理解為是指植物地上和地下的所有部分和器官。為了本發明的目的,術語植物部分包括但不限於插條、葉、枝、塊莖、花、種子、分枝、根,包括主根、側根、根毛、根尖、根冠、根狀莖、幼枝、芽、果實、子實體、樹皮、莖、芽、輔助芽、分生組織、節和節間。The term "plant parts" should be understood to mean all parts and organs of plants above and below the ground. For the purposes of the present invention, the term plant part includes but is not limited to cuttings, leaves, branches, tubers, flowers, seeds, branches, roots, including taproots, lateral roots, root hairs, root tips, root caps, rhizomes, young shoots , Buds, fruits, fruiting bodies, bark, stems, buds, auxiliary buds, meristems, nodes and internodes.

術語“其位點”包括土壤、植物或植物部分的周圍環境以及在播種/種植植物或植物部分之前、期間或之後使用的設備或工具。The term "its site" includes the soil, the surrounding environment of the plant or plant part, and the equipment or tools used before, during or after the sowing/planting of the plant or plant part.

本發明化合物或組合物(由本發明化合物和任意其他相容化合物組成的)中的本發明化合物在植物或植物材料或其所在位點上的應用包括通過本領域技術人員已知的技術施用,包括但不限於噴灑、塗料、浸漬、薰蒸、浸漬、注射和撒粉。The application of the compound of the present invention in the compound or composition of the present invention (consisting of the compound of the present invention and any other compatible compound) on plants or plant materials or their locus includes application by techniques known to those skilled in the art, including But not limited to spraying, coating, dipping, fumigation, dipping, injection and dusting.

術語“施用”是指物理或化學性粘附於植物或植物部分,包括浸漬。The term "application" refers to physical or chemical adhesion to plants or plant parts, including dipping.

在一個實施方案中,本發明提供了式(I)的化合物,

Figure 02_image001
式(I) 其中, R1 選自C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基和C3 -C8 -環烷基-C1 -C6 -烷基; Y獨立地選自O和/或NRy ; Ry 選自氫、氰基、C1 -C4 -烷基、C2 -C4 -烯基、C2 -C4 -炔基、C1 -C4 -鹵代烷基、C2 -C4 -鹵代烯基、C3 -C5 -環烷基和C3 -C5 -環烷基-C1 -C3 -烷基; Q代表5至10元雜環系統,其可任選地被一個或多個R2 基團取代; R2 選自氫、鹵素、氰基、硝基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、C1 -C6 -氰基烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、SCN、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、P(=O)(OR”)2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R2 可任選地被一個或多個R2a 基團取代; R2a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、SCN、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;或者 兩個R2a 取代基以及它們所連接的原子或其他選自C、N、O、S的原子,和任選地包括1至3個選自C(=O)、C(=S)、S(O)0-2 和Si(R”)2 的環成員一起可以形成3至7元環,其本身可任選地被一個或多個R2aa 基團取代; R2aa 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、C(=O)R8 、S(O)0-2 R7 、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; A1 和A2 獨立地代表N或CRA ; RA 選自氫、鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C3 -C8 -環烷基、OR”和N(R”)2 ;其中每個RA 基團可任選地被一個或多個RA' 基團取代; RA' 選自鹵素、氰基、C3 -C8 -環烷基、OR”和N(R”)2 ; Z代表O或S; G1 、G2 、G3 和G4 獨立地代表N或CR3 ;其中在環E中同時存在的N不超過兩個; R3 選自氫、鹵素、氰基、硝基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、SCN、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、P(=O)(OR”)2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R3 基團可任選地被一個或多個R3a 基團取代; R3a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R4 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、S(O)2 R7 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R4 基團可任選地被R4a 基團取代; R4a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R5 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR'R”、S(O)0-2 R7 、C(=O)R8 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R54 基團可任選地被R5a 取代; R5a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R6 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C1 -C6 -環烷基和C(=O)R8 ; R7 選自C1 -C6 -烷基, C2 -C6 -烯基, C2 -C6 -炔基, C1 -C6 -鹵代烷基, C2 -C6 -鹵代烯基, C3 -C8 -環烷基, NR5 R6 , C6 -C10 -芳基, C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R7 基團可任選地被一個或多個R7a 基團取代; R7a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R8 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、N=S(O)0-1 (R9 )2 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R8 可任選地被一個或多個R8a 基團取代; R8a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R9 選自C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基和C(=O)R8 ; R10 選自氫、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、Si(R”)3 、S(O)0-2 R7 和C(=O)R8 ; 或者兩個R9 取代基以及它們所連接的原子或其他選自C、N、O,和任選地包括C(=O)取代基的原子一起可以形成4至7元環,其本身可任選地被一個或多個鹵素、氰基、C1 -C6 -烷基、C1 -C6 -鹵代烷基或C1 -C6 -烷氧基基團取代; 或者R9 和R10 取代基以及它們所連接的原子或其他選自C、N、O,和任選地包括C(=O)取代基的原子一起可以形成4至7元環,其本身可任選地被一個或多個鹵素、氰基、C1 -C6 -烷基、C1 -C6 -鹵代烷基或C1 -C6 -烷氧基基團取代; R'選自氫、鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C3 -C8 -環烷基、OR”、N(R”)2 、S(O)0-2 R”、C(=O)R”、C(=O)OR”和C(=O)N(R”)2 ; R”選自氫、C1 -C6 -烷基、C2 -C6 -烯基和C2 -C6 -炔基和C3 -C8 -環烷基;其中每個R”基團可任選地被鹵素取代; 每個R1 至R10 、RA 、R2a 、R2aa 、R3a 、R4a 、R5a 、R7a 和R8a 可任選地被一個或多個選自X、CN、R'、OR”、SR'、N(R')2 、COOR”和CON(R')2 的基團取代; “n”為0〜2的整數; 或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、多晶型物、金屬絡合物、N-氧化物或S-氧化物。In one embodiment, the present invention provides a compound of formula (I),
Figure 02_image001
Formula (I) wherein, R 1 is selected from C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -Haloalkenyl, C 3 -C 8 -cycloalkyl and C 3 -C 8 -cycloalkyl-C 1 -C 6 -alkyl; Y is independently selected from O and/or NR y ; R y Selected from hydrogen, cyano, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -halo Alkenyl, C 3 -C 5 -cycloalkyl and C 3 -C 5 -cycloalkyl-C 1 -C 3 -alkyl; Q represents a 5- to 10-membered heterocyclic ring system, which may optionally be Or multiple R 2 groups; R 2 is selected from hydrogen, halogen, cyano, nitro, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, C 1 -C 6 -cyanoalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , SCN, S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , P(=O)(OR”) 2 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclic group; Wherein each R 2 may be optionally substituted by one or more R 2a groups; R 2a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2- C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , SCN, S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , Si( R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; or two R 2a substituents and the atoms to which they are connected or other options Atoms from C, N, O, S, and optionally including 1 to 3 rings selected from C(=O), C(=S), S(O) 0-2 and Si(R”) 2 The members together can form a 3 to 7 membered ring, which itself can be optionally substituted by one or more R 2aa groups; R 2aa is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , C(=O) R 8 , S(O) 0-2 R 7 , S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , Si( R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; A 1 and A 2 independently represent N or CR A ; R A is selected From hydrogen, halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 3 -C 8- cycloalkyl, oR "and N (R") 2; wherein each R a groups may be optionally substituted with one or more R a 'substituent group; R a' is selected from halo, cyano, C 3 - C 8 -Cycloalkyl, OR” and N(R”) 2 ; Z represents O or S; G 1 , G 2 , G 3 and G 4 independently represent N or CR 3 ; where both exist in ring E N does not exceed two; R 3 is selected from hydrogen, halogen, cyano, nitro, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1- C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S (O) 0-2 R 7 , SCN, S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , P(=O)(OR”) 2 , Si(R") 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl, and C 3 -C 10 -heterocyclic group; wherein each R 3 group can be optionally replaced by one or Multiple R 3a groups are substituted; R 3a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6- Haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 4 is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, S( O) 2 R 7 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl, and C 3 -C 10 -heterocyclic group; wherein each R 4 group can Optionally substituted by the R 4a group; R 4a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR'R", S(O) 0-2 R', C(=O)R ', Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclic group; R 5 is selected from hydrogen, C 1 -C 6- Alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl , OR 4 , NR'R”, S(O) 0-2 R 7 , C(=O)R 8 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aryl Alkyl and C 3 -C 10 -heterocyclyl; wherein each R 54 group may be optionally substituted by R 5a ; R 5a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2- C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR' R”, S(O) 0-2 R', C(=O)R', Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3- C 10 -heterocyclyl; R 6 is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 1 -C 6 -cycloalkyl and C(=O)R 8 ; R 7 is selected from C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, NR 5 R 6 , C 6 -C 10- Aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; wherein each R 7 group can be optionally taken by one or more R 7a groups R 7a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2- C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR'R", S(O) 0-2 R', C(=O)R', C 6 -C 10- Aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 8 is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2- C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , N=S(O) 0-1 (R 9 ) 2 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl, and C 3 -C 10 -heterocyclyl; wherein each R 8 may optionally be one or Multiple R 8a groups are substituted; R 8a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6- Haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR'R", S(O) 0-2 R', C(=O)R', C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 9 is selected from C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl , C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl and C(=O)R 8 ; R 10 Selected from hydrogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -halo Alkenyl, C 3 -C 8 -cycloalkyl, Si(R”) 3 , S(O) 0-2 R 7 and C(=O)R 8 ; or two R 9 substituents and their connection The atoms or other atoms selected from C, N, O, and optionally including C(=O) substituents together can form a 4 to 7-membered ring, which itself can be optionally substituted by one or more halogens, cyano groups , C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl or C 1 -C 6 -alkoxy group substitution; or R 9 and R 10 substituents and their attached atoms or other selected C, N, O, and atoms optionally including C(=0) substituents together can form a 4- to 7-membered ring, which itself may be optionally substituted by one or more halogen, cyano, C 1 -C 6 -Alkyl, C 1 -C 6 -halo Substituted alkyl or C 1 -C 6 -alkoxy group; R'is selected from hydrogen, halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, OR”, N(R”) 2 , S(O) 0-2 R”, C(=O)R”, C(=O)OR” And C(=O)N(R”) 2 ; R” is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl and C 2 -C 6 -alkynyl and C 3 -C 8 - cycloalkyl; wherein each R "group may optionally be substituted by halogen; each R 1 to R 10, R A, R 2a , R 2aa, R 3a, R 4a, R 5a, R 7a , and R 8a may be optionally substituted with one or more groups selected from X, CN, R', OR", SR', N(R') 2 , COOR" and CON(R') 2 ; "n" It is an integer from 0 to 2; or its agriculturally acceptable salts, isomers/structural isomers, stereoisomers, diastereomers, enantiomers, tautomers, polymorphs Type, metal complex, N-oxide or S-oxide.

在另一個實施方案中,式(I)的化合物由式(IA)化合物表示;

Figure 02_image004
式(IA)In another embodiment, the compound of formula (I) is represented by the compound of formula (IA);
Figure 02_image004
Formula (IA)

在另一個實施方案中,式(I)化合物由式(IB)化合物表示;

Figure 02_image006
式(IB)In another embodiment, the compound of formula (I) is represented by the compound of formula (IB);
Figure 02_image006
Formula (IB)

在一個實施方案中,Q環選自式Q1至Q14;

Figure 02_image008
其中,#表示與DE環的連接點,
Figure 02_image010
表示與-S(Y)n R1 基團的連接點,並且Q環可任選被一個或多個R2 基團取代; 其中每個脂族基團可以任選地被一個或多個R2a 基團取代,並且R2 的環狀基團可以任選地被一個或多個R2b 基團取代; “n”為0〜2的整數。In one embodiment, the Q ring is selected from formulas Q1 to Q14;
Figure 02_image008
Among them, # represents the connection point with the DE ring,
Figure 02_image010
Represents the point of attachment to the -S(Y) n R 1 group, and the Q ring may be optionally substituted by one or more R 2 groups; wherein each aliphatic group may be optionally substituted by one or more R The 2a group is substituted, and the cyclic group of R 2 may be optionally substituted with one or more R 2b groups; "n" is an integer from 0 to 2.

在一個實施方案中,優選的R2 取代基選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、C1 -C6 -氰基烷基、OR4 、NR5 R6 、S(O)0-2 R7 、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、P(=O)(OR”)2 、Si(R”)3 、苯基、芐基、苯氧基和C3 -C6 -雜環基;In one embodiment, preferred R 2 substituents are selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, C 1 -C 6 -cyanoalkyl, OR 4 , NR 5 R 6 , S(O) 0 -2 R 7 , S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , P(=O)(OR”) 2 , Si(R”) 3 , Phenyl, benzyl, phenoxy and C 3 -C 6 -heterocyclyl;

在另一個實施方案中,DE環選自式DE-a至DE-c;其中G1 、G2 、G3 和G4 獨立地代表N或CR3 ;A1 和A2 獨立地代表N或CRA ;其中在環E中同時存在的N不超過兩個;

Figure 02_image012
其中,#表示與Q環的連接點。In another embodiment, the DE ring is selected from formulas DE-a to DE-c; wherein G 1 , G 2 , G 3 and G 4 independently represent N or CR 3 ; A 1 and A 2 independently represent N or CR A ; where there are no more than two N simultaneously existing in ring E;
Figure 02_image012
Among them, # indicates the connection point with the Q ring.

在優選的實施方式中,DE環選自式DE1至DE16;

Figure 02_image014
其中,#表示與Q環的連接點,並且DE環可任選被一個或多個R3 和RA 基團取代。In a preferred embodiment, the DE ring is selected from formulas DE1 to DE16;
Figure 02_image014
Wherein # denotes the point of attachment of the Q ring, and the ring may DE optionally substituted with one or more substituents R 3 and R A groups.

在一個實施方案中,優選的R3 取代基選自鹵素、氰基、C1 -C6 -鹵代烷基、C3 -C8 -環烷基、OC1 -C6 -鹵代烷基、S(Y)0-2 -C1 -C6 -(鹵代)烷基。In one embodiment, preferred R 3 substituents are selected from halogen, cyano, C 1 -C 6 -haloalkyl, C 3 -C 8 -cycloalkyl, OC 1 -C 6 -haloalkyl, S(Y ) 0-2 -C 1 -C 6 -(halo)alkyl.

在一個實施方案中,特別地,式(I)的化合物選自2-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(5-甲基-3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(3-(三氟甲基)-1H-1,2,4-三唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙硫基)-6'-氟代-[3,3'-二吡啶]-6-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6'-氟代-[3,3'-二吡啶]-6-基)-6-(三氟甲基)酞嗪-1(2H)-酮;7-(5-溴-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(6-氯-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-氟代-4-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;4-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)苯並腈;7-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-苯基吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-6-(3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(6-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;3-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙硫基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;7-(3-(乙基磺醯基)-6-(3-甲基-1H-1,2,4-三唑-1-基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-6-(3-氟代-4-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;4-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-2-基)苯並腈;7-(3-(乙基磺醯基)-6-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-苯基吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-甲氧基苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;7-(3-(乙基磺醯基)-6-苯基吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(5-(2,2-二氟苯並[d][1,3]二氧雜環戊烯-5-基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(6-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;4-(5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)喹唑啉-3(4H)-基)吡啶-3-基)苯並腈;3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(3-氯-4-(三氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(2-氟代-5-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-3-甲氧基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,4-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-3-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-環丙基-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;2-(6-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3,4,5-三氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-2-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-氟代-2-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(6-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(3,4,5-三氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;4-(5-(乙基磺醯基)-6-(4-氧代-7-(三氟甲基)喹唑啉-3(4H)-基)吡啶-3-基)苯並腈;3-(3-(乙基磺醯基)-5-(4-甲氧基苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-(4-溴苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(2,2,2-三氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-(全氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(全氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯並腈;2-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,4-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-環丙基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯基)環丙烷-1-甲腈;2-(5-(4-(二氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6'-氟代-[3,3'-二吡啶]-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(甲硫基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(5-(3,4-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3-氯-5-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)煙腈;2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯-3-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-氯-5-(三氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-氯-5-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯並腈;2-(3-(乙基磺醯基)-5-(2-氟代-5-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯-2-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-溴苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙酸乙酯;2-(4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯氧基)-2,2-二氟-N,N-二甲基乙醯胺;2-(3-(乙基磺醯基)-5-(3,3,3-三氟丙基-1-烯-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(2,2,3,3,3-五氟丙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟苯並[d][1,3]二氧雜環戊烯-5-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)乙腈;2-(3-(乙基磺醯基)-5-(1,1,2,3,3,3-六氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-羥基苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5'-(乙基磺醯基)-6'-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-[2,3'-二吡啶]-5-甲腈;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)嘧啶-5-甲腈;2-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,3,3-五氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(嘧啶-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-甲基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((甲硫基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(環丙基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(5-((二甲基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((甲基磺醯基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(氧雜環丁烷-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙醯胺;2-(3-(乙基磺醯基)-6-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((二乙基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5'-(乙基磺醯基)-4-(三氟甲基)-[2,3'-二吡啶]-6'-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5'-(乙基磺醯基)-5-(三氟甲基)-[2,3'-二吡啶]-6'-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3-(苄氧基)環丁氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(3-(乙基磺醯基)-5-(2-甲氧基嘧啶-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)乙腈;2-(5-溴-3-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙硫基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(5-(2-溴-1,1,2,2-四氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙硫基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(3-氯-5-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(5-((4,4-二氟but-3-烯-1-基)氧)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-氟代-5-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈;2-(3-(乙基磺醯基)-5-(4-(甲基磺醯基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基) 乙基膦酸乙酯;2-(5-(二甲基磷醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((S-甲基磺醯亞胺基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯亞胺基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1,1,2,2-四氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-((二乙基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(3-(乙基磺醯基)-5-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氟苯基)-3-(N-甲基乙基磺醯亞胺基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮; (5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氨基甲酸叔丁酯;2-(5-((乙基(甲基)((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-((乙基(異丙基)((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基 氨基磺酸二甲酯;2-((5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基)氧)乙腈;3-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(環丙基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)-5-(甲氧基甲氧基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-((5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基)氧)-2-甲基丙醯胺;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2-甲基丙腈;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基氨基磺酸二甲酯;2-(5-氨基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((4-氧負離子基-1,4l6-氧雜蒽-4-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(乙硫基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺;2-(3-(乙基磺醯基)-6-(5-甲基-3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((2,2,2-三氟乙基)硫代)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3,5-雙(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氟乙基)硫代)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯亞胺基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氟乙基)磺醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-(二甲基磷醯基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷甲醯胺;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙腈;2-(3-(乙基磺醯基)-5-異丙氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((1,1,1-三氟-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-氧負離子基-4,5-二氫-3H-1l6-異噻唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((3-羥基-1-氧化四氫-1l6-噻吩-1-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((4-氧負離子基-1,4l6-氧雜蒽-4-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯磺醯氟;2-(5-(4-(二甲基磷醯基)苯基)-3-(乙基磺醯亞胺基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5'-(乙基磺醯基)-6'-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-[3,3'-二吡啶]-6-磺醯氟;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-磺醯氟;2-(5-(4-(1,1-二氟乙基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-(三氟甲基)環丙基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1,3,5-三甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-異丁基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲氧基-1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(1'-(二氟甲基)-5-(乙基磺醯基)-6'-氧代-1',6'-二氫-[3,3'-二吡啶]-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-異丙基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二甲基異唑-4-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯亞胺基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯基 氟化硫;2-(3-(乙基磺醯亞胺基)-5-((1,1,1-三氟-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯亞胺基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙腈;2-(3-(乙基磺醯基)-5-((甲基亞磺醯基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,3-四氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1,1,2-三氟-2-(三氟甲氧基)乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,4,4,4-六氟丁氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,3,3-五氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟-2-(三氟甲氧基)乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2,2-二氟環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2,2-二甲基環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-氟環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-N-甲基環丁烷甲醯胺;1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3,3-二甲基環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3,3-二氟環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丁烷甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3-甲基環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3-氧代環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環戊烷甲醯胺;1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環戊烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環戊烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環己烷甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4-甲基環己烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4,4-二氟環己烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氮雜環丁烷-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基氮雜環丁烷-3-甲醯胺;1-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氮雜環丁烷-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧雜環丁烷e-3-甲醯胺;3-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧雜環丁烷e-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基吡咯烷-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)四氫呋喃-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)呱啶-4-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基呱啶-4-甲醯胺;1-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)呱啶-4-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)四氫-2H-吡喃-4-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4-氟四氫-2H-吡喃-4-甲醯胺;2-(7-溴-3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-7-(三氟甲基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-基)乙腈;3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-甲腈;2-(3-(乙基磺醯基)-7-甲氧基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-基)環丙烷-1-甲腈;2-(3-(乙基磺醯基)-7-(2,2,2-三氟乙基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(三氟甲基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-甲腈;2-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-基)乙腈;2-(3-(乙基磺醯基)-7-(1-甲基環丙基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-7-(甲基氨基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)煙腈;2-(5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)乙腈;1-(5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)環丙烷-1-甲腈;2-((5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)氧)-2-甲基丙腈;7-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮;5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)煙腈;2-(5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)吡啶-3-基)乙腈;1-(5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈;5-(乙基磺醯基)-6-(1-氧代-7-((三氟甲基)磺醯基)酞嗪-2(1H)-基)煙腈;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-((三氟甲基)磺醯基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-((三氟甲基)磺醯基)酞嗪-1(2H)-酮;1-(5-(乙基磺醯基)-6-(1-氧代-7-((三氟甲基)磺醯基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈;7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)乙腈;1-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)環丙烷-1-甲腈;7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(3-(乙基磺醯基)-5-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((2-(三氟甲基)環丙基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲氧基雜氮環丁烷-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((1-甲基雜氮環丁烷-3-基)氧)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2H-1,2,3-三唑-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(2-羥基-2-甲基丙基)-1H-1,2,3-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-雙(三氟甲基)-1H-吡唑-1-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(2,2,2-三氟乙氧基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(2,2,3,3,3-五氟丙氧基)酞嗪-1(2H)-酮;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]嘧啶-7-基)環丙烷-1-甲腈;2-(3-(乙基磺醯基)-6-甲基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-(乙基磺醯基)-2-(三氟甲基)吡唑並[1,5-a]嘧啶-5-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[2,1-b]噻唑-2-甲腈;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]嘧啶-6-基)環丙烷-1-甲腈;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡唑並[1,5-a]吡啶-5-基)環丙烷-1-甲腈;2-(2-(乙基磺醯基)-7-甲基吡唑並[1,5-a]嘧啶-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-1-甲基-6-(三氟甲氧基)-1H-吲哚-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-1H-吡咯並[2,3-b]吡啶-1-基)乙腈;2-(5-(乙基磺醯基)-1-甲基-1H-吡唑並[3,4-b]吡啶-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(7-環丙基-2-(乙基磺醯基)咪唑並[1,2-a]嘧啶-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)咪唑並[1,2-a]吡嗪-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)咪唑並[1,2-b]噠嗪-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(溴二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(吡啶-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(吡啶-2-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((5-溴吡啶-2-基)氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(嘧啶-2-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((1-甲基-1H-吡唑-3-基)氧)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,3-二氟環丁氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,3-二氟丙烷-2-基)氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(新戊基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)甲基)環丙烷-1-甲腈;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丙腈;2-(3-(乙基磺醯基)-5-((1-氟代-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-甲氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2-氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-(甲硫基)乙腈;2-(5-((2,2-二氟環丙基)甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丁腈;2-(5-(環丁基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟丙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-N,N-二甲基-2-(甲硫基)乙醯胺;2-乙基-2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丁腈;2-(3-(乙基磺醯基)-5-異丁氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-溴-1,1-二氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((3-環丙基異惡唑-5-基)甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲氧基環丁氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基 二氟甲磺酸酯;3-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)環丁烷-1-甲腈;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基氟甲磺酸酯;3-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-3-甲基丁腈;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基三氟甲磺酸酯;2-(3-(乙基磺醯基)-5-((1-甲氧基-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-N,N,2-三甲基丙醯胺;2-(3-(乙基磺醯基)-5-((3-甲基氧雜環丁烷-3-基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;(E)-2-(3-(乙基磺醯基)-5-(2-(甲基亞氨基)丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((三甲基silyl)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2-氧丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((2-甲基-3-氧代丁烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(烯丙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-丙氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-乙氧基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(甲氧基甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-環丁基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟環丙基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2-甲基氧雜環丁烷-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲基硫雜環丁烷基-3-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(1,1-二氧負離子基硫雜環丁烷基-2-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;6-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)煙腈;2-(3-(乙基磺醯基)-5-(硫雜環丁烷基-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氧負離子基硫雜環丁烷基-3-基)氧)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氧負離子基硫雜環丁烷基-3-基)甲基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(3-(N-甲基乙基磺醯亞胺基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(N-甲基乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;N-(乙基((氧代)(2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-3-基)-l6-亞硫烷基)氰胺;2-(3-(N-乙基乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(乙基磺醯亞胺基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(N-甲基乙基磺醯亞胺基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(3-(乙基磺醯亞胺基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-基)環丙烷-1-甲腈;3-(乙基磺醯亞胺基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-甲腈;2-(6-(環丙基氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 和N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-2-基)環丙烷甲醯胺。In one embodiment, in particular, the compound of formula (I) is selected from 2-(3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H )-Ketone; 2-(3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-bromo-3-(ethyl) Sulfuryl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl) -6-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(6-chloro-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl) Phthalazine-1(2H)-one; 2-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl) Phthalazine-1(2H)-one; 2-(5-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl) Phthaloazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl) Yl)phthalazine-1(2H)-one; 2-(3-(ethylthio)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1 (2H)-ketone; 2-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-6-(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine -1(2H)-one; 2-(3-(ethylsulfonyl)-6-(5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridine-2 -Base)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(3-(trifluoromethyl)-1H-pyridine Azol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(3-( Trifluoromethyl)-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3 -(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(ethyl) Thio)-6'-fluoro-[3,3'-dipyridyl]-6-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl Sulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5 -(Ethylsulfonyl)-6'-fluoro-[3,3'-dipyridine]-6-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 7- (5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7- ( 3-(Ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(6-chloro- 3-(Ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethyl) Sulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7 -(3-(Ethylsulfonyl)-5-(3-fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2 ,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-3-(trifluoromethyl) )Pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridine- 2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4- Fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7- (3-(Ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H )-Ketone; 7-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2 ,3-d]pyridazine-8(7H)-one; 4-(5-(ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3 -d]Pyridazine-7(8H)-yl)pyridin-3-yl)benzonitrile; 7-(3-(ethylsulfonyl)-6-(4-(trifluoromethoxy)phenyl )Pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5- Phenylpyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(5-(3,5-difluorophenyl) )-3-(Ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(5- (3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H )-Ketone; 7-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-3-(trifluoro Methyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-6-(3-(trifluoromethyl)phenyl)pyridine -2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(6-(3,5-dichlorophenyl)-3 - (Ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 3-(3-(ethylsulfon) (Pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)pyridin-2-yl)-7- (Trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylthio)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl) ) Quinazolin-4(3H)-one; 7-(3-(ethylsulfonyl)-6-(3-methyl-1H-1,2,4-triazol-1-yl)pyridine- 2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-6-(3- Fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 4- (5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine-2- Group) benzonitrile; 7-(3-(ethylsulfonyl)-6-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoro Methyl)pyrido[2,3-d]pyridazine-8(7H)-one; 3-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoro Methyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl) Quinazolin-4(3H)-one; 3-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl ) Quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)quine Oxazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-phenylpyridin-2-yl)-6-(trifluoromethyl)quinazoline-4(3H) -Ketone; 3-(3-(ethylsulfonyl)-5-(4-methoxyphenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline-4(3H) -Ketone; 3-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline-4 (3H)-one; 7-(3-(ethylsulfonyl)-6-phenylpyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine- 8(7H)-ketone; 7-(3-(ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-3-( Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(5-(2,2-difluorobenzo[d][1,3] dioxane Penten-5-yl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one ; 7-(6 -(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H)-ketone; 7-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-3- (Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 3-(3-(ethylsulfonyl)-5-(3-(trifluoromethoxy) Phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 4-(5-(ethylsulfonyl)-6-(4-oxo- 6-(Trifluoromethyl)quinazolin-3(4H)-yl)pyridin-3-yl)benzonitrile; 3-(3-(ethylsulfonyl)-5-(4-(trifluoro) Methoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(3,5-difluorophenyl)-3 -(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(4-chlorophenyl)-3-( Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(3- (Trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5- (2-Fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(3 -Chloro-4-(trifluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(Ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazole Lin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-6- (Trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(2-fluoro-5-(trifluoromethoxy)phenyl) Pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluoro-3-( (Trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4 -Fluoro-3-methoxyphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,4-difluorobenzene) Yl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)- 5-(4-Fluoro-3-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chlorobenzene) Yl)-3-(ethylsulfonyl)pyridine -2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-cyclopropyl-3-(ethylsulfonyl)pyridin-2-yl)-6 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl)-6-(tris Fluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridine- 2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(4-(trifluoromethoxy)phenyl )Pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-(4-(1,1,2 ,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 2-(6-(4-chlorophenyl) -3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2-chloro-4-fluorophenyl) )-3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5 -(3,4,5-Trifluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) -5-(4-Fluoro-2-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-chloro-3- (Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(4- Fluoro-2-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-(2-chloro-4-fluorophenyl) )-3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6 -(3,4,5-trifluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-bromo-3-(ethyl) Sulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5-(3,5-dichlorophenyl)-3-(ethyl) Sulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-fluorobenzene) Yl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl) (Oxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(4- Fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(4-fluorophenyl) )Pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one; 2-(6-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl Yl)phthalazine-1(2H)-one; 3-(5-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl Yl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-7- (Trifluoromethyl)quinazoline-4(3H)-one; 4-(5-(ethylsulfonyl)-6-(4-oxo-7-(trifluoromethyl)quinazoline- 3(4H)-yl)pyridin-3-yl)benzonitrile; 3-(3-(ethylsulfonyl)-5-(4-methoxyphenyl)pyridin-2-yl)-7- (Trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(tris Fluoromethyl)quinazolin-4(3H)-one; 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl Yl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2 -(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 3-(3- (Ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3- (3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quine Oxazolin-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine-2- Group)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoro) Ethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4- (Trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6- (4-(Trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5-(4-bromophenyl) -3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5 -(3-Fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3- (Ethylsulfonyl)-5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazoline-4( 3H)-ketone; 3-(5-bromo-3 -(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one; 3-(5-(4-chloro Phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one; 3-(3 -(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one ; 3-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl Yl)pyrido[3,2-d]pyrimidin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridine- 2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(4-( Perfluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5-difluorophenyl)- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5-dichlorophenyl)- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-( 4-(Perfluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione; 2-(3-(ethylsulfonyl) -5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione; 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone; 4-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) Benzonitrile; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-one; 2-(5-(3,4-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-one; 2-(5-cyclopropyl-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 1 -(4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenyl) Cyclopropane-1-carbonitrile; 2-(5-(4-(difluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1 (2H)-ketone; 2-(5-(ethylsulfonyl)-6'-fluoro-[3,3'-dipyridyl]-6-yl)-7-(trifluoromethyl)phthalazine -1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-thione; 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine -1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(methylthio)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl )Phthalazine-1(2H)-one; 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-thione; 2-(5-(3,4-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(5-(3-chloro-5-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine-2- Yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy) )Phenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-( 4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione; 5-(ethylsulfonyl)-6-(1-oxo- 7-(Trifluoromethyl)phthalazine-2(1H)-yl)nicotinonitrile; 2-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridine-2- Yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridine- 2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5-difluorophenyl)-3-(ethylsulfon) (Pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chloro-3-fluorophenyl)- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2-chloro-5-(trifluoromethyl) Yl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-chloro-5-(5-( Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazin-2(1H)-yl)pyridin-3-yl)benzonitrile; 2-(3-(ethyl) Sulfonyl)-5-(2-fluoro- 5-(Trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chloro-2-fluoro) Phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-bromophenyl) -3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6 -(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2-methylpropionate; 2-(4-(5 -(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenoxy)-2,2- Difluoro-N,N-dimethylacetamide; 2-(3-(ethylsulfonyl)-5-(3,3,3-trifluoropropyl-1-en-2-yl)pyridine -2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(2,2,3,3 ,3-Pentafluoropropoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,2-difluorobenzene) And [d][1,3]dioxol-5-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl )Oxy)acetonitrile; 2-(3-(ethylsulfonyl)-5-(1,1,2,3,3,3-hexafluoropropoxy)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-hydroxyphenyl)pyridin-2-yl)-7-(trifluoromethyl) )Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-hydroxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(5-(2-chloro-4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -Ketone; 2-(3-(Ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one; 5'-(ethylsulfonyl)-6'-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)- Group)-[2,3'-dipyridine]-5-carbonitrile; 2-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine- 2(1H)-yl)pyridin-3-yl)pyrimidine-5-carbonitrile; 2-(3-(ethylsulfonyl)-5-(2,2,2-trifluoroethoxy)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2,2,3,3,3-penta Fluoropropoxy)pyridin-2-yl) -7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-fluorophenyl)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazole -5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(pyrimidine-5- Yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-methylpyridin-2-yl) -7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((methylthio)methoxy)pyridin-2-yl) -7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(cyclopropylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 3-(5-bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d ][1,2,3]triazine-4(3H)-one; 3-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzene And [d][1,2,3]triazine-4(3H)-one; 2-(5-((dimethyl((oxo)-l6-sulfinyl)amino)-3-( Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((methyl Sulfonyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(4-(ethylsulfonyl)-6-(3 -(Trifluoromethyl)phenyl)pyridazin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5 -(Oxetan-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl) Yl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2-methylpropanamide; 2-(3 -(Ethylsulfonyl)-6-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone; 2-(5-((diethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(5'-(ethylsulfonyl)-4-(trifluoromethyl)-[2,3'-dipyridine]- 6'-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5'-(ethylsulfonyl)-5-(trifluoromethyl)-[2, 3'-Dipyridine]-6'-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3-(benzyloxy)cyclobutoxy)- 3-(Ethylsulfonyl)pyridine Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3-chloro-4-fluorophenyl)-3-(ethylsulfonyl) )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridine- 2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(3-(ethylsulfonyl)-5- (2-Methoxypyrimidin-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(ethylsulfonyl)- 6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile; 2-(5-bromo-3-(ethylthio)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl )Pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(3-(ethylsulfonyl) -5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3 ] Triazine-4(3H)-one; 3-(3-(ethylthio)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d ][1,2,3]Triazine-4(3H)-one; 3-(5-(4-chlorophenyl)-3-(ethylthio)pyridin-2-yl)-6-(trifluoro Methyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(5-(2-bromo-1,1,2,2-tetrafluoroethoxy)- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylthio)-5-(4- (Trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-( 5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4 (3H)-one; 3-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d ][1,2,3]triazine-4(3H)-one; 3-(5-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)- 6-(Trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(5-(3-chloro-5-fluorophenyl)-3-( (Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(3-(ethyl) Sulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine- 4(3H)-ketone; 2-(5-((4 ,4-Difluorobut-3-en-1-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(ethylthio)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-1H-pyrazol-5-yl)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-1H-pyrazol-4-yl)pyridine-2- Group)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-fluoro-5-(trifluoromethyl) Phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 1-(5-(ethylsulfonyl)-6-(1-oxo-7 -(Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1-carbonitrile; 2-(3-(ethylsulfonyl)-5-(4-( Methylsulfonyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylthio)-5-(4- Fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; (5-(ethylsulfonyl)-6-(1-oxo-7- (Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) ethyl phosphonate; 2-(5-(dimethylphosphoryl)-3-(ethylsulfonyl) Yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonylimino)-5-(4-(1, 1,2,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonate) Yl)-5-((S-methylsulfonylimino)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3 -(Ethylsulfonylimino)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3- (Ethylsulfonyl)-5-(1,1,2,2-tetrafluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(Ethylsulfonyl)-5-(3-methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-hydroxypyridin-2-yl)-6-(trifluoromethyl)benzo[d] [1,2,3]Triazine-4(3H)-one; 3-(3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1, 2,3]Triazine-4(3H)-one; 3-(3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2 ,3]Triazine-4 (3H)-ketone; 3-(5-((diethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-6- (Trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(ethylthio)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-fluorophenyl)-3-(N-methylethylsulfonylimide) )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; (5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoro) Methyl)phthalazine-2(1H)-yl)pyridin-3-yl)tert-butyl carbamate; 2-(5-((ethyl(methyl)((oxo)-l6-sulfinyl) )Amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5-((ethyl(isopropyl) ((Oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1, 2,3]Triazine-4(3H)-one; 5-(ethylsulfonyl)-6-(4-oxo-6-(trifluoromethyl)benzo[d][1,2, 3] Triazine-3(4H)-yl)pyridin-3-yl dimethylsulfamate; 2-((5-(ethylsulfonyl)-6-(4-oxo-6-(three Fluoromethyl)benzo[d][1,2,3]triazine-3(4H)-yl)pyridin-3-yl)oxy)acetonitrile; 3-(3-(ethylsulfonyl)-5 -(2,2,2-Trifluoroethoxy)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one ; 3-(5-(Cyclopropylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3 ]Triazine-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(methoxymethoxy)pyridin-2-yl)-6-(trifluoromethyl)benzene And [d][1,2,3]triazine-4(3H)-one; 3-(5-(difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)- 6-(Trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-((5-(ethylsulfonyl)-6-(4-oxy Subo-6-(trifluoromethyl)benzo[d][1,2,3]triazine-3(4H)-yl)pyridin-3-yl)oxy)-2-methylpropanamide; 2 -(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-2-methylpropane Nitrile; 5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl dimethylsulfamate; 2-(5-Amino-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-chloro-3- (Ethyl Sulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(1H-1,2 ,4-Triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5- ((4-oxoanion-1,4l6-xanthene-4-yl subunit)amino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2 -(6-Bromo-3-(ethylthio)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-( 5-(Difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 1-cyano-N -(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1-methyl Amide; 2-(3-(Ethylsulfonyl)-6-(5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((2,2,2-trifluoroethyl)thio)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3,5-bis(ethylsulfonyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(5-((1,1-difluoroethyl)thio)-3-(ethylsulfonyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(ethylsulfonylimino)-3-(ethylsulfonyl)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-((1,1-difluoroethyl)sulfonyl)-3-(ethylsulfonyl)pyridine-2- Group)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-(dimethylphosphoryl)phenyl)-3-(ethylsulfonyl) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(three Fluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropanecarboxamide; 2-((5-(ethylsulfonyl)-6-(1-oxo-7- (Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2-methylpropionitrile; 2-(3-(ethylsulfonyl)-5-isopropoxy Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((1,1,1-tri Fluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) Yl)-5-(trifluoromethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)- 5-( 1-oxyanion group-4,5-dihydro-3H-1l6-isothiazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2 -(3-(Ethylsulfonyl)-5-((3-hydroxy-1-oxytetrahydro-1l6-thiophen-1-ylylene)amino)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((4-oxoanion-1,4l6-xanthene-4-yl subunit) Amino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 4-(5-(ethylsulfonyl)-6-(1-oxo-7- (Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)benzenesulfonyl fluoride; 2-(5-(4-(dimethylphosphoryl)phenyl)-3-( Ethylsulfonylimino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 5'-(ethylsulfonylimino)-6'-(1- Oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)-[3,3'-dipyridine]-6-sulfonyl fluoride; 5-(ethylsulfonyl)-6- (1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3-sulfonyl fluoride; 2-(5-(4-(1,1-difluoroethyl) Phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) -5-(1-(trifluoromethyl)cyclopropyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfon) (Actyl)-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one ; 2-(3-(Ethylsulfonyl)-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-isobutyl-1H-pyrazol-4-yl )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-methoxy-1- Methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(1'-(difluoromethyl)- 5-(Ethylsulfonyl)-6'-oxo-1',6'-dihydro-[3,3'-dipyridine]-6-yl)-7-(trifluoromethyl)phthalazine -1(2H)-one; 2-(3-(ethylsulfonyl)-5-isopropylpyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one ; 2-(5-(3,5-dimethylisoxazol-4-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine-2 -Yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonylimino)-5-(3-(1, 1,2,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 4-(5-(ethylsulfonyl) Yl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenylsulfur fluoride; 2-(3-(ethylsulfon Amino)-5-((1,1,1-trifluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-one; 2-((5-(ethylsulfonylimino)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine -3-yl)oxy)-2-methylpropionitrile; 2-(3-(ethylsulfonyl)-5-((methylsulfinyl)methoxy)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2,2,3,3-tetrafluoropropoxy)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1,1,2-trifluoro-2- (Trifluoromethoxy)ethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5 -(2,2,3,4,4,4-hexafluorobutoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3- (Ethylsulfonyl)-5-(2,2,3,3,3-pentafluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(5-(2,2-Difluoro-2-(trifluoromethoxy)ethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)- Yl)pyridin-3-yl)-2,2-difluorocyclopropane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoro Methyl)phthalazine-2(1H)-yl)pyridin-3-yl)-2,2-dimethylcyclopropane-1-carboxamide; N-(5-(ethylsulfonyl)-6 -(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-fluorocyclopropane-1-carboxamide; N-(5-( Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylcyclopropane-1-methyl Amide; N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-N -Methylcyclobutane carboxamide; 1 -Cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) ring Propane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3 -Yl)-3,3-dimethylcyclobutane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl) Phthalazine-2(1H)-yl)pyridin-3-yl)-3,3-difluorocyclobutane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1 -Oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclobutanecarboxamide; N-(5-(ethylsulfonyl)-6- (1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylcyclobutane-1-carboxamide; N-(5- (Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3-methylcyclobutane-1 -Formamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) -3-oxocyclobutane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H) )-Yl)pyridin-3-yl)cyclopentanecarboxamide; 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl) )Phthalazine-2(1H)-yl)pyridin-3-yl)cyclopentane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7- (Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylcyclopentane-1-carboxamide; N-(5-(ethylsulfonyl)- 6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclohexanecarboxamide; N-(5-(ethylsulfonyl) )-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4-methylcyclohexane-1-carboxamide; N -(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4,4-bis Fluorocyclohexane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl) Pyridin-3-yl)azetidine-3-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine- 2(1H)-yl)pyridin-3-yl)-1-methylazetidine-3-carboxamide; 1-ethyl-N-(5-(ethylsulfonyl)-6- (1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)azetidine-3-carboxamide; N-(5-(ethyl Sulfonyl)-6-(1-oxo-7-(three Fluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxetane e-3-formamide; 3-ethyl-N-(5-(ethylsulfonyl) -6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxetane e-3-formamide; N-(5 -(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylpyrrolidine-3 -Formamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) Tetrahydrofuran-3-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3 -Yl)piperidine-4-methylamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl) )Pyridin-3-yl)-1-methylpiperidine-4-methamide; 1-ethyl-N-(5-(ethylsulfonyl)-6-(1-oxo-7-( Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)piperidine-4-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo) -7-(Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)tetrahydro-2H-pyran-4-carboxamide; N-(5-(ethylsulfonyl) )-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4-fluorotetrahydro-2H-pyran-4-methan Amine; 2-(7-Bromo-3-(ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-7-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-one; 2-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1 ,2-a]pyridin-7-yl)acetonitrile; 3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazole And [1,2-a]pyridine-7-carbonitrile; 2-(3-(ethylsulfonyl)-7-methoxyimidazo[1,2-a]pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 1-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)- Yl)imidazo[1,2-a]pyridin-7-yl)cyclopropane-1-carbonitrile; 2-(3-(ethylsulfonyl)-7-(2,2,2-trifluoroethane Yl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-bromo-3-(ethylsulfonyl) Yl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6 -(Trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 3-(ethylsulfonyl) -2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-6-carbonitrile; 2-(3-(ethyl Sulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridin-6-yl)acetonitrile; 2 -(3-(Ethylsulfonyl)-7-(1-methylcyclopropyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-one; 2-(3-(ethylsulfonyl)-7-(methylamino)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl) ) Phthalazine-1(2H)-one; 7-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine-2 -Yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(3-( 1,1,2,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one ; 7-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3 -d]Pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-2-(trifluoromethyl) Pyrido[2,3-d]pyridazine-8(7H)-one; 5-(ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2, 3-d]pyridazine-7(8H)-yl)nicotinonitrile; 2-(5-(ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2 ,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)acetonitrile; 1-(5-(ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl) Yl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)cyclopropane-1-carbonitrile; 2-((5-(ethylsulfonyl)-6 -(8-oxo-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)oxy)-2-methylpropionitrile; 7-(5-(Difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone; 2-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-(perfluoroethyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(perfluoroethyl)phthalazine-1(2H)-one ; 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(perfluoroethyl Yl)phthalazine-1(2H)-one; 5-(ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)nicotinonitrile ; 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile; 1- (5-(Ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1-carbonitrile ; 5-(Ethylsulfonyl)-6-(1-oxo-7-((trifluoromethyl)sulfonyl)phthalazine-2(1H)-yl)nicotinonitrile; 2-(3- (Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-((trifluoromethyl)sulfonyl)phthalazine-1(2H)-one; 2-(3 -(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-((trifluoromethyl)sulfonyl)phthalazine-1(2H)-one; 1- (5-(Ethylsulfonyl)-6-(1-oxo-7-((trifluoromethyl)sulfonyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane -1-carbonitrile; 7-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3- d]Pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine- 2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4- (Trifluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 2-(5-( Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)acetonitrile; 1-(5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)cyclopropane-1-carbonitrile; 7-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido [2,3-d]Pyridazine-8(7H)-one; 2-(3-(ethylsulfonyl)-5-(ethylthio)pyridin-2-yl)-7-(trifluoromethyl Yl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((2-(trifluoromethyl)cyclopropyl)methoxy)pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-methoxyazetidine-1-yl) )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((1-methyl heterocyclo Butan-3-yl) Oxygen)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1H-1,2,4 -Triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2H -1,2,3-Triazol-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) )-5-(3-(trifluoromethyl)-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-Ketone; 2-(3-(ethylsulfonyl)-5-(4-(2-hydroxy-2-methylpropyl)-1H-1,2,3-triazol-1-yl) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)- 1H-pyrazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-( 3-Methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2- (5-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(2,2,2-trifluoro Ethoxy)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(2,2, 3,3,3-Pentafluoropropoxy)phthalazine-1(2H)-one; 1-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl) )Phthalazine-2(1H)-yl)imidazo[1,2-a]pyrimidin-7-yl)cyclopropane-1-carbonitrile; 2-(3-(ethylsulfonyl)-6-methan Glycine imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-(ethylsulfonyl)-2- (Trifluoromethyl)pyrazolo[1,5-a]pyrimidin-5-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 5-(ethylsulfonyl) -6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[2,1-b]thiazole-2-carbonitrile; 1-(3-(ethyl Sulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyrimidin-6-yl)cyclopropane- 1-carbonitrile; 1-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyrazolo[1, 5-a]pyridin-5-yl)cyclopropane-1-carbonitrile; 2-(2-(ethylsulfonyl)-7-methylpyrazolo[1,5-a]pyrimidin-3-yl )- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-1-methyl-6-(trifluoromethoxy)-1H-indole -2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoro) Methyl)phthalazine-2(1H)-yl)-1H-pyrrolo[2,3-b]pyridin-1-yl)acetonitrile; 2-(5-(ethylsulfonyl)-1-methyl -1H-pyrazolo[3,4-b]pyridin-6-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(7-cyclopropyl-2-( Ethylsulfonyl)imidazo[1,2-a]pyrimidin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) Yl)imidazo[1,2-a]pyrazin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)imidazole And [1,2-b]pyridazin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(bromodifluoromethoxy)-3- (Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(pyridine- 3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(pyridine-2 -Yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-((5-bromopyridin-2-yl)oxy)- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-( Pyrimidine-2-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(( 1-Methyl-1H-pyrazol-3-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,3 -Difluorocyclobutoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2 ,2-Difluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2-(5-( (1,3-Difluoropropan-2-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one ; 2-(3-(Ethylsulfonyl)-5-(neopentyloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 1- (((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)methyl) Cyclopropane-1-carbonitrile; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine- 3 -Yl)oxy)propionitrile; 2-(3-(ethylsulfonyl)-5-((1-fluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-methoxypyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2-fluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine -3-yl)oxy)-2-(methylthio)acetonitrile; 2-(5-((2,2-difluorocyclopropyl)methoxy)-3-(ethylsulfonyl)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 4-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoro) Methyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)butyronitrile; 2-(5-(cyclobutylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,2-difluoropropoxy)-3-(ethylsulfonyl)pyridine-2- Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-fluoroethoxy)pyridin-2-yl) -7-(trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalein Azin-2(1H)-yl)pyridin-3-yl)oxy)-N,N-dimethyl-2-(methylthio)acetamide; 2-ethyl-2-((5-(ethyl Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)butyronitrile; 2-(3-(ethyl) Sulfonyl)-5-isobutoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)- 5-(2,2,2-Trifluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2-bromo- 1,1-Difluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5- ((3-Cyclopropylisoxazol-5-yl)methoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-Ketone; 2-(3-(ethylsulfonyl)-5-(3-methoxycyclobutoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone; 5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl difluoromethanesulfonate Ester; 3-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy )Cyclobutane-1-carbonitrile ; 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl fluoromethanesulfonate; 3- ((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-3-methyl Butyronitrile; 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yltrifluoromethanesulfonic acid Ester; 2-(3-(Ethylsulfonyl)-5-((1-methoxy-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H) -Yl)pyridin-3-yl)oxy)-N,N,2-trimethylpropionamide; 2-(3-(ethylsulfonyl)-5-((3-methyloxetan Alk-3-yl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; (E)-2-(3-(ethylsulfonyl) )-5-(2-(methylimino)propoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-5-((trimethylsilyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-5-(2-oxypropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfon) ((2-methyl-3-oxobutan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(5-(allyloxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2- (3-(Ethylsulfonyl)-5-propoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-ethoxy- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-( Methoxymethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-cyclobutyl-3-(ethylsulfonyl) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,2-difluorocyclopropyl)-3-(ethylsulfonyl) )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2-methyloxetan Alk-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-methyl) Thioetanyl-3-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(1,1-dioxanion) Thietidine 2-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 6-((5-(ethyl Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)nicotinonitrile; 2-(3-(ethyl) Sulfonyl)-5-(thietanyl-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2-(5 -((1,1-Dioxanethioetanyl-3-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(5-((1,1-dioxanylthietane-3-yl)methyl)-3-(ethylsulfonyl)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 7-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl) -2-(Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 2-(3-(N-methylethylsulfonylimino)-5-( 3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3- (N-Methylethylsulfonylimido)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl Yl)phthalazine-1(2H)-one; N-(ethyl((oxo)(2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)- 5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-3-yl)-16-sulfinyl)cyanamide; 2-(3-(N-ethyl Ethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-one; 2-(6-bromo-3-(ethylsulfonylimino)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(6-bromo-3-(N-methylethylsulfonylimino)imidazo[1,2-a]pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one; 1-(3-(ethylsulfonylimino)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2 (1H)-yl)imidazo[1,2-a]pyridin-6-yl)cyclopropane-1-carbonitrile; 3-(ethylsulfonylimino)-2-(1-oxo-7 -(Trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-6-carbonitrile; 2-(6-(cyclopropylamino)-3-(ethyl Sulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one and N-(5-(ethylsulfonyl)-6-(1-oxo- 7-(Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-2-yl)cyclopropanecarboxamide.

本發明的化合物可以作為一種或多種立體異構體存在。各種立體異構體包括對映異構體、非對映異構體、阻轉異構體和幾何異構體。本領域技術人員將理解,當相對於其他一種或多種立體異構體富集時或與其他一種或多種立體異構體分離時,一種立體異構體可以更具活性和/或可以顯示有益的作用。另外,技術人員知道如何分離,富集和/或選擇性地製備所述立體異構體。本發明的化合物可以以立體異構體的混合物、單獨的立體異構體的形式存在或以光學活性形式存在。The compounds of the present invention may exist as one or more stereoisomers. The various stereoisomers include enantiomers, diastereomers, atropisomers and geometric isomers. Those skilled in the art will understand that one stereoisomer can be more active and/or can exhibit beneficial effect. In addition, the skilled person knows how to separate, enrich and/or selectively prepare the stereoisomers. The compound of the present invention may exist in the form of a mixture of stereoisomers, individual stereoisomers, or in an optically active form.

在式(I)化合物是陽離子或能夠形成陽離子的情況下,鹽的陰離子部分可以是無機或有機的。或者,在式I化合物是陰離子或能夠形成陰離子的情況下,鹽的陽離子部分可以是無機或有機的。鹽的無機陰離子部分的實例包括(但不限於)氯化物、溴化物、碘化物、氟化物、硫酸鹽、磷酸鹽、硝酸鹽、亞硝酸鹽、碳酸氫鹽、硫酸氫鹽。鹽的有機陰離子部分的實例包括(但不限於)甲酸鹽、鏈烷酸鹽、碳酸鹽、乙酸鹽、三氟乙酸鹽、三氯乙酸鹽、丙酸鹽、乙醇酸鹽、硫氰酸鹽、乳酸鹽、琥珀酸鹽、蘋果酸鹽、檸檬酸鹽、苯甲酸鹽、肉桂酸鹽、草酸鹽、烷基硫酸鹽、烷基磺酸鹽、芳基磺酸鹽、芳基二磺酸鹽、烷基膦酸鹽、芳基膦酸鹽、芳基二膦酸鹽、對甲苯磺酸鹽和水楊酸鹽。鹽的無機陽離子部分的實例包括(但不限於)鹼金屬和鹼土金屬。鹽的有機陽離子部分的實例包括(但不限於)吡啶、甲胺、咪唑、苯並咪唑、哌啶、磷腈、四甲基銨、四丁基銨、膽鹼和三甲胺。Where the compound of formula (I) is a cation or is capable of forming a cation, the anionic portion of the salt may be inorganic or organic. Alternatively, where the compound of formula I is an anion or is capable of forming an anion, the cationic portion of the salt may be inorganic or organic. Examples of the inorganic anion portion of the salt include, but are not limited to, chloride, bromide, iodide, fluoride, sulfate, phosphate, nitrate, nitrite, bicarbonate, and bisulfate. Examples of the organic anion portion of the salt include (but are not limited to) formate, alkanoate, carbonate, acetate, trifluoroacetate, trichloroacetate, propionate, glycolate, thiocyanate , Lactate, succinate, malate, citrate, benzoate, cinnamate, oxalate, alkyl sulfate, alkyl sulfonate, aryl sulfonate, aryl disulfonate Acid salts, alkyl phosphonates, aryl phosphonates, aryl diphosphonates, p-toluene sulfonate and salicylate. Examples of the inorganic cation portion of the salt include, but are not limited to, alkali metals and alkaline earth metals. Examples of the organic cationic portion of the salt include, but are not limited to, pyridine, methylamine, imidazole, benzimidazole, piperidine, phosphazene, tetramethylammonium, tetrabutylammonium, choline, and trimethylamine.

式I化合物的金屬配合物中的金屬離子最常見的有:第二主族元素的離子,尤其是鈣和鎂;第三和第四主族的,尤其是鋁、錫和鉛;還有第一至第八過渡族的,特別是鉻、錳、鐵、鈷、鎳、銅、鋅等。優選為第四周期的元素和第一至第八過渡族的金屬離子。這裡,金屬可以以它們可以呈現的各種價態存在。The most common metal ions in the metal complexes of the compound of formula I are: the ions of the elements of the second main group, especially calcium and magnesium; the third and fourth main groups, especially aluminum, tin and lead; and the first From the first to the eighth transition group, especially chromium, manganese, iron, cobalt, nickel, copper, zinc, etc. It is preferably an element of the fourth period and a metal ion of the first to eighth transition group. Here, metals can exist in various valence states that they can assume.

在另一實施方案中,本發明提供式I化合物、農業上可接受的鹽、金屬絡合物、結構異構體、立體異構體、非對映異構體、對映異構體、手性異構體、阻轉異構體、構象異構體、旋轉異構體、互變異構體、光學異構體、多晶型物、幾何異構體或其N-氧化物和其與賦形劑、惰性載體或任何其他基本成分(如表面活性劑、添加劑、固體稀釋劑和液體稀釋劑)組成的組合物。In another embodiment, the present invention provides compounds of formula I, agriculturally acceptable salts, metal complexes, structural isomers, stereoisomers, diastereomers, enantiomers, hand Isomers, atropisomers, conformational isomers, rotamers, tautomers, optical isomers, polymorphs, geometric isomers or their N-oxides and their excipients Forms, inert carriers, or any other basic ingredients (such as surfactants, additives, solid diluents and liquid diluents).

式I的化合物(包括其所有立體異構體、N-氧化物和鹽)通常可以以多於一種形式存在。因此,式I包括式I表示的化合物的所有結晶和非結晶形式。非結晶形式包括固體(如蠟和膠)的實施方案以及液體(如溶液和熔體)的實施方案。結晶形式包括實質上表示單晶型的實施方案和表示多晶型混合物(即不同的晶型)的實施方案。術語“多晶型物”是一種特定結晶形式——化學化合物可以以不同結晶形式結晶,這些形式在晶格中具有不同的分子排列和/或構造。儘管多晶型物可以具有相同的化學組成,但由於存在或不存在共結晶水或其他分子(這些共結晶水或其他分子可以在晶格中弱或強地結合),它們在組成上也可以不同。晶型在晶體形狀、密度、硬度、顏色、化學穩定性、熔點、吸濕性、懸浮性、溶解速度和生物利用度等化學、物理和生物特性上存在差異。本領域技術人員將理解,式I表示的化合物的多晶型物相對於另一種多晶型物或式I表示的相同化合物的多晶型物的混合物可顯示出有益效果(例如,適合製備有用的製劑、改善的生物學性能)。由式I表示的化合物的特定多晶型物的製備和分離可以通過本領域技術人員已知的方法實現,包括例如選擇溶劑在合適的溫度下結晶。The compound of formula I (including all its stereoisomers, N-oxides and salts) may generally exist in more than one form. Therefore, Formula I includes all crystalline and non-crystalline forms of the compound represented by Formula I. Amorphous forms include solid (such as wax and glue) embodiments as well as liquid (such as solution and melt) embodiments. The crystalline form includes an embodiment that substantially represents a single crystal form and an embodiment that represents a mixture of polymorphs (ie, different crystal forms). The term "polymorph" is a specific crystalline form-a chemical compound can crystallize in different crystalline forms that have different molecular arrangements and/or structures in the crystal lattice. Although polymorphs can have the same chemical composition, they can also be in composition due to the presence or absence of co-crystal water or other molecules (these co-crystal water or other molecules can be weakly or strongly combined in the crystal lattice). different. There are differences in the chemical, physical and biological properties of crystal forms, such as crystal shape, density, hardness, color, chemical stability, melting point, hygroscopicity, suspension, dissolution rate, and bioavailability. Those skilled in the art will understand that the polymorphic form of the compound represented by formula I can show beneficial effects relative to another polymorphic form or a mixture of polymorphic forms of the same compound represented by formula I (for example, suitable for preparing useful Formulations, improved biological performance). The preparation and isolation of specific polymorphs of the compound represented by Formula I can be achieved by methods known to those skilled in the art, including, for example, selecting a solvent for crystallization at a suitable temperature.

在一個實施方案中,本發明提供了製備式(I)化合物或農業上可接受的鹽的方法。

Figure 02_image001
式(I)In one embodiment, the present invention provides a method of preparing a compound of formula (I) or an agriculturally acceptable salt.
Figure 02_image001
Formula (I)

由式(I)和/或表(I)定義的本發明化合物可以以已知的方式,按照方案1-6中所述的各種方式來製備。可以按照以下方案來製備本發明的化合物,其中除非另有說明,否則每個變量的定義與為式(I)化合物所做的定義相同。The compounds of the present invention defined by formula (I) and/or table (I) can be prepared in a known manner according to various methods described in schemes 1-6. The compounds of the present invention can be prepared according to the following scheme, in which unless otherwise specified, the definition of each variable is the same as that made for the compound of formula (I).

根據本發明的特徵,式(I)化合物(其中所有取代基如前文所定義的)可以通過方案-1、方案-2、方案3、方案-4、方案-5和方案-6或示例中給出的方法製備。具有代表性的步驟如下所示,但是本公開內容不應解釋為限製本發明獲得式(I)化合物的方式的範圍。According to the features of the present invention, the compound of formula (I) (wherein all the substituents are as defined above) can be given in Scheme-1, Scheme-2, Scheme 3, Scheme-4, Scheme-5 and Scheme-6 or examples. The method of preparation. Representative steps are shown below, but the present disclosure should not be construed as limiting the scope of the manner in which the compound of formula (I) can be obtained in the present invention.

根據方案-1,本發明提供了一種用式(2)的羧酸衍生物(其中DE環,G1 , G2 , G3 , G4 , R1 , R2 和n如上文所定義,A1 為N,A2 為CRA (其中RA 為氫,Z為氧))製備式(I)化合物的方法。L和L'為鹵化物、碸和磺酸酯等離去基團。離去基團的非限制性實例有氟、氯、溴、碘、甲基磺酰基、甲苯磺酸酯‎、甲苯磺酸酯‎、三氟甲磺酸酯等。

Figure 02_image017
According to Scheme-1, the present invention provides a carboxylic acid derivative of formula (2) (wherein DE ring, G 1 , G 2 , G 3 , G 4 , R 1 , R 2 and n are as defined above, A 1 is N, A 2 is CR A (where R A is hydrogen and Z is oxygen)) A method for preparing the compound of formula (I). L and L'are leaving groups such as halide, sulfonate and sulfonate. Non-limiting examples of leaving groups are fluorine, chlorine, bromine, iodine, methylsulfonyl, tosylate, tosylate, triflate, and the like.
Figure 02_image017

式(2)化合物的羧基可以轉化為更高反應性的官能團,例如酰氯、混合酐、酰基疊氮、N-酰基苯並三唑、活性酯,或者用肽偶聯劑例如N, N'-二環己基碳二亞胺(DCC)、1-乙基-3-(3-二甲基氨基丙基)碳二亞胺(EDCI)、雙(2-氧代-3-噁唑烷基)次膦酰氯(BOP-Cl)通過原位活化進行轉化。然後在二氯甲烷、二氯乙烷、N,N-二甲基甲酰胺、N,N-二甲基乙酰胺、四氫呋喃、乙腈或它們的混合物等溶劑中與二異丙胺反應,得到式( 3)化合物。可以使用有機非親核鹼,例如三乙胺、乙基二異丙基胺、吡啶、N-甲基吡咯烷、1,8-二氮雜雙環[5.4.0]十一碳-7-烯(DBU)。反應溫度可以優選在約0℃至約150℃的範圍內。The carboxyl group of the compound of formula (2) can be converted into a more reactive functional group, such as acid chloride, mixed anhydride, acyl azide, N-acyl benzotriazole, active ester, or peptide coupling agent such as N, N'- Dicyclohexylcarbodiimide (DCC), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI), bis(2-oxo-3-oxazolidinyl) Phosphinyl chloride (BOP-Cl) is transformed by in-situ activation. Then react with diisopropylamine in a solvent such as dichloromethane, dichloroethane, N,N-dimethylformamide, N,N-dimethylacetamide, tetrahydrofuran, acetonitrile or their mixtures to obtain the formula ( 3) Compound. Organic non-nucleophilic bases can be used, such as triethylamine, ethyldiisopropylamine, pyridine, N-methylpyrrolidine, 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). The reaction temperature may preferably be in the range of about 0°C to about 150°C.

式(3)化合物可以在步驟2的鄰位金屬化反應中用作潛在的羧酸。如此獲得的式(3)的N,N-二異丙基苯甲酰胺衍生物可通過在-50o C至-78o C下在溶劑如乙醚、四氫呋喃中與受阻非親核性二烷基氨基鋰鹼如二異丙基氨基鋰(LDA)、2,2,6,6-四甲基哌啶鋰(LiTMP)、雙(三甲基矽烷基)酰胺鋰(LTSA)或正丁基鋰與N,N,N',N'-四亞甲基二胺(TMEDA)的組合進行甲酰化反應,然後用N,N-二甲基甲酰胺、N-甲基甲酰苯胺、comin試劑或N-甲酰基哌啶淬滅,得到式(4)化合物。The compound of formula (3) can be used as a potential carboxylic acid in the ortho-metallation reaction of step 2. N of formula (3) thus obtained, N- diisopropyl-benzamide derivatives can be prepared by -50 o C to -78 o C in a solvent such as diethyl ether, tetrahydrofuran and the non-nucleophilic hindered dialkyl Lithium amide bases such as lithium diisopropylamide (LDA), lithium 2,2,6,6-tetramethylpiperidine (LiTMP), lithium bis(trimethylsilyl)amide (LTSA) or n-butyl lithium With N,N,N',N'-tetramethylene diamine (TMEDA) for formylation reaction, then use N,N-dimethylformamide, N-methylformanilide, comin reagent Or N-formylpiperidine can be quenched to obtain the compound of formula (4).

式(4)化合物的酸催化環化反應可以通過在純鹽酸或鹽酸和乙酸的混合物中回流10至24小時來進行,反應得到式(5)化合物。The acid-catalyzed cyclization reaction of the compound of formula (4) can be carried out by refluxing in pure hydrochloric acid or a mixture of hydrochloric acid and acetic acid for 10 to 24 hours to obtain the compound of formula (5).

或者,式(5)化合物也可以通過在大約-50o C至大約-78o C的溫度下使用烷基鋰試劑在乙醚、四氫呋喃等溶劑中進行鹵素-金屬交換反應,然後用親電子試劑(例如N,N-二甲基甲酰胺,N-甲基甲酰苯胺,Comin試劑或N-甲酰基哌啶)進行分子內淬滅而製得。Alternatively, the formula (5) compound may be by about -50 to about -78 o C o C is performed at a temperature in a halogen solvent such as ether, tetrahydrofuran and the like using an alkyl lithium reagent - metal exchange reaction, followed by an electrophile ( For example, N,N-dimethylformamide, N-methylformanilide, Comin reagent or N-formyl piperidine) are prepared by intramolecular quenching.

可以使用本領域通常已知的方法,例如《合成科學》(2004,16,315-372)、歐洲專利申請號634404號中公開的方法,用式(7)的肼衍生物進一步處理式(5)化合物以得到式(8)化合物。該反應通常在質子溶劑如水、甲醇、乙醇、異丙醇、正丁醇、異戊醇、羧酸(如乙酸、甲酸或丙酸)、上述溶劑的合適混合物、與水的混合物(例如乙醇水溶液)中進行。當式(7)的肼以鹽(例如鹽酸鹽)的形式使用時,該反應通常可以在鹼例如三乙胺、乙酸鈉或碳酸鉀的存在下進行。該反應可在約0℃至約150℃下進行,時間約為1至48小時。式(7)的化合物的製備已在文獻WO2018008727中有描述。The methods generally known in the art can be used, such as the method disclosed in "Synthetic Science" (2004, 16, 315-372), European Patent Application No. 634404, and the hydrazine derivative of formula (7) is used to further treat formula (5). ) Compound to obtain the compound of formula (8). The reaction is usually carried out in a protic solvent such as water, methanol, ethanol, isopropanol, n-butanol, isoamyl alcohol, carboxylic acid (such as acetic acid, formic acid, or propionic acid), a suitable mixture of the above solvents, and a mixture with water (such as aqueous ethanol). ). When the hydrazine of formula (7) is used in the form of a salt (for example, hydrochloride), the reaction can usually be carried out in the presence of a base such as triethylamine, sodium acetate or potassium carbonate. The reaction can be carried out at about 0°C to about 150°C for about 1 to 48 hours. The preparation of the compound of formula (7) has been described in the document WO2018008727.

式(8)化合物可以方便地在標準的Suzuki交叉偶聯條件下或在Buchwald-Hartwig交叉偶聯條件下分別與硼酸或式(9)的硼酸酯化合物或式(10)化合物偶聯,得到式(I)化合物。Suzuki交叉偶聯反應可以在合適的溶劑(例如四氫呋喃、N,N'-二甲基甲酰胺(DMF)、1,2-二甲氧基乙烷、1,4-二噁烷)或溶劑系統(例如四氫呋喃(THF)/水、1,2-二甲氧基乙烷/水、1,4-二噁烷/水等的混合物)中通過鈀基催化劑(包括但不限於1,1'-雙(二苯基膦基)二茂鐵]二氯鈀(II)或四(三苯基膦)鈀(0)來催化)。該反應通常在碳酸鉀、碳酸銫或磷酸鉀等鹼的存在下進行。反應溫度可優選在環境溫度(20℃)至反應混合物的沸點的範圍內。這種獲得式(I)化合物的方法在文獻(例如《化學學會評論》2014, 43, 412-443或WO2014070978)中有描述。Buchwald-Hartwig交叉偶聯條件是本領域技術人員眾所周知的,許多變化已在文獻中(例如在《有機合成》( 愛思唯爾出版社,2005,第70頁)中命名反應的戰略應用和引用的參考文獻中)有描述,並已被評審通過。通常,該反應是在溶劑或溶劑混合物(例如甲苯)中,在鹼(例如碳酸銫或叔丁醇鈉)的存在下,通過鈀基催化劑(例如乙酸鈀)催化進行,該反應優選在惰性氣氛下,在適當的螯合膦如2,2'-雙(二苯基膦基)-1,1'-聯萘基(BINAP)或Xantphos的存在下進行。反應溫度可優選在環境溫度(20℃)至製備式(I)化合物的過程中反應混合物的沸點的範圍內。The compound of formula (8) can be conveniently coupled with boronic acid or the borate compound of formula (9) or the compound of formula (10) under standard Suzuki cross-coupling conditions or Buchwald-Hartwig cross-coupling conditions, respectively, to obtain Compound of formula (I). The Suzuki cross-coupling reaction can be carried out in a suitable solvent (such as tetrahydrofuran, N,N'-dimethylformamide (DMF), 1,2-dimethoxyethane, 1,4-dioxane) or solvent system (For example, mixtures of tetrahydrofuran (THF)/water, 1,2-dimethoxyethane/water, 1,4-dioxane/water, etc.) are passed through a palladium-based catalyst (including but not limited to 1,1'- Bis(diphenylphosphino)ferrocene]dichloropalladium(II) or tetrakis(triphenylphosphine)palladium(0) to catalyze). This reaction is usually carried out in the presence of a base such as potassium carbonate, cesium carbonate, or potassium phosphate. The reaction temperature may preferably be in the range of ambient temperature (20°C) to the boiling point of the reaction mixture. This method of obtaining the compound of formula (I) is described in the literature (for example, "Review of the Chemical Society" 2014, 43, 412-443 or WO2014070978). The Buchwald-Hartwig cross-coupling conditions are well known to those skilled in the art, and many changes have been made in the literature (for example, in "Organic Synthesis" (Elsevier Press, 2005, p. 70) the strategic applications and citations of naming reactions References) have descriptions and have been reviewed and approved. Generally, the reaction is carried out in a solvent or solvent mixture (such as toluene) in the presence of a base (such as cesium carbonate or sodium tert-butoxide) and catalyzed by a palladium-based catalyst (such as palladium acetate). The reaction is preferably carried out in an inert atmosphere. Next, in the presence of a suitable chelating phosphine such as 2,2'-bis(diphenylphosphino)-1,1'-binapthyl (BINAP) or Xantphos. The reaction temperature may preferably be in the range of ambient temperature (20°C) to the boiling point of the reaction mixture in the process of preparing the compound of formula (I).

在一個實施方案中,式(I)的化合物可以根據如下所述的方案2製備,其中DE環、G1 、G2 、G3 、G4 、R1 、R2 和n如上文所定義,A1 為N且A2 為CRA (其中RA 為氫,Z為氧)。L和L1 為鹵化物、碸和磺酸酯等離去基團。離去基團的非限制性實例有氟、氯、溴、碘、甲基磺酰基、甲苯磺酸酯、甲苯磺酸酯、三氟甲磺酸酯等。

Figure 02_image019
In one embodiment, the compound of formula (I) can be prepared according to Scheme 2 as described below, wherein the DE ring, G 1 , G 2 , G 3 , G 4 , R 1 , R 2 and n are as defined above, A 1 is N and A 2 is CR A (wherein R A is hydrogen, Z is oxygen). L and L 1 are leaving groups such as halide, sulfonate and sulfonate. Non-limiting examples of leaving groups are fluorine, chlorine, bromine, iodine, methylsulfonyl, tosylate, tosylate, triflate and the like.
Figure 02_image019

可以使用本領域中通常已知的方法以及如方案1的第4步中所述的方法,用水合肼處理式(5)化合物以獲得式(11)化合物。The compound of formula (5) can be treated with hydrazine hydrate to obtain the compound of formula (11) using methods generally known in the art and the method described in step 4 of Scheme 1.

式(8)化合物可以通過在合適的鹼例如有機鹼、鹼金屬碳酸鹽、鹼金屬氫化物等的存在下,在合適的溶劑(例如醚、芳族烴、腈、非質子極性溶劑及其混合物)中使式(11)化合物與式(12)化合物反應來製備。該反應可以在約50℃至約150℃的溫度下進行,反應時間約為1至48小時。在該反應中還可以使用合適的金屬催化劑和配體。合適的金屬催化劑可包括碘化銅(I)、溴化銅(I)、氯化銅(I)、氧化銅(I)、三氟甲磺酸銅(I)苯絡合物、四(乙腈)六氟磷酸銅(I)、噻吩-2-羧酸銅(I)等; 雙(環辛二烯)鎳(0)、鎳催化劑,例如氯化鎳(II)、乙酸鈀(II)、四(三苯基膦)鈀(0)。合適的配體可包括三苯基膦、4,5-雙(二苯基膦基)-9,9-二甲基氧雜蒽、二茂鐵、2-二環己基膦基-2′, 4′,6′-三異丙基聯苯、2-二環己基膦基-2',6'-二甲氧基聯苯、2-氨基乙醇、8-羥基喹啉、1,10-菲咯啉、反式1,2-環己二胺、反式-N,N'-二甲基環己烷-1,2-二胺和N,N'-二甲基乙二胺等。優選反應溫度為環境溫度(20℃)至反應混合物的沸點。The compound of formula (8) can be prepared in the presence of a suitable base such as organic bases, alkali metal carbonates, alkali metal hydrides, etc., in a suitable solvent (such as ethers, aromatic hydrocarbons, nitriles, aprotic polar solvents and mixtures thereof ) Is prepared by reacting a compound of formula (11) with a compound of formula (12). The reaction can be carried out at a temperature of about 50°C to about 150°C, and the reaction time is about 1 to 48 hours. Suitable metal catalysts and ligands can also be used in this reaction. Suitable metal catalysts may include copper(I) iodide, copper(I) bromide, copper(I) chloride, copper(I) oxide, copper(I) triflate, benzene complex, tetrakis(acetonitrile) ) Copper (I) hexafluorophosphate, copper (I) thiophene-2-carboxylate, etc.; bis(cyclooctadiene) nickel (0), nickel catalysts, such as nickel chloride (II), palladium acetate (II), Tetrakis(triphenylphosphine)palladium(0). Suitable ligands may include triphenylphosphine, 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene, ferrocene, 2-dicyclohexylphosphino-2', 4',6'-triisopropylbiphenyl, 2-dicyclohexylphosphino-2',6'-dimethoxybiphenyl, 2-aminoethanol, 8-hydroxyquinoline, 1,10-phenanthrene Pyroline, trans-1,2-cyclohexanediamine, trans-N,N'-dimethylcyclohexane-1,2-diamine and N,N'-dimethylethylenediamine, etc. Preferably, the reaction temperature is from ambient temperature (20°C) to the boiling point of the reaction mixture.

式(12)的化合物可以根據《有機化學學報》(68(12), 4918, 2003)或WO 2013/086397中所述的方法合成。The compound of formula (12) can be synthesized according to the method described in Chinese Journal of Organic Chemistry (68(12), 4918, 2003) or WO 2013/086397.

可以按通用方案-1第5步所述的方法將式(8)化合物轉化為式(I)化合物。The compound of formula (8) can be converted to the compound of formula (I) according to the method described in step 5 of general scheme-1.

方案3描述了式(I)化合物的製備,其中DE環、G1 、G2 、G3 、G4 、R1 、R2 和n如上文所定義。A1 為N且A2 為CRA ,其中RA 為取代或未取代的烷基、取代或未取代的環烷基,Z為氧。L和L1 為鹵化物、碸和磺酸酯等離去基團。離去基團的非限制性實例有氟、氯、溴、碘、甲基磺酰基、甲苯磺酸酯、甲苯磺酸酯、三氟甲磺酸酯等。

Figure 02_image021
Scheme 3 describes the preparation of the compound of formula (I), wherein the DE ring, G 1 , G 2 , G 3 , G 4 , R 1 , R 2 and n are as defined above. A 1 is N and A 2 is CR A, wherein R A is a substituted or unsubstituted alkyl group, a substituted or unsubstituted cycloalkyl group, Z is oxygen. L and L 1 are leaving groups such as halide, sulfonate and sulfonate. Non-limiting examples of leaving groups are fluorine, chlorine, bromine, iodine, methylsulfonyl, tosylate, tosylate, triflate and the like.
Figure 02_image021

可以在適當的溶劑如乙醇、甲醇、正丙醇中,通過與適當的氨基甲酸酯反應,將式(13)的酰基取代的酚化合物轉化為式(14)的N-羰酰腙。優選反應溫度為約0℃至約150℃的範圍內。The acyl-substituted phenol compound of formula (13) can be converted into the N-carbonyl hydrazone of formula (14) by reacting with a suitable carbamate in a suitable solvent such as ethanol, methanol, and n-propanol. The reaction temperature is preferably in the range of about 0°C to about 150°C.

步驟2是通過在0℃至25℃下在四氫呋喃、1,4-二噁烷等溶劑中使用乙酸鉛(IV)或在二氯甲烷或氯仿等溶劑中使用[雙(乙酰氧基)碘]苯氧化式(14)的N-羰基腙來製備式(15)的二酰基衍生物。Step 2 is by using lead(IV) acetate in solvents such as tetrahydrofuran and 1,4-dioxane or [bis(acetoxy)iodide] in solvents such as dichloromethane or chloroform at 0°C to 25°C The N-carbonyl hydrazone of formula (14) is oxidized with benzene to prepare the diacyl derivative of formula (15).

可以使用本領域已知的方法以及按方案1第4步所述的方法,將式(15)的二酰基衍生物用水合肼處理得到式(11a)化合物。The method known in the art and the method described in step 4 of Scheme 1 can be used to treat the diacyl derivative of formula (15) with hydrazine hydrate to obtain the compound of formula (11a).

可以按照方案2第2步和第3步所述的方法將式(11a)化合物轉化為式(I)化合物。The compound of formula (11a) can be converted into the compound of formula (I) according to the methods described in the second and third steps of Scheme 2.

在另一個實施方案中,本發明的式(I)化合物可以按方案-4中所述的方法製備,其中環DE、G1 、G2 、G3 、G4 、R1 、R2 和n如上文所定義,且A2 為N;A1 為CRA (其中RA 為氫,Z為氧)。L是鹵化物、碸和磺酸酯等離去基團。離去基團的非限制性實例有氟、氯、溴、碘、甲基磺酰基、甲苯磺酸酯、甲苯磺酸酯、三氟甲磺酸酯等。

Figure 02_image023
In another embodiment, the compound of formula (I) of the present invention can be prepared according to the method described in Scheme-4, wherein the rings DE, G 1 , G 2 , G 3 , G 4 , R 1 , R 2 and n as defined above, and A 2 is N; A 1 is CR A (wherein R A is hydrogen, Z is oxygen). L is a leaving group such as halide, sulfonate and sulfonate. Non-limiting examples of leaving groups are fluorine, chlorine, bromine, iodine, methylsulfonyl, tosylate, tosylate, triflate and the like.
Figure 02_image023

式(21)的化合物可以由式(16)化合物(其中R表示氫原子或低級烷基)和甲酰胺(18)或甲脒(19)等及其鹽等甲酰胺同等物製備。在一個實例中(其中R為氫原子),該反應可通過在50℃至溶劑的沸點的溫度範圍內,在有或沒有酸(如乙酸,甲酸)存在下,將式(16)化合物與甲酰胺混合來進行,得到式(21)的化合物。在另一個實例中(其中R是烷基),該反應可以通過在50℃至溶劑的沸點的溫度範圍內,在有或沒有酸(如乙酸,甲酸)存在下,將式(16)化合物與乙酸甲脒混合來進行,得到式(21)的化合物。The compound of the formula (21) can be prepared from the compound of the formula (16) (wherein R represents a hydrogen atom or a lower alkyl group) and formamide (18) or formamidine (19) and their salts and other formamide equivalents. In one example (wherein R is a hydrogen atom), the reaction can be achieved by combining the compound of formula (16) with a The amides are mixed to obtain the compound of formula (21). In another example (wherein R is an alkyl group), the reaction can be achieved by combining the compound of formula (16) with the solvent at a temperature ranging from 50°C to the boiling point of the solvent in the presence or absence of acid Formamidine acetate is mixed to obtain a compound of formula (21).

式(21)化合物也可以在存在或不存在溶劑(例如乙酸酐)的情況下用式(17)化合物和式(20)的原甲酸酯(R'代表低級烷基)製備。反應溫度可優選為環境溫度(20℃)至反應混合物的沸點。The compound of formula (21) can also be prepared by using the compound of formula (17) and the orthoformate of formula (20) (R' represents a lower alkyl group) in the presence or absence of a solvent (such as acetic anhydride). The reaction temperature may preferably be from ambient temperature (20°C) to the boiling point of the reaction mixture.

可以按照方案2的第2步和第3步所述的方法用化合物(22)製備式(I)化合物。The compound of formula (I) can be prepared from compound (22) according to the methods described in step 2 and step 3 of Scheme 2.

在一個實施方案中,式(I)化合物可以按方案-5中所述的方法製備,其中DE環、G1 、G2 、G3 、G4 、A1 、A2 、R1 、R2 和n如上文所定義,Z為硫原子。

Figure 02_image025
In one embodiment, the compound of formula (I) can be prepared according to the method described in Scheme-5, wherein DE ring, G 1 , G 2 , G 3 , G 4 , A 1 , A 2 , R 1 , R 2 And n are as defined above, and Z is a sulfur atom.
Figure 02_image025

式(I)化合物(其中Z=S)可以通過方案1第5步所述的方法,通常在50至160o C的溫度下,在溶劑(如N,N-二甲基甲酰胺或甲苯)中使式(23)化合物(Z=O)與可以轉移硫原子的合適的試劑(例如勞森試劑)反應,獲得式(24)的化合物,然後按照方案-1第5步將其進一步轉化為式(I)的化合物來製備。這樣的轉化對於本領域技術人員是眾所周知的,例如在《四面體》(2007, 63, 11862)或US20120309796中有描述。The compound of formula (I) (where Z=S) can be passed through the method described in step 5 of Scheme 1, usually at a temperature of 50 to 160 o C in a solvent (such as N,N-dimethylformamide or toluene) The compound of formula (23) (Z=O) is reacted with a suitable reagent (such as Lawson's reagent) that can transfer sulfur atoms to obtain the compound of formula (24), which is then further converted into The compound of formula (I) is prepared. Such transformations are well known to those skilled in the art, and are described in "Tetrahedron" (2007, 63, 11862) or US20120309796, for example.

或者,如方案6所示,可以根據方案2的第2步和第3步所述的方法製備式(I)化合物,其中L'、A1 、A2 、G1 -G4 、Z、R1 、R2 和Q如上文所定義。化合物25可以根據方案4的第1步或第1步或方案2的第1步所述的方法合成。

Figure 02_image027
Alternatively, as shown in Scheme 6, the compound of formula (I) can be prepared according to the methods described in steps 2 and 3 of scheme 2, wherein L', A 1 , A 2 , G 1 -G 4 , Z, R 1 , R 2 and Q are as defined above. Compound 25 can be synthesized according to the method described in Step 1 or Step 1 of Scheme 4 or Step 1 of Scheme 2.
Figure 02_image027

如方案7所示,本發明提供了一種用式(27)的鄰氨基苯甲酸衍生物製備式(I)化合物的方法,其中DE環、G1 、G2 、G3 、G4 、R1 、R2 和n如上所定義,A1 為N,A2 為N且Z為氧。L是離去基團。離去基團的非限制性實例有氟、氯、溴、碘、甲基磺酰基、‎甲苯磺酸酯‎、‎甲苯磺酸酯‎、三氟甲磺酸酯等。As shown in Scheme 7, the present invention provides a method for preparing a compound of formula (I) by using an anthranilic acid derivative of formula (27), wherein DE ring, G 1 , G 2 , G 3 , G 4 , R 1 , R 2 and n are as defined above, A 1 is N, A 2 is N, and Z is oxygen. L is a leaving group. Non-limiting examples of leaving groups are fluorine, chlorine, bromine, iodine, methylsulfonyl, tosylate, tosylate, triflate and the like.

式(28)化合物可以在適當的非質子溶劑(如四氫呋喃、1,4-二噁烷、二氯甲烷、二氯乙烷)中,使用三光氣、光氣等試劑,用相應的鄰氨基苯甲酸(27)衍生物來製備。式(29)化合物可通過在適當溶劑(如四氫呋喃、1,4-二氧六環等)中使用有機鹼(如三乙胺、二異丙基乙胺)或無機鹼(如叔丁醇鉀、叔丁醇鈉),用式(32)的胺處理式(28)化合物來製備。The compound of formula (28) can be used in a suitable aprotic solvent (such as tetrahydrofuran, 1,4-dioxane, dichloromethane, dichloroethane), using reagents such as triphosgene, phosgene, and the corresponding o-aminobenzene Formic acid (27) derivatives were prepared. The compound of formula (29) can be prepared by using an organic base (such as triethylamine, diisopropylethylamine) or an inorganic base (such as potassium tert-butoxide) in a suitable solvent (such as tetrahydrofuran, 1,4-dioxane, etc.) , Sodium tert-butoxide), prepared by treating a compound of formula (28) with an amine of formula (32).

可以通過在酸性條件下(如6N鹽酸)使用重氮化試劑(如亞硝酸鈉、亞硝酸叔丁酯),用式(29)化合物製備式(30)化合物。然後在0℃至溶劑沸點的溫度範圍內,在合適的無機鹼(例如氫化鈉、碳酸鉀、叔丁醇鉀、叔丁醇鈉)存在下,在適合的溶劑(例如N,N-二甲基甲酰胺、N,N-二甲基乙酰胺、四氫呋喃、乙腈)中,使式(30)化合物與相應的烷基硫醇反應,得到式(30-a)化合物。The compound of formula (30) can be prepared from the compound of formula (29) by using a diazotizing reagent (such as sodium nitrite, tert-butyl nitrite) under acidic conditions (such as 6N hydrochloric acid). Then in the temperature range of 0 ℃ to the boiling point of the solvent, in the presence of a suitable inorganic base (such as sodium hydride, potassium carbonate, potassium tert-butoxide, sodium tert-butoxide) in a suitable solvent (such as N,N-dimethyl The compound of formula (30) is reacted with the corresponding alkyl mercaptan in methyl formamide, N,N-dimethylacetamide, tetrahydrofuran, acetonitrile) to obtain the compound of formula (30-a).

式(31)的化合物可以根據《有機化學學報》(68(12), 4918, 2003)或WO 2013/086397中所述的方法,用式30或(30-a)的化合物製備。The compound of formula (31) can be prepared with the compound of formula 30 or (30-a) according to the method described in "Acta Organic Chemistry" (68(12), 4918, 2003) or WO 2013/086397.

可以按照通用方案-1第5步所述的方法將式(31)化合物轉化為式(I)化合物。

Figure 02_image029
The compound of formula (31) can be converted to the compound of formula (I) according to the method described in step 5 of general scheme-1.
Figure 02_image029

式(23)化合物(其中L為氯、溴或碘)可以用有機金屬物質(例如丁基鋰或有機鎂化合物)處理,然後用硼酸酯化合物B(X)3 (其中X為C1 -C6 烷基基團)處理,得到式(33)的化合物。該反應優選在-78℃至25℃下在四氫呋喃等無水非質子溶劑中進行。根據硼酸酯的性質和隨後的處理條件,可以將式(33)化合物分離出硼酸(其中BX2 為-B(OH)2 )或者是二烷基硼酸酯。The compound of formula (23) (wherein L is chlorine, bromine or iodine) can be treated with organometallic substances (such as butyl lithium or organomagnesium compounds), and then with borate compound B(X) 3 (where X is C 1- C 6 alkyl group) to obtain the compound of formula (33). This reaction is preferably carried out in an anhydrous aprotic solvent such as tetrahydrofuran at -78°C to 25°C. According to the properties of the borate and the subsequent processing conditions, the compound of formula (33) can be separated into boric acid (where BX 2 is -B(OH) 2 ) or dialkyl borate.

或者,可以通過以雙頻哪醇二硼烷(B2Pin2)為試劑的鈀催化反應將頻哪醇硼酸酯官能團引入式(23)的化合物上(其中L為氯、溴、碘或三氟甲烷磺酸鹽)。該反應產生式(33)的環狀硼酸鹽化合物(其中BX2

Figure 02_image031
)。該反應可以在非質子溶劑中,在鹼,優選弱鹼(如乙酸鉀)和催化劑(如[1,1'-雙(二苯基膦基)二茂鐵]二氯鈀(II)或Pd (dppf)Cl2 )存在下進行。反應優選在80℃至溶劑沸點的溫度下進行。Alternatively, the pinacol borate functional group can be introduced into the compound of formula (23) (where L is chlorine, bromine, iodine or trifluoromethane) through a palladium catalyzed reaction using bipinacol diborane (B2Pin2) as a reagent. Sulfonate). This reaction produces a cyclic borate compound of formula (33) (where BX 2 is
Figure 02_image031
). The reaction can be carried out in an aprotic solvent, in a base, preferably a weak base (such as potassium acetate) and a catalyst (such as [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II)) or Pd (dppf)Cl 2 ) in the presence of. The reaction is preferably carried out at a temperature from 80°C to the boiling point of the solvent.

通過在優選的溶劑(如四氫呋喃)中用氧化劑(優選過氧化氫或脲絡合物)處理,可以將式(33)的化合物轉化為式(34)的化合物。By treating with an oxidizing agent (preferably hydrogen peroxide or urea complex) in a preferred solvent (such as tetrahydrofuran), the compound of formula (33) can be converted into the compound of formula (34).

隨後,可在鹼(例如氫化鈉、碳酸鉀或碳酸銫)的存在下,在惰性溶劑(如四氫呋喃、N,N-二甲基甲酰胺或乙腈)中用通式為RXa (其中Xa 優選為Br、I或三氟甲磺酸鹽)的烷化劑處理式(34)化合物,得到通式(I)的化合物。Subsequently, in the presence of a base (such as sodium hydride, potassium carbonate or cesium carbonate) in an inert solvent (such as tetrahydrofuran, N,N-dimethylformamide or acetonitrile), the general formula is RX a (where X a The compound of formula (34) is treated with an alkylating agent preferably Br, I or triflate) to obtain a compound of general formula (I).

或者,可以在20°C至120℃範圍內,在氫氧化物鹽(如氫氧化銫、氫氧化鈉或氫氧化鉀)、鈀源(如Pd(dba)2 )和膦配體(如tBu-XPhos (CAS 564483-19-8))和式ROH化合物的存在下,在溶劑如1,4-二噁烷或四氫呋喃中,將式(23)化合物進行鈀催化的羥基化,轉化為式(34)的化合物。Alternatively, it can be used in the range of 20°C to 120°C in hydroxide salts (such as cesium hydroxide, sodium hydroxide or potassium hydroxide), palladium sources (such as Pd(dba) 2 ) and phosphine ligands (such as tBu -XPhos (CAS 564483-19-8)) and the compound of formula ROH, in a solvent such as 1,4-dioxane or tetrahydrofuran, the compound of formula (23) is subjected to palladium-catalyzed hydroxylation and converted to formula ( 34) The compound.

可以按方案1第5步所述的方法,在常規反應條件下,使用氨基甲酸叔丁酯作為胺配體,將式(23)化合物進行鈀催化的Buchwald-Hartwig交叉偶聯,轉化為式(35)的化合物。然後按照標準方法在酸性條件下(使用鹽酸、三氟乙酸、乙酸或路易斯酸(如溴化鋅)、氯化錫等); 在一種或多種溶劑(例如二氯甲烷、四氫呋喃、甲醇、水、甲苯、1,4-二噁烷或它們的混合物)中使式(35)化合物中的被保護的氨基如氨基甲酸叔丁酯部分脫保護,得到式(36)化合物。

Figure 02_image033
According to the method described in Step 5 of Scheme 1, under conventional reaction conditions, using tert-butyl carbamate as the amine ligand, the compound of formula (23) can be subjected to palladium-catalyzed Buchwald-Hartwig cross-coupling to convert it to formula ( 35) The compound. Then follow standard methods under acidic conditions (using hydrochloric acid, trifluoroacetic acid, acetic acid or Lewis acid (such as zinc bromide), tin chloride, etc.); in one or more solvents (such as dichloromethane, tetrahydrofuran, methanol, water, The protected amino group in the compound of formula (35), such as tert-butyl carbamate, is partially deprotected in toluene, 1,4-dioxane or a mixture thereof, to obtain a compound of formula (36).
Figure 02_image033

可以通過在一種或多種溶劑如N,N-二甲基甲酰胺、N,N-二甲基乙酰胺、四氫呋喃或其混合物中用鹼(例如碳酸銫、碳酸鉀、碳酸鈉等)和式R2 -L化合物將式(35)化合物烷基化,得到式(35a)的化合物。然後可在標準條件下按方案-9第3步所述的方法使式(35a)化合物脫保護,得到式(36a)化合物。It can be used in one or more solvents such as N,N-dimethylformamide, N,N-dimethylacetamide, tetrahydrofuran or mixtures thereof with a base (such as cesium carbonate, potassium carbonate, sodium carbonate, etc.) and formula R The 2- L compound alkylates the compound of formula (35) to obtain the compound of formula (35a). Then, the compound of formula (35a) can be deprotected according to the method described in step 3 of Scheme-9 under standard conditions to obtain the compound of formula (36a).

可在一般反應條件下按方案9第2步所述的方法將式(36a)化合物進一步烷基化,得到式(I)化合物。The compound of formula (36a) can be further alkylated according to the method described in step 2 of Scheme 9 under general reaction conditions to obtain the compound of formula (I).

最後,可在酰胺偶聯條件(使用羧酸氯化物或使用肽偶聯劑如雙(2-氧代-3-噁唑烷基)次膦酰氯、N,N'-二環己基碳二亞胺、1-乙基-3-(3-二甲基氨基丙基)碳二亞胺、1-[雙(二甲基氨基)亞甲基]-1H-1,2,3-三唑並[4,5-b]吡啶鎓3-氧化物六氟磷酸鹽原位活化羧酸)下,在溶劑如二氯甲烷、二氯乙烷、N,N-二甲基甲酰胺、N,N-二甲基乙酰胺、四氫呋喃、乙腈或它們的混合物中用式(36)或式(36a)化合物獲得式(I)化合物。有機非親核鹼(例如三乙胺,乙基二異丙基胺,吡啶,N-甲基吡咯烷,1,8-二氮雜雙環[5.4.0]十一烷基-7-烯)可用於這一步驟。該反應優選在約0℃至約150℃的溫度下進行。Finally, it can be used in amide coupling conditions (using carboxylic acid chloride or using peptide coupling agents such as bis(2-oxo-3-oxazolidinyl) phosphinyl chloride, N,N'-dicyclohexylcarbodiimide Amine, 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide, 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo [4,5-b]pyridinium 3-oxide hexafluorophosphate in-situ activated carboxylic acid), in a solvent such as dichloromethane, dichloroethane, N,N-dimethylformamide, N,N -Dimethylacetamide, tetrahydrofuran, acetonitrile or their mixtures are used in formula (36) or formula (36a) to obtain the compound of formula (I). Organic non-nucleophilic bases (eg triethylamine, ethyldiisopropylamine, pyridine, N-methylpyrrolidine, 1,8-diazabicyclo[5.4.0]undecyl-7-ene) Can be used for this step. The reaction is preferably carried out at a temperature of about 0°C to about 150°C.

可以通過上述方法製備式(I)化合物、其立體異構體、鹽和N-氧化物以及在合成過程中的前體。如果不能通過上述途徑製備單獨的化合物,則可以通過其他化合物(I)或相應的前體的衍生化或通過對所述合成路線進行常規改變來製備它們。例如,在個別情況下,某些式(I)化合物可以方便地由其他式(I)化合物通過衍生反應(例如通過酯水解、酰胺化、酯化、醚裂解、烯化、還原、氧化等反應)或通過對所述合成路線 進行常規改變製得。The compound of formula (I), its stereoisomers, salts and N-oxides and precursors in the synthesis process can be prepared by the above-mentioned methods. If the individual compounds cannot be prepared by the above-mentioned route, they can be prepared by derivatization of other compounds (I) or corresponding precursors or by conventional changes to the synthetic route. For example, in individual cases, certain compounds of formula (I) can be conveniently derived from other compounds of formula (I) through derivatization reactions (such as ester hydrolysis, amidation, esterification, ether cleavage, olefination, reduction, oxidation, etc.) ) Or through conventional changes to the synthetic route.

反應混合物按慣例進行處理,例如與水混合、分離相、對粗產品進行色譜純化(如果合適的話)。一些中間體和終產物以無色或略帶褐色的黏性油的形式獲得,這些油需要在減壓和適當的高溫下被純化或除去揮發性成分。如果中間體和最終產物以固體形式獲得,也可以通過重結晶或消化進行提純。The reaction mixture is processed as usual, such as mixing with water, separating the phases, and chromatographic purification of the crude product (if appropriate). Some intermediates and final products are obtained in the form of colorless or slightly brown viscous oils, which need to be purified or volatile components removed under reduced pressure and moderately high temperatures. If the intermediates and final products are obtained in solid form, they can also be purified by recrystallization or digestion.

如果某個化合物(I)不能通過上述途徑獲得,則可以通過將其他化合物(I)衍生化來製備它們。但是,如果合成產生的是異構體的混合物,則通常不需要分離,因為在某些情況下,單個異構體可以在後處理使用期間或施用期間(例如在光,酸或鹼的作用下)相互轉化。此類轉化也可以在使用後(例如在處理過的植物中或在要控制的有害真菌中)進行。If a certain compound (I) cannot be obtained through the above-mentioned route, they can be prepared by derivatizing other compounds (I). However, if the synthesis produces a mixture of isomers, separation is usually not necessary, because in some cases, a single isomer can be used during post-treatment or during application (for example, under the action of light, acid or base). ) Mutual transformation. Such transformation can also be carried out after use (for example in treated plants or in harmful fungi to be controlled).

在一個實施方案中,本發明提供了用於控製或預防無脊椎害蟲的組合物。該組合物包含生物有效量的式(I)化合物或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、金屬絡合物、多晶型物或N-氧化物,以及至少一種選自表面活性劑和助劑其他組分。In one embodiment, the present invention provides a composition for controlling or preventing invertebrate pests. The composition contains a biologically effective amount of the compound of formula (I) or its agriculturally acceptable salt, isomer/structural isomer, stereoisomer, diastereomer, enantiomer, mutual Mutants, metal complexes, polymorphs or N-oxides, and at least one other component selected from surfactants and auxiliary agents.

在另一個實施方案中,該組合物另外包含至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物農藥、除草劑、植物生長調節劑、抗生素、肥料或營養物的生物。In another embodiment, the composition additionally comprises at least one biological agent selected from the group consisting of suicide fungicides, insecticides, nematicides, acaricides, biopesticides, herbicides, plant growth regulators, antibiotics, fertilizers or nutrients. .

在另一個實施方案中,本發明提供的式(I)化合物或其N-氧化物和鹽為常規類型的農業化學組合物,例如溶液、乳液、懸浮液、粉劑、粉末、糊劑、顆粒、壓制劑、膠囊及其混合物。 組合物類型的實例是懸浮液(例如SC、OD、FS)、可乳化濃縮物(例如EC)、乳液(例如EW、EO、ES、ME)、膠囊(例如CS、ZC)、糊劑、錠劑、可濕性粉劑或粉劑(例如WP,SP,WS,DP,DS)、壓制劑(例如BR、TB、DT)、顆粒(例如WG、SG、GR、FG、GG、MG)、殺蟲製品(例如LN),以及用於處理植物繁殖材料如種子(例如GF)的凝膠製劑。這些和其他組合物類型在《農藥製劑類型和國際編碼系統》(技術專論第2號.61h版.2008年5月.國際作物生命協會)有定義。In another embodiment, the compound of formula (I) or its N-oxides and salts provided by the present invention are conventional agrochemical compositions, such as solutions, emulsions, suspensions, powders, powders, pastes, granules, Compressed preparations, capsules and mixtures thereof. Examples of composition types are suspensions (e.g. SC, OD, FS), emulsifiable concentrates (e.g. EC), emulsions (e.g. EW, EO, ES, ME), capsules (e.g. CS, ZC), pastes, tablets Formulations, wettable powders or powders (such as WP, SP, WS, DP, DS), compressed formulations (such as BR, TB, DT), granules (such as WG, SG, GR, FG, GG, MG), insecticides Products (such as LN), and gel formulations used to treat plant propagation materials such as seeds (such as GF). These and other composition types are defined in "Pesticide Formulation Types and International Coding System" (Technical Monograph No. 2.61h Edition. May 2008. International Crop Life Association).

該組合物以已知的方式製備,製備方法在例如莫列特和格魯伯 貝恩(Mollet and Grube mann),《製劑技術》,Wiley VCH出版社,魏因海姆,2001; 或諾爾斯(Knowles),《作物保護產品製劑的新發展》(Agrow Reports DS243,T&F lnforma,倫敦,2005)中有描述。The composition is prepared in a known manner, and the preparation method is described in, for example, Mollet and Grube mann, "Formulation Technology", Wiley VCH Press, Weinheim, 2001; or Knowles (Knowles ), described in "New Development of Crop Protection Product Formulations" (Agrow Reports DS243, T&F lnforma, London, 2005).

合適的助劑有溶劑、液體載體、固體載體或填料、表面活性劑、分散劑、乳化劑、濕潤劑、佐劑、增溶劑、滲透促進劑、保護膠體、黏合劑、增稠劑、保濕劑、驅蟲劑、引誘劑、餵食興奮劑、增容劑、殺菌劑、抗-凍結劑、消泡劑、著色劑、增黏劑和黏合劑。Suitable auxiliary agents include solvents, liquid carriers, solid carriers or fillers, surfactants, dispersants, emulsifiers, wetting agents, adjuvants, solubilizers, penetration enhancers, protective colloids, binders, thickeners, and humectants , Insect repellent, attractant, feeding stimulant, compatibilizer, fungicide, anti-freezing agent, defoamer, coloring agent, viscosity increasing agent and adhesive.

合適的溶劑和液體載體有水和有機溶劑,例如中沸點至高沸點的礦物油餾分,例如煤油、柴油;植物油或動物油;脂族、環狀和芳族烴,例如甲苯、石蠟、四氫化萘、烷基化萘;醇類,例如乙醇、丙醇、丁醇、苯甲醇、環己醇;乙二醇;DMSO;酮類,例如環己酮;酯類,例如乳酸、碳酸酯、脂肪酸酯、γ-丁內酯;脂肪酸;膦酸酯;胺;醯胺類,例如N-甲基吡咯烷酮、脂肪酸二甲基醯胺;及其混合物。Suitable solvents and liquid carriers are water and organic solvents, such as medium to high boiling point mineral oil fractions, such as kerosene, diesel; vegetable oil or animal oil; aliphatic, cyclic and aromatic hydrocarbons, such as toluene, paraffin, tetralin, Alkylated naphthalene; alcohols, such as ethanol, propanol, butanol, benzyl alcohol, cyclohexanol; ethylene glycol; DMSO; ketones, such as cyclohexanone; esters, such as lactic acid, carbonate, fatty acid ester , Γ-butyrolactone; fatty acid; phosphonate; amine; amides, such as N-methylpyrrolidone, fatty acid dimethyl amide; and mixtures thereof.

合適的固體載體或填料有礦物土,例如,矽酸鹽、矽膠、滑石、高嶺土、石灰石、石灰、白堊、黏土、白雲石、矽藻土、膨潤土、硫酸鈣、硫酸鎂、氧化鎂;多糖,例如纖維素、澱粉;肥料,例如硫酸銨、磷酸銨、硝酸銨、脲;植物來源的產品,例如穀物粉、樹皮粉、木粉,堅果殼粉及其混合物。Suitable solid carriers or fillers include mineral earths, for example, silicate, silica gel, talc, kaolin, limestone, lime, chalk, clay, dolomite, diatomaceous earth, bentonite, calcium sulfate, magnesium sulfate, magnesium oxide; polysaccharides, For example, cellulose, starch; fertilizers, such as ammonium sulfate, ammonium phosphate, ammonium nitrate, urea; products of plant origin, such as grain flour, bark powder, wood flour, nut shell powder and mixtures thereof.

合適的表面活性劑有表面活性化合物,例如陰離子,陽離子,非離子和兩性表面活性劑,嵌段聚合物,聚電解質及其混合物。這些表面活性劑可用作乳化劑,分散劑,增溶劑,潤濕劑,滲透增強劑,保護膠體或佐劑。表面活性劑的實例列於麥克卡森(McCutcheon),卷1:乳化劑和洗滌劑,《麥克卡森目錄》(McCutcheon's Directories),格蘭岩市,美國,2008(國際版或北美版)中。Suitable surfactants are surface-active compounds such as anionic, cationic, nonionic and amphoteric surfactants, block polymers, polyelectrolytes and mixtures thereof. These surfactants can be used as emulsifiers, dispersants, solubilizers, wetting agents, penetration enhancers, protective colloids or adjuvants. Examples of surfactants are listed in McCutcheon, Volume 1: Emulsifiers and Detergents, "McCutcheon's Directories", Gran Rock City, USA, 2008 (International or North American Edition) .

合適的陰離子表面活性劑有磺酸鹽、硫酸鹽、磷酸鹽、羧酸鹽及其混合物的鹼金屬、鹼土金屬或銨鹽。磺酸鹽的實例有烷基芳基磺酸鹽、二苯基磺酸鹽、α-烯烴磺酸鹽、木質素磺酸鹽、脂肪酸和油的磺酸鹽、乙氧基化烷基酚的磺酸鹽、烷氧基化芳基酚的磺酸鹽、縮合萘的磺酸鹽、十二烷基和十三烷基苯磺酸鹽、萘磺酸鹽和烷基萘、磺基琥珀酸鹽或磺基琥珀醯胺酸鹽。硫酸鹽的實例有脂肪酸和油的硫酸鹽、乙氧基化烷基酚、醇、乙氧基化醇或脂肪酸酯的硫酸鹽。磷酸酯的實例有磷酸酯。 羧酸鹽的實例有烷基羧酸鹽和羧化醇或烷基酚乙氧基化物。Suitable anionic surfactants are alkali metal, alkaline earth metal or ammonium salts of sulfonates, sulfates, phosphates, carboxylates and mixtures thereof. Examples of sulfonates are alkyl aryl sulfonates, diphenyl sulfonates, α-olefin sulfonates, lignosulfonates, sulfonates of fatty acids and oils, and ethoxylated alkyl phenols. Sulfonate, sulfonate of alkoxylated arylphenol, sulfonate of condensed naphthalene, dodecyl and tridecylbenzene sulfonate, naphthalene sulfonate and alkyl naphthalene, sulfosuccinic acid Salt or sulfosuccinate. Examples of sulfates are the sulfates of fatty acids and oils, ethoxylated alkylphenols, alcohols, ethoxylated alcohols or fatty acid esters. Examples of phosphate esters are phosphate esters. Examples of carboxylates are alkyl carboxylates and carboxylated alcohol or alkylphenol ethoxylates.

合適的非離子表面活性劑有烷氧基化物,N-取代的脂肪酸醯胺、氧化胺、酯、糖基表面活性劑、聚合物表面活性劑,以及它們的混合物。 烷氧基化物的實例有1至50當量烷氧基化醇類、烷基酚類、胺類、醯胺類、芳基酚類、脂肪酸或脂肪酸酯化合物。環氧乙烷和/或環氧丙烷可用於烷氧基化,優選環氧乙烷。N-取代的脂肪酸醯胺的實例有脂肪酸葡糖醯胺或脂肪酸鏈烷醇醯胺。酯的實例有脂肪酸酯,甘油酯或甘油單酯。 糖基表面活性劑的實例有脫水山梨糖醇,乙氧基化脫水山梨糖醇、蔗糖和葡萄糖酯或烷基聚葡糖苷。聚合物表面活性劑的實例有乙烯基吡咯烷酮、乙烯醇或乙酸乙烯酯的均聚物或共聚物。Suitable nonionic surfactants are alkoxylates, N-substituted fatty acid amides, amine oxides, esters, sugar-based surfactants, polymeric surfactants, and mixtures thereof. Examples of alkoxylates include 1 to 50 equivalents of alkoxylated alcohols, alkylphenols, amines, amines, arylphenols, fatty acids or fatty acid ester compounds. Ethylene oxide and/or propylene oxide can be used for alkoxylation, preferably ethylene oxide. Examples of N-substituted fatty acid amides are fatty acid glucosamines or fatty acid alkanol amides. Examples of esters are fatty acid esters, glycerides or monoglycerides. Examples of sugar-based surfactants are sorbitan, ethoxylated sorbitan, sucrose and glucose esters or alkyl polyglucosides. Examples of polymeric surfactants are homopolymers or copolymers of vinylpyrrolidone, vinyl alcohol or vinyl acetate.

合適的陽離子表面活性劑有季銨表面活性劑,例如具有一個或兩個疏水基團的季銨化合物,或長鏈伯胺的鹽。合適的兩性表面活性劑有烷基甜菜鹼和咪唑啉。合適的嵌段聚合物有包含聚環氧乙烷和聚環氧丙烷嵌段的A-B或A-B-A型嵌段聚合物,或包含鏈烷醇、聚環氧乙烷和聚環氧丙烷的A-B-C型嵌段聚合物。合適的聚電解質有多元酸或多元醇。多元酸的實例有聚丙烯酸或聚酸梳狀聚合物的鹼鹽。多鹼的實例有聚乙烯胺或聚乙烯胺。Suitable cationic surfactants are quaternary ammonium surfactants, such as quaternary ammonium compounds having one or two hydrophobic groups, or salts of long-chain primary amines. Suitable amphoteric surfactants are alkyl betaine and imidazoline. Suitable block polymers include AB or ABA type block polymers containing polyethylene oxide and polypropylene oxide blocks, or ABC type block polymers containing alkanol, polyethylene oxide and polypropylene oxide. Segment polymer. Suitable polyelectrolytes are polyacids or polyols. Examples of polyacids are alkali salts of polyacrylic acid or polyacid comb polymers. Examples of polybases are polyvinylamine or polyvinylamine.

合適的佐劑為本身幾乎沒有殺蟲活性能夠提高式(I)化合物對目標的生物性能的化合物。實例有表面活性劑、礦物質或植物油以及其他助劑。其他例子列於諾爾斯的《佐劑和添加劑》(Agrow報告DS256, T&F lnforma英國,2006年,第5章)。Suitable adjuvants are compounds that have little insecticidal activity by themselves and can improve the biological properties of the compound of formula (I) on the target. Examples are surfactants, mineral or vegetable oils and other additives. Other examples are listed in Knowles' "Adjuvants and Additives" (Agrow report DS256, T&F lnforma UK, 2006, Chapter 5).

合適的增稠劑有多糖(例如黃原膠、羧甲基纖維素)、無機黏土(有機改性或未改性的)、多羧酸鹽和矽酸鹽。合適的殺菌劑有溴硝醇和異噻唑啉酮衍生物,例如烷基異噻唑啉酮和苯並異噻唑啉酮。合適的防凍劑有乙二醇、丙二醇、尿素和甘油。合適的消泡劑有矽氧烷、長鏈醇和脂肪酸鹽。合適的著色劑(如紅色、藍色或綠色)有低水溶性顏料和水溶性染料。實例是無機著色劑(如氧化鐵、氧化鈦、六氰基鐵酸鐵)和有機著色劑(如茜素-、偶氮-和酞菁著色劑)。合適的增黏劑或黏合劑有聚乙烯吡咯烷酮、聚乙酸乙烯酯、聚乙烯醇、聚丙烯酸酯、生物或合成蠟和纖維素醚。Suitable thickeners are polysaccharides (such as xanthan gum, carboxymethyl cellulose), inorganic clays (organically modified or unmodified), polycarboxylates and silicates. Suitable bactericides are bronopol and isothiazolinone derivatives, such as alkyl isothiazolinones and benzisothiazolinones. Suitable antifreeze agents are ethylene glycol, propylene glycol, urea and glycerin. Suitable defoamers are silicones, long-chain alcohols and fatty acid salts. Suitable coloring agents (such as red, blue or green) are low water-soluble pigments and water-soluble dyes. Examples are inorganic colorants (such as iron oxide, titanium oxide, iron hexacyanoferrate) and organic colorants (such as alizarin-, azo- and phthalocyanine colorants). Suitable tackifiers or binders are polyvinylpyrrolidone, polyvinyl acetate, polyvinyl alcohol, polyacrylates, biological or synthetic waxes and cellulose ethers.

組合物類型及其製備的實例有: i) 水溶性濃縮物 (SL, LS) 將重量比為10-60%的式(I)化合物和重量比為5-15%的潤濕劑(例如醇烷氧基化物)溶解在重量比為100%的水和/或水溶性溶劑(例如醇)中。活性物質在用水稀釋即溶解。 ii) 分散性濃縮物 (DC) 將重量比為5-25%的式(I)化合物和重量比為1-10%的分散劑(例如聚乙烯吡咯烷酮)溶解在重量比為100%的有機溶劑(例如環己酮)中。用水稀釋得到分散性濃縮物。 iii) 可乳化濃縮物 (EC) 將重量比為15-70%的式(I)化合物和重量比為5-10%的乳化劑(例如十二烷基苯磺酸鈣和蓖麻油乙氧基化物)溶解在重量比為100%的水不溶性有機溶劑(例如芳族烴碳)中。用水稀釋得到乳液。 iv) 乳液 (EW, EO, ES) 將重量比為5-40%的式(I)化合物和重量比為1-10%的乳化劑(例如十二烷基苯磺酸鈣和蓖麻油乙氧基化物)溶解在重量比為20-40%的水不溶性有機溶劑(例如芳烴)中。通過乳化機將該混合物溶在重量比為100%的水中並製成均相乳液。用水稀釋得到乳液。 v) 懸浮液 (SC, OD, FS) 在攪拌球磨機中,將重量比為20-60%的式(I)化合物粉碎,加入重量比為2-10%的分散劑和潤濕劑(例如木質素磺酸鈉和醇乙氧基化物),重量比為0.1-2%的增稠劑(例如, 黃原膠)和重量比為100%的水,得到細活性物質懸浮液。用水稀釋得到活性物質的穩定懸浮液。對於FS型組合物,加入重量比高達40%的黏合劑(例如聚乙烯醇)。 vi) 水分散性顆粒和水溶性顆粒 (WG, SG) 將重量比為50-80%的式(I)化合物粉碎,加入重量比為100%的分散劑和潤濕劑(例如木質素磺酸鈉和醇乙氧基化物),並通過技術器具(例如擠壓、噴霧塔、流化床)作為水分散性或水溶性顆粒製備。用水稀釋可得穩定的具有活性物質的分散體或溶液。 vii) 水分散性粉末和水溶性粉末 (WP, SP, WS) 將重量比為50-80%的式(I)化合物在轉子-定子磨機中研磨並添加重量比為1-5%的分散劑(例如木質素磺酸鈉)、重量比為1-3%的潤濕劑(例如醇乙氧基化物)和重量比為100%固體載體(例如矽膠)。用水稀釋得到穩定的具有活性物質的分散體或溶液。 viii) 凝膠 (GW, GF) 在攪拌球磨機中,將重量比為5-25%的式(I)化合物粉碎,加入重量比為3-10%分散劑(例如木質素磺酸鈉),重量比為1-5%增稠劑(例如羧甲基纖維素)和重量比為100%的水,得到有活性物質的細懸浮液。用水稀釋得到有活性物質的穩定懸浮液。 ix) 微乳劑 (ME) 將重量比為5-20%的式(I)化合物加入到重量比為5-30%的有機溶劑混合物(例如脂肪酸二甲基醯胺和環己酮),重量比為10-25%的表面活性劑混合物(例如醇乙氧基化物和芳基酚乙氧基化物),和重量比為100%的水。將該混合物攪拌1小時,自發產生熱力學穩定的微乳液。 x) 微膠囊 (CS) 將其含有重量比為5-50%的式(I)化合物、重量比為0-40%的水不溶性有機溶劑(例如芳烴)、重量比為2-15%的丙烯酸單體(例如甲基丙烯酸甲酯,甲基丙烯酸和二-或將三丙烯酸酯)油相分散在保護膠體(例如聚乙烯醇)的水溶液中。自由基聚合形成聚(甲基)丙烯酸酯微膠囊。或者,將含有重量比為5-50%的根據本發明的式(I)的化合物,重量比為0-40%的水不溶性有機溶劑(例如芳烴)和異氰酸酯單體(例如二苯基甲烷-4,4'-二異氰酸酯)的油相分散到保護膠體(例如聚乙烯醇)的水溶液中。加入多胺(例如六甲基苯二胺)形成聚脲微膠囊。 單體量占重量的1-10%。wt%為占微膠囊組合物總重量百分比。 xi) 可撒粉的粉末 (DP, DS) 將重量比為1-10%的式(I)化合物細碎研磨並與重量比為100%的固體載體(例如細碎的高嶺土)充分混合。 xii) 顆粒 (GR, FG) 將重量比為0.5-30%的式(I)化合物細碎研磨並與重量比為100%的固體載體(例如矽酸鹽)混合。通過擠制加工、噴霧乾燥或流化床實現造粒。 xiii) 超低量液 (UL) 將重量比為1-50%的式(I)化合物溶於重量比為100%的有機溶劑(例如芳烴)中。 i)至xiii)的組合物可任選地包含其他助劑,例如重量比為0.1-1%的殺菌劑,重量比為5-15%的防凍劑,重量比為0.1-1%的消泡劑和重量比為0.1-1%的著色劑。Examples of composition types and their preparation are: i) Water-soluble concentrates (SL, LS) The compound of formula (I) with a weight ratio of 10-60% and a wetting agent (such as alcohol alkoxylate) with a weight ratio of 5-15% are dissolved in water and/or a water-soluble solvent with a weight ratio of 100% ( For example, alcohol). The active substance dissolves when diluted with water. ii) Dispersible concentrate (DC) The compound of formula (I) with a weight ratio of 5-25% and a dispersant (such as polyvinylpyrrolidone) with a weight ratio of 1-10% are dissolved in an organic solvent (such as cyclohexanone) with a weight ratio of 100%. Dilution with water gives a dispersible concentrate. iii) Emulsifiable concentrate (EC) The compound of formula (I) with a weight ratio of 15-70% and an emulsifier (such as calcium dodecylbenzene sulfonate and castor oil ethoxylate) with a weight ratio of 5-10% are dissolved in a weight ratio of 100% In water-insoluble organic solvents (such as aromatic hydrocarbon carbon). Dilution with water gives an emulsion. iv) Emulsion (EW, EO, ES) The compound of formula (I) with a weight ratio of 5-40% and an emulsifier (such as calcium dodecylbenzene sulfonate and castor oil ethoxylate) with a weight ratio of 1-10% are dissolved in a weight ratio of 20- 40% in water-insoluble organic solvents (such as aromatic hydrocarbons). The mixture is dissolved in water with a weight ratio of 100% by an emulsifier to prepare a homogeneous emulsion. Dilution with water gives an emulsion. v) Suspension (SC, OD, FS) In a stirred ball mill, pulverize the compound of formula (I) with a weight ratio of 20-60%, and add a dispersant and a wetting agent (such as sodium lignosulfonate and alcohol ethoxylate) with a weight ratio of 2-10%. , A thickener (for example, xanthan gum) with a weight ratio of 0.1-2% and water with a weight ratio of 100% to obtain a fine active substance suspension. Dilution with water gives a stable suspension of the active substance. For FS-type compositions, a binder (such as polyvinyl alcohol) is added up to 40% by weight. vi) Water-dispersible particles and water-soluble particles (WG, SG) Crush the compound of formula (I) with a weight ratio of 50-80%, add a dispersant and a wetting agent (such as sodium lignosulfonate and alcohol ethoxylate) with a weight ratio of 100%, and pass technical tools (such as Extrusion, spray tower, fluidized bed) are prepared as water-dispersible or water-soluble particles. Dilution with water can obtain a stable dispersion or solution with active substances. vii) Water-dispersible powder and water-soluble powder (WP, SP, WS) Grind the compound of formula (I) with a weight ratio of 50-80% in a rotor-stator mill and add a dispersant (such as sodium lignosulfonate) with a weight ratio of 1-5% at a weight ratio of 1-3% The wetting agent (such as alcohol ethoxylate) and the weight ratio of 100% solid carrier (such as silicone). Dilution with water gives a stable dispersion or solution with active substance. viii) Gel (GW, GF) In a stirred ball mill, crush the compound of formula (I) with a weight ratio of 5-25%, add a dispersant (such as sodium lignosulfonate) with a weight ratio of 3-10%, and a thickener with a weight ratio of 1-5% (Such as carboxymethyl cellulose) and 100% water by weight to obtain a fine suspension of active substance. Dilution with water gives a stable suspension of active substance. ix) Microemulsion (ME) Add the compound of formula (I) with a weight ratio of 5-20% to an organic solvent mixture (such as fatty acid dimethylamide and cyclohexanone) with a weight ratio of 5-30%, and the surface with a weight ratio of 10-25% Mixtures of active agents (such as alcohol ethoxylates and arylphenol ethoxylates), and 100% water by weight. The mixture was stirred for 1 hour, and a thermodynamically stable microemulsion was spontaneously produced. x) Microcapsule (CS) It contains 5-50% by weight of the compound of formula (I), 0-40% by weight of water-insoluble organic solvents (such as aromatic hydrocarbons), and 2-15% by weight of acrylic monomers (such as methacrylic acid). The oil phase of methyl ester, methacrylic acid and di- or triacrylate) is dispersed in an aqueous solution of protective colloid (such as polyvinyl alcohol). Free radical polymerization forms poly(meth)acrylate microcapsules. Alternatively, the compound of formula (I) according to the present invention in a weight ratio of 5-50%, a water-insoluble organic solvent (such as aromatic hydrocarbon) and an isocyanate monomer (such as diphenylmethane) in a weight ratio of 0-40% The oil phase of 4,4'-diisocyanate is dispersed in an aqueous solution of protective colloid (such as polyvinyl alcohol). Polyamines (such as hexamethylphenylenediamine) are added to form polyurea microcapsules. The amount of monomer accounts for 1-10% by weight. The wt% is the percentage of the total weight of the microcapsule composition. xi) Dustable powder (DP, DS) The compound of formula (I) with a weight ratio of 1-10% is finely ground and mixed with a solid carrier (for example, finely divided kaolin) with a weight ratio of 100%. xii) Granules (GR, FG) The compound of formula (I) in a weight ratio of 0.5-30% is finely ground and mixed with a solid carrier (such as silicate) in a weight ratio of 100%. Granulation is achieved through extrusion processing, spray drying or fluidized bed. xiii) Ultra low volume liquid (UL) The compound of formula (I) with a weight ratio of 1-50% is dissolved in an organic solvent (for example, aromatic hydrocarbon) with a weight ratio of 100%. The compositions of i) to xiii) may optionally contain other adjuvants, such as a biocide at a weight ratio of 0.1-1%, an antifreeze at a weight ratio of 5-15%, and a defoamer at a weight ratio of 0.1-1% The weight ratio of agent to coloring agent is 0.1-1%.

在本發明的另一個實施方案中,提供了一種式(I)的農化學組合物,其包含重量比為0.01至95%,優選0.1至90%,更優選1至70%,特別是10%至60%的活性物質。和60重量%的活性物質。活性物質的使用純度為90%至100%,優選為95%至100%(根據NMR譜)。In another embodiment of the present invention, there is provided an agrochemical composition of formula (I), which comprises 0.01 to 95% by weight, preferably 0.1 to 90%, more preferably 1 to 70%, especially 10% Up to 60% of active substances. And 60% by weight of active substance. The use purity of the active material is 90% to 100%, preferably 95% to 100% (according to the NMR spectrum).

處理植物繁殖材料(特別是種子)時,常使用種子處理溶液(LS)、懸浮乳液(SE)、可流動濃縮物(FS)、乾燥處理粉末(DS)、漿液處理用水分散性粉末(WS)通常使用水溶性粉末(SS)、乳液(ES)、可乳化濃縮物(EC)和凝膠(GF)。在二至十倍稀釋後,所述組合物在即用製劑中產生重量比為0.01至60%,優選0.1至40%的活性物質濃度。施用可在播種前或播種期間進行。When processing plant propagation materials (especially seeds), seed treatment solutions (LS), suspension emulsions (SE), flowable concentrates (FS), dry treatment powders (DS), and water dispersible powders for slurry treatment (WS) are often used Water-soluble powders (SS), emulsions (ES), emulsifiable concentrates (EC) and gels (GF) are commonly used. After a two to ten-fold dilution, the composition produces an active substance concentration in a ready-to-use formulation of 0.01 to 60% by weight, preferably 0.1 to 40%. Application can be carried out before or during sowing.

將式(I)化合物及其組合物分別施用到植物繁殖材料(特別是種子)上的方法包括敷料、包覆、造粒、撒粉和浸泡以及犁溝施用方法。優選地,分別通過拌種、造粒、包覆和撒粉這些不誘導發芽的方法將式(I)化合物或其組合物施用於植物繁殖材料上。The methods for applying the compound of formula (I) and the composition thereof to plant propagation materials (especially seeds) include dressing, coating, granulation, dusting and soaking, and furrow application methods. Preferably, the compound of formula (I) or its composition is applied to the plant propagation material by methods that do not induce germination, such as seed dressing, granulation, coating, and dusting.

當用於植物保護時,根據所需效果,施用的活性物質的量為每公頃0.001至2千克,優選每公頃0.005至2千克,更優選每公頃0.05至0.9千克(特別是每公頃0.1至0.75千克)。When used for plant protection, the amount of active substance applied is 0.001 to 2 kg per hectare, preferably 0.005 to 2 kg per hectare, more preferably 0.05 to 0.9 kg per hectare (especially 0.1 to 0.75 kg per hectare, depending on the desired effect). kilogram).

在處理植物繁殖材料如種子時,例如, 通過撒粉、塗覆或浸透種子,活性物質的量為每100千克植物繁殖材料(通常需要優選種子)0.1至1000克,優選1至500克,更優選1至100克,最優選5至100克。When treating plant propagation materials such as seeds, for example, by dusting, coating or soaking seeds, the amount of active substance is 0.1 to 1000 g, preferably 1 to 500 g, per 100 kg of plant propagation material (usually preferably seeds), and more It is preferably 1 to 100 grams, most preferably 5 to 100 grams.

當用於材料或儲存物的保護時,所施加的活性物質的量取決於施用的類型和所需的效果。通常用於保護材料的量為每立方米經處理的材料施用0.001g至2kg,優選0.005g至1kg活性物質。When used for the protection of materials or storage, the amount of active substance applied depends on the type of application and the desired effect. The amount usually used to protect the material is 0.001 g to 2 kg, preferably 0.005 g to 1 kg of active substance per cubic meter of treated material.

可以將各種類型的油、濕潤劑、佐劑、肥料或微量營養素以及其他農藥(例如除草劑、殺蟲劑、殺真菌劑、生長調節劑、安全劑、生物殺蟲劑)添加到活性物質或包含它們的組合物中作為預混物,或者如果合適的話使用前再加(罐裝混合)。這些試劑可以按照本發明的組合物以1:100至100:1,優選1:10至10:1的重量比混合。Various types of oils, wetting agents, adjuvants, fertilizers or micronutrients and other pesticides (such as herbicides, insecticides, fungicides, growth regulators, safeners, biological insecticides) can be added to the active substance or Include them in the composition as a premix or, if appropriate, add before use (can mix). These agents can be mixed in a weight ratio of 1:100 to 100:1, preferably 1:10 to 10:1 according to the composition of the present invention.

可以將各種類型的油、濕潤劑、佐劑、肥料或微量營養素以及其他農藥(例如除草劑、殺蟲劑、殺真菌劑、生長調節劑、安全劑、生物殺蟲劑)添加到活性物質或包含它們的組合物中作為預混物,或者如果合適的話使用前再加(罐裝混合)。這些試劑可以按照本發明的組合物以1:100至100:1,優選1:10至10:1的重量比混合。Various types of oils, wetting agents, adjuvants, fertilizers or micronutrients and other pesticides (such as herbicides, insecticides, fungicides, growth regulators, safeners, biological insecticides) can be added to the active substance or Include them in the composition as a premix or, if appropriate, add before use (can mix). These agents can be mixed in a weight ratio of 1:100 to 100:1, preferably 1:10 to 10:1 according to the composition of the present invention.

在一個實施方案中,根據本發明的組合物的各個成分,例如部分試劑或部分二元或三元混合物可以由用戶自己在噴霧罐或用於施用的任何其他種類的容器(如種子處理器鼓、種子造粒機械、背負式噴霧器)中混合,而且可以選擇添加其他輔助劑。In one embodiment, the individual components of the composition according to the present invention, such as part of the reagent or part of the binary or ternary mixture, can be stored by the user in a spray tank or any other kind of container for application (such as a seed processor drum). , Seed granulation machinery, knapsack sprayer), and can choose to add other auxiliary agents.

因此,本發明的化合物和組合物在農業上可用於保護大田作物免受食植性無脊椎動物害蟲的侵害,並且在非農業上可用於保護其他園藝作物和植物免受食植性無脊椎動物害蟲的侵害。 該效用包括保護包含通過基因工程(即轉基因)引入或通過誘變修飾的遺傳物質以提供有利性狀的農作物和其他植物(即農學和非農學的)。Therefore, the compounds and compositions of the present invention can be used to protect field crops from phytophagous invertebrate pests in agriculture, and can be used to protect other horticultural crops and plants from phytophagous invertebrates in non-agriculture. Infestation by pests. This utility includes the protection of crops and other plants (ie, agronomic and non-agronomic) that contain genetic material introduced through genetic engineering (ie, transgene) or modified by mutagenesis to provide beneficial traits.

本發明的化合物具有有利的代謝和/或土壤殘留模式,並表現出控制一系列農學和非農學無脊椎動物害蟲的活性。本發明的化合物在害蟲控制領域中是有價值的預防性和/或治療性活性成分(即使施用率較低),可用於針對昆蟲和蟎蟲等殺蟲劑抗性害蟲。此外,溫血動物、魚類和植物都能很好地耐受它們。The compounds of the present invention have favorable metabolic and/or soil residue patterns, and exhibit the activity of controlling a series of agronomic and non-agronomic invertebrate pests. The compounds of the present invention are valuable preventive and/or therapeutic active ingredients in the field of pest control (even if the application rate is low), and can be used to target insecticide-resistant pests such as insects and mites. In addition, warm-blooded animals, fish and plants can tolerate them well.

在本發明的上下文中,“無脊椎動物害蟲防治”是指抑制無脊椎動物害蟲的生長(包括死亡),顯著減少其進食或由其引起的其他傷害或破壞。在本發明中,術語“無脊椎動物害蟲”包括作為害蟲具有經濟重要性的節肢動物、腹足動物和線蟲。術語“節肢動物”包括昆蟲,蟎蟲,蜘蛛,蠍子,蜈蚣,千足蟲,球潮蟲和綜合綱。In the context of the present invention, "invertebrate pest control" refers to inhibiting the growth (including death) of invertebrate pests, significantly reducing their eating or other damage or destruction caused by them. In the present invention, the term "invertebrate pests" includes arthropods, gastropods, and nematodes that are economically important as pests. The term "arthropod" includes insects, mites, spiders, scorpions, centipedes, millipedes, coccidioides, and syngas.

術語“腹足動物”包括蝸牛、鼻涕蟲和其他有柱腹足目。術語“線蟲”包括所有蠕蟲,例如:蛔蟲、犬惡絲蟲和食植性線蟲,吸蟲,棘頭蟲以及絛蟲。本領域技術人員將認識到,並非所有化合物都同樣有效地對抗所有害蟲。The term "gastropod" includes snails, slugs, and other columnar gastropods. The term "nematode" includes all worms, such as roundworms, heartworms and phytophagous nematodes, flukes, acanthocephalans and tapeworms. Those skilled in the art will recognize that not all compounds are equally effective against all pests.

本發明的化合物顯示出對經濟上重要的農藝、森林、溫室、苗圃、觀賞植物、食物和纖維、公共和動物健康、家庭和商業結構、家庭和儲存的產品的害蟲的活性。這些包括鱗翅目的幼蟲,例如夜蛾科中的黏蟲、地老虎、彎曲蟲(例如秋黏蟲)、甜菜夜蛾、黑夜蛾、捲心菜、煙夜蛾;來自螟科的蛀蟲、鞘蛾、結網毛蟲、圓錐線蟲、卷葉蛾、雕葉蟲(例如歐洲玉米螟、臍橙螟、玉米根蚯蚓、草皮蚯蚓; 卷葉蛾科的葉蟬、煙青蟲、種子蠕蟲和果子蠕蟲(例如蘋果蠹蛾)、葡萄漿果蛾、東方水果蛾; 和許多其他經濟上重要的鱗翅目昆蟲 (例如小菜蛾、粉紅鈴蟲、吉普賽蛾); 蟑螂目若蟲和成蟲包括蟑螂科 (例如東方蟑螂、亞洲蟑螂、德國蟑螂、褐蟑螂、美洲蟑螂、棕色蟑螂、馬德拉蟑螂); 葉鞘幼蟲和鞘翅目的成蟲包括來自長角象蟲科、豆象科和象甲科的象鼻蟲(例如棉鈴象蟲、水稻象鼻蟲、糧倉象甲、水稻象鼻蟲); 甲殼類動物中的跳蚤甲蟲、黃瓜甲蟲、根蟲、葉甲蟲、馬鈴薯甲蟲和斑潛蠅(例如科羅拉多馬鈴薯甲蟲、西部玉米根蟲); 來自金龜科中的金龜子和其他甲蟲(例如日本甲蟲和歐洲金龜子); 來自皮蠹科的地毯甲蟲; 來自叩頭蟲科的金針蟲; 來自小蠹蟲科的樹皮甲蟲和來自擬步行蟲科的麵粉甲蟲。此外,它還包括:革翅目的成蟲和幼蟲,包括來自球螋科的地蜈蚣(例如歐洲球螋、黑色蠼螋); 半翅目和同翅目的成蟲和若蟲,如盲蝽科的植物蟲、蟬科的蟬、來自葉蟬科的葉蟬、來自蟬科和飛虱科的稻飛虱、來自角蟬科的蚱蜢、來自木虱科科的木虱、來自粉虱科的粉虱、來自蚜蟲科的蚜蟲、來自根瘤蚜科的根瘤蚜、來自粉蚧科的粉蚧、來自蚧科、盾蚧科和球蛛科的鱗片、來自網蝽科家族的花邊蟲、來自蝽科的臭蟲、和來自長蝽科家族的扁蟲和其他種子蟲、來自沫蟬科的沫蟬、來自緣蝽科的南瓜蟲、來自紅蝽科的紅色臭蟲和汙棉蟲。 還包括蜱蟎(蟎類)的成蟲和幼蟲,例如葉蟎科的蜘蛛蟎和紅蟎。(例如歐洲紅蟎、兩個斑點的蜘蛛蟎 、麥克丹尼爾蟎、細須蟎科的扁蟎(例如柑橘扁蟎))、癭蟎科家族中的銹病和芽蟎以及其他對人類和動物健康有重要作用的葉蟎蟎和蟎蟲,即表皮蟎科的塵蟎、蛻皮科的卵蟎、穀蟎科的穀蟎、按硬蜱科的順序排列的蜱,例如鹿蜱(肩胛硬蜱)、澳大利亞麻痹蜱(全血球硬蜱)、美國狗蜱(變異革蜱)、孤星蜱(美洲軟蜱)和疥蟎科、疥蟎科和疥蟎科的疥蟎和蟎蟲; 直翅目的成蟲和不成熟物種,包括蝗蟲、蝗蟲和蟋蟀,例如洄遊蚱蜢(例如血吸蟲黑鱸)、美國蚱蜢(例如美洲血吸蟲)、沙漠蝗蟲、 遷徙蝗蟲、家蟋蟀、鼴鼠; 雙翅目的成蟲和幼蟲,包括葉蠅、蠓、果蠅、玻璃蠅、土壤蛆、家蠅(例如家蠅、小家蠅(例如廁蠅屬)、穩定蠅(例如廄螫蠅)、臉蠅、角蠅、吹蠅和其他肌肉樣蒼蠅害蟲、馬蠅(例如虻蟲 ))、牛蠐、鹿蠅、蝽螈(如綿羊蝽螈屬)和其他短尾蚴、蚊子(如伊蚊屬、按蚊屬、庫蚊屬)、黑蠅(如蝽螈屬、螈螈屬)、咬蚊、沙蠅、剪刀蟲和其他線蟲; 纓尾目的成蟲和幼蟲,包括洋蔥薊馬和其他葉面薊馬; 膜翅目昆蟲害蟲包括螞蟻(例如紅木匠螞蟻、黑木匠螞蟻、法老螞蟻、小火蟻、火蟻、紅色進口火蟻、阿根廷螞蟻、瘋狂螞蟻、路面螞蟻、玉米田螞蟻、氣味螞蟻)、蜜蜂(包括木匠蜜蜂)、黃蜂、黃茄克和黃蜂; 等翅目昆蟲害蟲,包括東部地下白蟻、西部地下白蟻、臺灣地下白蟻、西印度幹木白蟻和其他具有經濟重要性的白蟻; 纓尾目的害蟲如銀魚和家衣魚; 食毛目的害蟲,包括頭蝨、體虱、雞體虱、狗咬虱、絨毛虱、綿羊體虱、短鼻牛虱、長鼻牛虱和其他吮吸和咀嚼攻擊人和動物寄生蝨子; 蚤目的昆蟲害蟲包括東方鼠蚤、貓蚤、狗蚤、母雞跳蚤、黏性跳蚤、人類跳蚤和其他折磨哺乳動物和鳥類的跳蚤。 其他被覆蓋的節肢動物害蟲包括:蜘蛛目蜘蛛、如棕色隱居蜘蛛和黑色寡婦蜘蛛、 和蚰蜒目的蜈蚣、如家蜈蚣。活性還包括線蟲綱、頭足綱、吸蟲綱和棘頭綱的成員,包括經濟上重要的圓線蟲目、蛔蟲科、尖尾目、小杆目、旋尾目和嘴刺目的成員,例如但不限於經濟上重要的農業害蟲(如根結線蟲屬中的根結線蟲、短體線蟲屬中的病斑線蟲、毛刺線蟲屬的短根線蟲等。)以及動物和人類健康害蟲(即所有經濟上重要的吸蟲、絛蟲和蛔蟲,如馬中的強直線蟲、犬中的犬弓首線蟲、羊中的撚轉血茅線蟲、狗中的惡絲蟲、馬中的裸頭絛蟲屬、反芻動物中的肝片吸蟲等。The compounds of the present invention show activity against pests of economically important agronomy, forests, greenhouses, nurseries, ornamental plants, food and fiber, public and animal health, household and commercial structures, households and stored products. These include lepidopteran larvae, such as armyworms in the Noctuidae family, cutworms, bentworms (such as autumn armyworm), beet armyworm, black armyworm, cabbage, tobacco armyworm; borers from the family Pyrididae, sheath moths, Netting caterpillars, cone nematodes, leaf rollers, leaf worms (such as European corn borer, orange borer, corn root earthworms, turf earthworms; leafhoppers, tobacco caterpillars, seed worms and fruit worms ( Such as codling moth), grape berry moth, oriental fruit moth; and many other economically important lepidopteran insects (such as diamondback moth, pink bollworm, gypsy moth); cockroach nymphs and adults include cockroaches (such as oriental cockroach) , Asian cockroaches, German cockroaches, brown cockroaches, American cockroaches, brown cockroaches, Madeira cockroaches); leaf sheath larvae and coleoptera adult insects include weevil (such as cotton boll Weevil, rice weevil, granary weevil, rice weevil); flea beetle, cucumber beetle, root beetle, leaf beetle, potato beetle and Liriomyza in crustaceans (e.g. Colorado potato beetle, western corn root Beetles); beetles and other beetles from the family Scarabidae (e.g. Japanese beetles and European beetles); carpet beetles from the Dermatodidae; golden needle beetles from the Clickworm family; bark beetles from the Beetles family and from the Pedidae The flour beetle. In addition, it also includes: Dermatoptera adults and larvae, including ground centipedes from the Glycidae family (e.g. European coccinea, black earwig); Hemiptera and Homoptera adults and nymphs, such as Miliidae Plant insects from the family Cicadaceae, leafhoppers from the Cicada family, Rice planthoppers from the Cicada family and Planthopper family, Grasshoppers from the Cicada family, Psyllids from the Psyllidae family, and Whitefly family Whiteflies, aphids from Aphididae, Phylloxera from Phylloxera, mealybugs from Mealcoccidae, scales from Coccidae, Scutellaidae and Coccididae, lace insects from Dictyidae family, from Stink bugs from the family Pyrididae, flatworms and other seed insects from the Pyrididae family, squash insects from the Mycoididae family, pumpkin insects from the Pyrididae family, red bed bugs and dirty cotton worms from the Rhododidae family. Also included are ticks. Adults and larvae of mites (mites), such as spider mites and red mites of the Tetranychus family. (e.g. European red mites, two-spotted spider mites, McDaniel mites, and flat mites of the family Tetranychus (such as citrus mites) )), rust disease and bud mites in the mites family, and other spider mites and mites that have important effects on human and animal health, namely dust mites of the epidermidaceae, egg mites of the ecdysidae, and grain mites of the mites , Ticks arranged in the order of the Ixodes family, such as the deer tick (Ixodes scapularis), the Australian paralysis tick (Ixodes scapularis), the American dog tick (Dermots variabilis), the lone star tick (American soft tick), and the scabies mite Scabies and mites of the family, Scabidae and Scabidae; Adult and immature species of Orthoptera, including locusts, locusts and crickets, such as migratory grasshoppers (such as Schistosoma black bass), American grasshoppers (such as Schistosoma americana), Desert locusts, migratory locusts, house crickets, moles; Diptera adults and larvae, including leaf flies, midges, fruit flies, glass flies, soil maggots, house flies (e.g. house flies, small house flies (e.g. ), stable flies (such as stinging flies), face flies, horned flies, blow flies and other muscle-like flies pests, horse flies (such as worms), bovine grubs, deer flies, and axolotl (such as the genus Sheep Stinging Flies) And other Brachycercaria, mosquitoes (such as Aedes, Anopheles, Culex), black flies (such as Axolotl, Axolotl), biting mosquitoes, sand flies, scissors insects and other nematodes; Adults of the Thysanidae And larvae, including onion thrips and other foliar thrips; Hymenoptera pests include ants (such as red carpenter ants, black carpenter ants, pharaoh ants, small fire ants, fire ants, red imported fire ants, Argentine ants, crazy Ants, road ants, cornfield ants, smell ants), bees (including carpenter bees), wasps, yellow jackets and wasps; isoptera insect pests, including eastern subterranean termites, western subterranean termites, Taiwan subterranean termites, and West Indian dry wood Termites and other economically important termites; Thysanidae pests such as whitebait and silverfish; Trichophagous pests, including head lice, body lice, chicken body lice, dog bite lice, hairy lice, sheep body lice, and short Nose bull lice, proboscis bull lice, and other sucking and chewing parasitic lice that attack humans and animals; Phleadian insect pests include Eastern rat fleas, cat fleas, dog fleas, hen fleas, sticky fleas, human fleas and other tormenting mammals And bird fleas. Other covered arthropod pests include: arachnid spiders, such as brown recluse spiders and black widow spiders, and scorpid centipedes, such as house centipedes. The activity also includes members of the classes Nematodes, Cephalopods, Flukes, and Acanthocephalus, including economically important members of Strongyloides, Ascarididae, Acerococcus, Microcephalus, Trichocera, and Sclerotium, such as but not Limited to economically important agricultural pests (such as root-knot nematodes in the genus Root-knot nematodes, spot nematodes in the genus Brachytematia, and short root-knot nematodes in the genus Trichoderma, etc.) and animal and human health pests (that is, all economically Important trematodes, tapeworms and roundworms, such as strong linear worms in horses, Toxoplasma canis in dogs, Haematocodon contortus in sheep, Heartworms in dogs, Gymnocephalum in horses, ruminants Fasciola hepatica and so on.

本發明化合物對鱗翅目的害蟲表現出特別高的活性,這些害蟲包括棉葉波紋夜蛾 (棉葉蟲)、果樹黃卷蛾 (果樹葉輥)、歐洲卷葉蛾和其他黃卷蛾屬、二化螟(水稻螟蟲)、稻縱卷葉螟(水稻螟蟲)、玉米根草螟、藍草蚯蚓、蘋果蠹蛾、多刺棉鈴蟲、斑點棉鈴蟲、美國棉鈴蟲、玉米穗蟲、煙草夜蛾、草皮蚯蚓、葡萄漿果蛾、粉紅鈴蟲、柑橘、大白蝴蝶、小白蝴蝶、小菜蛾、甜菜夜蛾、斜紋夜蛾(煙草夜蛾、叢生毛蟲)、秋季黏蟲、甘藍銀紋夜蛾和番茄潛葉蠅。The compounds of the present invention show particularly high activity against lepidopteran pests. These pests include cotton leaf moth (cotton leaf insect), fruit tree yellow roller moth (fruit leaf roller), European leaf roller moth and other yellow leaf moths, two Chinese rice borer (rice stem borer), rice leaf roller (rice stem borer), corn root grass borer, blue grass earthworm, codling moth, spiny cotton bollworm, spotted cotton bollworm, American cotton bollworm, corn earworm, tobacco armyworm , Turf earthworm, grape berry moth, pink bollworm, citrus, big white butterfly, small white butterfly, diamondback moth, beet armyworm, prodenia litura (tobacco armyworm, tufted caterpillar), autumn armyworm, cabbage armyworm and Tomato leaf miner.

本發明的化合物對同翅目的成員也具有商業上顯著的活性,這些包括豌豆蚜蟲、豇豆蚜蟲、黑豆蚜蟲、棉蚜、甜瓜蚜蟲、蘋果蚜蟲、繡線菊蚜蟲、毛地黃蚜蟲、草莓蚜蟲、俄羅斯小麥蚜蟲、玫瑰蘋果蚜蟲、羊毛蘋果蚜蟲、桃大尾蚜蟲、穀物蚜蟲、馬鈴薯蚜蟲、桃蚜蚜蟲、綠桃蚜蟲、萵苣蚜蟲、根蚜和癭蚜、玉米葉蚜蟲、鳥櫻桃燕麥蚜蟲、綠蚜、麥長管蚜、苜蓿斑蚜、茶蚜、黑柑橘蚜蟲)和褐色柑橘蚜蟲; 球蚜屬; 根瘤蚜;美核桃根瘤蚜; 粉虱(煙草粉虱、甘薯粉虱)、類作物的銀葉粉虱(銀葉粉虱)、 柑橘粉虱和溫室粉虱; 馬鈴薯葉蟬、較小的褐飛虱、紫菀葉蟬、綠葉蟬、稻葉蟬、褐飛虱、玉米飛虱、白背飛虱、稻飛虱、白蘋果葉蟬、葡萄葉蟬; 叢生蟬;冰草屬(棉墊鱗)、毒死蜱屬(聖約瑟鱗);柑桔疫黴屬(柑桔粉虱);假球菌屬(其他粉虱複合體);赤黴屬(梨木虱)、柿子木虱。The compounds of the present invention also have commercially significant activities against members of the order Homoptera. These include pea aphids, cowpea aphids, black bean aphids, cotton aphids, melon aphids, apple aphids, spiraea aphids, caterpillar yellow aphids, strawberry aphids, Russian wheat aphids, rose apple aphids, wool apple aphids, peach aphids, grain aphids, potato aphids, green peach aphids, green peach aphids, lettuce aphids, phylloxera and gall aphids, corn leaf aphids, bird cherry oat aphids, green Aphid, Piper aphid, Alfalfa aphid, tea aphid, black citrus aphid) and brown citrus aphid; Aphid genus; Phylloxera; American walnut phylloxera; Whitefly (Whitefly, Sweet potato whitefly), crop-like Silver leaf whitefly (silver leaf whitefly), citrus whitefly and greenhouse whitefly; potato leafhopper, smaller brown planthopper, aster leafhopper, green leafhopper, rice leafhopper, brown planthopper, corn planthopper, white back Planthoppers, rice planthoppers, white apple leafhoppers, grape leafhoppers; clustered cicadas; wheatgrass (cotton pad scale), chlorpyrifos (San Jose scale); citrus phytophthora (citrus whitefly); false Coccus (other whitefly complexes); Gibberella (pear psyllids), persimmon psyllids.

這些化合物還對半翅目的成員具有活性,這些成員包括綠色臭蟲、南瓜蟲、長蝽若蟲、棉花邊蟲、番茄蟲、汙棉蟲、桉褐色臭蟲(棕色臭蟲)、桉褐色斑潛蠅(單點臭蟲)、葡萄球菌(種蟲複合體)、葉足松種子蟲、桉褐斑潛蠅、變色植物蟲、內紮拉病毒性林奈(南方綠臭蟲)、美洲大蠹(稻臭蟲)、大乳草蟲、棉蚤。These compounds are also active against members of the order Hemiptera, which include green bugs, pumpkin bugs, long bug nymphs, cotton edge bugs, tomato bugs, cotton worms, eucalyptus brown bugs (brown bugs), eucalyptus brown spotted liriomycetes (single Spot bugs), Staphylococcus (seed insect complex), Pine seed insects, Liriomyza eucalyptus, color-changing plant insects, Nezha virus Linnaeus (southern green bug), American beetles (rice bug), Large milkweed insects, cotton fleas.

本發明化合物可以控制的其他昆蟲目包括纓翅目(例如、西花薊馬、柑橘薊馬、大豆薊、和洋蔥薊馬;和鞘翅目(例如,科羅拉多馬鈴薯甲蟲、墨西哥豆甲蟲和屬於金針蟲、或吸蟲屬的線蟲)。Other insect orders that can be controlled by the compounds of the present invention include Thysanoptera (e.g., Western flower thrips, citrus thrips, soybean thistle, and onion thrips; and Coleoptera (e.g., Colorado potato beetle, Mexican bean beetle and belonging to the golden needle insect , Or nematodes of the genus Fluke).

特別地,式(I)化合物,它們的N-氧化物、它們的異構體、它們的多晶型物和它們的鹽特別適用於有效地對抗下列害蟲: 來自鱗翅類(鱗翅目)的昆蟲, 例如小地老虎、黃地老虎、棉葉波紋夜蛾、黎豆夜蛾、銀蛾科的蘋果銀蛾、紋夜蛾、松尺蠖、樅卷葉蛾、煙捲蛾、冬尺蛾、二點螟、雲杉卷葉蛾、樅色卷蛾、一點黏蟲、蘋果蠹蛾、歐洲松毛蟲、黃瓜絹野螟、西南玉米螟、棉斑實蛾、翠紋鑽夜蛾、南美玉米苗斑螟、葡萄與蘋果卷葉蛾、斑點夜蛾、大蠟螟、小卷葉蛾、梨小食心蟲、棉鈴蟲、棉鈴夜蛾、玉米穗蟲、菜心螟、美國白蛾、蘋果巢蛾、番茄莖麥蛾、鐵杉尺蠖、甜菜夜蛾、咖啡潛葉蛾、旋紋潛葉蛾、金紋細蛾、葡萄蛾、草地螟、黃斑螟、舞毒蛾、舞白頭鶴、桃潛葉蛾、走狗蛾、甘藍夜蛾、黃杉毒蛾、歐洲玉米螟、小眼夜蛾、棉紅鈴蟲、疆夜蛾、圓掌舟蛾、馬鈴薯塊莖蛾、柑桔潛葉蛾、菜粉蝶、苜蓿綠夜蛾、小菜蛾、大豆夜蛾、美松梢小卷蛾、三化螟、陰囊蚤、麥蛾、葡萄長須卷蛾、草地貪夜蛾、棉貪夜蛾、斜紋夜蛾、甜菜夜蛾、松行列蛾、櫟綠卷蛾、粉紋夜蛾和加拿大一枝黃花小卷蛾; 和甲蟲(鞘翅目),例如梨窄吉丁、直條叩頭蟲、暗色叩頭蟲、六月金龜子、茴香屬、棉鈴象甲、蘋花象、蚜蠅科、舌甘菜隱食甲、縱坑切梢小蠹、蠶豆象、豌豆象、歐洲兵豆象、梨卷葉象、甜菜大龜甲、菜豆瑩葉甲、金花金龜、白菜籽龜象、白菜籽龜象、甜菜脛跳甲、煙草金針蟲、刁柏負泥蟲、長角葉甲,葉甲屬、黃瓜甲蟲、南美葉甲、玉米根蟲、墨西哥豆瓢蟲、煙草跳甲、象變種、松象甲、葉象甲屬、葉象甲、雲杉樹皮甲蟲、勒馬天蛾、黑角負泥蟲、馬鈴薯甲蟲、甜菜叩甲、稻水象甲、油菜露尾甲、鰓金龜、 大栗鰓角金龜、水稻負泥蟲、黑葡萄耳象、、樹葉象、油菜金頭跳甲、食葉鰓金龜屬種、庭園發麗金龜、菁淡足跳甲、黃曲條菜跳甲、日本麗金龜、和穀象;蒼蠅、蚊子(雙翅目),例如埃及伊蚊、白紋伊蚊、白紋伊蚊、按實蠅、五斑按蚊、災難按蚊、白魔按蚊、岡比亞按蚊、泛生按蚊、白斑按蚊、小按蚊、四孔按蚊、紅頭麗蠅、地中海實蠅、蛆症金蠅、古人類按蚊、黃斑按蚊、盤金龜子、矽金龜子、大西洋按蚊、嗜人錐蠅、 高梁癭蚊、人皮蠅、毛庫蠓、尖音庫蚊、黑須庫蚊、致倦庫蚊、跗葉庫蚊、紫色庫蚊、黑尾賽蚊、瓜實蠅、油橄欖實蠅、油菜葉癭蚊、蔥蠅、麥地種蠅、灰地種蠅、甘藍地種蠅、人膚皮蠅、夏廁蠅、尺禾蠅屬、腸胃蠅、 刺舌蠅、須舌蠅、須舌蠅、舌蠅屬、擬寄舌蠅、西方角蠅、潛蠅屬、種蠅、紋皮蠅、托氏細蠓、美洲斑潛蠅、三葉斑潛蠅、巴西綠蠅、銅綠蠅、絲光綠蠅、曼蚊屬、黑森癭蚊、秋家蠅、家蠅、廄腐蠅、發情羊屬、禾蠅屬、瑞典麥稈蠅、天仙子泉妮、廄腐蠅、蘿蔔蠅、草種蠅屬、銀足白蛉、哥倫比亞鱗蚊、胡蘿蔔莖蠅、鱗蚊屬、原蚋屬、櫻桃繞實繩、蘋果實蠅、赤尾麻蠅、麻蠅屬、帶蚋、廄螫蠅、牛虻、北美黑虻、馬蠅、和虻屬、大蚊屬、和沼澤大蚊; 白蟻目 (等翅目),例如異白蟻、北美散白蟻、南方散白蟻、南歐網紋白蟻、桑特散白蟻、臺灣乳白蟻; 蟑螂 (蜚蠊目),例如德國蜚蠊、亞洲蜚蠊、美洲大蠊、日本大蠊、棕色蟑螂、黑胸大蠊、澳洲大蠊、和東方蜚蠊; 螞蟻、蜜蜂、黃蜂、葉蜂(膜翅目)例如菜葉蜂、熱帶切葉蟻屬、大頭美切葉蟻,切葉蟻、德克薩斯切葉蟻、舉腹蟻屬、黑蟻、黃家蟻、火蟻、紅火蟻、黑火蟻、 紅收穫蟻、收割機螞蟻、大頭蟻、袋蚊蜂屬、熊蜂屬、黃斑胡蜂、賓夕凡尼亞木蠊、黃邊胡蜂、長腳蜂、佛羅裏達弓背蟻、和阿根廷蟻; 蟋蟀、蚱蜢、蝗蟲(直翅目),例如家蟋蟀、歐洲螻蛄、東亞飛蝗、雙帶蚱蜢、紅足黑蝗、墨西哥黑蟲皇、血黑蝗、落磯山蝗、紅翅蝗、美洲沙漠蟲皇、沙漠蝗蟲、摩洛哥戟紋蝗、加爾小車蟲皇、印度黃檀蝗、義大利蝗、澳洲疫蝗、和褐飛蝗; 蜘蛛目,例如黑寡婦蜘蛛和人類被棕色遁蛛; 跳蚤 (蚤目),例如貓櫛首蚤、狗跳蚤、印鼠客蚤、致癢蚤、穿皮潛蚤、和具帶病蚤、蠹蟲,家衣魚(纓尾目),例如小灶衣魚、蜈蚣(蜈蚣類),例如取食螞蟻、多足類(倍足綱),例如蠼螋(革翅目),例如地蜈蚣、蝨子(虱毛目),例如人頭虱、人體虱、人體陰虱、牛血風、豬血虱、牛顎虱、牛羽虱和水牛盲虱;彈尾目(跳蟲),例如棘跳蟲屬。In particular, the compounds of formula (I), their N-oxides, their isomers, their polymorphs and their salts are particularly suitable for effectively fighting against the following pests: Insects from the Lepidoptera (Lepidoptera), For example, small cutworm, yellow cutworm, cotton leaf moth, Lidou armyworm, silver moth of the silver moth family, silver moth, pine looper, fir leaf roller, tobacco moth, winter foot moth, two-spotted borer , Spruce leaf roller moth, Fir-colored roller moth, Mythimna separata, Codling moth, European pine caterpillar, Cucumber silk borer, Southwestern corn borer, cotton spotted moth, Emerald spodoptera, South American corn seedling moth, Grape and apple leaf roller moth, spotted armyworm, wax moth, small leaf roller moth, pear coreworm, cotton bollworm, cotton bollworm, corn earworm, cabbage borer, American white moth, apple nest moth, tomato stem wheat Moth, Hemlock Geometrid, Beet Armyworm, Coffee Leaf Miner, Swirl Leaf Miner, Golden Leaf Miner, Grape Moth, Grass Borer, Yellow Spot Borer, Gypsy Moth, Hooded Crane, Peach Leaf Miner, Running Dog Moth, Cabbage Noctuidae, Pseudosciaena chinensis, European corn borer, Spodoptera exigua, Cotton red bollworm, Spodoptera exigua, Cyclopus spp, potato tuber moth, Citrus leaf miner, Pieris rapae, Alfalfa green armyworm, Plutella xylostella , Soybean Spodoptera, Pinus sylvestris, Chilo suppressalis, Scrotal Flea, Wheat Moth, Grape Spodoptera, Spodoptera frugiperda, Spodoptera litura, Spodoptera exigua, Beet Armyworm, Pine Row Moth, Quercus Green roll moth, Fennel armyworm, and Canadian goldenrod small roll moth; and beetles (Coleoptera), such as pear chitin, straight click beetle, dark click beetle, June beetle, fennel, cotton boll weevil, apple Flower elephant, Syrphididae, Brassica oleracea, Toxicola vulgaris, Broad bean weevil, Pea weevil, European lentil weevil, Pear leaf weevil, Beet tortoise shell, Phaseolus vulgaris, Golden beetle, Cabbage seed turtle weevil, cabbage seed turtle weevil, beet shin beetle, tobacco golden needle beetle, cypress mudworm, longhorn leaf beetle, leaf beetle, cucumber beetle, South American leaf beetle, corn root beetle, Mexican bean scoop Insects, tobacco jump beetles, elephant variants, pine weevil, leaf weevil, leaf weevil, spruce bark beetle, lema hawkmoth, black horned mud beetle, potato beetle, beet knock beetle, rice water weevil, canola beetle , Gill beetle, big chestnut beetle, rice minus worm, black grape ear weevil, leaf weevil, rape gold-headed beetle, leaf-eating beetle, garden beetle beetle, light-footed beetle, yellow striped beetle Aegilops, Japanese beetle, and valley weevil; flies, mosquitoes (Diptera), such as Aedes aegypti, Aedes albopictus, Aedes albopictus, An. flies, Anopheles quinquefolius, Anopheles catharticus, White devil Anopheles, Anopheles gambiae, Anopheles panbos, Anopheles albopictus, Anopheles minor, Anopheles tetragonata, Blow-headed blowfly, Mediterranean fruit fly, Golden maggot, Anopheles ancient human, Anopheles maculatus, Anopheles platypus, Silica beetle, Anopheles atlanticus, Triatomine anthropophagus, Sorghum gall midge, Human skin fly, Culex pilaris, Culex pipiens pipiens, Culex pipiens rubrum, Culex quinquefasciatus, Culex tarsalis, Culex purple, Black tail Cymbidium, cucurbita, olive fruit fly, rape leaf gall midge, onion fly, wheat field fly, gray ground fly, cabbage field fly, human skin fly, summer toilet fly, geometrid, gastrointestinal fly , Tsetse fly, Glossy fly, Tsetse fly, Tsetse genus, Parasitic tsetse fly, Western horned fly, Liriomyza, Species, Glossy flies, Liriomyza todii, Liriomyza sativae, Liriomyza trilobata, Lucilia brasiliensis, Lucilia sericata, Lucilia sericata, Manglietia, Hessian gall midge, Autumn housefly, Housefly, Rot fly, Oestrus , Gramineae, Swedish wheat stalk fly, Hydrangea sylvatica, Rot fly, Turnip fly, Grass species fly, Silver-footed sandfly, Colombian scale mosquito, Carrot stalk fly, Scale mosquito, Protosimum, Cherry ring Real rope, apple fruit fly, red-tailed Sarcophaga, Sarcophaga, Gadfly, Sting Fly, Gadfly, North American Black Fly, Horse Fly, Gadfly, Crane, and Swamp Crane; Termite (Isoptera), For example, heterotermites, North American white ants, Southern white ants, Southern European reticulated white ants, Santer white ants, Taiwanese white ants; cockroaches (Blatidae), such as German cockroaches, Asian cockroaches, American cockroaches, Japanese cockroaches, Brown cockroach, black-breasted cockroach, Australian cockroach, and oriental cockroach; ants, bees, wasps, leaf bees (Hymenoptera) such as cabbage bees, tropical leaf-cutting ants, big-headed leaf-cutting ants, leaf-cutting ants , Texas leaf-cutting ants, ant, black ants, yellow house ants, fire ants, red fire ants, black fire ants, red harvest ants, harvester ants, big-headed ants, tasmania, bumblebees, Yellow spotted wasp, Pennsylvanian cockroach, yellow-side wasp, long-legged wasp, Florida ant, and Argentine ant; crickets, grasshoppers, locusts (Orthoptera), such as house cricket, European mole cricket, Oriental migratory locust, double Grasshopper, red-footed black locust, Mexican black locust, blood black locust, Rocky mountain locust, red-winged locust, American desert locust, desert locust, Moroccan halodendron, Gard locust, Indian locust, Italian locust , Australian plague, and brown migratory locust; Arachnid, such as black widow spiders and human arachnid spiders; Fleas (Sylla), such as cat ctenops, dog fleas, squirrel fleas, itchy fleas, skin diving Fleas, and disease-bearing fleas, silverfish (Thysanoptera), such as small fish, centipedes (centipedes), such as feeding ants, polypods (Dipoda), such as earwigs (Dermoptera) ), for example, centipede, lice (Coleoptera), such as human head lice, human lice, human pubic lice, bovine blood wind, blood lice, bovine jaw lice, cattle feather lice and buffalo blind lice; Collembola ), such as the genus Acanthopanax.

他們也適用於控制線蟲:植物寄生線蟲,如根結線蟲、北方根結線蟲、南方根結線蟲、爪哇根結線蟲和其他根結線蟲;囊腫形成線蟲、馬鈴薯金線蟲和其他線蟲物種; 燕麥胞囊線蟲、大豆胞囊線蟲、甜菜胞囊線蟲、三葉草胞囊線蟲和其他異皮蟲物種; 種子線蟲、蛇墊刃種; 莖和葉線蟲、滑刃線蟲物種; 刺線蟲、芹刺線蟲和其他刺線蟲物種; 松材線蟲、傘滑刃松材線蟲和其他松材線蟲; 環線蟲、環屬物種、小環線蟲物種、輪線蟲物種、中環線蟲物種; 莖和鱗莖線蟲、甘薯莖線蟲、鱗球莖莖線蟲和其他莖線蟲屬物種; 錐線蟲、錐線蟲物種;螺旋線蟲、香蕉螺旋線蟲和其他螺旋線蟲物種; 鞘和鞘線蟲、鞘線蟲物種和半輪線蟲物種; 潛根線蟲屬物種; 矛線蟲, 矛線蟲屬; 假根線蟲、珍珠線蟲物種; 針線蟲、延伸長針線蟲和其他長針線蟲物種; 病斑線蟲、落選短體線蟲、穿刺短體線蟲、彎曲針線蟲、短體線蟲和其他短體線蟲物種; 穴居線蟲、香蕉穿孔線蟲和其他穿孔線蟲物種; 腎形腎狀線蟲, 盤旋線蟲和盤旋線蟲物種; 盾線蟲物種; 短粗根線蟲、軟骨毛刺線蟲和其他毛刺線蟲物種、擬毛刺物種; 矮化線蟲, 克萊頓矮化線蟲, 順逆矮化線蟲和其他矮化線蟲物種; 柑橘線蟲、穿刺線蟲物種; 匕首線蟲、劍線蟲物種; 和其他植物寄生線蟲種類。They are also suitable for controlling nematodes: plant parasitic nematodes such as root knot nematode, northern root knot nematode, southern root knot nematode, Java root knot nematode and other root knot nematodes; cyst forming nematode, potato golden nematode and other nematode species; oat spores Cyst nematode, soybean cyst nematode, sugar beet cyst nematode, clover cyst nematode, and other heteroderma Spiny nematode species; Bursaphelenchus xylophilus, Bursaphelenchus xylophilus, and other pine wood nematodes; Ring nematodes, Ringworm species, Microcircle nematode species, Rotifer species, Central ring nematode species; Stem and bulb nematodes, Ditylenchus sweetpotato, scale Ditylenchus corms and other Ditylenchus species; Trypanosoma, Trypanosoma species; Helix nematode, Banana spiral nematode, and other Helix nematode species; Sheath and sheath nematodes, Coleoptile nematode species and Hemicyclic nematode species; Hypotomyza species; Spear Nematodes, Spike nematodes; Pseudoroot nematode, Pearl nematode species; Needle nematodes, Elongated long needle nematodes, and other long needle nematode species; Spotted nematodes, Unselected short needle nematodes, Punctured short needle nematodes, bent needle nematodes, short needle nematodes, and other short needle nematodes Nematode species; burrowing nematode, banana perforation nematode, and other perforating nematode species; kidney-shaped nematodes, spiral nematodes and spiral nematode species; Scutellaria species; Scutellaria species; Scutellaria spp., Trichocarhinia cartilaginous and other Trichodonta species, and prickly-like species Dwarf nematodes, Clayton dwarf nematodes, reciprocal dwarf nematodes and other dwarf nematode species; Citrus nematodes, piercing nematode species; Dagger nematodes, sword nematode species; and other plant parasitic nematode species.

式(I)化合物及其鹽也可用於控制蛛形綱動物(蛛形綱),例如蟎蟲(蜱蟎目), 例如隱喙蜱、硬蜱科和疥蟎物種,如美洲花蜱、飾鈍眼蜱、波斯銳緣蜱、具環牛蜱、微小牛蜱、森林革蜱、長喙璃眼蜱、篦子硬蜱、淺紅硬蜱、非洲鈍緣蜱、與壁蟲、雞皮刺蟎、羊癢蟎、附加扇頭蜱、外翻扇頭蜱、疥蟎,和癭蟎科物種,如蘋果刺鏽蟎, 柑橘鏽蟎和柑橘癭蟎; 跗線蟎科,如側多食跗線蟎; 細須蟎科,如紫紅短須蟎; 葉蟎科,如朱砂葉蟎、神澤氏葉蟎、太平洋葉蟎、棉葉蟎和二斑葉蟎、蘋果全爪蟎、全爪蟎和草地小爪蟎。The compounds of formula (I) and their salts can also be used to control arachnids (Arachnida), such as mites (Acarina), such as cryptorhynchus, Ixodes and scabies species, such as American flower tick, Acarina Eye tick, Persian sharp tick, ringed cattle tick, micro tick, Dermatophaga forest, Hyalopsis longiborus, Ixodes vulgaris, Ixodes light red tick, Ornithodoros africa, and wall worms, Spiny dermatoglyphus, sheep Itch mites, additional Rhipicephalus ticks, Rhizophora valgus, scabies, and mites of the family mites, such as apple spiny rust mites, citrus rust mites and citrus gall mites; Tarsus mites, such as polyphagous tarsus mites; Tetranychus family, such as purplish red short hair mites; Tetranychus family, such as cinnabarinus spider mite, Kanzawa's spider mite, Pacific spider mite, cotton spider mite and two-spotted spider mite, apple panonychus mite, panonychus mites and grass mites Claw mite.

在本發明的另一個實施方案中、式(I)化合物可用於防治選自吮吸或刺穿昆蟲的昆蟲、例如來自纓翅目、雙翅目和半翅目的昆蟲,特別是以下物種: 纓翅目:富氏小蠊、枕骨小蠊、黑線小蠊、檸檬黃薊馬、稻瘟病薊馬、棕櫚薊馬和薊馬; 雙翅目:例如埃及伊蚊、白紋伊蚊、白紋伊蚊、按實蠅、五斑按蚊、災難按蚊、白魔按蚊、岡比亞按蚊、泛生按蚊、白斑按蚊、小按蚊、四孔按蚊、紅頭麗蠅、地中海實蠅、蛆症金蠅、古人類按蚊、黃斑按蚊、盤金龜子、矽金龜子、大西洋按蚊、嗜人錐蠅、 高梁癭蚊、人皮蠅、毛庫蠓、尖音庫蚊、黑須庫蚊、致倦庫蚊、跗葉庫蚊、紫色庫蚊、黑尾賽蚊、瓜實蠅、油橄欖實蠅、油菜葉癭蚊、蔥蠅、麥地種蠅、灰地種蠅、甘藍地種蠅、人膚皮蠅、夏廁蠅、尺禾蠅屬、腸胃蠅、刺舌蠅、須舌蠅、舌蠅屬、擬寄舌蠅、西方角蠅、潛蠅屬、種蠅、紋皮蠅、托氏細蠓、美洲斑潛蠅、三葉斑潛蠅、巴西綠蠅、銅綠蠅、絲光綠蠅、曼蚊屬、黑森癭蚊、秋家蠅、家蠅、廄腐蠅、發情羊屬、禾蠅屬、瑞典麥稈蠅、天仙子泉妮、廄腐蠅、蘿蔔蠅、草種蠅屬、銀足白蛉、哥倫比亞鱗蚊、胡蘿蔔莖蠅、鱗蚊屬、原蚋屬、櫻桃繞實繩、蘋果實蠅、赤尾麻蠅、麻蠅屬、帶蚋、廄螫蠅、牛虻、北美黑虻、馬蠅、和虻屬、大蚊屬和沼澤大蚊; 半翅目,尤其是蚜蟲類: 無網管蚜、落葉松球蚜、納豆蚜、蠶豆蚜、福建蚜、蘋果蚜、棉蚜、北美荼簏子姆、苔草蚜、卷葉蟲牙、豌豆長管蚜、茄溝無網蚜、短尾蚜屬、李短尾蚜、桃仁短尾蚜、短尾蝗、菜蚜、釘毛蚜、中瘤釘毛蚜、荼薦隱瘤姆、椎球蟲牙、雲杉椎球蟲牙、圓尾蚜、車前圓尾蚜、馬鈴薯小綠葉蟬、大尾蟲牙、超瘤蚜屬、麥長管蚜、馬鈴薯長管蚜、管蟲牙、巢菜修尾蚜、色蚜、麥無網長管蚜、冬蔥瘤額蚜、瘤蚜、衲長管蚜屬、褐飛虱、囊柄瘦綿蟲牙、甘蔗扁角飛虱、忽布疣額蚜、及蘋果木虱、梨木虱、玉米縊管蚜、稻麥蚜、圓尾蚜、麥二叉蚜、裂鞘葉蚜、麥長管蚜、溫室粉虱、桔二叉蚜和葡萄根瘤蚜。In another embodiment of the present invention, the compound of formula (I) can be used to control insects selected from sucking or piercing insects, for example from Thysanoptera, Diptera and Hemiptera, especially the following species: Thysanoptera: Blattella fuschia, Blattella occipitalis, Blattella nigra, Lemon yellow thrips, Rice blast thrips, Palm thrips and thrips; Diptera: For example, Aedes aegypti, Aedes albopictus, Aedes albopictus, Anopheles quinquefolius, Anopheles vulgaris, Anopheles albopictus, Anopheles gambiae, Anopheles panax, Anopheles leucocephalus, small Anopheles, Anopheles tetragonus, Blowfly, Mediterranean fruit fly, Anopheles maggot, Anopheles ancient, Anopheles maculatus, Chafer, Anopheles siella, Anopheles anthropophagus, Anopheles anthropophagus, Sorghum gall midge, human Skin flies, Culex pipiens, Culex pipiens, Culex black-bearded, Culex pipiens fatigue, Culex tarsalis, Culex purple, black-tailed mosquito, fruit fly, olive fruit fly, rape leaf gall midge, green onion Flies, wheat field flies, gray field flies, cabbage field flies, human skin skin flies, summer toilet flies, geometridae, gastrointestinal flies, tsetse flies, tsetse flies, tsetse flies, parasitic tsetse flies , Western horn fly, Liriomyza, Species, Liriomyza, Liriomyza todii, Liriomyza sativae, Liriomyza triloba, Lucilia brazilian, Lucilia sericata, Lucilia sericata, Manna, Hessian Gall Mosquitoes, autumn house flies, house flies, rotting flies, oestrus, gramineus, swedish wheat stalk flies, hydrangea springni, rotting flies, turnip flies, grass species, silver-footed sandflies, Colombian scales Mosquitoes, carrot stalk flies, scale mosquitoes, original gnats, cherry stalks, apple fruit flies, red-tailed Sarcophaga, Sarcophaga, gnats, stinging flies, gadfly, North American black horsefly, horsefly, and horsefly, large Mosquitoes and marsh crane mosquitoes; Hemiptera, especially aphids: aphid, larch aphid, natto aphid, broad bean aphid, fujian aphid, apple aphid, cotton aphid, sphaeranthus vulgaris, carex aphid, leaf roller tooth, pipe pea aphid , Aphid spp., Aphid spp., Aphid plum, Aphid prunus, Brachyura aphid, Aphid locust, Aphid aphid, Aphid aphid, Aphid spp, Aphid spp, Spondylococcal tooth, cloud Cunninghamia lanceolata, round-tailed aphid, plantain aphid, potato green leafhopper, big-tailed ivory, hyperurophis, tube aphid, potato tube aphid, tube worm tooth, vetch aphid, color aphid, wheat Aphids without nets, Aphids on winter onion, Aphids, Aphids, Nilaparvata lugens, Lean worm teeth, Sugarcane planthoppers, Aphids, Apple psyllids, Psylla pears , Corn Aphid, Rice Wheat Aphid, Round Tail Aphid, Wheat Aphid, Schizophyllum, Pipe Aphid, Greenhouse Whitefly, Citrus Aphid and Grape Phylloxera.

在一個實施方案中,本發明提供包含生物有效量的式(I)化合物和至少一種另外的選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素、WO2016156129和WO2017153200中報導的殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素、肥料和營養素與至少一種本發明的式(I)化合物的結合應納入本文作為非限制性實施例。肥料和營養素的生物活性相容化合物的組合物。該組合物中使用的化合物和與式(I)化合物組合的化合物也稱為活性相容化合物。In one embodiment, the present invention provides a compound comprising a biologically effective amount of formula (I) and at least one additional selected suicide fungicide, insecticide, nematicide, acaricide, bioinsecticide, herbicide, plant Growth regulators, antibiotics, fungicides, insecticides, nematicides, acaricides, bioinsecticides, herbicides, plant growth regulators, antibiotics, fertilizers and nutrients reported in WO2016156129 and WO2017153200 and at least one of these substances Inventive combinations of compounds of formula (I) should be included herein as non-limiting examples. A combination of fertilizers and nutrients with bioactive compatible compounds. The compound used in the composition and the compound combined with the compound of formula (I) are also referred to as active compatible compounds.

已知的和報導的殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素和營養素可以與至少一種本公開的式(I)化合物組合。例如,WO2016156129和WO2017153200中公開和報導的殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物殺蟲劑、除草劑、植物生長調節劑、抗生素、肥料和營養素可以與至少一種本公開的式(I)化合物組合。Known and reported fungicides, insecticides, nematicides, acaricides, bioinsecticides, herbicides, plant growth regulators, antibiotics and nutrients can be combined with at least one compound of formula (I) of the present disclosure combination. For example, the fungicides, insecticides, nematicides, acaricides, bioinsecticides, herbicides, plant growth regulators, antibiotics, fertilizers, and nutrients disclosed and reported in WO2016156129 and WO2017153200 can be combined with at least one of the present disclosure. A combination of compounds of formula (I).

特別地,本發明的化合物可以與至少一種另外的生物活性相容化合物混合形成多組分農藥,提供更廣泛的農業用途。所述化合物包括但不限於殺蟲劑、殺真菌劑、殺線蟲劑、殺菌劑、殺蟎劑、生長調節劑如生根刺激劑、化學絕育劑、化學資訊素、驅避劑、引誘劑、資訊素、餵食興奮劑、其他生物活性化合物或昆蟲病原細菌、病毒或真菌。In particular, the compound of the present invention can be mixed with at least one other biologically active compatible compound to form a multi-component pesticide, providing a wider range of agricultural applications. The compounds include, but are not limited to, insecticides, fungicides, nematicides, fungicides, acaricides, growth regulators such as rooting stimulants, chemical sterilization agents, chemical information elements, repellents, attractants, information Vegetarian, feeding stimulants, other biologically active compounds or insect pathogenic bacteria, viruses or fungi.

WO2019072906A1(第27至37頁)公開了可以與本發明的式(I)化合物組合/配製的此類生物活性化合物或試劑/配製物的實例。WO2019072906A1 (pages 27 to 37) discloses examples of such biologically active compounds or reagents/formulations that can be combined/formulated with the compound of formula (I) of the present invention.

在一個實施方案中,用於與本發明化合物混合的生物製劑包括蘇雲金芽孢桿菌、蘇雲金芽孢桿菌δ內毒素以及天然存在的和基因改造的病毒殺蟲劑,包括杆狀病毒科的成員以及昆蟲真菌。In one embodiment, the biological agents used for mixing with the compounds of the present invention include Bacillus thuringiensis, Bacillus thuringiensis delta endotoxin, and naturally-occurring and genetically modified viral insecticides, including members of the baculoviridae family and insect fungi .

在某些情況下,與其他無脊椎害蟲防治化合物或具有相似控制譜但具有不同作用模式的試劑的組合特別有利於抗性管理。因此,本發明的組合物可以進一步包含至少一種另外的生物有效量的無脊椎害蟲防治化合物或具有相似控制譜但具有不同作用模式的試劑。接觸經生物學有效量的本發明化合物基因改造的植物或植物的的位點以表達植物保護化合物(例如,蛋白質)也可以提供更廣譜的植物保護並且有利於抗性管理。In some cases, the combination with other invertebrate pest control compounds or agents with similar control profiles but different modes of action is particularly beneficial for resistance management. Therefore, the composition of the present invention may further comprise at least one additional biologically effective amount of an invertebrate pest control compound or an agent having a similar control spectrum but a different mode of action. Contacting plants or plant sites genetically modified with a biologically effective amount of the compounds of the present invention to express plant protection compounds (for example, proteins) can also provide a broader spectrum of plant protection and facilitate resistance management.

在本發明的一個實施方案中,組合物中式(I)化合物的生物有效量為組合物總重量的0.1%至99%,優選5%至50%。In one embodiment of the present invention, the biologically effective amount of the compound of formula (I) in the composition is 0.1% to 99%, preferably 5% to 50% of the total weight of the composition.

本發明還涉及一種對抗昆蟲和蟎害蟲的方法,所述方法包括用生物有效量的本發明化合物或組合物接觸無脊椎動物害蟲、其棲息地、繁殖地、食物、植物、種子、土壤、無脊椎動物害蟲生長或可能生長的區域、材料或環境,或希望免受蟲害或侵擾的材料、植物、種子、土壤。The present invention also relates to a method for combating insects and mite pests, the method comprising contacting invertebrate pests, their habitats, breeding grounds, food, plants, seeds, soil, and invertebrate pests with a biologically effective amount of the compound or composition of the present invention. The area, material, or environment where vertebrate pests grow or are likely to grow, or materials, plants, seeds, and soil that are desired to be protected from pests or infestations.

通過將一種或多種本發明化合物以有效量施用於害蟲的環境,包括農藝和/或農藝上侵染的位點、要保護的區域或直接在要控制的害蟲上來實現對無脊椎動物害蟲的控制和對農藝、園藝和特種作物的保護、實現動物和人類健康。 因此,本發明進一步包括控制葉和土壤棲息的無脊椎動物和保護農藝和/或非農作物的方法,包括使無脊椎動物或其環境與生物有效量的一種或多種本發明化合物接觸,或包含至少一種這樣的化合物的組合物或包含至少一種這樣的化合物和有效量的至少一種另外的生物活性化合物或藥劑的組合物。優選的接觸方法是噴霧。或者, 包含本發明化合物的顆粒組合物可以施用於植物葉子或土壤。本發明的化合物通過使植物與包含本發明化合物的組合物接觸而通過植物攝取有效遞送,所述組合物作為液體製劑的土壤浸漬劑、顆粒製劑施用於土壤,育苗箱處理或浸漬。其他接觸方法包括通過直接和殘留噴霧、空氣噴霧、種皮、微囊化、全身攝取、誘餌、耳標、大丸劑、噴霧劑、薰蒸劑、氣溶膠、粉塵和許多其他方法施用本發明的化合物或組合物。The control of invertebrate pests is achieved by applying one or more compounds of the present invention in an effective amount to the pest environment, including agronomic and/or agronomically infested sites, areas to be protected or directly on the pests to be controlled And the protection of agronomy, horticulture and special crops, and the realization of animal and human health. Therefore, the present invention further includes methods for controlling leaf and soil-inverted invertebrates and protecting agronomic and/or non-agricultural crops, including contacting the invertebrates or their environment with a biologically effective amount of one or more compounds of the present invention, or containing at least A composition of such a compound or a composition comprising at least one such compound and an effective amount of at least one additional biologically active compound or agent. The preferred contact method is spraying. Alternatively, the granular composition containing the compound of the present invention can be applied to plant leaves or soil. The compound of the present invention is effectively delivered by plant ingestion by contacting the plant with a composition containing the compound of the present invention, the composition is applied to the soil as a soil soaking agent of a liquid formulation, a granular formulation, treatment or dipping in a nursery box. Other methods of contact include direct and residual spray, air spray, seed coat, microencapsulation, systemic ingestion, bait, ear tag, bolus, spray, fumigant, aerosol, dust and many other methods to apply the compound of the present invention Or composition.

本發明的化合物可以摻入由無脊椎動物喜愛的誘餌中或在諸如誘捕器等裝置內。包含0.01-5%活性成分、0.05-10%保濕劑和40-99%植物粉的顆粒或誘餌,特別是通過攝入而不是通過直接接觸活性成分劑量下致死能在非常低的施用率下有效控制土壤昆蟲。本發明的化合物可以其純態施用,但最常應用的施用是配合包含一種或多種具有合適載體、稀釋劑和表面活性劑的化合物的製劑,也有可能與食物組合,這取決於預期的最終用途。優選的施用方法包括噴灑化合物的水分散體或精製油溶液。與噴霧油、噴霧油濃度、塗布劑貼劑、佐劑、其他溶劑和增效劑(如胡椒基丁醚)的組合通常可提高化合物功效。The compounds of the present invention can be incorporated into baits favored by invertebrates or in devices such as traps. Granules or baits containing 0.01-5% active ingredient, 0.05-10% moisturizer and 40-99% plant powder, especially lethal by ingestion rather than by direct contact with the active ingredient dose, can be effective at very low application rates Control soil insects. The compound of the present invention can be administered in its pure form, but the most commonly used application is a formulation containing one or more compounds with suitable carriers, diluents and surfactants, and it may also be combined with food, depending on the intended end use . A preferred method of application includes spraying an aqueous dispersion of the compound or a refined oil solution. Combinations with spray oils, spray oil concentrations, coating patches, adjuvants, other solvents, and synergists (such as piperonyl butoxide) can often improve compound efficacy.

有效控制所需的施用率(即“生物有效量”)將取決於諸如待控制的無脊椎動物的種類、有害生物的生命週期、生命階段、其大小、位置、季節、宿主作物或動物、攝食行為、交配行為、環境濕度、溫度等。在正常情況下,每公頃約0.01至2千克活性成分的施用量足以控制農業生態系統中的害蟲,但也有公頃可能只需要0.0001千克,或需要多達8千克。 對於非農藝用途,有效使用率範圍約為1.0至50毫克/平方米,但也可能只需0.1毫克/平方米,最多可能需要150毫克/平方米。本領域技術人員可以容易地確定防治無脊椎害蟲水準所需的生物有效量。The application rate required for effective control (ie, the "biologically effective amount") will depend on such things as the type of invertebrate to be controlled, the life cycle of the pest, its life stage, its size, location, season, host crop or animal, and food intake. Behavior, mating behavior, environmental humidity, temperature, etc. Under normal circumstances, an application rate of about 0.01 to 2 kg of active ingredients per hectare is sufficient to control pests in agro-ecosystems, but some hectares may only require 0.0001 kg, or as much as 8 kg. For non-agricultural purposes, the effective utilization rate ranges from about 1.0 to 50 mg/m², but it may only be 0.1 mg/m², and up to 150 mg/m² may be required. Those skilled in the art can easily determine the biologically effective amount required to control the level of invertebrate pests.

可以通過本領域已知的施用方法使植物生長的動物害蟲(即昆蟲、蜘蛛和線蟲)、植物、土壤或水與式(I)化合物和它們的N-氧化物和鹽或含有它們的組合物接觸。因此,“接觸”包括直接接觸(將化合物/組合物直接施用於動物害蟲或植物上通常施用於植物的葉子,莖或根)和間接接觸(將化合物/組合物施用於動物害蟲或植物的所在地)。Animal pests (ie insects, spiders and nematodes), plants, soil or water that can grow plants by application methods known in the art, and compounds of formula (I) and their N-oxides and salts or compositions containing them contact. Therefore, "contact" includes direct contact (applying the compound/composition directly to animal pests or plants that are usually applied to the leaves, stems or roots of plants) and indirect contact (applying the compound/composition to the locus of animal pests or plants ).

本發明的化合物或包含它們的殺蟲組合物可用於通過使植物/作物與殺蟲有效量的至少一種本發明的化合物接觸來保護生長的植物和作物免受動物害蟲(特別是昆蟲、蟎科或蜘蛛)的侵擾或侵染。“作物”一詞指正在生長的和收穫的作物。The compounds of the present invention or insecticidal compositions containing them can be used to protect growing plants and crops from animal pests (especially insects, acarids, etc.) by contacting plants/crops with an insecticidal effective amount of at least one compound of the present invention. Or spider) infestation or infestation. The term "crops" refers to crops that are growing and harvested.

在一個實施方案中,本發明提供了一種保護作物免受無脊椎動物有害生物攻擊或侵擾的方法,該方法包括使作物與生物有效量的本發明化合物或組合物、異構體、多晶型、N-氧化物或其鹽接觸。In one embodiment, the present invention provides a method for protecting crops from attack or infestation by invertebrate pests. The method includes combining the crop with a biologically effective amount of the compound or composition, isomer, or polymorph of the present invention. , N-oxide or its salt contact.

本發明的化合物可以原樣使用或以組合物的形式使用殺蟲有效量的活性化合物處理昆蟲或植物、植物繁殖材料,如種子、土壤、表面、材料或空間使其免受殺蟲性攻擊。施用可以在植物、植物繁殖材料、例如昆蟲的種子,土壤,表面,材料或感染之前和之後間進行感染之前和之後。The compound of the present invention can be used as it is or in the form of a composition using an insecticidal effective amount of the active compound to treat insects or plants, plant propagation materials, such as seeds, soil, surfaces, materials, or spaces, to protect them from insecticidal attack. Application can be carried out before and after infection of plants, plant propagation material, such as insect seeds, soil, surface, material or between before and after infection.

在一個實施方案中,本發明提供了一種保護種子免受土壤昆蟲侵害和保護幼苗免受土壤和葉蟲侵害的根和芽的方法,該方法包括在種子播種之前和/或萌芽之後與本發明化合物或其組合物、N-氧化物或其鹽接觸種子。In one embodiment, the present invention provides a method of protecting seeds from soil insects and protecting seedlings from soil and leaf insects’ roots and shoots. The method includes contacting the present invention with seeds before sowing and/or after germination. The compound or its composition, the N-oxide or its salt contacts the seed.

此外,本發明涉及治療或保護動物免受寄生蟲侵擾或感染的方法,該方法包括口服,局部或腸胃外給予或給動物施用生物有效量的本發明化合物或組合物、異構體、多晶型物、N-氧化物或獸醫學上可接受的鹽。In addition, the present invention relates to a method for treating or protecting an animal from infestation or infection by parasites. The method includes oral, topical or parenteral administration or administering to the animal a biologically effective amount of the compound or composition, isomer, or polymorph of the present invention. Type, N-oxide or veterinary acceptable salt.

對於在農業或園藝作物中用於處理農作物植物,本發明化合物的施用率(施用有效劑量)可以在1g至5000 /公頃的範圍內,優選25g至600g / 公頃,更優選每公頃50g至 500g克。For the treatment of crop plants in agricultural or horticultural crops, the application rate (effective dose applied) of the compound of the present invention may be in the range of 1 g to 5000 /ha, preferably 25 g to 600 g / hectare, more preferably 50 g to 500 g per hectare .

本發明的化合物和組合物特別適用於控制各種栽培植物上的多種昆蟲,例如穀類、塊根作物、油料作物、蔬菜、香料、觀賞植物,例如硬粒小麥和其他小麥的種子、大麥、燕麥、黑麥、玉米(飼料玉米和糖玉米/甜和田玉米)、大豆、油料作物、十字花科植物、棉花、向日葵、香蕉、大米、油菜、蕪菁油菜、甜菜、飼料甜菜、茄子、土豆、草、草坪、草皮、飼料草、番茄、韭菜、南瓜/南瓜、白菜、卷心萵苣、胡椒、黃瓜、甜瓜、芸苔屬植物、甜瓜、豆類、豌豆、大蒜、洋蔥、胡蘿蔔、馬鈴薯等塊莖植物、 甘蔗、煙草、葡萄、矮牽牛、天竺葵/香葉天竺葵、三色紫羅蘭和鳳仙花。The compounds and compositions of the present invention are particularly suitable for controlling various insects on various cultivated plants, such as cereals, root crops, oil crops, vegetables, spices, ornamental plants, such as durum wheat and other wheat seeds, barley, oats, black Wheat, corn (forage corn and sugar corn/sweet corn), soybeans, oil crops, cruciferous plants, cotton, sunflower, banana, rice, rape, turnip rape, sugar beet, fodder beet, eggplant, potato, grass, lawn , Turf, fodder grass, tomato, leeks, pumpkin/pumpkin, cabbage, iceberg lettuce, pepper, cucumber, melon, brassica, cantaloupe, beans, peas, garlic, onion, carrot, potato and other tuber plants, sugar cane, Tobacco, grapes, petunia, geranium/geranium, pansies and impatiens.

特別地,本發明的化合物或組合物可用於保護農作物,例如穀物、玉米、水稻、大豆和其他豆科植物、水果和果樹、葡萄、堅果和堅果樹、柑橘和柑橘樹、任何園藝植物、葫蘆科、含油植物、煙草、咖啡、茶、可哥、甜菜、甘蔗、棉花、馬鈴薯、番茄、洋蔥、辣椒和其他蔬菜和觀賞植物。In particular, the compounds or compositions of the present invention can be used to protect crops, such as cereals, corn, rice, soybeans and other legumes, fruits and fruit trees, grapes, nuts and nut trees, citrus and citrus trees, any horticultural plants, gourds Family, oily plants, tobacco, coffee, tea, cocoa, sugar beet, sugar cane, cotton, potato, tomato, onion, pepper and other vegetables and ornamental plants.

本發明的化合物通過接觸(通過土壤、草、牆壁、床網、地毯、植物部分或動物部分)和攝取(誘餌或植物部分)都有效。The compounds of the present invention are effective both through contact (through soil, grass, walls, bed nets, carpets, plant parts or animal parts) and ingestion (bait or plant parts).

本發明的化合物還可以用於非作物昆蟲和蟎害蟲,例如螞蟻、白蟻、黃蜂、蒼蠅、蚊子、蟋蟀或蟑螂。為了對抗所述非作物害蟲,本發明化合物優選用於誘餌合成物中。The compounds of the present invention can also be used for non-crop insects and mite pests, such as ants, termites, wasps, flies, mosquitoes, crickets or cockroaches. In order to combat the non-crop pests, the compounds of the present invention are preferably used in bait compositions.

誘餌可以是液體,固體或半固體製劑(例如凝膠)。固體誘餌可以形成適合於各自的施用的各種形狀和形式,例如顆粒、塊、棒、盤。液體誘餌可以填充到各種裝置中以確保適當的應用,例如開口容器、噴霧裝置、液滴源或蒸發源。 凝膠可以基於水性或油性基質,並且可以在黏性、保濕性或老化特性方面配製成特定的必需品。The bait can be a liquid, solid or semi-solid preparation (eg gel). The solid bait can be formed into various shapes and forms suitable for the respective application, such as granules, blocks, rods, discs. The liquid bait can be filled into various devices to ensure proper application, such as open containers, spray devices, droplet sources, or evaporation sources. Gels can be based on water-based or oily bases, and can be formulated into specific necessities in terms of viscosity, moisturizing or aging properties.

該組合物中使用的誘餌是一種產品,其足以吸引諸如螞蟻、白蟻、黃蜂、蒼蠅、蚊子、蟋蟀等昆蟲或蟑螂來食用它。可以通過使用餵食興奮劑或性資訊素來操縱吸引力。例如,可以但不限於是從動物和/或植物蛋白(肉、魚粉、昆蟲部分、蛋黃)、動物和/或植物來源的脂肪和油、或單-、寡糖聚有機糖類、低聚聚有機糖、尤其是蔗糖、乳糖、果糖、右旋糖、葡萄糖、澱粉、果膠或甚至糖蜜或蜂蜜選擇食物興奮劑。水果、作物、植物、動物、昆蟲或其特定部分的新鮮或腐爛部分也可用作餵食刺激劑。已知性資訊素更具昆蟲特異性。 特定的資訊素在文獻中描述並且是本領域技術人員已知的。The bait used in the composition is a product that is sufficient to attract insects such as ants, termites, wasps, flies, mosquitoes, crickets, or cockroaches to eat it. The attraction can be manipulated through the use of feeding stimulants or sex pheromone. For example, it can be, but not limited to, animal and/or vegetable protein (meat, fish meal, insect parts, egg yolk), fat and oil of animal and/or vegetable origin, or mono-, oligosaccharide polyorganic sugars, oligomeric organic Sugars, especially sucrose, lactose, fructose, dextrose, glucose, starch, pectin or even molasses or honey select food stimulants. Fresh or rotten parts of fruits, crops, plants, animals, insects or specific parts thereof can also be used as feeding stimulants. It is known that sex pheromone is more insect-specific. Specific pheromones are described in the literature and are known to those skilled in the art.

用於誘餌組合物時,活性成分的典型含量為占重量比的0.001%至15%,理想地為占重量比的0.001%至5%。When used in a bait composition, the typical content of the active ingredient is 0.001% to 15% by weight, ideally 0.001% to 5% by weight.

配置本發明化合物作為噴霧劑(例如噴霧罐)、油噴霧劑或泵式噴霧劑非常適合於非專業用戶控制害蟲如蒼蠅、跳蚤、蜱、蚊子或蟑螂。噴霧劑配方優選由活性化合物,溶劑如低級醇(如甲醇、乙醇、丙醇、丁醇),酮類(如丙酮、甲基乙基酮),沸程約為50-250°C石蠟烴(如煤油)、二甲基甲醯胺、N-甲基吡咯烷酮、二甲基亞碸、芳香族烴類如甲苯、二甲苯、水、以及輔助劑如乳化劑如山梨糖醇單油酸酯、油醯基乙氧基化物、具有3-7摩爾環氧乙烷、脂肪醇乙氧基化物、香料油等作為醚油、中等脂肪酸與低級醇的酯、芳香族化合物、如果合適的話,穩定劑如苯甲酸鈉、兩性表面活性劑、低級環氧化物、原甲酸三乙酯、如果需要,推進劑如丙烷、丁烷、氮氣、壓縮空氣、二甲醚、二氧化碳、硝基氧化物或這些氣體的混合物組成。The preparation of the compound of the present invention as a spray (such as a spray can), an oil spray or a pump spray is very suitable for non-professional users to control pests such as flies, fleas, ticks, mosquitoes or cockroaches. The spray formulation is preferably composed of active compounds, solvents such as lower alcohols (such as methanol, ethanol, propanol, butanol), ketones (such as acetone, methyl ethyl ketone), with a boiling range of about 50-250°C paraffin hydrocarbons ( Such as kerosene), dimethylformamide, N-methylpyrrolidone, dimethyl sulfide, aromatic hydrocarbons such as toluene, xylene, water, and auxiliary agents such as emulsifiers such as sorbitol monooleate, Oleoyl ethoxylates, with 3-7 moles of ethylene oxide, fatty alcohol ethoxylates, perfume oils, etc. as ether oils, esters of medium fatty acids and lower alcohols, aromatic compounds, stabilizers if appropriate Such as sodium benzoate, amphoteric surfactants, lower epoxides, triethyl orthoformate, if necessary, propellants such as propane, butane, nitrogen, compressed air, dimethyl ether, carbon dioxide, nitroxide or these gases Mixture composition.

噴油配方與噴霧配方的不同之處在於不使用推進劑。在噴霧組合物中,活性成分的占總重量的0.001至80%,優選0.01至50%,最優選0.01至15%。The difference between the spray formula and the spray formula is that no propellant is used. In the spray composition, the active ingredient accounts for 0.001 to 80% of the total weight, preferably 0.01 to 50%, most preferably 0.01 to 15%.

本發明的化合物及其各自的組合物也可用於蚊香和薰蒸線圈,煙盒,蒸發器板或長期的噴霧器以及蛾紙、蛾墊或其他不依賴於熱的蒸發器系統。The compounds of the present invention and their respective compositions can also be used in mosquito coils and fumigation coils, cigarette cases, evaporator plates or long-term sprayers, as well as moth paper, moth pads or other heat-independent evaporator systems.

用式(I)化合物及其各自的組合物控制由昆蟲(例如瘧疾,登革熱和黃熱病,淋巴絲蟲病和利什曼病)傳播的傳染病的方法也包括小屋和房屋的表面處理、空氣噴灑和窗簾、帳篷、衣物、蚊帳的浸漬、採蠅捕捉器等。用於纖維、織物、針織品、非織造織物、網狀材料或箔和防水油布的殺蟲組合物優選包含含有殺蟲劑,任選的驅蟲劑和至少一種黏合劑的混合物。合適的驅蟲劑有例如N,N-二乙基-間甲苯醯胺(DEET)、N,N-二乙基苯基乙醯胺(DEPA)、1-(3-環己烷-1-基-羰基)-2-甲基呱啶、(2-羥甲基環己基)乙酸內酯、2-乙基-1,3-己醇和醇、甲基十二醯胺(MNDA)、一種不用於昆蟲控制的擬除蟲菊酯,如(+/-)-3-烯丙基-2-甲基-4-氧代環戊-2-(+)-烯基-(+)-反式-菊酸酯(殺蚊靈)、一種來自或與植物提取物相同的驅蟲劑,如檸檬烯、丁子香酚、來自像單葉蔓荊、檸檬草等粗植物提取物。合適的黏合劑選自例如脂族酸的乙烯基酯(例如乙酸乙烯酯和叔碳酸乙烯酯)的聚合物和共聚物,醇的丙烯酸和甲基丙烯酸酯,例如丙烯酸丁酯、2-乙基己基丙烯酸酯、和丙烯酸甲酯、單和二烯屬不飽和烴,如苯乙烯和脂族二烯,如丁二烯。The method of using the compound of formula (I) and their respective compositions to control infectious diseases spread by insects (such as malaria, dengue fever and yellow fever, lymphatic filariasis and leishmaniasis) also includes surface treatment of cabins and houses, air Spraying and impregnation of curtains, tents, clothing, mosquito nets, fly traps, etc. The insecticidal composition for fibers, fabrics, knitwear, nonwoven fabrics, mesh materials or foils and tarpaulins preferably contains a mixture containing an insecticide, an optional insect repellent and at least one binder. Suitable insect repellents are, for example, N,N-diethyl-m-toluamide (DEET), N,N-diethylphenylacetamide (DEPA), 1-(3-cyclohexane-1- -Carbonyl)-2-methylpiperidine, (2-hydroxymethylcyclohexyl) lactone, 2-ethyl-1,3-hexanol and alcohol, methyl dodecamide (MNDA), one kind Pyrethroids for insect control, such as (+/-)-3-allyl-2-methyl-4-oxocyclopentan-2-(+)-enyl-(+)-trans -Chrysanthemum mosquito ester, an insect repellent derived from or the same as plant extracts, such as limonene, eugenol, and crude plant extracts such as Vitex simplicifolia and lemongrass. Suitable binders are selected from, for example, polymers and copolymers of vinyl esters of aliphatic acids (such as vinyl acetate and vinyl versatate), alcoholic acrylic and methacrylic esters, such as butyl acrylate, 2-ethyl acrylate Hexyl acrylate, and methyl acrylate, mono- and diethylenically unsaturated hydrocarbons such as styrene and aliphatic dienes such as butadiene.

通常簾子和蚊帳的浸漬方法是通過將紡織材料浸入殺蟲劑的乳液或分散劑中或將它們噴灑到網上。Generally, curtains and mosquito nets are impregnated by dipping textile materials into insecticide emulsions or dispersions or spraying them on the net.

本發明的化合物及其組合物可用於保護木質材料,例如樹木、板圍欄、枕木等、以及建築物,例如房屋、外屋、工廠,以及建築材料、傢俱、皮革、纖維、乙烯基製品,電線和電纜等免受螞蟻和/或白蟻的侵擾,用於控制螞蟻和白蟻對作物或人類造成傷害(例如當害蟲侵入房屋和公共設施時)。本發明的化合物不僅應用於周圍的土壤表面或地板下的土壤中以保護木質材料,而且還可以應用於諸如地板下混凝土、壁龕柱、梁、膠合板、傢俱等,木質製品如刨花板、半板等和乙烯基製品如塗層電線、乙烯基片、絕緣材料如苯乙烯泡沫等等的表面上。The compounds of the present invention and their compositions can be used to protect wooden materials, such as trees, board fences, sleepers, etc., and buildings, such as houses, outbuildings, factories, and building materials, furniture, leather, fibers, vinyl products, and wires And cables are protected from ants and/or termites, and used to control ants and termites causing damage to crops or humans (for example, when pests invade houses and public facilities). The compound of the present invention is not only applied to the surrounding soil surface or the soil under the floor to protect wood materials, but also can be applied to such as underfloor concrete, niche pillars, beams, plywood, furniture, etc., wood products such as particle board, half board Etc. and vinyl products such as coated wires, vinyl sheets, insulating materials such as styrene foam, etc. on the surface.

本發明的化合物用於防治螞蟻危害農作物或者人類的,施用於農作物或者周圍土壤,或者直接應用於螞蟻窩等。The compound of the present invention is used to prevent and control ants from harming crops or humans, applied to crops or surrounding soil, or directly applied to ant nests and the like.

種子處理Seed treatment

本發明還進一步涉及包含本發明化合物的種子,特別地,其含量為處理前種子重量的約0.0001%至約1%。The present invention still further relates to seeds containing the compound of the present invention, in particular, the content thereof is about 0.0001% to about 1% of the weight of the seed before treatment.

本發明的化合物還可用於處理種子來保護種子免受昆蟲蟲害,特別是土壤生活昆蟲和蟎蟲的侵擾,而且所得植物的根和芽可抵抗土壤害蟲和葉子昆蟲。The compound of the present invention can also be used to treat seeds to protect seeds from insect pests, especially soil living insects and mites, and the roots and shoots of the resulting plants can resist soil pests and leaf insects.

本發明的化合物用於保護種子免受土壤害蟲的侵擾,以及保護植物長出的根和芽免受土壤害蟲和葉子昆蟲的侵擾尤其有用。可優選用來保護植物長出的根和芽。更優選的是保護所得植物的枝條免受刺穿和吸吮昆蟲的侵擾,最優選的是保護其免受蚜蟲、葉蟬、薊馬和粉虱的侵擾。The compounds of the present invention are particularly useful for protecting seeds from soil pests, as well as protecting plant roots and shoots from soil pests and leaf insects. It can be preferably used to protect the roots and shoots of plants. It is more preferred to protect the branches of the resulting plant from piercing and sucking insects, and most preferred is to protect it from aphids, leafhoppers, thrips and whiteflies.

因此,本發明包括保護種子免受昆蟲(特別是土壤昆蟲)侵擾,保護的幼苗根和芽免受昆蟲(特別是土壤和葉子昆蟲)侵擾的方法,所述方法包括在播種前和/或在催芽後使其本發明化合物接觸種子。在這種方法中,特別優選的是保護其中植物的根和枝被,更優選地是保護其中植物枝條免受昆蟲刺穿和吸吮,最優選的方法保護其中植物枝條免受蚜蟲的侵擾。Therefore, the present invention includes methods for protecting seeds from insects (especially soil insects), and protecting seedling roots and shoots from insects (especially soil and leaf insects), the method comprising before sowing and/or at After accelerating germination, the compound of the invention is brought into contact with the seed. In this method, it is particularly preferred to protect the roots and branches of the plants therein, more preferably to protect the branches of the plants from piercing and sucking by insects, and the most preferred method is to protect the branches of the plants from aphids.

術語“種子”包括各種種子和植物繁殖體,包括但不限於真實種子、種子片、吸盤、球莖、球莖、果實、塊莖、穀粒、插條、切枝等,並且在優選實施方案中是指真正的種子。The term "seed" includes various seeds and plant propagules, including but not limited to real seeds, seed pieces, suckers, bulbs, bulbs, fruits, tubers, grains, cuttings, cut branches, etc., and in a preferred embodiment refers to The real seed.

術語種子處理包括本領域已知的所有合適的種子處理技術,例如拌種、種子包衣、種子撒粉、種子浸泡和種子制粒。The term seed treatment includes all suitable seed treatment techniques known in the art, such as seed dressing, seed coating, seed dusting, seed soaking and seed granulation.

本發明還包括塗有或含有活性化合物的種子。種子可以用含有本發明化合物的種子包衣組合物包衣。例如,在EP3165092、EP3158864、WO2016198644、WO2016039623、WO2015192923、CA2940002、US2006150489、US2004237395、WO2011028115、EP2229808、WO2007067042、EP1795071、EP1273219、WO200178507、EP1247436、NL1012918和CA2083415中報導的種子包衣組合物。The invention also includes seeds coated with or containing active compounds. The seeds can be coated with a seed coating composition containing the compound of the present invention. For example, there are seed coating compositions reported in EP3165092, EP3158864, WO2016198644, WO2016039623, WO2015192923, CA2940002, US2006150489, US2004237395, WO2011028115, EP2229808, WO2007067042, EP1795071, EP1273219, WO200178507, EP1247436, NL1012918, and CA2083415.

術語“塗有和/或含有”通常表示活性成分在施用時大部分在繁殖產品的表面上,儘管成分的更多或更少部分可以滲透到繁殖產品中,取決於應用方法。當(再)種植所述繁殖產品時,它可以吸收活性成分。The term "coated and/or containing" generally means that the active ingredient is mostly on the surface of the reproductive product when applied, although more or less of the ingredient can penetrate into the reproductive product, depending on the method of application. When the propagation product is (re)planted, it can absorb the active ingredients.

合適的種子是穀物、塊根作物、油料作物、蔬菜、香料、觀賞植物的種子、例如硬粒小麥種子和其他小麥、大麥、燕麥、黑麥、玉米(飼料玉米和糖玉米/甜玉米田)、大豆、油料作物、十字花科植物、棉花、向日葵、香蕉、大米、油菜、蕪菁油菜、甜菜、飼料甜菜、茄子、土豆、草、草坪、草皮、飼料草、番茄、韭菜、南瓜/南瓜、捲心菜、卷心萵苣、胡椒、黃瓜、甜瓜、芸苔屬植物、甜瓜、豆類、豌豆、大蒜、洋蔥、胡蘿蔔、塊莖植物如土豆、甘蔗、煙草、葡萄、矮牽牛、天竺葵、三色紫羅蘭和鳳仙花。Suitable seeds are grains, root crops, oil crops, vegetables, spices, seeds of ornamental plants, such as durum wheat seeds and other wheat, barley, oats, rye, corn (forage corn and sugar corn/sweet corn fields), Soybeans, oil crops, cruciferous plants, cotton, sunflower, banana, rice, rapeseed, turnip rape, sugar beet, fodder beet, eggplant, potato, grass, lawn, turf, fodder grass, tomato, leeks, pumpkin/pumpkin, cabbage , Iceberg lettuce, pepper, cucumber, melon, Brassica, melon, beans, peas, garlic, onion, carrot, tubers such as potatoes, sugar cane, tobacco, grapes, petunia, geranium, pansies and impatiens.

此外,本發明的化合物可用於處理由於育種(包括基因工程方法)而耐受除草劑或殺真菌劑或殺蟲劑的作用的植物種子。In addition, the compounds of the present invention can be used to treat plant seeds that are tolerant to herbicides or fungicides or insecticides due to breeding (including genetic engineering methods).

例如,本發明的化合物可用於處理植物的種子,所述植物對除磺醯脲、咪唑啉酮、草銨膦或草甘膦-異丙基銨和類似活性物質的除草劑具有抗性(參見,例如,EP242236,EP242246)(WO92 / 00377)(EP257993,US5013659)或轉基因作物植物(例如棉花)具有產生蘇雲金芽孢桿菌毒素(Bt毒素)的能力,其使植物對某些害蟲具有抗性(EP142924,EP193259)。For example, the compounds of the invention can be used to treat the seeds of plants that are resistant to herbicides other than sulfonylurea, imidazolinone, glufosinate-ammonium or glyphosate-isopropylammonium and similar active substances (see For example, EP242236, EP242246) (WO92/00377) (EP257993, US5013659) or genetically modified crop plants (such as cotton) have the ability to produce Bacillus thuringiensis toxin (Bt toxin), which makes plants resistant to certain pests (EP142924 , EP193259).

此外,本發明的化合物可用於處理來自植物的種子,所述植物與現有植物組成相比具有改變的特徵——其可(例如)通過傳統育種方法和/或突變體的或通過重組程式產生。例如,已經有許多案例描述了為了修飾植物中合成的澱粉而進行重組修飾的作物植物(例如WO92 / 11376,WO92 / 14827,WO91 / 19806)或具有改性脂肪酸組合物的轉基因作物植物 (WO91 / 13972)。In addition, the compounds of the present invention can be used to treat seeds from plants that have modified characteristics compared to existing plant compositions-they can be produced, for example, by traditional breeding methods and/or mutants or by recombinant procedures. For example, there have been many cases describing crop plants that are recombinantly modified in order to modify the starch synthesized in plants (such as WO92/1376, WO92/14827, WO91/19806) or genetically modified crop plants with modified fatty acid compositions (WO91/ 13972).

本發明化合物處理種子的應用是通過在播種植物之前和植物出苗之前噴灑或撒粉種子來進行。The application of the compound of the present invention to treat seeds is carried out by spraying or dusting the seeds before sowing the plants and before the emergence of the plants.

對種子處理特別有用的組合物有,例如: A.   可溶性濃縮物 (SL, LS) B.   乳劑 (EW, EO, ES) C.   懸浮劑 (SC, OD, FS) D.   水分散性顆粒和水溶性顆粒 (WG, SG) E.   水分散性粉末和水溶性粉末 (WP, SP, WS) F.    凝膠製劑 (GF) G.   可撒粉的粉末 (DP, DS) 常規的種子處理製劑包括例如可流動的濃縮物FS、溶液LS、用於乾燥處理的粉末DS、用於漿料處理的水分散性粉末WS、水溶性粉末SS和乳劑ES和EC和凝膠製劑GF。這些製劑可以施用於稀釋或未稀釋的種子。對種子的施用是在播種前進行的,既可以直接施用在種子上,也可以在種子預催芽後施用。Compositions that are particularly useful for seed treatment include, for example: A. Soluble concentrates (SL, LS) B. Emulsion (EW, EO, ES) C. Suspending agent (SC, OD, FS) D. Water-dispersible particles and water-soluble particles (WG, SG) E. Water-dispersible powder and water-soluble powder (WP, SP, WS) F. Gel formulation (GF) G. Powder that can be dusted (DP, DS) Conventional seed treatment formulations include, for example, flowable concentrate FS, solution LS, powder DS for drying treatment, water-dispersible powder WS for slurry treatment, water-soluble powder SS and emulsion ES and EC, and gel formulations GF. These formulations can be applied to diluted or undiluted seeds. The application to the seeds is carried out before sowing, either directly on the seeds or after pre-germination of the seeds.

在一個實施方案中,FS製劑用於種子處理。 特別地,FS製劑可包含1-800g/l活性成分、1-200g/l表面活性劑、0-200g/l防凍劑、0-400g/l黏合劑、0-200g/l顏料和至多1升溶劑(優選水)。In one embodiment, the FS formulation is used for seed treatment. In particular, the FS formulation may contain 1-800g/l active ingredient, 1-200g/l surfactant, 0-200g/l antifreeze, 0-400g/l binder, 0-200g/l pigment and at most 1 liter Solvent (preferably water).

特別地,用於種子處理的本發明化合物的FS製劑通常包含重量比為0.1至80%(1至800g / l)的活性成分,重量比為0.1至20%(1至200g / l)的至少一種表面活性劑,重量比為0.05至5%的濕潤劑和0.5至15%(至多20%)的分散劑,5至20%的防凍劑,重量比為從0至15%(例如1至15%)的顏料和/或染料,重量比為0至40%(例如1至40%)的黏合劑(黏著劑/黏合劑),任選地重量比為至多5%(例如0.1至5%)的增稠劑,任選地重量比為0.1至2%的消泡劑,和任選的防腐劑(例如殺生物劑,抗氧化劑等),例如重量比為0.01 至1%,加上填料/載體組成100%重量。In particular, the FS preparation of the compound of the present invention used for seed treatment usually contains 0.1 to 80% (1 to 800 g / l) of active ingredient in a weight ratio of 0.1 to 20% (1 to 200 g / l) of at least A surfactant with a weight ratio of 0.05 to 5% of wetting agent and 0.5 to 15% (up to 20%) of dispersant, 5 to 20% of antifreeze, and a weight ratio of from 0 to 15% (for example, 1 to 15 %) of pigments and/or dyes, 0 to 40% by weight (for example, 1 to 40%) of binder (adhesive/adhesive), optionally with a weight ratio of up to 5% (for example, 0.1 to 5%) Thickener, optional defoamer with a weight ratio of 0.1 to 2%, and optional preservatives (such as biocides, antioxidants, etc.), for example, with a weight ratio of 0.01 to 1%, plus filler/ The carrier constitutes 100% by weight.

種子處理製劑可另外包含黏合劑和著色劑。The seed treatment formulation may additionally contain a binder and a coloring agent.

可以添加黏合劑以改善活性材料在處理後對種子的黏附。合適的黏合劑是來自亞烷基氧化物的均聚和共聚物,如環氧乙烷或環氧丙烷、聚乙酸乙烯酯、聚乙烯醇、聚乙烯吡咯烷酮及其共聚物、乙烯-乙酸乙烯酯共聚物、丙烯酸均聚和共聚物、聚乙烯胺、聚乙烯醯胺和聚乙烯嘧啶、多糖如纖維素、侵填體和澱粉、聚烯烴均聚和共聚物如烯烴/馬來酸酐共聚物、聚氨酯、聚酯、聚苯乙烯均聚物和共聚物。Binders can be added to improve the adhesion of the active material to the seed after treatment. Suitable binders are homopolymers and copolymers from alkylene oxides, such as ethylene oxide or propylene oxide, polyvinyl acetate, polyvinyl alcohol, polyvinylpyrrolidone and its copolymers, ethylene-vinyl acetate Copolymers, acrylic acid homopolymers and copolymers, polyvinylamines, polyvinylamides and polyvinylpyrimidines, polysaccharides such as cellulose, infills and starches, polyolefin homopolymers and copolymers such as olefin/maleic anhydride copolymers, Polyurethane, polyester, polystyrene homopolymer and copolymer.

任選地,著色劑也可包含在製劑中。用於種子處理製劑的合適的著色劑或染料有羅丹明B,C.I,顏料紅112,C.I,溶劑紅1,顏料藍15:4,顏料藍15:3,顏料藍15:2,顏料藍15:1,顏料藍80,顏料黃1,顏料黃13,顏料紅112,顏料紅48:2,顏料紅48:1,顏料紅57:1,顏料紅53:1,顏料橙43,顏料橙34,顏料橙5,顏料綠36,顏料綠7,顏料白6,顏料棕25,鹼性紫10 ,鹼性紫49,酸性紅51,酸性紅52,酸性紅14,酸性藍9,酸性黃23,鹼性紅10,鹼性紅108。Optionally, coloring agents may also be included in the formulation. Suitable coloring agents or dyes for seed treatment preparations are Rhodamine B, CI, Pigment Red 112, CI, Solvent Red 1, Pigment Blue 15:4, Pigment Blue 15:3, Pigment Blue 15:2, Pigment Blue 15 :1, Pigment Blue 80, Pigment Yellow 1, Pigment Yellow 13, Pigment Red 112, Pigment Red 48:2, Pigment Red 48:1, Pigment Red 57:1, Pigment Red 53:1, Pigment Orange 43, Pigment Orange 34 , Pigment Orange 5, Pigment Green 36, Pigment Green 7, Pigment White 6, Pigment Brown 25, Basic Violet 10, Basic Violet 49, Acid Red 51, Acid Red 52, Acid Red 14, Acid Blue 9, Acid Yellow 23 , Basic Red 10, Basic Red 108.

膠凝劑的例子有卡拉膠(Satiagel®)Examples of gelling agents are carrageenan (Satiagel®)

在種子處理中,本發明化合物的施用率通常為每100kg種子0.1g至10kg,優選為每100kg種子1g至5kg,更優選為每100kg種子1g至1000g(尤其是每100kg種子1g至200g)。因此,本發明還提供了包含如本文所定義的式(I)化合物或I的農業上有用的鹽的種子。化合物I或其可農用鹽的量通常為每100kg種子0.1g至10kg,優選每100kg種子1g至5kg(尤其是每100kg種子1g至1000g)。 對於特定作物如萵苣,施用率可以更高。In seed treatment, the application rate of the compound of the present invention is usually 0.1 g to 10 kg per 100 kg of seeds, preferably 1 g to 5 kg per 100 kg of seeds, more preferably 1 g to 1000 g per 100 kg of seeds (especially 1 g to 200 g per 100 kg of seeds). Therefore, the present invention also provides seeds comprising a compound of formula (I) or an agriculturally useful salt of I as defined herein. The amount of compound I or its agriculturally acceptable salt is usually 0.1 g to 10 kg per 100 kg of seeds, preferably 1 g to 5 kg per 100 kg of seeds (especially 1 g to 1000 g per 100 kg of seeds). For certain crops such as lettuce, the application rate can be higher.

動物健康Animal health

本發明還提供了包含至少一種本發明化合物的農業和/或獸醫用組合物。The present invention also provides agricultural and/or veterinary compositions comprising at least one compound of the present invention.

本發明還進一步涉及化合物、N-氧化物或獸醫學上可接受的鹽或本發明組合物在用於製備治療或保護動物免受昆蟲和蟎蟲或寄生蟲侵擾或感染的藥物中的用途。The present invention further relates to the use of the compound, N-oxide or veterinarily acceptable salt or the composition of the present invention in the preparation of a medicament for treating or protecting animals from infestation or infection by insects and mites or parasites.

式(I)化合物、其N-氧化物和/或獸醫學上可接受的鹽特別適合用於對抗動物中的寄生蟲。The compounds of formula (I), their N-oxides and/or veterinarily acceptable salts are particularly suitable for use against parasites in animals.

因此,本發明的一個目的是提供控制動物體內寄生蟲的新方法。 本發明的另一個目的是提供更安全的動物殺蟲劑。本發明的另一個目的是提供可以比現有殺蟲劑更低劑量使用的動物殺蟲劑。本發明的另一個目的是提供用於動物的殺蟲劑,以提供對寄生蟲的長期殘留控制。Therefore, an object of the present invention is to provide a new method for controlling parasites in animals. Another object of the present invention is to provide safer animal insecticides. Another object of the present invention is to provide animal insecticides that can be used in lower doses than existing insecticides. Another object of the present invention is to provide insecticides for animals to provide long-term residual control of parasites.

本發明還涉及含有殺寄生物有效量的至少一種式(I)化合物、N-氧化物或獸醫學上可接受的鹽和可接受的載體的組合物,用於對抗動物體內的寄生蟲。The present invention also relates to a composition containing at least one compound of formula (I), an N-oxide or a veterinarily acceptable salt and an acceptable carrier in an effective amount of parasiticidal, which is used to combat parasites in animals.

本發明還提供了治療、控制、預防和保護動物免受寄生蟲感染和感染的方法,該方法包括口服、局部或腸胃外給予或施用殺寄生物有效量的本發明化合物或包含它的組合物。The present invention also provides a method of treating, controlling, preventing and protecting animals from parasitic infections and infections, the method comprising oral, topical or parenteral administration or administration of a parasiticidal effective amount of the compound of the present invention or a composition containing it .

本發明還提供了製備用於治療、控制、預防或保護動物免受寄生蟲侵擾或感染的組合物(該組合物包含殺寄生物有效量的本發明化合物或包含它的組合物)的方法。The present invention also provides a method for preparing a composition for treating, controlling, preventing or protecting animals from infestation or infection by parasites (the composition contains a parasiticidal effective amount of the compound of the present invention or a composition containing it).

化合物對農業害蟲的活性並不表明它們適合控制動物體內的內寄生蟲和體表上的外寄生蟲、在口服施用時需要低的非催吐劑量、與動物的代謝相容性、低毒性和安全操作。The activity of the compounds against agricultural pests does not indicate that they are suitable for controlling endoparasites in animals and ectoparasites on the body surface, low non-emetic doses required for oral administration, metabolic compatibility with animals, low toxicity and safety operating.

令人驚奇的是,現已發現本發明化合物適用於對抗動物體內的內寄生蟲和體表上的外寄生蟲。Surprisingly, it has now been found that the compounds of the present invention are suitable for combating endoparasites in animals and ectoparasites on the body surface.

本發明化合物和含有該化合物的組合物適用於控制和預防對動物的侵擾和感染,這些動物包括溫血動物(包括人)和魚。它們適用於控制和預防對哺乳動物(如牛、羊、豬、駱駝、鹿、馬、豬、家禽、兔子、山羊、狗和貓、水牛、驢、小鹿和馴鹿)、毛皮動物(如水貂、栗鼠和浣熊、鳥類,如母雞、鵝、火雞和鴨子)以及魚類(如新鮮和鹹水魚、如鱒魚、鯉魚和鰻魚)的侵擾和感染。The compound of the present invention and the composition containing the compound are suitable for controlling and preventing infestation and infection to animals, including warm-blooded animals (including humans) and fish. They are suitable for the control and prevention of mammals (such as cattle, sheep, pigs, camels, deer, horses, pigs, poultry, rabbits, goats, dogs and cats, buffalo, donkeys, deer and reindeer), fur animals (such as mink, Infestation and infection of chinchillas and raccoons, birds such as hens, geese, turkeys and ducks, and fish (such as fresh and saltwater fish such as trout, carp and eel).

本發明化合物和含有該化合物的組合物適用於控制和預防對家畜(例如狗或貓)的侵擾和感染。The compound of the present invention and the composition containing the compound are suitable for controlling and preventing infestation and infection of domestic animals (such as dogs or cats).

對溫血動物和魚類侵擾的害蟲包括但不限於蝨子、咬虱、蜱、鼻蠅、綿羊蜱、叮咬蒼蠅、蠅蠅、蒼蠅、蠅蛆幼蟲、恙蟎、蚊蠅、蚊子和跳蚤。Pests that infest warm-blooded animals and fish include, but are not limited to, lice, biting lice, ticks, nose flies, sheep ticks, biting flies, flies, flies, fly larvae, chiggers, mosquitoes, mosquitoes, and fleas.

本發明化合物和含有該化合物的組合物適用於系統性和/或非系統性控制外寄生蟲和/或體內寄生蟲。他們可以有效抵抗所有或某些發展階段。The compound of the present invention and the composition containing the compound are suitable for systemic and/or non-systemic control of ectoparasites and/or endoparasites. They can effectively resist all or some stages of development.

本發明化合物尤其可用於對抗外寄生蟲。The compounds of the invention are particularly useful for combating ectoparasites.

本發明化合物特別適用於對抗下列目和物種的寄生蟲:跳蚤(劍翅目),例如貓頭蚤、圓頭蝽螂、爪蟾、蝽螂、蟑螂,如德國小蠊、細紋小蠊、美洲大蠊、日本大蠊、褐大蠊等,美洲大蠊、澳洲大蠊、東方蠊、蒼蠅、蚊子(雙翅目),例如埃及伊蚊、白紋伊蚊、伊蚊、墨西哥按實蠅、五斑按蚊、鯽魚按蚊、甘比亞按蚊、泛生按蚊、白踝瘧蚊、微小按蚊、四斑、紅頭麗蠅、大頭金蠅、腐敗錐蠅、中室斑虻、靜斑虻、大西洋斑虻、嗜人錐蠅、人皮蠅、毛庫蠓、黑須庫蚊、致倦庫蚊、環跗庫蚊、卡奇穀病毒之傳播媒介、黑尾賽蚊、人膚皮蠅、夏廁蠅、腸胃蠅、刺舌蠅、須舌蠅、擬寄舌蠅、西方角蠅、潛蠅屬、紋皮蠅、銅綠蠅、絲光綠蠅、曼蚊屬、家蠅、廄腐蠅、羊狂蠅、足白蛉、哥倫比亞鱗蚊、鱗蚊屬、原蚋屬、赤尾麻蠅、麻蠅屬、帶蚋、廄螫蠅、牛虻、北美黑虻、馬蠅、和虻屬、蝨子 (虱毛目), 例如人頭虱、人體虱、人體陰虱、牛血風、豬血虱、牛顎虱、牛羽虱、雞羽虱、和水牛盲虱。扁虱和寄生蟎蟲 (寄蟎目): 扁虱 (真蜱目), 例如肩突硬蜱、全環硬蜱、太平洋硬蜱、安氏革蜱、變異革蜱、美洲花蜱、斑點鈍口螈、鈍緣蜱、和寄生蟎蟲 (中氣門亞目), 例如柏氏禽刺蟎和雞皮刺蟎、輻蟎、粉蟎亞目、例如蜂盾蟎屬、姬螯蟎屬、肉蟎屬、瘡蟎屬、蠕形蟎屬、恙蟎屬、持鏟屬、粉蟎屬、食酪蟎屬、嗜木蟎屬、皮蟎科翼蟎屬、癢蟎屬、足蟎屬、耳蟎屬、疥蟎屬、癡蟎屬、膝蟎屬、和臭蟲 (異翅目): 溫帶臭蟲、熱帶臭蟲、獵蝽屬、錐獵蝽屬、長紅獵蝽、攀錐蝽屬和輪背獵蝽、虱目, 例如獸虱科、毛虱屬、人體虱屬、和管虱屬、食毛目 (細角亞目), 例如毛鳥虱科、短羽虱屬、鴨虱屬、牛羽虱屬、韋尼克菌屬、齧毛虱屬和貓羽虱屬。The compounds of the present invention are particularly suitable for combating parasites of the following orders and species: fleas (Hipoptera), such as cat head fleas, round head bugs, clawed frogs, bugs, cockroaches, such as German cockroaches, Blattella gracilis, American cockroach, Japanese cockroach, brown cockroach, etc., American cockroach, Australian cockroach, Oriental cockroach, flies, mosquitoes (Diptera), such as Aedes aegypti, Aedes albopictus, Aedes, A. mexicanus , Anopheles pentaphyllum, Anopheles crucian, Anopheles gambiae, Anopheles panbos, Anopheles albopictus, Anopheles mini, Fourspots, Red-headed blowfly, Big-headed golden flies, Corrupted cone flies, Central spotted fly, Plague fly, Atlantic fly, Trypanosoma anthropophagus, Human skin fly, Culex pipiens, Culex black beard, Culex pipiens vulgaris, Culex tarsalis, the vector of Kachi Valley virus, Cyperus black tail, human Skin skin flies, summer toilet flies, gastrointestinal flies, tsetse flies, tsetse flies, parasitic tsetse flies, western horned flies, Liriomyza, sclerotia, Lucilia sericata, Lucilia sericata, Manna, housefly, Rot fly, sheep fly, foot sandfly, Colombian scale mosquito, scale mosquito, protognathus, red-tailed sarcophagus, Sarcophagus, gnat, gnat fly, gadfly, black horsefly, horsefly, and horsefly, Louses (Epidoptera), such as human head lice, human lice, human pubic lice, bovine blood wind, blood louse, bovine jaw lice, cattle feather lice, chicken feather lice, and buffalo blind lice. Ticks and parasitic mites (Paramites): Ticks (True ticks), such as Ixodes scapularis, Ixodes pertussis, Ixodes pacificum, Dermacentor angifera, Dermacentor variabilis, American flower tick, Amnioticus Newts, Ornithology ticks, and parasitic mites (Mesophaga suborder), such as Avian spiny mites Burrito and Dermatophagocarpus, Radix mites, Acaroid mites, e.g. Acarina spp, Acarina spp, Sarcophagous mites, Sores Acarina, Demodex, Chigger, Shovel, Acaroid, Tyrophagous, Xylophilus, Dermatophagidae, Pterodactylus, Itchy mites, Foot mites, Ear mites, Scabies Acarina, Acarina, Acarina, and Bedbugs (Heteroptera): Temperate bed bugs, tropical bed bugs, assassin bugs, Trinops, long red assassin bugs, pantoris and wheel bugs, lice Orders, such as Pteridae, Trichosanthes, Human Psylidae, and Tubelouses, Trichophagous orders (Lepidoptera suborders), such as Trichosanthes, Brachychidae, Duck louse, Bovine louse, Wei The genus Nicotiana, the spp. and the spp.

線形線蟲:Nematodes:

鐵線蟲和毛線蟲病 (毛管目)、例如毛線蟲科 (毛形屬)、鞭蟲屬、毛細線蟲屬、小杆亞綱、例如小杆線蟲屬、類圓線蟲屬、厚蟹屬、圓線蟲目、例如圓線蟲屬、鉤蟲屬、美洲鉤蟲、仰口線蟲屬 (十二指腸蟲)、撚轉血矛線蟲、奧斯特屬、古柏屬、細頸線蟲屬、網尾線蟲屬、杯口屬、結節線蟲屬、有齒冠尾線蟲、盤頭線蟲屬、夏柏特線蟲屬、有齒冠尾線蟲、氣管比翼線蟲、鉤蟲屬、彎口屬、球首屬、板口線蟲屬、後圓線蟲屬、貓圓線蟲、和 腎膨結線蟲、腸蛔蟲 (蛔蟲科), 例如人蛔蟲、豬蛔蟲、雞蛔蟲、馬副蛔蟲、蠕形住腸蟯蟲 (蟯蟲)、犬弓首蛔蟲、獅弓蛔蟲、斯氏蟲屬、和 馬蟯蟲、駝形目、例如麥地那龍線蟲、旋尾目、例如吸吮線蟲屬、吳策線蟲屬、布魯格絲蟲屬、盤尾屬、惡絲蟲屬、棘唇線蟲屬、腹腔絲蟲屬、絲絨蟲屬、狼尾旋線蟲、和麗線蟲屬、多刺有頭蠕蟲 (棘頭綱), 例如 棘頭蟲屬、豬巨吻棘頭蟲和鉤棘頭蟲屬、渦蟲 (扁形動物門): 吸蟲 (吸蟲綱), 例如條華蝸牛、大擬片形吸蟲、並殖吸蟲屬、雙腔吸蟲屬、布氏薑片蟲、華支睾吸蟲、血吸蟲屬、毛畢屬吸蟲、有翼翼形吸蟲、並殖吸蟲屬、和角蟾目, 尤其是多節絛蟲亞綱 (絛蟲類), 例如裂頭屬、條蟲屬、棘球屬、犬複孔絛蟲、多頭絛蟲屬、膜殼絛蟲屬、中帶絛蟲屬、吸漿蟲屬、莫尼茨屬、裸頭絛蟲屬。Ironworms and Trichinella diseases (Capillary tube), such as Trichinellaceae (Trichoderma), Trichinella, Capillaria, Microbes, for example, Microcaria, Strongyloides, Thick crabs, Cymbidium Nematodes, such as Strongyloides, Ancylostoma, Ancylostoma, Ancylostoma (Duodenum), Haemonchus contortus, Oersted, Coopera, Nematodes, Dictyocaulis, Cupmouth Genus, Nodular Nematodes, Crown Nematodes, Panhead nematodes, Chabot Nematodes, Crown Cysts, Tracheal Pterodactylidae, Ancylostoma, Benthos, Globosporus, Bankou Nematodes, Hippocampus Strongyloides, strongyloides cat, and nematode nematodes, intestinal roundworms (Ascarididae), such as roundworms, Ascaris suum, Ascaris gallisepticum, Paraworms equine, Intestinal roundworms (pinworms), Toxoplasma canis , Toxoplasma lionii, Steinella, and horse pinworms, Camelids, such as Dracunculiasis, Trichocerca, such as Sucking Nematodes, Wu Tse Nematodes, Bruegrass, Onchocerca, Heartworm genus, Acanthopanax genus, Celiac filarial genus, Silkworm genus, Pennisetum genus, and Nematode genus, spiny headed worms (Acanthocephalus), such as Acanthocephalum, Swine giant snout Acanthocepha and Uncariacephala, Planaria (Platyma): Flukes (Flames), such as Chinese snails, Fasciola grandis, Paragonimus, Dichaenia, Ginger brachia, Clonorchis sinensis, Schistosoma, Trichomonas, Pteranodon, Paragonimus, and Ceratops, especially the subclass Polynodular tapeworms (taenia), For example, the genus Schistocephala, the genus Echinococcus, the genus Dippia canis, the genus Polycephalus, the genus Hymenocystis, the genus Taenia, the genus Midge, the genus Moniz, and the genus Gymnocephalus.

式(I)化合物和含有它們的組合物特別適用於控制雙翅目、蚤目和真蜱目的害蟲。The compounds of formula (I) and compositions containing them are particularly suitable for controlling pests of the orders Diptera, Siphonaptera and True ticks.

在一個實施方案中,本發明提供用式(I)化合物及其組合物對抗蚊子的用途。In one embodiment, the present invention provides the use of the compound of formula (I) and the composition thereof against mosquitoes.

在一個實施方案中,本發明提供用式(I)化合物及其組合物對抗蠅的用途。In one embodiment, the present invention provides the use of the compound of formula (I) and the composition thereof against flies.

在一個實施方案中,本發明提供用式(I)化合物及其組合物對抗跳蚤的用途。In one embodiment, the present invention provides the use of the compound of formula (I) and the composition thereof against fleas.

本發明化合物及其組合物用於對抗扁虱的用途是本發明的另一個實施方案。The use of the compounds of the present invention and their compositions for combating ticks is another embodiment of the present invention.

本發明的化合物還特別適用於對抗體內寄生蟲(線形線蟲、多刺有頭蠕蟲和渦蟲)。The compounds of the present invention are also particularly suitable for combating endoparasites (nematodes, spiny head worms and planarians).

在一個實施方案中,本發明化合物的給藥可以預防性和治療性進行。In one embodiment, the administration of the compounds of the invention can be done prophylactically and therapeutically.

在另一個實施方案中,本發明化合物的給藥可以直接或以合適製劑的形式口服、局部/皮膚或腸胃外給藥進行。In another embodiment, the administration of the compound of the present invention can be carried out directly or in the form of a suitable formulation orally, topical/dermal or parenteral.

對於溫血動物的口服給藥,本發明化合物可配製成動物飼料、動物飼料預混物、動物飼料濃縮物、丸劑、溶液、糊劑、懸浮液、浸液、凝膠、片劑、大丸劑和膠囊。此外,本發明化合物可以在其飲用水中給予動物。對於口服給藥,所選擇的劑量應為動物提供每天0.01mg / kg至100mg / kg ×動物體重的本發明化合物,優選每天0.5mg / kg至100mg / kg ×動物體重。For oral administration to warm-blooded animals, the compounds of the present invention can be formulated into animal feed, animal feed premixes, animal feed concentrates, pills, solutions, pastes, suspensions, infusions, gels, tablets, and pellets. And capsules. In addition, the compounds of the present invention can be administered to animals in their drinking water. For oral administration, the selected dose should provide animals with the compound of the present invention from 0.01 mg/kg to 100 mg/kg × animal body weight per day, preferably 0.5 mg/kg to 100 mg/kg × animal body weight per day.

或者,本發明化合物可以胃腸外給予動物,例如通過腔內、肌肉內、靜脈內或皮下注射。本發明化合物可以分散或溶解在生理學上可接受的載體中用於皮下注射。或者,可以將本發明化合物配製成用於皮下給藥的植入物。此外,本發明化合物可以透皮給藥於動物。對於腸胃外給藥,所選擇的劑量應為動物提供每天0.01mg / kg至100mg / kg ×動物體重的本發明化合物。Alternatively, the compounds of the invention can be administered to animals parenterally, for example by intracavity, intramuscular, intravenous or subcutaneous injection. The compound of the present invention can be dispersed or dissolved in a physiologically acceptable carrier for subcutaneous injection. Alternatively, the compounds of the invention can be formulated as implants for subcutaneous administration. In addition, the compounds of the present invention can be administered to animals transdermally. For parenteral administration, the selected dose should provide the animal with the compound of the present invention from 0.01 mg/kg to 100 mg/kg × animal body weight per day.

本發明的化合物還可以以浸漬劑、粉劑、粉劑、衣領、獎章劑、噴霧劑、洗發劑、點滴劑和澆潑劑和軟膏劑或水包油劑的形式局部施用於動物。對於局部施用,浸漬和噴霧通常含有0.5ppm至5,000ppm,優選1ppm至3,000ppm的本發明化合物。此外,本發明的化合物可以配製成動物(特別地四足動物如牛和綿羊)的耳標。The compounds of the present invention can also be topically applied to animals in the form of impregnants, powders, powders, collars, medals, sprays, shampoos, drops and splashes and ointments or oil-in-water agents. For topical application, dipping and spraying usually contain 0.5 ppm to 5,000 ppm, preferably 1 ppm to 3,000 ppm of the compound of the invention. In addition, the compounds of the present invention can be formulated as ear tags for animals (particularly quadrupeds such as cows and sheep).

合適的製劑有:溶液,例如口服溶液、稀釋後用於口服給藥的濃縮物、用於皮膚或體腔的溶液,澆注製劑、凝膠、用於口服或皮膚給藥的乳液和懸浮液、半固體製劑、活性化合物在軟膏基質或油包水或油包水乳劑基質中加工的製劑、固體製劑(如粉末、預混料或濃縮物、顆粒、小丸、片劑、大丸劑、膠囊、氣溶膠和吸入劑、含活性化合物的成型製品)。Suitable formulations are: solutions, such as oral solutions, concentrates for oral administration after dilution, solutions for skin or body cavity, pouring formulations, gels, emulsions and suspensions for oral or skin administration, semi- Solid preparations, preparations in which the active compound is processed in an ointment base or a water-in-oil or water-in-oil emulsion base, solid preparations (such as powders, premixes or concentrates, granules, pellets, tablets, boluses, capsules, aerosols) And inhalants, shaped products containing active compounds).

適於注射的組合物通過將活性成分溶解在合適的溶劑中並任選地加入其他成分如酸、鹼、緩衝鹽、防腐劑和增溶劑來製備。溶劑過濾和殺菌。Compositions suitable for injection are prepared by dissolving the active ingredient in a suitable solvent and optionally adding other ingredients such as acids, bases, buffer salts, preservatives and solubilizers. Solvent filtration and sterilization.

合適的溶劑有生理上可耐受的溶劑(例如水)、鏈烷醇(例如乙醇、丁醇、苯甲醇、甘油、丙二醇、聚乙二醇、N-甲基吡咯烷酮、2-吡咯烷酮及其混合物)。Suitable solvents include physiologically tolerable solvents (such as water), alkanols (such as ethanol, butanol, benzyl alcohol, glycerin, propylene glycol, polyethylene glycol, N-methylpyrrolidone, 2-pyrrolidone and mixtures thereof) ).

活性化合物可任選地溶於適於注射的生理學上可耐受的植物油或合成油中。The active compound may optionally be dissolved in a physiologically tolerable vegetable oil or synthetic oil suitable for injection.

合適的增溶劑是促進活性化合物在主要溶劑中溶解或防止其沉澱的溶劑。例如聚乙烯吡咯烷酮、聚乙烯醇、聚氧乙烯化蓖麻油和聚氧乙烯化脫水山梨糖醇酯。Suitable solubilizers are solvents that promote the dissolution of the active compound in the main solvent or prevent its precipitation. For example, polyvinylpyrrolidone, polyvinyl alcohol, polyoxyethylated castor oil, and polyoxyethylated sorbitan ester.

合適的防腐劑有苯甲醇、三氯丁醇、對羥基苯甲酸酯和正丁醇。Suitable preservatives are benzyl alcohol, trichlorobutanol, parabens and n-butanol.

口服溶液直接給藥。在預先稀釋至使用濃度後,將濃縮物口服給藥。口服溶液和濃縮物根據現有技術和如上製備注射溶液的方法製備,不需要無菌操作。The oral solution is administered directly. After pre-diluted to use concentration, the concentrate is administered orally. Oral solutions and concentrates are prepared according to the prior art and the method for preparing injection solutions as described above, without aseptic operation.

用於皮膚方法是將溶液滴上、塗抹、揉搓、灑上或噴上。The method for skin application is to drip, smear, rub, sprinkle or spray on the solution.

用於皮膚的溶液根據現有技術和根據如上製備注射溶液的方法製備,不需要無菌操作。The solution for the skin is prepared according to the prior art and according to the method for preparing an injection solution as described above, and does not require aseptic operation.

其他合適的溶劑有聚丙二醇,苯乙醇,苯氧基乙醇,酯如乙酸乙酯或乙酸丁酯,苯甲酸苯甲酯,醚類如烷基乙二醇基醚,如二丙二醇單甲醚,酮類如丙酮,甲乙酮等,芳烴,植物和合成油,二甲基甲醯胺,二甲基乙醯胺,還氧二元醇,丙酮縮甘油,碳酸丙烯酯,及其混合物。Other suitable solvents are polypropylene glycol, phenethyl alcohol, phenoxyethanol, esters such as ethyl acetate or butyl acetate, benzyl benzoate, ethers such as alkyl glycol ethers, such as dipropylene glycol monomethyl ether, Ketones such as acetone, methyl ethyl ketone, etc., aromatic hydrocarbons, vegetable and synthetic oils, dimethylformamide, dimethylacetamide, reducing diols, acetone glycidyl, propylene carbonate, and mixtures thereof.

在製備過程中加入增稠劑可能有好處。合適的增稠劑有無機增稠劑(例如膨潤土,膠體矽酸,單硬脂酸鋁)、有機增稠劑(如纖維素衍生物、聚乙烯醇及其共聚物、丙烯酸酯和甲基丙烯酸酯)。It may be beneficial to add thickeners during the preparation process. Suitable thickeners include inorganic thickeners (such as bentonite, colloidal silicic acid, aluminum monostearate), organic thickeners (such as cellulose derivatives, polyvinyl alcohol and its copolymers, acrylates and methacrylic acid). ester).

凝膠應用於皮膚或塗抹在皮膚上或引入體腔。凝膠是通過在根據製備注射溶液的方法製備的溶液中增加足夠的增稠劑從而產生具有軟膏狀稠度的透明材料來製備。使用的增稠劑是上面列出的增稠劑。The gel is applied to the skin or applied to the skin or introduced into the body cavity. The gel is prepared by adding enough thickener to a solution prepared according to the method of preparing an injection solution to produce a transparent material with an ointment-like consistency. The thickeners used are those listed above.

將澆潑製劑傾倒或噴灑到皮膚的有限區域上,活性化合物滲透皮膚並作用到全身。通過在合適的皮膚相容性溶劑或溶劑混合物中將活性化合物溶解、懸浮或乳化來製備澆潑製劑。如果合適,可以加入其他助劑如著色劑、生物吸收促進物質、抗氧化劑、光穩定劑、黏合劑。The pour-on preparation is poured or sprayed onto a limited area of the skin, and the active compound penetrates the skin and acts on the whole body. Pouring formulations are prepared by dissolving, suspending or emulsifying the active compound in a suitable skin compatible solvent or solvent mixture. If appropriate, other additives such as coloring agents, bioabsorption promoting substances, antioxidants, light stabilizers, and adhesives can be added.

合適的溶劑有:水、鏈烷醇、二醇、聚乙二醇、聚丙二醇、甘油、芳基醇如苯甲醇、苯基乙醇、苯氧基乙醇、酯類如乙酸乙酯、乙酸丁酯、苯甲酸苯甲酯、諸如亞烷基二醇醚、二乙二醇單丁醚、丙酮、甲基乙基酮等酮類、碳酸亞丙酯等環狀碳酸酯、芳香族和/或脂肪族烴等亞烷基乙二醇醚等醚類、植物油或合成油、DMF、二甲基乙醯胺、n-烷基吡咯烷酮、如甲基吡咯烷酮、正丁基吡咯烷酮或N-辛基吡咯烷酮、N-甲基吡咯烷酮、2-吡咯烷酮、2,2-二甲基-4-氧-亞甲基-1,3-二氧戊環 和甘油縮甲醛。Suitable solvents are: water, alkanol, glycol, polyethylene glycol, polypropylene glycol, glycerin, aryl alcohol such as benzyl alcohol, phenylethanol, phenoxyethanol, esters such as ethyl acetate, butyl acetate , Benzyl benzoate, ketones such as alkylene glycol ether, diethylene glycol monobutyl ether, acetone, methyl ethyl ketone, cyclic carbonate such as propylene carbonate, aromatic and/or fatty Group hydrocarbons and other ethers such as alkylene glycol ethers, vegetable oils or synthetic oils, DMF, dimethylacetamide, n-alkylpyrrolidone, such as methylpyrrolidone, n-butylpyrrolidone or N-octylpyrrolidone, N-methylpyrrolidone, 2-pyrrolidone, 2,2-dimethyl-4-oxo-methylene-1,3-dioxolane and glycerol formal.

合適的著色劑是允許在動物上使用並且可以溶解或懸浮的所有著色劑。Suitable coloring agents are all coloring agents that are allowed to be used on animals and can be dissolved or suspended.

合適的吸收促進物質有:二甲基亞碸、塗布油、如肉豆蔻酸異丙酯、二丙二醇壬酸酯、矽油及其與聚醚的共聚物、脂肪酸酯、甘油三酯、脂肪醇等。Suitable absorption promoting substances include: dimethyl sulfide, coating oils, such as isopropyl myristate, dipropylene glycol nonanoate, silicone oil and its copolymers with polyethers, fatty acid esters, triglycerides, fatty alcohols Wait.

合適的抗氧化劑有亞硫酸鹽或偏亞硫酸氫鹽,例如偏亞硫酸氫鉀、抗壞血酸、丁基羥基甲苯、丁基羥基苯甲醚、生育酚等。Suitable antioxidants are sulfites or metabisulfites, such as potassium metabisulfite, ascorbic acid, butylhydroxytoluene, butylhydroxyanisole, tocopherol and the like.

合適的光穩定劑有正-鄰二酸等。合適的黏合劑有,纖維素衍生物、澱粉衍生物、聚丙烯酸酯、天然聚合物如藻酸鹽、明膠等。乳劑可以口服、皮膚或注射給藥。乳液可以是油包水型或水包油型。Suitable light stabilizers include ortho-phthalic acid and the like. Suitable binders include cellulose derivatives, starch derivatives, polyacrylates, natural polymers such as alginate, gelatin and the like. Emulsion can be administered orally, skin or injection. The emulsion may be of the water-in-oil type or the oil-in-water type.

它們是通過將活性化合物溶解在疏水相或親水相中,並借助合適的乳化劑和適當的其他助劑(如著色劑、促進吸收物質、防腐劑、抗氧化劑、光穩定劑、增黏物質)將其與另一相的溶劑均化而製備的。They are by dissolving the active compound in the hydrophobic or hydrophilic phase, with the help of suitable emulsifiers and other suitable additives (such as coloring agents, absorption promoting substances, preservatives, antioxidants, light stabilizers, viscosity-increasing substances) It is prepared by homogenizing it with the solvent of the other phase.

合適的疏水相(油)有:Suitable hydrophobic phases (oils) are:

液體石蠟、矽油、天然植物油、如芝麻油、杏仁油、蓖麻油、合成甘油三酸酯、如辛酸/癸酸甘油三酯、甘油三酯混合物、鏈長為C1 -C12 的植物脂肪酸或其他特別選擇的天然脂肪酸、飽和或不飽和脂肪酸的偏甘油酯混合物、可能還含有羥基、Cs-do脂肪酸的單甘油酯和甘油二酯、脂肪酸酯如硬脂酸乙酯、己二酸二正丁酯、月桂酸己酯、二丙二醇壬酸酯、酯鏈長為C16 -C18 的飽和脂肪醇、肉豆蔻酸異丙酯、棕櫚酸異丙酯、鏈長為C12 -C18 的飽和脂肪醇的辛酸/癸酸酯、硬脂酸異丙酯、油酸油酯、油酸癸酯的中鏈長支鏈脂肪酸、油酸乙酯、乳酸乙酯、蠟狀脂肪酸酯、如合成鴨尾骨腺脂肪和脂肪、鄰苯二甲酸二丁酯、己二酸二異丙酯、以及與後者有關的酯混合物、脂肪醇如異十三烷醇、2-辛基十二烷醇、十六烷基硬脂醇、油醇、和脂肪酸如油酸及其混合物。合適的親水相是:水、醇如丙二醇、甘油、山梨糖醇及其混合物。Liquid paraffin, silicone oil, natural vegetable oils, such as sesame oil, almond oil, castor oil, synthetic triglycerides, such as caprylic/capric triglycerides, triglyceride mixtures, vegetable fatty acids with chain lengths of C 1 -C 12 or others Special selection of natural fatty acids, partial glycerides of saturated or unsaturated fatty acids, monoglycerides and diglycerides that may also contain hydroxyl, Cs-do fatty acids, fatty acid esters such as ethyl stearate, di-n-adipate Butyl ester, hexyl laurate, dipropylene glycol nonanoate, saturated fatty alcohol with ester chain length C 16 -C 18 , isopropyl myristate, isopropyl palmitate, chain length C 12 -C 18 Caprylic acid/capric acid ester of saturated fatty alcohol, isopropyl stearate, oleyl oleate, decyl oleate, medium-chain long-chain branched fatty acid, ethyl oleate, ethyl lactate, waxy fatty acid ester, such as Synthetic duck tailbone gland fat and fat, dibutyl phthalate, diisopropyl adipate, and ester mixtures related to the latter, fatty alcohols such as isotridecanol, 2-octyldodecanol, Cetyl stearyl alcohol, oleyl alcohol, and fatty acids such as oleic acid and mixtures thereof. Suitable hydrophilic phases are: water, alcohols such as propylene glycol, glycerin, sorbitol and mixtures thereof.

合適的乳化劑有非離子表面活性劑,例如聚乙氧基化蓖麻油、聚乙氧基化脫水山梨糖醇單油酸酯、脫水山梨糖醇單硬脂酸酯、甘油單硬脂酸酯、聚氧乙烯硬脂酸酯、或烷基酚聚乙二醇醚;兩性表面活性劑,例如N-月桂基-對-亞氨基二丙酸二鈉或卵磷脂。Suitable emulsifiers are nonionic surfactants, such as polyethoxylated castor oil, polyethoxylated sorbitan monooleate, sorbitan monostearate, glycerol monostearate , Polyoxyethylene stearate, or alkylphenol polyethylene glycol ether; amphoteric surfactants, such as disodium N-lauryl-p-iminodipropionate or lecithin.

合適的陰離子表面活性劑有十二烷基硫酸鈉、脂肪醇醚硫酸鹽、單/二烷基聚乙二醇醚正磷酸酯單乙醇胺鹽;合適的陽離子活性表面活性劑是十六烷基三甲基氯化銨等。Suitable anionic surfactants include sodium lauryl sulfate, fatty alcohol ether sulfate, mono/dialkyl polyglycol ether orthophosphate monoethanolamine salt; suitable cationic surfactant is cetyl tris Methyl ammonium chloride and so on.

合適的其他助劑是增強黏度和穩定乳液的物質,如羧甲基纖維素、甲基纖維素和其他纖維素和澱粉衍生物、聚丙烯酸酯、藻酸鹽、明膠、阿拉伯樹膠、聚乙烯吡咯烷酮、聚乙烯醇、甲基乙烯基醚和馬來酸酐的共聚物、聚乙二醇、蠟、膠體矽酸或這些物質的混合物。Suitable other additives are substances that enhance viscosity and stabilize emulsions, such as carboxymethyl cellulose, methyl cellulose and other cellulose and starch derivatives, polyacrylates, alginates, gelatin, gum arabic, polyvinylpyrrolidone , Polyvinyl alcohol, methyl vinyl ether and maleic anhydride copolymer, polyethylene glycol, wax, colloidal silicic acid or a mixture of these substances.

懸浮液可以口服或局部/皮膚給藥。 它們通過將活性化合物懸浮在懸浮劑中來製備,如果合適的話還加入其他助劑如潤濕劑、著色劑、生物吸收促進物質、防腐劑、抗氧化劑、光穩定劑。The suspension can be administered orally or topically/cutaneously. They are prepared by suspending the active compound in a suspending agent, if appropriate, adding other auxiliary agents such as wetting agents, coloring agents, bioabsorption promoting substances, preservatives, antioxidants, and light stabilizers.

液體懸浮劑均為均相溶劑和溶劑混合物。Liquid suspending agents are homogeneous solvents and solvent mixtures.

合適的潤濕劑(分散劑)是上文列舉的乳化劑。Suitable wetting agents (dispersants) are the emulsifiers listed above.

上文還給出了可能提及的其他助劑。Other additives that may be mentioned are also given above.

半固體製劑可以口服或局部/皮膚給藥。它們與上述懸浮液和乳液的不同之處僅在於其黏度較高。Semi-solid preparations can be administered orally or topically/cutaneously. They differ from the above-mentioned suspensions and emulsions only in their higher viscosity.

固體製劑的製備是將活性化合物與合適的賦形劑混合(如果合適的話加入助劑),然後製成所需的形式。The preparation of solid preparations is to mix the active compound with suitable excipients (adding adjuvants if appropriate), and then prepare the desired form.

合適的賦形劑是所有生理上可耐受的固體惰性物質,包括無機和有機的物質。無機物質有氯化鈉、碳酸鹽如碳酸鈣、碳酸氫鹽、氧化鋁、氧化鈦、矽酸、泥質土、沉澱或膠體二氧化矽或磷酸鹽等。有機物質有糖、纖維素、食品和嬰兒食品(例如奶粉、動物粉、穀物粉和碎片、澱粉)等。Suitable excipients are all physiologically tolerable solid inert substances, including inorganic and organic substances. Inorganic substances include sodium chloride, carbonates such as calcium carbonate, bicarbonate, aluminum oxide, titanium oxide, silicic acid, clay soil, precipitated or colloidal silica or phosphate. Organic substances include sugar, cellulose, food and baby food (such as milk powder, animal meal, cereal powder and chips, starch) and so on.

合適的助劑是上面提到的防腐劑、抗氧化劑、和/或著色劑。Suitable adjuvants are the preservatives, antioxidants, and/or coloring agents mentioned above.

其他合適的助劑是潤滑劑和助流劑,如硬脂酸鎂、硬脂酸、滑石粉、膨潤土、崩解促進物質如澱粉或交聯聚乙烯吡咯烷酮、黏合劑如澱粉、明膠或線性聚乙烯吡咯烷酮、和乾黏合劑如微晶纖維素。Other suitable additives are lubricants and glidants, such as magnesium stearate, stearic acid, talc, bentonite, disintegration promoting substances such as starch or cross-linked polyvinylpyrrolidone, binders such as starch, gelatin or linear poly Vinylpyrrolidone, and dry binders such as microcrystalline cellulose.

一般而言,“殺寄生物有效量”是指實現對生長的可觀察效果(包括壞死、死亡、阻滯、預防、去除、破壞或以其他方式減少目標生物體的發生和活動的效果)所需的活性成分的量。殺寄生物有效量可以根據本發明中使用的各種化合物/組合物而變化。殺寄生物有效量的組合物也將根據主要條件而變化,例如所需的寄生蟲效應和持續時間、目標物種、施用方式等。可用於本發明的組合物通常含有約0.001-95%的本發明化合物。Generally speaking, the "effective amount of parasiticide" refers to the effect of achieving an observable effect on growth (including necrosis, death, arrest, prevention, removal, destruction or other ways to reduce the occurrence and activity of the target organism). The amount of active ingredient required. The effective amount of parasiticide can vary according to the various compounds/compositions used in the present invention. The composition of the effective amount of parasiticide will also vary according to the main conditions, such as the desired parasitic effect and duration, target species, method of application, and the like. The compositions useful in the present invention generally contain about 0.001-95% of the compound of the present invention.

通常,以每天0.5mg / kg至100mg / kg,優選每天1mg / kg至50mg / kg的總量施用本發明的化合物是有利的。即用製劑含有對寄生蟲(優選外寄生蟲)起作用的化合物,其濃度範圍為10ppm至總重量的80%,優選占總重量的0.1至65%,更優選占總重量的1至50%,最優選占總重量的5-40%。製劑在使用前稀釋,含有對外寄生蟲起作用的化合物,其濃度為占重量的0.5-90%,優選占重量的1-50%。此外,對抗體內寄生蟲的本發明化合物製劑的濃度範圍為從10ppm至占總重量2%,優選占總重量0.05至0.9%,非常特別優選占總重量0.005至0.25%。Generally, it is advantageous to administer the compound of the present invention in a total amount of 0.5 mg/kg to 100 mg/kg per day, preferably 1 mg/kg to 50 mg/kg per day. The ready-to-use preparation contains a compound that acts on parasites (preferably ectoparasites) in a concentration range of 10 ppm to 80% of the total weight, preferably 0.1 to 65% of the total weight, more preferably 1 to 50% of the total weight , Most preferably 5-40% of the total weight. The preparation is diluted before use and contains a compound that acts on ectoparasites at a concentration of 0.5-90% by weight, preferably 1-50% by weight. In addition, the concentration of the compound preparation of the present invention against endoparasites ranges from 10 ppm to 2% of the total weight, preferably 0.05 to 0.9% of the total weight, very particularly preferably 0.005 to 0.25% of the total weight.

在一個實施方案中,包含本發明化合物的組合物經皮/局部施用。In one embodiment, the composition comprising the compound of the invention is administered transdermally/topically.

在另一個實施方案中,局部施用以含有化合物的成形製品的形式進行,例如固定在身體部位的頸圈、佩戴章、耳標、繃帶以及黏合的細條和薄片。In another embodiment, the topical application is in the form of shaped articles containing the compound, such as collars, wearing badges, ear tags, bandages, and adhesive strips and sheets that are fixed to body parts.

通常按一個週期(三周)10mg / kg至300mg / kg,優選20mg / kg至200mg / kg,最優選25mg / kg至160mg / kg的施用量施用本發明化合物的固體製劑是有利的。It is generally advantageous to administer the solid formulation of the compound of the present invention in an application amount of 10 mg/kg to 300 mg/kg, preferably 20 mg/kg to 200 mg/kg, and most preferably 25 mg/kg to 160 mg/kg in one cycle (three weeks).

使用熱塑性塑膠和柔性塑膠以及彈性體和熱塑性彈性體製備成型製品。合適的塑膠和彈性體是聚乙烯樹脂、聚氨酯、聚丙烯酸酯、環氧樹脂、纖維素、纖維素衍生物、聚醯胺和聚酯,它們與本發明的化合物充分相容。如WO2003 / 086075中給出了塑膠和彈性體的詳細列表以及成型製品的製備方法。Use thermoplastics and flexible plastics as well as elastomers and thermoplastic elastomers to prepare molded products. Suitable plastics and elastomers are polyethylene resins, polyurethanes, polyacrylates, epoxy resins, cellulose, cellulose derivatives, polyamides and polyesters, which are fully compatible with the compounds of the present invention. For example, WO2003/086075 gives a detailed list of plastics and elastomers and the preparation methods of molded products.

作物正反應:The crop is responding:

本發明的化合物不僅有效地控制昆蟲和蟎害蟲,而且還顯示出積極的作物反應,例如植物生長增強效果,如增強的根生長,增強的耐旱性、高鹽、高溫、寒冷、冰霜或光輻射、改善 開花、提高養分利用率(例如改善的氮同化作用)、提高植物產品品質、增加分蘖數、增加對真菌、昆蟲、害蟲等的抵抗力,從而提高產量。The compounds of the present invention not only effectively control insects and mite pests, but also show positive crop responses, such as plant growth enhancing effects, such as enhanced root growth, enhanced drought tolerance, high salt, high temperature, cold, frost or light Irradiation, improved flowering, increased nutrient utilization (such as improved nitrogen assimilation), improved plant product quality, increased tillers, increased resistance to fungi, insects, pests, etc., thereby increasing yield.

化學實例:Chemical examples:

下列實施例闡述了製備本發明化合物的方式和方法,並且包括發明人設想的實施本發明的最佳方式,但不對本發明施加任何限制。The following examples illustrate the methods and methods for preparing the compounds of the present invention, and include the best mode contemplated by the inventors to implement the present invention, but do not impose any limitation on the present invention.

例1:2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮( 化合物103號)的合成:a) 1 步: 3- 羥基 -6-( 三氟甲基 ) 異苯並呋喃 -1(3H)- 酮: 在-78°C下,向正丁基鋰(21.86 mL,54.6 mmol)的四氫呋喃(50 mL)攪拌溶液中加入2-溴-5-(三氟甲基)苯甲酸(7.0 g,26.0 mmol)的四氫呋喃溶液,加入時間在15分鐘以上。將反應攪拌,同時將溫度維持在-78℃,保持1小時。將無水N,N-二甲基甲酰胺(20.2mL,260.0mmol)加入到所得反應混合物中,並將反應混合物攪拌6小時,同時使反應升溫至25℃。反應完成後,將反應混合物冷卻至0℃,通過逐滴添加2N氫氧化鈉(15mL)淬滅反應混合物。將反應混合物用乙酸乙酯(50mL)萃取兩次。分離水層,小心地加入10N鹽酸中和,直到pH-4,然後用乙酸乙酯(100mL)萃取兩次。混合的乙酸乙酯層用無水硫酸鈉乾燥,並減壓濃縮,得到粗製的3-羥基-6-(三氟甲基)異苯並呋喃-1(3H)-酮(2.4g,11.00 mmol,42%產率),其無需進一步純化即可用於下一步。ESI MS (m/z) 217.00 (MH)+b) 2 步: 2-(5- -3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向3-羥基-6-(三氟甲基)異苯並呋喃-1(3H)-酮(1.3 g, 5.96 mmol) 的乙酸(20 mL)攪拌溶液中加入5-溴-3-(乙基磺醯基)-2-肼吡啶鹽酸鹽(1.67 g, 5.96 mmol) [按照((WO2018/008727))中所述的步驟製備]。將反應混合物在115℃下加熱2小時。反應完成後,將反應混合物冷卻至25℃,用水(100mL)稀釋,用乙酸乙酯(100mL)萃取兩次。混合的乙酸乙酯層用鹽水(100mL)和水(100mL)洗滌,用無水硫酸鈉乾燥並濃縮,得到粗產物,將其通過矽膠柱色譜法(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到 2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(880 mg , 1.9 mmol, 32%產率)。1 H-NMR (400 MHz, DMSO-d6 ) δ 9.19 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.52 (d, J = 0.9 Hz, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.6 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H) );ESI-MS(m/z) 463.55 (MH)+。c) 3 步: 2-(3-( 乙基磺醯基 )-5-(4-(1,1,2,2- 四氟乙氧基 ) 苯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(150 mg,0.32 mmol)和(4-(1,1,2,2-四氟乙氧基)苯基)硼酸(93.0 mg,0.39 mmol)的1,4-二噁烷(2 mL)和水(0.5 mL )的攪拌溶液中加入乙酸鈉(80 mg,0.974 mmol)和1,1'-雙(二苯基膦基)二茂鐵-二氯化鈀(II)二氯甲烷加合物(26.5 mg,0.032 mmol )。將反應混合物進行3次真空/氮氣循環,並在110℃下加熱1小時。反應完成後,將反應混合物用乙酸乙酯(50mL)和水(10mL)稀釋。分離,用無水硫酸鈉乾燥,並減壓濃縮,得到粗產物,將其通過矽膠柱色譜法(使用60%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3-(苯甲醛))-5-(4-(1,1,2,2-四氟乙氧基)苯基)苯-2-基)-7-(三氟甲基)苯甲酸-1(2H)-酮2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基) 酞嗪-1(2H)-酮(80 mg, 0.14 mmol, 42%產率),為固體。1 H-NMR (400 MHz, DMSO-d6 ) δ 9.32 (d, J = 2.4 Hz, 1H), 8.75-8.78 (m, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.07 (dd, J = 6.7, 2.1 Hz, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.74-7.00 (m, 1H ), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 576.05 (MH)+Example 1: 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(three Synthesis of fluoromethyl phthalazine-1(2H)-one (Compound No. 103): a) Step 1 : 3- hydroxy -6-( trifluoromethyl ) isobenzofuran -1(3H) -one : At -78°C, add 2-bromo-5-(trifluoromethyl)benzoic acid (7.0 g, 26.0 mmol) to a stirred solution of n-butyllithium (21.86 mL, 54.6 mmol) in tetrahydrofuran (50 mL) ) The tetrahydrofuran solution, the addition time is more than 15 minutes. The reaction was stirred while maintaining the temperature at -78°C for 1 hour. Anhydrous N,N-dimethylformamide (20.2 mL, 260.0 mmol) was added to the resulting reaction mixture, and the reaction mixture was stirred for 6 hours while the reaction was warmed to 25°C. After the reaction was completed, the reaction mixture was cooled to 0° C., and the reaction mixture was quenched by the dropwise addition of 2N sodium hydroxide (15 mL). The reaction mixture was extracted twice with ethyl acetate (50 mL). The aqueous layer was separated, and 10N hydrochloric acid was carefully added to neutralize it until pH-4, and then extracted twice with ethyl acetate (100 mL). The mixed ethyl acetate layer was dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain crude 3-hydroxy-6-(trifluoromethyl)isobenzofuran-1(3H)-one (2.4g, 11.00 mmol, 42% yield), which can be used in the next step without further purification. ESI MS (m/z) 217.00 (MH) + . b) Step 2 : 2-(5- Bromo- 3-( ethylsulfonyl ) pyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H) -one: To 3- Hydroxy-6-(trifluoromethyl)isobenzofuran-1(3H)-one (1.3 g, 5.96 mmol) in acetic acid (20 mL) was added to a stirred solution of 5-bromo-3-(ethylsulfonyl) )-2-hydrazinepyridine hydrochloride (1.67 g, 5.96 mmol) [prepared according to the procedure described in ((WO2018/008727))]. The reaction mixture was heated at 115°C for 2 hours. After the reaction was completed, the reaction mixture was cooled to 25°C, diluted with water (100 mL), and extracted twice with ethyl acetate (100 mL). The mixed ethyl acetate layer was washed with brine (100 mL) and water (100 mL), dried over anhydrous sodium sulfate and concentrated to obtain a crude product, which was passed through silica gel column chromatography (using 40% ethyl acetate in hexane as washing Removal) purification to obtain 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (880 mg, 1.9 mmol, 32% yield). 1 H-NMR (400 MHz, DMSO- d6 ) δ 9.19 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.52 (d, J = 0.9 Hz, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.6 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H) ); ESI-MS (m/z) 463.55 (MH)+. c) Step 3 : 2-(3-( Ethylsulfonyl )-5-(4-(1,1,2,2- tetrafluoroethoxy ) phenyl ) pyridin -2- yl) -7 -( Trifluoromethyl ) phthalazine -1(2H) -one: to 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one (150 mg, 0.32 mmol) and (4-(1,1,2,2-tetrafluoroethoxy)phenyl)boronic acid (93.0 mg, 0.39 mmol) in 1,4- To a stirred solution of dioxane (2 mL) and water (0.5 mL) was added sodium acetate (80 mg, 0.974 mmol) and 1,1'-bis(diphenylphosphino)ferrocene-palladium dichloride ( II) Dichloromethane adduct (26.5 mg, 0.032 mmol). The reaction mixture was subjected to 3 vacuum/nitrogen cycles and heated at 110°C for 1 hour. After the reaction was completed, the reaction mixture was diluted with ethyl acetate (50 mL) and water (10 mL). Separate, dry with anhydrous sodium sulfate, and concentrate under reduced pressure to obtain the crude product, which is purified by silica gel column chromatography (using 60% ethyl acetate in hexane as the eluent) to obtain 2-(3-(benzene) Formaldehyde))-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)phenyl-2-yl)-7-(trifluoromethyl)benzoic acid-1(2H)- Ketone 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl Base) phthalazine-1(2H)-one (80 mg, 0.14 mmol, 42% yield), as a solid. 1 H-NMR (400 MHz, DMSO- d6 ) δ 9.32 (d, J = 2.4 Hz, 1H), 8.75-8.78 (m, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.07 (dd, J = 6.7, 2.1 Hz, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.74-7.00 (m, 1H ), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 576.05 (MH) + .

例2:2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮(化合物15號)的合成:a) 1 步: N,N- 二異丙基 -4-( 三氟甲基 ) 苯甲醯胺: 在0℃下向4-(三氟甲基)苯甲酸(10.00 g,52.6 mmol)的無水二氯乙烷(80 mL)和無水N,N-二甲基甲酰胺(0.4 mL,5.26 mmol)的攪拌溶液中加入草酰氯(9.21 mL,105.0mmol)。將反應在25℃下攪拌2小時,然後在減壓下濃縮。將獲得的殘餘物溶於無水二氯乙烷(60mL)中,然後在0℃下逐滴添加二甲苯基胺(18.74mL,131.0mmol)。將反應混合物在25℃下攪拌4小時。反應完成後,將反應混合物在減壓下濃縮。將獲得的殘餘物用1N鹽酸處理,並用二氯甲烷(200mL)萃取兩次。用水(100mL)洗滌混合的二氯甲烷層,用無水硫酸鈉乾燥並在減壓下濃縮以獲得粗產物。粗產物通過矽膠快速柱色譜法(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到N,N-二異丙基-4-(三氟甲基)苯甲醯胺(12.0 g, 43.9 mmol, 83%產率)。1 H-NMR (400 MHz, DMSO-d6 ) δ 7.78 (d, J = 8.1 Hz, 2H), 7.50 (d, J = 8.1 Hz, 2H), 3.53-3.60 (m, 2H), 1.47 (d, J = 27.4 Hz, 6H), 1.14 (d, J = 34.0 Hz, 6H);ESI MS (m/z) 274.0 (MH)+。b) 2 步: 2- 甲醯基 -N,N- 二異丙基 -4-( 三氟甲基 ) 苯甲醯胺: 在-78℃下向N,N-二異丙基-4-(三氟甲基)苯甲醯胺(5.0 g, 18.29 mmol)的無水四氫呋喃(60 mL)攪拌溶液中加入正丁基鋰(24.0 mL,38.4 mmol)。在該溫度下攪拌1小時後,分批加入無水N,N-二甲基甲酰胺(3.54mL,45.7mmol),同時使反應溫度在1小時內逐漸升至25℃。將反應混合物冷卻至0℃,逐滴添加氯化銨飽和溶液淬滅反應混合物,並用水(100mL)稀釋。將反應混合物用乙酸乙酯(100mL)萃取兩次。用水(100mL)洗滌混合的乙酸乙酯層,用無水硫酸鈉乾燥並在減壓下濃縮,得到粗產物。粗產物通過矽膠快速色譜(使用30%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-甲醯基-N,N-二異丙基-4-(三氟甲基)苯甲醯胺  (4.9 g, 16.26 mmol, 89%產率)。1 H-NMR (400 MHz, DMSO-d6 ) δ 10.03 (d, J = 1.5 Hz, 1H), 8.32 (s, 1H), 8.08 (d, J = 7.3 Hz, 1H), 7.51-7.60 (m, 1H), 3.60 (m, 1H), 3.40 (m, 1H), 1.47 (d, J = 27.4 Hz, 6H), 1.14 (d, J = 34.0 Hz, 6H);ESI MS (m/z) 302.20 ( MH)+c) 3 步: 3- 羥基 -5-( 三氟甲基 ) 異苯並呋喃 -1(3H)- 酮: 向2-甲酰基-N, N-二異丙基-4-(三氟甲基)苯甲酰胺(10.0 g, 33.2 mmol)的乙酸(50 mL)的攪拌溶液中加入6N鹽酸( 30.2 mL)。將反應混合物加熱至110℃,保持40小時。反應完成後,將反應混合物冷卻至0℃,並通過逐滴添加10%氫氧化鈉(pH 8-9)淬滅。將反應混合物用乙酸乙酯(100mL)萃取,並將所得水層用10%鹽酸酸化(pH 3-4),然後用乙酸乙酯(200mL)萃取。用水(100mL)洗滌乙酸乙酯層,用無水硫酸鈉乾燥,並在減壓下濃縮,得到3-羥基-5-(三氟甲基)異苯並呋喃-1(3H)-酮(2.7 g, 12.38 mmol, 37%產率),其無需進一步純化即可用於下一步驟。1 H-NMR (400 MHz, DMSO-d6 ) δ 8.38 (d, J = 8.3 Hz, 1H), 8.00-8.10 (m, 3H), 6.74 (d, J = 8.3 Hz, 1H);ESI MS (m /z) 217.15 (MH)+d) 4 步: 2-(5- -3-( 乙基磺醯基 ) 吡啶 -2- 基) -6-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向3-羥基-5-(三氟甲基)異苯並呋喃-1(3H)-酮(1.5 g, 6.88 mmol) 的乙酸(20 mL)攪拌溶液中加入5-溴-3-(乙基磺醯基)-2-肼吡啶鹽酸鹽(1.93 g, 6.88 mmol) [按照(WO2018008727)中所述的步驟製備]。將反應混合物在115℃下加熱2小時。反應完成後,將反應混合物升至25℃,用水(100mL)稀釋,並用乙酸乙酯(100mL)萃取兩次。混合的乙酸乙酯層用鹽水(100mL)洗滌,用無水硫酸鈉乾燥並濃縮,得到粗產物,將其通過矽膠柱色譜(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮(2.50 g, 5.41 mmol, 79%產率)。1 H-NMR (400 MHz, DMSO-d6 ) δ 9.20 (d, J = 2.4 Hz, 1H), 8.81 (d, J = 2.2 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.7, 1.6 Hz, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.19 ( t, J = 7.5 Hz, 3H);ESI MS (m /z) 462.0, 464.0 [(MH)+ Br79, 81 ]。e) 5 步: 2-(3-( 乙基磺醯基 )-5-(4- 氟苯基 ) 吡啶 -2- 基) -6-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮(200 mg, 0.43 mmol)和(4-氟苯基)硼酸(72.6 mg,0.52 mmol)的1,4-二噁烷(5 mL)和水(1 mL)的攪拌溶液中加入乙酸鈉(106 mg,1.30 mmol)和1,1'-雙(二苯基膦基)二茂鐵-二氯化鈀(II)二氯甲烷加合物(31.0 mg,0.043 mmol),將反應混合物進行3次真空/氮氣循環,使其完全脫氧,然後加熱至110℃,保持1小時,反應完成後,將反應混合物用乙酸乙酯(50mL)和水(10mL)稀釋。分離乙酸乙酯層,用無水硫酸鈉乾燥,減壓濃縮,得到粗產物,將其通過矽膠柱色譜(使用50%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3 -(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮(138 mg, 0.29 mmol, 67%產率),為固體。1 H-NMR (400 MHz, DMSO-d6 ) δ 9.29 (d, J = 2.2 Hz, 1H), 8.71-8.74 (m, 2H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.26-8.28 (m, 1H), 8.01-8.04 (m, 2H), 7.42-7.47 (m, 2H), 3.49 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz , 3H);ESI MS (m/z) 477.9 (MH)+Example 2: 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one( Compound No. 15) Synthesis: a) Step 1 : N,N -Diisopropyl- 4-( trifluoromethyl ) benzamide: To 4-(trifluoromethyl)benzoic acid at 0℃ To a stirred solution of (10.00 g, 52.6 mmol) of anhydrous dichloroethane (80 mL) and anhydrous N,N-dimethylformamide (0.4 mL, 5.26 mmol) was added oxalyl chloride (9.21 mL, 105.0 mmol). The reaction was stirred at 25°C for 2 hours and then concentrated under reduced pressure. The obtained residue was dissolved in anhydrous dichloroethane (60 mL), and then xylylamine (18.74 mL, 131.0 mmol) was added dropwise at 0°C. The reaction mixture was stirred at 25°C for 4 hours. After the completion of the reaction, the reaction mixture was concentrated under reduced pressure. The obtained residue was treated with 1N hydrochloric acid, and extracted twice with dichloromethane (200 mL). The mixed dichloromethane layer was washed with water (100 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash column chromatography (using 40% ethyl acetate in hexane as the eluent) to obtain N,N-diisopropyl-4-(trifluoromethyl)benzamide (12.0 g, 43.9 mmol, 83% yield). 1 H-NMR (400 MHz, DMSO- d6 ) δ 7.78 (d, J = 8.1 Hz, 2H), 7.50 (d, J = 8.1 Hz, 2H), 3.53-3.60 (m, 2H), 1.47 (d, J = 27.4 Hz, 6H), 1.14 (d, J = 34.0 Hz, 6H); ESI MS (m/z) 274.0 (MH)+. b) Step 2 : 2- Methyl- N,N -diisopropyl- 4-( trifluoromethyl ) benzamide: To N,N-diisopropyl-4 at -78℃ -(Trifluoromethyl)benzamide (5.0 g, 18.29 mmol) in anhydrous tetrahydrofuran (60 mL) was added to a stirred solution of n-butyl lithium (24.0 mL, 38.4 mmol). After stirring at this temperature for 1 hour, anhydrous N,N-dimethylformamide (3.54 mL, 45.7 mmol) was added in batches, while the reaction temperature was gradually raised to 25° C. within 1 hour. The reaction mixture was cooled to 0° C., a saturated solution of ammonium chloride was added dropwise to quench the reaction mixture, and it was diluted with water (100 mL). The reaction mixture was extracted twice with ethyl acetate (100 mL). The combined ethyl acetate layer was washed with water (100 mL), dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash chromatography (using 30% ethyl acetate in hexane as the eluent) to give 2-methanyl-N,N-diisopropyl-4-(trifluoromethyl)benzyl Amide (4.9 g, 16.26 mmol, 89% yield). 1 H-NMR (400 MHz, DMSO- d6 ) δ 10.03 (d, J = 1.5 Hz, 1H), 8.32 (s, 1H), 8.08 (d, J = 7.3 Hz, 1H), 7.51-7.60 (m, 1H), 3.60 (m, 1H), 3.40 (m, 1H), 1.47 (d, J = 27.4 Hz, 6H), 1.14 (d, J = 34.0 Hz, 6H); ESI MS (m/z) 302.20 ( MH) + . c) Step 3 : 3- Hydroxy -5-( trifluoromethyl ) isobenzofuran -1(3H) -one: To 2-formyl-N, N-diisopropyl-4-(trifluoromethyl) To a stirred solution of methyl)benzamide (10.0 g, 33.2 mmol) in acetic acid (50 mL) was added 6N hydrochloric acid (30.2 mL). The reaction mixture was heated to 110°C for 40 hours. After the reaction was completed, the reaction mixture was cooled to 0°C and quenched by the dropwise addition of 10% sodium hydroxide (pH 8-9). The reaction mixture was extracted with ethyl acetate (100 mL), and the resulting aqueous layer was acidified (pH 3-4) with 10% hydrochloric acid, and then extracted with ethyl acetate (200 mL). The ethyl acetate layer was washed with water (100 mL), dried over anhydrous sodium sulfate, and concentrated under reduced pressure to obtain 3-hydroxy-5-(trifluoromethyl)isobenzofuran-1(3H)-one (2.7 g , 12.38 mmol, 37% yield), it can be used in the next step without further purification. 1 H-NMR (400 MHz, DMSO- d6 ) δ 8.38 (d, J = 8.3 Hz, 1H), 8.00-8.10 (m, 3H), 6.74 (d, J = 8.3 Hz, 1H); ESI MS (m /z) 217.15 (MH) + . d) Step 4 : 2-(5- Bromo- 3-( ethylsulfonyl ) pyridin -2- yl) -6-( trifluoromethyl ) phthalazine -1(2H) -one: To 3- Hydroxy-5-(trifluoromethyl)isobenzofuran-1(3H)-one (1.5 g, 6.88 mmol) in acetic acid (20 mL) was added to a stirred solution of 5-bromo-3-(ethylsulfonyl) )-2-hydrazinepyridine hydrochloride (1.93 g, 6.88 mmol) [prepared according to the procedure described in (WO2018008727)]. The reaction mixture was heated at 115°C for 2 hours. After the reaction was completed, the reaction mixture was raised to 25°C, diluted with water (100 mL), and extracted twice with ethyl acetate (100 mL). The mixed ethyl acetate layer was washed with brine (100 mL), dried over anhydrous sodium sulfate and concentrated to obtain the crude product, which was purified by silica gel column chromatography (using 40% ethyl acetate in hexane as the eluent) to obtain 2-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one (2.50 g, 5.41 mmol, 79% yield rate). 1 H-NMR (400 MHz, DMSO- d6 ) δ 9.20 (d, J = 2.4 Hz, 1H), 8.81 (d, J = 2.2 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.7, 1.6 Hz, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m /z) 462.0, 464.0 [(MH) + Br 79, 81 ]. e) Step 5 : 2-(3-( Ethylsulfonyl )-5-(4- fluorophenyl ) pyridin -2- yl) -6-( trifluoromethyl ) phthalazine -1(2H) - one: to a 2- (5-bromo-3- (sulfo acyl-ethyl) pyridin-2-yl) -6- (trifluoromethyl) phthalazine -1 (2H) - one (200 mg, 0.43 mmol ) And (4-fluorophenyl)boronic acid (72.6 mg, 0.52 mmol) in 1,4-dioxane (5 mL) and water (1 mL) were added to a stirred solution of sodium acetate (106 mg, 1.30 mmol) and 1,1'-bis(diphenylphosphino)ferrocene-palladium(II) dichloride dichloromethane adduct (31.0 mg, 0.043 mmol), the reaction mixture was subjected to 3 vacuum/nitrogen cycles to make It was completely deoxygenated and then heated to 110°C for 1 hour. After the reaction was completed, the reaction mixture was diluted with ethyl acetate (50 mL) and water (10 mL). The ethyl acetate layer was separated, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to obtain the crude product, which was purified by silica gel column chromatography (using 50% ethyl acetate in hexane as the eluent) to obtain 2-(3- (Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one (138 mg, 0.29 mmol, 67% Yield), as a solid. 1 H-NMR (400 MHz, DMSO- d6 ) δ 9.29 (d, J = 2.2 Hz, 1H), 8.71-8.74 (m, 2H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.26-8.28 (m, 1H), 8.01-8.04 (m, 2H), 7.42-7.47 (m, 2H), 3.49 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz , 3H); ESI MS (m/z) 477.9 (MH) + .

例3:3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮(化合物87號) 的合成:a) 1 步: 3-(5- -3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 喹唑啉 -4(3H)- 酮: 向7-(三氟甲基)喹唑啉-4(3H)-酮(1.6 g, 7.47 mmol)[按照《有機快報》(18(11), 2580-2583;2016)中所述的方法製備]和5-溴-3-(乙基磺醯基)-2-氟吡啶(2.60 g, 9.71 mmol)[按照WO2018008727中所述的方法製備]的攪拌懸浮液中加入碳酸銫(2.92 g,8.97 mmol),並將反應混合物在微波中於80°C照射1小時。反應完成後,將反應混合物用水(50mL)稀釋,並用乙酸乙酯(200mL)萃取。分離乙酸乙酯層,用無水硫酸鈉乾燥並減壓濃縮,得到粗產物,將其通過矽膠柱色譜(使用60%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到3-(5 -溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮(645 mg, 1.34 mmol, 19 %產率)。1 H-NMR (400 MHz, DMSO-d6 ) δ 9.22 (dd, J = 8.8, 6.4 Hz, 1H), 8.86-8.93 (m, 1H), 8.63 (t, J = 6.4 Hz, 1H), 8.36- 8.48 (m, 1H), 8.13 (s, 1H), 7.94 (dd, J = 8.4, 1.6 Hz, 1H), 3.38-3.62 (m, 2H), 1.14-1.20 ( t, J = 7.3 Hz, 3H ) ;ESI MS (m/z) 461.55, 463.55 [(MH)+ Br79, 81 ]。b) 2 步: 3-(3-( 乙基磺醯基 )-5-(4- 氟苯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 喹唑啉 -4(3H)- 酮: 向3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮(150.0 mg, 0.325 mmol)和(4-氟苯基)硼酸(45.4 mg,0.33 mmol)的1,4-二噁烷(2.5 mL)和水(0.3 mL)攪拌溶液中加入乙酸鈉(133.0 mg,1.62 mmol)和1,1'-雙(二苯基膦基)二茂鐵-二氯化鈀(II)二氯甲烷加合物(24.0mg,0.03mmol),對反應混合物進行3次真空/氮氣循環使其完全脫氧,然後在110℃下加熱1小時。反應完成後,將反應混合物用水(10mL)稀釋,用乙酸乙酯(50mL)萃取,分離乙酸乙酯層,用無水硫酸鈉乾燥並在90℃下濃縮。減壓得到粗產物,將其通過矽膠柱色譜法(使用50%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮(115.0 mg, 0.24 mmol, 74%產率)。1 H-NMR (400 MHz, DMSO-d6 ) δ 9.35 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.2 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.15 (s, 1H), 8.02-8.06 (m, 2H), 7.96 (dd, J = 8.4, 1.6 Hz, 1H), 7.42-7.48 (m, 2H), 3.42-3.59 (m , 2H), 1.18 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 477.95 (MH)+。Example 3: 3-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one Synthesis of (Compound No. 87): a) Step 1 : 3-(5- Bromo- 3-( ethylsulfonyl ) pyridin -2- yl) -7-( trifluoromethyl ) quinazoline- 4 (3H) -one: To 7-(trifluoromethyl)quinazolin-4(3H)-one (1.6 g, 7.47 mmol) [according to "Organic Express" (18(11), 2580-2583; 2016) Prepared by the method described in] and 5-bromo-3-(ethylsulfonyl)-2-fluoropyridine (2.60 g, 9.71 mmol) [prepared according to the method described in WO2018008727] adding carbonic acid to the stirred suspension Cesium (2.92 g, 8.97 mmol), and the reaction mixture was irradiated in a microwave at 80°C for 1 hour. After the reaction was completed, the reaction mixture was diluted with water (50 mL) and extracted with ethyl acetate (200 mL). The ethyl acetate layer was separated, dried over anhydrous sodium sulfate and concentrated under reduced pressure to obtain the crude product, which was purified by silica gel column chromatography (using 60% ethyl acetate in hexane as the eluent) to obtain 3-(5- Bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one (645 mg, 1.34 mmol, 19% yield). 1 H-NMR (400 MHz, DMSO- d6 ) δ 9.22 (dd, J = 8.8, 6.4 Hz, 1H), 8.86-8.93 (m, 1H), 8.63 (t, J = 6.4 Hz, 1H), 8.36- 8.48 (m, 1H), 8.13 (s, 1H), 7.94 (dd, J = 8.4, 1.6 Hz, 1H), 3.38-3.62 (m, 2H), 1.14-1.20 (t, J = 7.3 Hz, 3H) ; ESI MS (m/z) 461.55, 463.55 [(MH)+ Br 79, 81 ]. b) Step 2 : 3-(3-( Ethylsulfonyl )-5-(4- fluorophenyl ) pyridin -2- yl) -7-( trifluoromethyl ) quinazoline- 4(3H ) -One: To 3-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one (150.0 mg, 0.325 mmol) and (4-fluorophenyl)boronic acid (45.4 mg, 0.33 mmol) in 1,4-dioxane (2.5 mL) and water (0.3 mL) were stirred with sodium acetate (133.0 mg, 1.62 mmol) And 1,1'-bis(diphenylphosphino)ferrocene-palladium(II) dichloromethane adduct (24.0mg, 0.03mmol), the reaction mixture was subjected to 3 vacuum/nitrogen cycles to make It was completely deoxygenated and then heated at 110°C for 1 hour. After the completion of the reaction, the reaction mixture was diluted with water (10 mL), extracted with ethyl acetate (50 mL), the ethyl acetate layer was separated, dried over anhydrous sodium sulfate and concentrated at 90°C. The crude product was obtained under reduced pressure and purified by silica gel column chromatography (using 50% ethyl acetate in hexane as the eluent) to obtain 3-(3-(ethylsulfonyl)-5-(4- Fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one (115.0 mg, 0.24 mmol, 74% yield). 1 H-NMR (400 MHz, DMSO- d6 ) δ 9.35 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.2 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.15 (s, 1H), 8.02-8.06 (m, 2H), 7.96 (dd, J = 8.4, 1.6 Hz, 1H), 7.42-7.48 (m, 2H), 3.42-3.59 (m , 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.95 (MH)+.

例4:2-(3-(乙基磺醯基)-5-(1,1,2,2-四氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1( 2H)-酮(化合物210號)的合成:a) 1 步: (5-( 乙基磺醯基 )-6-(1- 氧代 -7-( 三氟甲基 ) 酞嗪 -2(1H)- ) 吡啶 -3- ) 硼酸: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(500 mg, 1.08 mmol)的1,4-二噁烷(10 mL)攪拌溶液中加入乙酸鉀(212 mg,2.16 mmol)和聯硼酸頻那醇酯(549 mg,2.16 mmol)。通過真空/氮循三次將反應混合物完全脫氧,然後加入1,1'-雙(二苯基膦基)二茂鐵二氯鈀(II)二氯甲烷加合物(88 mg,0.11 mmol)。將反應在90°C加熱4小時。反應完成後,將反應混合物冷卻至25℃,用水(20mL)稀釋,用乙酸乙酯(50mL)萃取。乙酸乙酯層用硫酸鈉乾燥,減壓濃縮,得到粗化合物(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H) -基)吡啶-3-基)硼酸(350 mg, 0.82 mmol, 76%產率),其無需進一步純化即可用於下一步。ESI-MS (M/Z) 427.70 (MH)+b) 2 步: 2-(3-( 乙基磺醯基 )-5- 羥基吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 向(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)硼酸(200 mg, 0.47 mmol)的四氫呋喃(5 mL)攪拌溶液中加入過氧化氫(1.196 ml,11.71 mmol)。將反應混合物在25℃下攪拌16小時。完成後,將反應混合物用飽和硫代硫酸鈉(10mL)淬滅,用乙酸乙酯(50mL)萃取。分離乙酸乙酯層,經硫酸鈉乾燥,在減壓下濃縮。將粗產物通過矽膠快速柱色譜法(使用80%二氯甲烷的甲醇溶液作為洗脫劑)純化,得到2-(3-(乙基磺醯基)-5-羥基吡啶-2-基)- 7-(三氟甲基)酞嗪-1(2H)-酮(110 mg, 0.23 mmol, 59%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 11.36 (s, 1H), 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 2.8 Hz, 1H), 3.37 (q, J = 6.8 Hz, 2H), 1.06-1.13 (m, 4H);ESI MS (m/z) 399.95 (MH)+c) 3 步: 2-(5-(2- -1,1,2,2- 四氟乙氧基 )-3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 在25°C下,在氮氣環境中向2-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(0.5g, 1.25 mmol)的N,N-二甲基甲酰胺(20 mL)攪拌溶液中加入碳酸銫(0.612 g,1.88 mmol),然後將反應混合物攪拌5分鐘。然後在25℃下向反應混合物中加入1,2-二溴-1,1,2,2-四氟乙烷(0.23 mL,1.88 mmol),將反應在25℃下攪拌16小時。反應結束後,通過加入水(15mL)淬滅反應。將反應混合物用乙酸乙酯(50mL)萃取兩次,混合的有機層用硫酸鈉乾燥,過濾並濃縮,得到粗產物,將粗產物通過矽膠柱色譜法(使用乙酸乙酯的己烷溶液作為洗脫液)純化,得到2-(5-(2-溴-1,1,2,2-四氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(0.31 g, 0.54 mmol, 43%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 9.17 (d, J = 2.7 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.59 (d, J = 2.7 Hz, 1H), 8.52 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 579.90 (MH)+d) 4 步: 2-(3-( 乙基磺醯基 )-5-(1,1,2,2- 四氟乙氧基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1( 2H)- 酮: 在25°C下向2-(5-(2-溴-1,1,2,2-四氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)- 7-(三氟甲基)酞嗪-1(2H)-酮(200 mg, 0.35 mmol)的乙酸(5 mL)攪拌溶液中加入鋅粉(45.2 mg,0.69 mmol)。將反應混合物在120°C下加熱6小時,完成後,通過加入水(15mL)淬滅反應,並將反應混合物用乙酸乙酯(50mL)萃取兩次,混合的有機層經硫酸鈉乾燥,過濾並濃縮,得到粗產物。將其通過矽膠柱色譜法(用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3-(乙基磺醯基)-5-(1,1,2,2-四氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(100 mg, 0.20 mmol, 58%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 9.10 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.6 Hz, 1H), 8.53 (d, J = 2.4 Hz, 2H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.98 (tt, J = 51.6, 3.0 Hz, 1H), 3.49 (q, J = 7.3 Hz, 2H) , 1.14 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 500.00 (MH)+Example 4: 2-(3-(Ethylsulfonyl)-5-(1,1,2,2-tetrafluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine Synthesis of -1( 2H)-one (Compound No. 210): a) Step 1 : (5-( Ethylsulfonyl )-6-(1- oxo- 7-( trifluoromethyl ) phthalazine) -2(1H) -yl ) pyridin- 3 -yl ) boronic acid: to 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-ketone (500 mg, 1.08 mmol) in 1,4-dioxane (10 mL) stirred solution was added potassium acetate (212 mg, 2.16 mmol) and pinacol diborate (549 mg, 2.16 mmol). The reaction mixture was completely deoxygenated by vacuum/nitrogen cycles three times, and then 1,1'-bis(diphenylphosphino)ferrocene dichloropalladium(II) dichloromethane adduct (88 mg, 0.11 mmol) was added. The reaction was heated at 90°C for 4 hours. After the reaction was completed, the reaction mixture was cooled to 25°C, diluted with water (20 mL), and extracted with ethyl acetate (50 mL). The ethyl acetate layer was dried over sodium sulfate and concentrated under reduced pressure to obtain the crude compound (5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)) -Yl)pyridin-3-yl)boronic acid (350 mg, 0.82 mmol, 76% yield), which can be used in the next step without further purification. ESI-MS (M/Z) 427.70 (MH) + . b) Step 2 : 2-(3-( Ethylsulfonyl )-5- hydroxypyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H) -one to (5- (Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)boronic acid (200 mg, 0.47 mmol) in tetrahydrofuran (5 mL) Add hydrogen peroxide (1.196 ml, 11.71 mmol) to the stirred solution. The reaction mixture was stirred at 25°C for 16 hours. After completion, the reaction mixture was quenched with saturated sodium thiosulfate (10 mL) and extracted with ethyl acetate (50 mL). The ethyl acetate layer was separated, dried over sodium sulfate, and concentrated under reduced pressure. The crude product was purified by silica gel flash column chromatography (using 80% dichloromethane in methanol as the eluent) to obtain 2-(3-(ethylsulfonyl)-5-hydroxypyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one (110 mg, 0.23 mmol, 59% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 11.36 (s, 1H), 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 2.8 Hz, 1H), 3.37 (q, J = 6.8 Hz, 2H), 1.06-1.13 (m, 4H); ESI MS (m/z) 399.95 (MH) + . c) Step 3 : 2-(5-(2- Bromo -1,1,2,2- tetrafluoroethoxy )-3-( ethylsulfonyl ) pyridin -2- yl) -7-( Trifluoromethyl ) phthalazine -1(2H) -one : at 25°C, in a nitrogen atmosphere to 2-(3-(ethylsulfonyl)-5-hydroxypyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one (0.5g, 1.25 mmol) in N,N-dimethylformamide (20 mL) was added to a stirred solution of cesium carbonate (0.612 g, 1.88 mmol) , And then the reaction mixture was stirred for 5 minutes. Then 1,2-dibromo-1,1,2,2-tetrafluoroethane (0.23 mL, 1.88 mmol) was added to the reaction mixture at 25°C, and the reaction was stirred at 25°C for 16 hours. After the reaction was over, the reaction was quenched by adding water (15 mL). The reaction mixture was extracted twice with ethyl acetate (50 mL), the combined organic layer was dried over sodium sulfate, filtered and concentrated to obtain a crude product. The crude product was passed through silica gel column chromatography (using ethyl acetate in hexane as the washing Liquid removal) purification to obtain 2-(5-(2-bromo-1,1,2,2-tetrafluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one (0.31 g, 0.54 mmol, 43% yield), as a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 9.17 (d, J = 2.7 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.59 (d, J = 2.7 Hz, 1H), 8.52 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 579.90 (MH) + . d) Step 4 : 2-(3-( Ethylsulfonyl )-5-(1,1,2,2- tetrafluoroethoxy ) pyridin -2- yl) -7-( trifluoromethyl ) Phthalazine- 1( 2H) -one: at 25°C to 2-(5-(2-bromo-1,1,2,2-tetrafluoroethoxy)-3-(ethylsulfonyl )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (200 mg, 0.35 mmol) in acetic acid (5 mL) was added to a stirred solution of zinc powder (45.2 mg, 0.69 mmol) ). The reaction mixture was heated at 120°C for 6 hours. After completion, the reaction was quenched by adding water (15 mL), and the reaction mixture was extracted twice with ethyl acetate (50 mL), the mixed organic layer was dried over sodium sulfate, and filtered And concentrated to obtain the crude product. It was purified by silica gel column chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-(3-(ethylsulfonyl)-5-(1,1,2,2-tetrafluoro) Ethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (100 mg, 0.20 mmol, 58% yield), as a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 9.10 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.6 Hz, 1H), 8.53 (d, J = 2.4 Hz, 2H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.98 (tt, J = 51.6, 3.0 Hz, 1H), 3.49 (q, J = 7.3 Hz, 2H) , 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 500.00 (MH) + .

例5:2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(化合物211號)的合成: a) 1 步: 2-(3-( 乙基磺醯基 )-5-(3- 甲基 -5-( 三氟甲基 )-1H- 吡唑 -1- ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(600 mg, 1.29 mmol)和3-甲基-5-(三氟甲基)-1H-吡唑(292 mg,1.95 mmol)的N,N-二甲基甲酰胺(10 mL)攪拌溶液中加入碘化亞銅(I)(74.2 mg,0.39 mmol)、N,N′-二甲基乙二胺(68.7mg,0.78mmol)和碳酸鉀(269mg,1.95mmol),將所得混合物在130℃下攪拌5小時。反應完成後,將反應混合物冷卻至25℃,加入水(20mL)淬滅反應,將反應混合物用乙酸乙酯(50mL)萃取兩次,將混合的有機層用硫酸鈉乾燥,過濾,並在減壓下濃縮,得到粗產物。將粗產物通過矽膠快速色譜法(使用30%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3-(乙基磺醯基)-5-(3-甲基-5- (三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(51 mg, 0.09 mmol, 7.0%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 2H), 8.55 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.35 (d, J = 8.1 Hz, 1H), 6.94 (s, 1H), 3.50 (q, J = 7.4 Hz, 2H), 2.55 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H);ESI MS (m/z) 532.00 (MH)+Example 5: 2-(3-(Ethylsulfonyl)-5-(3-methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7 Synthesis of -(trifluoromethyl)phthalazine-1(2H)-one (Compound No. 211): a) Step 1 : 2-(3-( Ethylsulfonyl )-5-(3 -methyl) -5-( trifluoromethyl )-1H- pyrazol- 1 -yl ) pyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H) -one: To 2-(5- Bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (600 mg, 1.29 mmol) and 3-methyl-5- To a stirred solution of (trifluoromethyl)-1H-pyrazole (292 mg, 1.95 mmol) in N,N-dimethylformamide (10 mL) was added copper(I) iodide (74.2 mg, 0.39 mmol) , N,N'-dimethylethylenediamine (68.7mg, 0.78mmol) and potassium carbonate (269mg, 1.95mmol), and the resulting mixture was stirred at 130°C for 5 hours. After the reaction was completed, the reaction mixture was cooled to 25°C, water (20 mL) was added to quench the reaction, the reaction mixture was extracted twice with ethyl acetate (50 mL), the mixed organic layer was dried with sodium sulfate, filtered, and reduced Concentrate under pressure to obtain a crude product. The crude product was purified by silica gel flash chromatography (using 30% ethyl acetate in hexane as the eluent) to obtain 2-(3-(ethylsulfonyl)-5-(3-methyl-5- (Trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (51 mg, 0.09 mmol, 7.0% yield Rate), as a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 2H), 8.55 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.35 (d, J = 8.1 Hz, 1H), 6.94 (s, 1H), 3.50 (q, J = 7.4 Hz, 2H), 2.55 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 532.00 (MH) + .

例6:2-(5-(二甲基磷醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(化合物206號)的合成:a) 1 步: 2-(5-( 二甲基磷醯基 )-3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 在25°C下向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮( 300 mg, 0.65 mmol)的1,4-二噁烷(5 mL)攪拌溶液中加入二甲基氧化膦(51.0 mg,0.65 mmol)。然後加入三(二亞芐基丙酮)二鈀(0)(36.0 mg,0.04 mmol)、9,9-二甲基-4,5-雙(二苯基膦基)氧雜蒽(18.8 mg,0.03 mmol)和三乙胺(0.12 ml,0.85 mmol),並將該反應在110℃加熱24小時。反應完成後,將反應混合物用水稀釋,用乙酸乙酯(50mL)萃取,將乙酸乙酯用硫酸鈉乾燥,過濾並濃縮,得到粗產物,將粗產物通過製備型高效液相色譜純化,得到2-(5-(二甲基磷醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(150 mg, 0.33 mmol, 50.0%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 9.32 (dd, J = 5.4, 2.0 Hz, 1H), 8.83 (dd, J = 10.0, 2.0 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.53 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.90 ( s, 3H), 1.87 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 460 (MH)+Example 6: 2-(5-(Dimethylphosphoryl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one Synthesis of (Compound No. 206): a) Step 1 : 2-(5-( Dimethylphosphoryl )-3-( ethylsulfonyl ) pyridin -2- yl) -7-( trifluoromethyl) Yl ) phthalazine -1(2H) -one: to 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein at 25°C Dimethylphosphine oxide (51.0 mg, 0.65 mmol) was added to a stirred solution of azin-1(2H)-one (300 mg, 0.65 mmol) in 1,4-dioxane (5 mL). Then add tris(dibenzylideneacetone)dipalladium(0) (36.0 mg, 0.04 mmol), 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (18.8 mg, 0.03 mmol) and triethylamine (0.12 ml, 0.85 mmol), and the reaction was heated at 110°C for 24 hours. After the completion of the reaction, the reaction mixture was diluted with water, extracted with ethyl acetate (50 mL), the ethyl acetate was dried over sodium sulfate, filtered and concentrated to obtain a crude product, which was purified by preparative high performance liquid chromatography to obtain 2 -(5-(Dimethylphosphoryl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (150 mg, 0.33 mmol, 50.0% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 9.32 (dd, J = 5.4, 2.0 Hz, 1H), 8.83 (dd, J = 10.0, 2.0 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.53 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.90 ( s, 3H), 1.87 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 460 (MH) + .

例7:2-(5-((二甲基((氧代)-l6-亞磺醯基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(化合物171號)的合成: a) 1 步: 2-(5-(( 二甲基 ( (氧代) -l6- 亞磺醯基 ) 氨基) -3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(300 mg, 0.65 mmol)的甲苯(6 mL)攪拌溶液中加入亞氨基二甲基-l6-磺胺酮(121 mg, 1.29 mmol)、磷酸氫三鉀(276 mg,1.29 mmol)和2-二環己基膦基-2',4',6'-三異丙基雙苯基(62.0 mg,0.13 mmol)。在15-20分鐘內將反應混合物通過真空/氮氣循環3次以徹底脫氧,然後加入三(二亞芐基丙酮)二鈀(0)(59.4 mg,0.06 mmol)。將反應混合物在110℃下加熱2小時,反應完成後,將反應混合物通過矽藻土床過濾,用乙酸乙酯(30mL)洗滌,將有機溶劑用鹽水洗滌,經硫酸鈉乾燥,過濾並濃縮,得到粗產物。將粗產物經矽膠快速柱色譜法(用60%乙酸乙酯的己烷溶液為洗脫劑)純化,得到2-(5-((二甲基((氧代)-l6-亞磺醯基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(190 mg, 0.40 mmol, 62%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.44 (d, J = 2.7 Hz, 1H), 8.39 (dd, J = 8.4, 1.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.88 (d, J = 2.7 Hz, 1H), 3.41-3.46 (m, 6H), 3.36 (q, J = 7.2 Hz, 2H), 1.12 ( t, J = 7.5 Hz, 3H) ESI MS (m/z);474.95 (MH)+Example 7: 2-(5-((Dimethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoro Synthesis of methyl)phthalazine-1(2H)-one (Compound No. 171): a) Step 1 : 2-(5-(( Dimethyl ( (oxo) -l6 - sulfinyl) amino) ) -3-( ethylsulfonyl ) pyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H) -one: to 2-(5-bromo-3-(ethylsulfonyl) (Pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one (300 mg, 0.65 mmol) in toluene (6 mL) was added to the stirred solution of iminodimethyl- l6-sulfaketone (121 mg, 1.29 mmol), tripotassium hydrogen phosphate (276 mg, 1.29 mmol) and 2-dicyclohexylphosphino-2',4',6'-triisopropyl bisphenyl (62.0 mg, 0.13 mmol). The reaction mixture was completely deoxygenated by vacuum/nitrogen cycle 3 times within 15-20 minutes, and then tris(dibenzylideneacetone)dipalladium(0) (59.4 mg, 0.06 mmol) was added. The reaction mixture was heated at 110°C for 2 hours. After the reaction was completed, the reaction mixture was filtered through a bed of celite, washed with ethyl acetate (30 mL), the organic solvent was washed with brine, dried over sodium sulfate, filtered and concentrated to give Crude product. The crude product was purified by silica gel flash column chromatography (using 60% ethyl acetate in hexane as the eluent) to obtain 2-(5-((dimethyl((oxo)-l6-ylidene)) Sulfonyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (190 mg, 0.40 mmol, 62% yield Rate). 1 H-NMR (400 MHz, DMSO-D6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.44 (d, J = 2.7 Hz, 1H), 8.39 (dd, J = 8.4, 1.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.88 (d, J = 2.7 Hz, 1H), 3.41-3.46 (m, 6H), 3.36 (q, J = 7.2 Hz, 2H) , 1.12 (t, J = 7.5 Hz, 3H) ESI MS (m/z); 474.95 (MH) + .

例8:2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)乙腈(化合物184號)的合成:a) 1 步: 2-(6- -5-( 乙硫基 ) 吡啶 -3- ) 乙腈: 向5-溴-2-氯-3-(乙硫基)吡啶(3.0 g, 11.88 mmol)和三甲基甲矽烷基乙腈(3.25 mL,23.76 mmol)的N,N-二甲基甲酰胺(15mL)攪拌溶液中加入氟化鋅(737mg,7.13mmol)和9,9-二甲基-4,5-雙(二苯基膦基)氧雜蒽(687mg,1.19mmol)。通過在15-20分鐘內對反應混合物進行真空/氮氣循環三次,使反應混合物完全脫氧,然後加入三(二亞芐基丙酮)二鈀(0)(544 mg,0.59 mmol)。將反應混合物在110℃下加熱5小時。反應完成後,將反應混合物用水(20mL)稀釋,並用乙酸乙酯(50mL)萃取。有機層用硫酸鈉乾燥,過濾並減壓蒸發,得到2-(6-氯-5-(乙硫基)吡啶-3-基)乙腈(1.9 g, 8.93 mmol, 75%產率),為固體。1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (q, J = 0.7 Hz, 1H), 7.48 (d, J = 2.4 Hz, 1H), 3.76 (d, J = 0.7 Hz, 2H), 3.00 (q, J = 7.4 Hz, 2H), 1.42 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 212.65 (MH)+b) 2 步: 2-(6- -5-( 乙基磺醯基 ) 吡啶 -3- ) 乙腈: 在0°C下向2-(6-氯-5-(乙硫基)吡啶-3-基)乙腈(0.60 g, 2.82 mmol)的二氯甲烷(20 mL)攪拌溶液中加入間氯過苯甲酸(1.0 g,5.92 mmol)。將反應混合物在25℃下攪拌12小時。反應完成後,將反應混合物用水稀釋並用二氯甲烷(50mL)萃取。有機層用1N氫氧化鈉溶液洗滌,經硫酸鈉乾燥,過濾並減壓蒸發,得到粗產物。將粗產物通過矽膠快速柱色譜法(使用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(6-氯-5-(乙基磺醯基)吡啶-3-基)乙腈( 0.35 g, 1.43 mmol, 51%產率);ESI MS (m/z) 244.70 (MH)+c) 3 步: 2-(5-( 乙基磺醯基 )-6- 肼基吡啶 -3- ) 乙腈: 在25℃下向2-(6-氯-5-(乙基磺醯基)吡啶-3-基)乙腈(250 mg, 1.02 mmol)的乙醇(5 mL)攪拌溶液中加入水合肼(0.4 mL,5.11 mmol),並將反應混合物在90℃下加熱16小時。反應完成後,將反應混合物用水(10mL)稀釋,並用乙酸乙酯(50mL)萃取。有機層經硫酸鈉乾燥,過濾並在減壓下蒸發,得到2-(5-(乙基磺醯基)-6-肼基吡啶-3-基) 乙腈(210 mg, 0.87 mmol, 86%產率),為固體。ESI MS (m/z) 241.00 (MH)+d) 4 步: 2-(5-( 乙基磺醯基 )-6-(1- 氧代 -7-( 三氟甲基 ) 酞嗪 -2(1H)- ) 吡啶 -3- ) 乙腈: 向3-羥基-6-(三氟甲基)異苯並呋喃-1(3H)-酮(250 mg, 1.146 mmol)的乙酸(10 mL)攪拌溶液中加入2-(5-(乙基磺醯基)-6-肼基吡啶-3-基)乙腈(275 mg, 1.15 mmol),並將反應混合物在115℃下加熱2小時。反應完成後,將水(20mL)加入到反應混合物中,然後用乙酸乙酯(70mL)萃取。有機層用鹽水洗滌,用無水硫酸鈉乾燥並蒸發,得到粗產物,將其通過矽膠快速色譜法(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)乙腈(190 mg, 0.45 mmol, 39%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 8.98 (d, J = 2.2 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.58 (d, J = 2.2 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 4.38 (s, 2H), 3.36-3.43 (m, 2H), 1.13 ( t, J = 7.3 Hz, 3H) ESI MS (m/z) 423 (MH)+Example 8: 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile ( Compound No. 184): a) Step 1 : 2-(6- Chloro -5-( ethylthio ) pyridin- 3 -yl ) acetonitrile: To 5-bromo-2-chloro-3-(ethylthio) ) To a stirred solution of pyridine (3.0 g, 11.88 mmol) and trimethylsilylacetonitrile (3.25 mL, 23.76 mmol) in N,N-dimethylformamide (15 mL) was added zinc fluoride (737 mg, 7.13 mmol) And 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (687mg, 1.19mmol). The reaction mixture was completely deoxygenated by vacuum/nitrogen cycling three times within 15-20 minutes, and then tris(dibenzylideneacetone)dipalladium(0) (544 mg, 0.59 mmol) was added. The reaction mixture was heated at 110°C for 5 hours. After the reaction was completed, the reaction mixture was diluted with water (20 mL) and extracted with ethyl acetate (50 mL). The organic layer was dried over sodium sulfate, filtered and evaporated under reduced pressure to give 2-(6-chloro-5-(ethylthio)pyridin-3-yl)acetonitrile (1.9 g, 8.93 mmol, 75% yield) as a solid . 1 H-NMR (400 MHz, CHLOROFORM-D) δ 8.08 (q, J = 0.7 Hz, 1H), 7.48 (d, J = 2.4 Hz, 1H), 3.76 (d, J = 0.7 Hz, 2H), 3.00 (q, J = 7.4 Hz, 2H), 1.42 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 212.65 (MH) + . b) Step 2 : 2-(6- Chloro -5-( ethylsulfonyl ) pyridin- 3 -yl ) acetonitrile: to 2-(6-chloro-5-(ethylthio) at 0°C To a stirred solution of pyridin-3-yl)acetonitrile (0.60 g, 2.82 mmol) in dichloromethane (20 mL) was added m-chloroperbenzoic acid (1.0 g, 5.92 mmol). The reaction mixture was stirred at 25°C for 12 hours. After the reaction was completed, the reaction mixture was diluted with water and extracted with dichloromethane (50 mL). The organic layer was washed with 1N sodium hydroxide solution, dried over sodium sulfate, filtered and evaporated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash column chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-(6-chloro-5-(ethylsulfonyl)pyridin-3-yl)acetonitrile ( 0.35 g, 1.43 mmol, 51% yield); ESI MS (m/z) 244.70 (MH) + . c) Step 3 : 2-(5-( Ethylsulfonyl )-6- hydrazinopyridin- 3 -yl ) acetonitrile: To 2-(6-chloro-5-(ethylsulfonyl) at 25°C To a stirred solution of pyridin-3-yl)acetonitrile (250 mg, 1.02 mmol) in ethanol (5 mL) was added hydrazine hydrate (0.4 mL, 5.11 mmol), and the reaction mixture was heated at 90°C for 16 hours. After the reaction was completed, the reaction mixture was diluted with water (10 mL) and extracted with ethyl acetate (50 mL). The organic layer was dried over sodium sulfate, filtered and evaporated under reduced pressure to give 2-(5-(ethylsulfonyl)-6-hydrazinopyridin-3-yl)acetonitrile (210 mg, 0.87 mmol, 86% yield) Rate), as a solid. ESI MS (m/z) 241.00 (MH) + . d) Step 4 : 2-(5-( Ethylsulfonyl )-6-(1- oxo- 7-( trifluoromethyl ) phthalazine -2(1H) -yl ) pyridin- 3 -yl ) Acetonitrile: To the stirred solution of 3-hydroxy-6-(trifluoromethyl)isobenzofuran-1(3H)-one (250 mg, 1.146 mmol) in acetic acid (10 mL) was added 2-(5-( Ethylsulfonyl)-6-hydrazinopyridin-3-yl)acetonitrile (275 mg, 1.15 mmol), and the reaction mixture was heated at 115°C for 2 hours. After the reaction was completed, water (20 mL) was added to the reaction mixture, which was then extracted with ethyl acetate (70 mL). The organic layer was washed with brine, dried over anhydrous sodium sulfate and evaporated to obtain a crude product, which was purified by silica gel flash chromatography (using 40% ethyl acetate in hexane as the eluent) to give 2-(5-( Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile (190 mg, 0.45 mmol, 39% yield rate). 1 H-NMR (400 MHz, DMSO-D6) δ 8.98 (d, J = 2.2 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.58 (d, J = 2.2 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 4.38 (s, 2H), 3.36-3.43 (m, 2H), 1.13 ( t, J = 7.3 Hz, 3H) ESI MS (m/z) 423 (MH) + .

例9:1-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈(化合物202號)的合成:a) 1 步: 1-(6- -5-( 乙硫基 ) 吡啶 -3- ) 環丙烷 -1- 甲腈: 在0℃下向2-(6-氯-5-(乙硫基)吡啶-3-基)乙腈(0.5g, 2.35 mmol)的四氫呋喃(10 mL)攪拌溶液中加入1,2-二溴乙烷(0.3 mL,3.06 mmol)。然後在0℃下將氫化鈉(0.2g,8.23mmol)加入到反應混合物中,將反應在25℃下攪拌3小時。反應完成後,將反應混合物用水(15mL)稀釋,用乙酸乙酯(75mL)萃取。有機層經硫酸鈉乾燥,過濾並減壓蒸發,得到粗產物。將粗產物通過矽膠快速色譜法(用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到1-(6-氯-5-(乙硫基)吡啶-3-基)環丙烷-1-甲腈(350 mg, 1.47 mmol, 62%產率),為固體。ESI MS (m/z) 238.80 (MH)+b) 2 步: 1-(6- -5-( 乙基磺醯基 ) 吡啶 -3- ) 環丙烷 -1- 甲腈: 在0℃下向1-(6-氯-5-(乙硫基)吡啶-3-基)環丙烷-1-甲腈(350 mg, 1.47 mmol)的二氯甲烷(10 mL)攪拌溶液中加入間氯過苯甲酸(531mg,3.08mmol),將反應混合物在25℃下攪拌12小時。反應完成後,將反應混合物用1N氫氧化鈉(10mL)溶液稀釋,用二氯甲烷(50mL)萃取。有機層經無水硫酸鈉乾燥,過濾並減壓蒸發,得到粗產物。粗產物通過矽膠快速色譜法(使用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到1-(6-氯-5-(乙基磺醯基)吡啶-3-基)環丙烷-1 -甲腈(250 mg, 0.92 mmol, 63.0%產率),為固體。ESI MS (m/z) 270.85 (MH)+c) 3 步: 1-(5-( 乙基磺醯基 )-6- 肼基吡啶 -3- ) 環丙烷 -1- 甲腈: 在25℃下向1-(6-氯-5-(乙基磺醯基)吡啶-3-基)環丙烷-1-甲腈(250 mg, 0.92 mmol)的乙醇(5 mL)攪拌溶液中加入水合肼(0.35mL,4.62mmol)。將反應混合物在90℃下加熱16小時。反應完成後,將反應混合物用水(10mL)稀釋,用乙酸乙酯(50mL)萃取。有機層用無水硫酸鈉乾燥,過濾,並減壓蒸發,得到1-(5-(乙基磺醯基)-6-肼基吡啶-3-基)環丙烷-1-甲腈(210 mg , 0.8 mmol, 85%產率),為固體。ESI MS (m/z): 264.95 (MH)-d) 4 步: 1-(5-( 乙基磺醯基 )-6-(1- 氧代 -7-( 三氟甲基 ) 酞嗪 -2(1H)- ) 吡啶 -3- ) 環丙烷 -1- 甲腈: 向3-羥基-6-(三氟甲基)異苯並呋喃-1(3H)-酮(250 mg, 1.15 mmol)的乙酸(10 mL)攪拌溶液中加入1-(5-(乙基磺醯基)-6-肼基吡啶-3-基)環丙烷-1-甲腈(305 mg, 1.15 mmol),然後將反應混合物在115℃下加熱2小時。反應完成後,將反應用水(10mL)淬滅,將反應混合物用乙酸乙酯(75mL)萃取。有機層用鹽水洗滌,經硫酸鈉乾燥並減壓蒸發,得到粗產物,將其通過矽膠快速色譜法(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到1-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈(190 mg , 0.42 mmol, 37.0%產率).1 H-NMR (400 MHz, DMSO-D6) δ 8.93 (d, J = 2.4 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.51 (s , 1H), 8.40-8.42 (m, 2H), 8.33 (d, J = 8.3 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.95-1.99 (m, 2H), 1.88-1.93 ( m, 2H), 1.12-1.16 (t, 3H);ESI MS (m/z) 449.05(MH)+Example 9: 1-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane Synthesis of -1-carbonitrile (Compound No. 202): a) Step 1 : 1-(6- Chloro -5-( ethylthio ) pyridin- 3 -yl ) cyclopropane- 1 -carbonitrile: at 0°C To a stirred solution of 2-(6-chloro-5-(ethylthio)pyridin-3-yl)acetonitrile (0.5g, 2.35 mmol) in tetrahydrofuran (10 mL) was added 1,2-dibromoethane (0.3 mL, 3.06 mmol). Then sodium hydride (0.2 g, 8.23 mmol) was added to the reaction mixture at 0°C, and the reaction was stirred at 25°C for 3 hours. After the reaction was completed, the reaction mixture was diluted with water (15 mL) and extracted with ethyl acetate (75 mL). The organic layer was dried over sodium sulfate, filtered, and evaporated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 1-(6-chloro-5-(ethylthio)pyridin-3-yl)cyclopropane-1- Formonitrile (350 mg, 1.47 mmol, 62% yield) as a solid. ESI MS (m/z) 238.80 (MH) + . b) Step 2 : 1-(6- Chloro -5-( ethylsulfonyl ) pyridin- 3 -yl ) cyclopropane- 1 -carbonitrile: to 1-(6-chloro-5- (Ethylthio)pyridin-3-yl)cyclopropane-1-carbonitrile (350 mg, 1.47 mmol) in dichloromethane (10 mL) was added to a stirred solution of m-chloroperbenzoic acid (531 mg, 3.08 mmol), and The reaction mixture was stirred at 25°C for 12 hours. After the reaction was completed, the reaction mixture was diluted with 1N sodium hydroxide (10 mL) solution and extracted with dichloromethane (50 mL). The organic layer was dried over anhydrous sodium sulfate, filtered and evaporated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 1-(6-chloro-5-(ethylsulfonyl)pyridin-3-yl)cyclopropane-1 -Formonitrile (250 mg, 0.92 mmol, 63.0% yield) as a solid. ESI MS (m/z) 270.85 (MH) + . c) Step 3 : 1-(5-( Ethylsulfonyl )-6- hydrazinopyridin- 3 -yl ) cyclopropane- 1 -carbonitrile: To 1-(6-chloro-5 -(Ethylsulfonyl)pyridin-3-yl)cyclopropane-1-carbonitrile (250 mg, 0.92 mmol) in ethanol (5 mL) was added to a stirred solution of hydrazine hydrate (0.35 mL, 4.62 mmol). The reaction mixture was heated at 90°C for 16 hours. After the reaction was completed, the reaction mixture was diluted with water (10 mL) and extracted with ethyl acetate (50 mL). The organic layer was dried over anhydrous sodium sulfate, filtered, and evaporated under reduced pressure to give 1-(5-(ethylsulfonyl)-6-hydrazinopyridin-3-yl)cyclopropane-1-carbonitrile (210 mg, 0.8 mmol, 85% yield), as a solid. ESI MS (m/z): 264.95 (MH) - . d) Step 4 : 1-(5-( Ethylsulfonyl )-6-(1- oxo- 7-( trifluoromethyl ) phthalazine -2(1H) -yl ) pyridin- 3 -yl ) Cyclopropane- 1 -carbonitrile: Add 3-hydroxy-6-(trifluoromethyl)isobenzofuran-1(3H)-one (250 mg, 1.15 mmol) in a stirred solution of acetic acid (10 mL) 1-(5-(Ethylsulfonyl)-6-hydrazinopyridin-3-yl)cyclopropane-1-carbonitrile (305 mg, 1.15 mmol), and then the reaction mixture was heated at 115°C for 2 hours. After the reaction was completed, the reaction was quenched with water (10 mL), and the reaction mixture was extracted with ethyl acetate (75 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated under reduced pressure to obtain the crude product, which was purified by silica gel flash chromatography (using 40% ethyl acetate in hexane as the eluent) to obtain 1-(5- (Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1-carbonitrile (190 mg , 0.42 mmol, 37.0% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 8.93 (d, J = 2.4 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.51 (s , 1H), 8.40-8.42 (m, 2H), 8.33 (d, J = 8.3 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.95-1.99 (m, 2H), 1.88-1.93 ( m, 2H), 1.12-1.16 (t, 3H); ESI MS (m/z) 449.05 (MH) + .

例10:1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺(化合物236號)的合成:a) 1 步: (5-( 乙基磺醯基 )-6-(1- 氧代 -7-( 三氟甲基 ) 酞嗪 -2(1H)- ) 吡啶 -3- ) 氨基甲酸叔丁酯: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(1.5 g, 3.25 mmol)的1,4-二噁烷(15 mL)攪拌溶液(1.5 g,3.25 mmol )中加入氨基甲酸叔丁酯(0.5 g,4.22 mmol)、9,9-二甲基-4,5-雙(二苯基膦基)氧雜蒽(0.2 g,0.32 mmol)、碳酸銫(1.56 g,4.87 mmol)和三(二亞芐基丙酮)二鈀(0)(0.3 g,0.32 mmol),將反應混合物在110°C 下加熱5小時。反應完成後將反應混合物用水(10mL)稀釋,用乙酸乙酯(50mL)萃取兩次。混合的有機層用鹽水洗滌,經硫酸鈉乾燥,蒸發,得到粗產物,將其通過矽膠快速色譜法(使用乙酸乙酯的己烷溶液中作為洗脫劑)純化,得到(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氨基甲酸叔丁酯(1 g,2.01 mmol,62%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 10.30 (s, 1H), 8.87 (d, J = 2.4 Hz, 1H), 8.72 (d, J = 0.5 Hz, 1H), 8.68 (d, J = 2.4 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 3.35 (q, J = 7.3 Hz, 2H) , 1.52 (s, 9H), 1.12 (t, J = 7.5 Hz, 3H);ESI MS (m/z) 499 (MH)+b) 2 步: 2-(5- 氨基 -3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 在0℃下向(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氨基甲酸叔丁酯(1.1 g, 2.21 mmol)的二氯甲烷(10mL)攪拌溶液中加入三氟乙酸(2.0 mL,26.5 mmol)。將反應混合物在25℃下攪拌4小時。反應完成後,將反應混合物用水(15mL)稀釋,用乙酸乙酯(100mL)萃取。有機層用鹽水洗滌,用硫酸鈉乾燥,蒸發,得到粗產物,將其通過矽膠快速色譜法(使用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(5-氨基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(0.5 g, 1.25 mmol, 57%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 8.66 (s, 1H), 8.49 (d, J = 0.9 Hz, 1H), 8.37 (dd, J = 8.4, 1.7 Hz, 1H), 8.29 (d, J = 8.3 Hz, 1H), 8.12-8.14 (m, 1H), 7.57 (d, J = 2.8 Hz, 1H), 6.31 (d, J = 16.2 Hz, 2H), 3.21-3.29 (q, J = 7.3 Hz, 2H), 1.09 (t, J = 7.6 Hz, 3H);ESI MS (m/z) 399.00 (MH)+c) 3 步: 1- 氰基 -N-(5-( 乙基磺醯基 )-6-(1- 氧代 -7-( 三氟甲基 ) 酞嗪 -2(1H)- ) 吡啶 -3- ) 環丙烷 -1- 甲醯胺: 在0°C下向1-氰基環丙烷-1-羧酸(42 mg,0.38 mmol)和2-(5-氨基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮( 200 mg, 0.50 mmol)的二氯甲烷(5 mL)攪拌溶液中加入二甲苯基乙胺(0.17 mL,1.01 mmol)和六氟磷酸鹽(382 mg,1.004 mmol),將反應混合物在25°C下攪拌16小時。反應完成後,將反應混合物用水(10mL)稀釋並用二氯甲烷(50mL)萃取兩次。用硫酸鈉乾燥,過濾並濃縮,得到粗產物,將其通過矽膠快速色譜(使用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺(100 mg, 0.20 mmol, 41%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 10.80 (s, 1H), 9.16 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 2.8 Hz, 1H), 8.74 (s, 1H) , 8.52 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 3.37 (q, J = 7.3 Hz, 2H), 1.79 (d, J = 4.3 Hz, 4H), 1.13 (t, J = 7.5 Hz, 3H);ESI MS (m/z) . 492.00(MH)+Example 10: 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3 Synthesis of -yl)cyclopropane-1-methanamide (Compound No. 236): a) Step 1 : (5-( Ethylsulfonyl )-6-(1- oxo- 7-( trifluoromethyl) yl) phthalazine -2 (1H) - yl) pyridin-3-yl) carbamate: to a solution of 2- (5-bromo-3- (sulfo acyl-ethyl) pyridin-2-yl) -7- (Trifluoromethyl)phthalazine-1(2H)-one (1.5 g, 3.25 mmol) in 1,4-dioxane (15 mL) stirred solution (1.5 g, 3.25 mmol) was added tert-butyl carbamate (0.5 g, 4.22 mmol), 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (0.2 g, 0.32 mmol), cesium carbonate (1.56 g, 4.87 mmol) and three (Dibenzylideneacetone)dipalladium(0) (0.3 g, 0.32 mmol), and the reaction mixture was heated at 110°C for 5 hours. After the completion of the reaction, the reaction mixture was diluted with water (10 mL) and extracted twice with ethyl acetate (50 mL). The combined organic layer was washed with brine, dried over sodium sulfate, and evaporated to obtain a crude product, which was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain (5-(ethyl) Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) tert-butyl carbamate (1 g, 2.01 mmol, 62 % Yield), as a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 10.30 (s, 1H), 8.87 (d, J = 2.4 Hz, 1H), 8.72 (d, J = 0.5 Hz, 1H), 8.68 (d, J = 2.4 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 3.35 (q, J = 7.3 Hz, 2H) , 1.52 (s, 9H), 1.12 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 499 (MH) + . b) Step 2 : 2-(5 -Amino- 3-( ethylsulfonyl ) pyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H) -one: at 0°C Downward tert-butyl (5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)carbamate Trifluoroacetic acid (2.0 mL, 26.5 mmol) was added to a stirred solution of (1.1 g, 2.21 mmol) in dichloromethane (10 mL). The reaction mixture was stirred at 25°C for 4 hours. After the reaction was completed, the reaction mixture was diluted with water (15 mL) and extracted with ethyl acetate (100 mL). The organic layer was washed with brine, dried over sodium sulfate, and evaporated to obtain a crude product, which was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-(5-amino-3- (Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (0.5 g, 1.25 mmol, 57% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 8.66 (s, 1H), 8.49 (d, J = 0.9 Hz, 1H), 8.37 (dd, J = 8.4, 1.7 Hz, 1H), 8.29 (d, J = 8.3 Hz, 1H), 8.12-8.14 (m, 1H), 7.57 (d, J = 2.8 Hz, 1H), 6.31 (d, J = 16.2 Hz, 2H), 3.21-3.29 (q, J = 7.3 Hz, 2H), 1.09 (t, J = 7.6 Hz, 3H); ESI MS (m/z) 399.00 (MH) + . c) Step 3 : 1- cyano -N-(5-( ethylsulfonyl )-6-(1- oxo- 7-( trifluoromethyl ) phthalazine -2(1H) -yl ) (Pyridin- 3 -yl ) cyclopropane- 1 -carboxamide: to 1-cyanocyclopropane-1-carboxylic acid (42 mg, 0.38 mmol) and 2-(5-amino-3-( Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one (200 mg, 0.50 mmol) in dichloromethane (5 mL) was added to the stirring solution Tolylethylamine (0.17 mL, 1.01 mmol) and hexafluorophosphate (382 mg, 1.004 mmol), the reaction mixture was stirred at 25°C for 16 hours. After the reaction was completed, the reaction mixture was diluted with water (10 mL) and extracted twice with dichloromethane (50 mL). Dry with sodium sulfate, filter and concentrate to obtain the crude product, which was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 1-cyano-N-(5-(ethylsulfonate) Amino)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1-carboxamide (100 mg, 0.20 mmol , 41% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 10.80 (s, 1H), 9.16 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 2.8 Hz, 1H), 8.74 (s, 1H) , 8.52 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 3.37 (q, J = 7.3 Hz, 2H), 1.79 (d, J = 4.3 Hz, 4H), 1.13 (t, J = 7.5 Hz, 3H); ESI MS (m/z). 492.00(MH) + .

例11:2-(3-(乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(化合物207號)的合成:a) 1 步: 5- -3-( 乙硫基 )-2- 肼吡啶鹽酸鹽: 在25℃下向5-溴-2-氯-3-(乙硫基)吡啶(2.5 g, 9.90 mmol)的乙醇(20mL)攪拌溶液中加入水合肼(3.70mL,49.5mmol)。將反應混合物在90℃下加熱60小時。完成後,將反應混合物用水(20mL)稀釋,用乙酸乙酯(100mL)萃取。有機層經無水硫酸鈉乾燥,過濾並減壓蒸發,得到5-溴-3-(乙硫基)-2-肼吡啶鹽酸鹽(2.1 g, 8.46 mmol, 85%產率),為一種油。ESI MS (m/z) 247.90 (MH)+b) 2 步: 2-(5- -3-( 乙硫基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向3-羥基-6-(三氟甲基)異苯並呋喃-1(3H)-酮(2.0 g, 9.27 mmol)的乙酸(25 mL)攪拌溶液中加入5-溴-3-(乙硫基)-2-肼吡啶鹽酸鹽(1.0 g, 4.03 mmol),並將反應混合物在115℃下加熱2小時。反應完成後,將反應用水(20mL)淬滅,將反應混合物用乙酸乙酯(150mL)萃取。有機層用鹽水洗滌,用硫酸鈉乾燥並蒸發,得到粗產物,將其通過矽膠快速色譜(使用30%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(5-溴-3-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(1.1g, 2.56 mmol, 63%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 8.75 (d, J = 0.5 Hz, 1H), 8.55 (d, J = 2.0 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.2, 1.6 Hz, 1H), 8.29-8.32 (m, 2H), 3.06 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 431.85 ( MH)+c) 3 步: 2-(3-( 乙硫基 )-5-(4-(1,1,2,2- 四氟乙氧基 ) 苯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(5-溴-3-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(400 mg, 0.93 mmol)的1,4-二噁烷(5 mL)和水(1 mL)的混合物攪拌溶液中加入3,3,4,4-四甲基-1-(4-(1,1,2,2-四氟乙氧基)苯基)硼烷(353 mg,1.12 mmol)、碳酸鉀(321 mg,2.32 mmol)和1,1'-雙(二苯基膦基)二茂鐵-二氯化鈀(II)二氯甲烷複合物(76 mg,0.09 mmol)。將反應混合物通過真空/氮循環3次使其完全脫氧,並將反應在110℃下加熱3小時。反應完成後,將反應混合物用乙酸乙酯(50mL)和水(10 mL)稀釋。分離乙酸乙酯層,用硫酸鈉乾燥並減壓濃縮,得到粗產物,將其通過矽膠柱色譜(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3-(乙硫基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(270mg, 0.49 mmol, 53%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 8.76 (s, 1H), 8.71 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.3, 1.5 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.25 (d, J = 2.1 Hz, 1H), 7.96-7.99 (m, 2H), 7.46 (d, J = 8.6 Hz, 2H), 6.72- 6.99 (m, 1H), 3.12 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 544.05 (MH)+d) 4 步: 2-(3-( 乙基磺醯亞胺基 )-5-(4-(1,1,2,2- 四氟乙氧基 ) 苯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(3-(乙硫基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(250 mg, 0.46 mmol)的甲醇(5 mL)攪拌溶液中加入二乙酸碘苯酯(370 mg,1.15 mmol)和氨基甲酸銨(71.8 mg,0.92 mmol)。將混合物在25℃下攪拌5小時,反應完成後,加入水(20mL),並將反應混合物用乙酸乙酯(75mL)萃取兩次,將混合的有機層用硫酸鈉乾燥,過濾濃縮,得到粗產物。將粗產物通過矽膠快速色譜法(使用60%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3-(乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(140mg, 0.24 mmol, 53.0%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 9.23 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.69 (d, J = 2.1 Hz, 1H), 8.52 (s, 1H) , 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 8.01-8.04 (m, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.86 ( tt, J = 52.0, 2.9 Hz, 1H), 4.61 (d, J = 38.8 Hz, 1H), 3.27 (q, J = 6.7 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 575.10 (MH)+Example 11: 2-(3-(Ethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7- Synthesis of (trifluoromethyl)phthalazine-1(2H)-one (Compound No. 207): a) Step 1 : 5- Bromo- 3-( ethylthio )-2- hydrazinepyridine hydrochloride: in To a stirred solution of 5-bromo-2-chloro-3-(ethylthio)pyridine (2.5 g, 9.90 mmol) in ethanol (20 mL) at 25°C was added hydrazine hydrate (3.70 mL, 49.5 mmol). The reaction mixture was heated at 90°C for 60 hours. After completion, the reaction mixture was diluted with water (20 mL) and extracted with ethyl acetate (100 mL). The organic layer was dried over anhydrous sodium sulfate, filtered and evaporated under reduced pressure to give 5-bromo-3-(ethylthio)-2-hydrazinepyridine hydrochloride (2.1 g, 8.46 mmol, 85% yield) as an oil . ESI MS (m/z) 247.90 (MH) + . b) Step 2 : 2-(5- Bromo- 3-( ethylthio ) pyridin -2- yl) -7-( trifluoromethyl ) phthalazin -1(2H) -one: to 3-hydroxy- To a stirred solution of 6-(trifluoromethyl)isobenzofuran-1(3H)-one (2.0 g, 9.27 mmol) in acetic acid (25 mL) was added 5-bromo-3-(ethylthio)-2- Hydrazine pyridine hydrochloride (1.0 g, 4.03 mmol), and the reaction mixture was heated at 115°C for 2 hours. After the reaction was completed, the reaction was quenched with water (20 mL), and the reaction mixture was extracted with ethyl acetate (150 mL). The organic layer was washed with brine, dried over sodium sulfate and evaporated to obtain the crude product, which was purified by silica gel flash chromatography (using 30% ethyl acetate in hexane as the eluent) to obtain 2-(5-bromo-3) -(Ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (1.1 g, 2.56 mmol, 63% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 8.75 (d, J = 0.5 Hz, 1H), 8.55 (d, J = 2.0 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.2, 1.6 Hz, 1H), 8.29-8.32 (m, 2H), 3.06 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 431.85 ( MH) + . c) Step 3 : 2-(3-( Ethylthio )-5-(4-(1,1,2,2- tetrafluoroethoxy ) phenyl ) pyridin -2- yl) -7-( Trifluoromethyl ) phthalazine -1(2H) -one: To 2-(5-bromo-3-(ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone (400 mg, 0.93 mmol) in a mixture of 1,4-dioxane (5 mL) and water (1 mL) was added to the stirred solution of 3,3,4,4-tetramethyl-1-( 4-(1,1,2,2-tetrafluoroethoxy)phenyl)borane (353 mg, 1.12 mmol), potassium carbonate (321 mg, 2.32 mmol) and 1,1'-bis(diphenyl) Phosphine) ferrocene-palladium(II) dichloride dichloromethane complex (76 mg, 0.09 mmol). The reaction mixture was completely deoxygenated by a vacuum/nitrogen cycle 3 times, and the reaction was heated at 110°C for 3 hours. After the reaction was completed, the reaction mixture was diluted with ethyl acetate (50 mL) and water (10 mL). The ethyl acetate layer was separated, dried over sodium sulfate and concentrated under reduced pressure to obtain the crude product, which was purified by silica gel column chromatography (using 40% ethyl acetate in hexane as the eluent) to obtain 2-(3-( Ethylthio)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -Ketone (270 mg, 0.49 mmol, 53% yield), as a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 8.76 (s, 1H), 8.71 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.3, 1.5 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.25 (d, J = 2.1 Hz, 1H), 7.96-7.99 (m, 2H), 7.46 (d, J = 8.6 Hz, 2H), 6.72- 6.99 (m, 1H), 3.12 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 544.05 (MH) + . d) Step 4 : 2-(3-( Ethylsulfonylimino )-5-(4-(1,1,2,2- tetrafluoroethoxy ) phenyl ) pyridin -2- yl) -7-( Trifluoromethyl ) phthalazine -1(2H) -one: to 2-(3-(ethylthio)-5-(4-(1,1,2,2-tetrafluoroethoxy) )Phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (250 mg, 0.46 mmol) in methanol (5 mL) was added to a stirred solution of iodophenyl diacetate (370 mg, 1.15 mmol) and ammonium carbamate (71.8 mg, 0.92 mmol). The mixture was stirred at 25°C for 5 hours. After the reaction was completed, water (20 mL) was added, and the reaction mixture was extracted twice with ethyl acetate (75 mL). The combined organic layer was dried over sodium sulfate, filtered and concentrated to obtain a crude product. The crude product was purified by silica gel flash chromatography (using 60% ethyl acetate in hexane as the eluent) to obtain 2-(3-(ethylsulfonylimino)-5-(4-(1, 1,2,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (140mg, 0.24 mmol, 53.0% yield) , Is a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 9.23 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.69 (d, J = 2.1 Hz, 1H), 8.52 (s, 1H) , 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 8.01-8.04 (m, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.86 ( tt, J = 52.0, 2.9 Hz, 1H), 4.61 (d, J = 38.8 Hz, 1H), 3.27 (q, J = 6.7 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 575.10 (MH) + .

例12:3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮(化合物182號)的合成:a) 1 步: 6-( 三氟甲基 )-2H- 苯並 [d][1,3] 惡嗪 -2,4(1H)- 二酮: 在0°C下向2-氨基-5-(三氟甲基)苯甲酸(500mg,2.44mmol)的四氫呋喃(7mL)攪拌溶液中滴加三光氣(247mg,0.83mmol)的四氫呋喃( 2mL)溶液。將反應混合物在25℃下攪拌4小時。反應完成後,將反應混合物用水(20mL)稀釋,並用乙酸乙酯(50mL)萃取兩次。混合的乙酸乙酯層經硫酸鈉乾燥,並減壓濃縮,得到6-(三氟甲基)-2H-苯並[d][1,3]惡嗪-2,4(1H)-二酮(500 mg, 2.16 mmol, 89%產率)。1 H-NMR (400 MHz, DMSO-d6) δ 12.08 (s, 1H), 8.13 (t, J = 0.7 Hz, 1H), 8.05-8.08 (m, 1H), 7.31 (d, J = 8.8 Hz, 1H);ESI MS (m/z) 229.85 (MH)-b) 2 步: 2- 氨基 -N-(5- -3- 氟吡啶 -2- 基) -5-( 三氟甲基 ) 苯甲醯胺: 向叔丁醇鉀(3.40 g,30.3 mmol)的四氫呋喃(70 mL)懸浮液中加入5-溴-3-氟吡啶-2-胺(2.60 g,13.63 mmol)。將反應混合物在25°C下攪拌10分鐘,然後逐滴添加6-(三氟甲基)-2H-苯並[d] [1,3]惡嗪-2,4(1H)-二酮(3.5 g,15.14 mmol)。然後將反應在25℃下再攪拌1小時。反應完成後,將反應混合物用水(50mL)稀釋,用乙酸乙酯(200mL)萃取。分離乙酸乙酯層,經硫酸鈉乾燥並減壓濃縮,得到粗產物,將其通過矽膠柱色譜法(使用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-氨基-N-(5-溴-3-氟吡啶-2-基)-5-(三氟甲基)苯甲醯胺(2.8 g, 7.40 mmol, 48.9%產率)。1 H-NMR (400 MHz, DMSO-d6) δ 10.86 (s, 1H), 8.47-8.47 (m, 1H), 8.25 (dd, J = 9.4, 2.1 Hz, 1H), 8.12 (d, J = 1.0 Hz, 1H), 7.50 (dd, J = 8.9, 1.8 Hz, 1H), 7.19 (s, 2H), 6.89 (d, J = 8.6 Hz, 1H), ESI MS (m/z) 377.90 (MH)+c) 3 步: 3-(5- -3- 氟吡啶 -2- 基) -6-( 三氟甲基 ) 苯並 [d][1,2,3] 三嗪 -4(3H)- 酮: 在0℃下向2-氨基-N-(5-溴-3-氟吡啶-2-基)-5-(三氟甲基)苯甲醯胺(2.8 g, 7.40 mmol)的6N鹽酸(12 ml) 的攪拌溶液中逐滴加入亞硝酸鈉(0.8g,11.11mmol)的水(4mL)溶液,將反應在25℃下攪拌1小時。反應完成後,混合物用飽和碳酸氫鈉溶液鹼化,用乙酸乙酯(50mL)萃取。分離乙酸乙酯層,用硫酸鈉乾燥,減壓濃縮,得到粗產物,將其通過快速色譜純化,得到3-(5-溴-3-氟吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮(2.4 g, 6.17 mmol, 83%產率),為固體。1 H-NMR (400 MHz, DMSO-D6) δ 8.81-8.81 (m, 1H), 8.67 (dd, J = 8.8, 2.0 Hz, 1H), 8.56-8.59 (m, 2H), 8.53 (dd, J = 8.7, 1.8 Hz, 1H);ESI MS (m/z) 390.90 (MH)+d) 4 步: 3-(5- -3-( 乙硫基 ) 吡啶 -2- 基) -6- ( 三氟甲基 ) 苯並 [d][1,2,3] 三嗪 -4(3H)- 酮: 在0℃下向氫化鈉(34.5mg,0.86mmol)的N,N-二甲基甲酰胺(5mL)攪拌懸浮液中加入乙硫醇(0.1mL,0.86mmol)。將反應混合物在相同溫度下攪拌15分鐘。隨後,將3-(5-溴-3-氟吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮( 280 mg, 0.72 mmol)的N,N-二甲基甲酰胺(2mL)溶液滴加到上述反應混合物中,將反應在0℃下攪拌30分鐘。用水(10mL)稀釋混合物,並用乙酸乙酯(40mL)萃取,分離乙酸乙酯層,用無水硫酸鈉乾燥,並減壓濃縮,得到粗產物,將其通過矽膠柱色譜(使用乙酸乙酯在己烷中的溶液作為洗脫劑)純化,得到3-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1, 2,3]三嗪-4(3H)-酮(240 mg, 0.56 mmol, 77%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 8.66 (d, J = 2.1 Hz, 1H), 8.58 (d, J = 8.3 Hz, 2H), 8.54 (dd, J = 8.6, 1.8 Hz, 1H) , 8.41 (d, J = 2.1 Hz, 1H), 3.10 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 432.85 (MH)+e) 5 步: 3-(5- -3-( 乙基磺醯基 ) 吡啶 -2- 基) -6-( 三氟甲基 ) 苯並 [d][1,2,3] 三嗪 -4(3H)- 酮: 在0°C下向3-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮(120 mg, 0.28 mmol)的二氯甲烷(10 mL)攪拌溶液中加入間氯過苯甲酸(176 mg,0.61 mmol)。將反應混合物在25°C下攪拌12小時。反應結束後,將反應混合物用二氯甲烷(40mL)稀釋,先後用飽和碳酸氫鈉溶液(10mL)和飽和硫代硫酸鈉溶液(10mL)洗滌。分離有機層,用硫酸鈉乾燥,減壓濃縮,得到粗產物,將其通過矽膠柱色譜法(用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到3-(5-溴-3- (乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮(93 mg, 0.20 mmol, 72%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 9.28 (d, J = 2.4 Hz, 1H), 8.94 (d, J = 2.2 Hz, 1H), 8.60 (d, J = 8.1 Hz, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.4 Hz, 3H);ESI MS (m/z) 464.85 (MH)+f) 6 步: 3-(3-( 乙基磺醯基 )-5-(4- 氟苯基 ) 吡啶 -2- 基) -6( 三氟甲基 ) 苯並 [d][1,2,3] 三嗪 -4(3H)- 酮: 向3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪- 4(3H)-酮(400 mg, 0.86 mmol)和(4-氟苯基)硼酸(181 mg,1.29 mmol)的1,4-二噁烷(6 mL)和水(1 mL)的混合物攪拌溶液中加入乙酸鈉(133.0mg,1.62mmol)和1,1′-雙(二苯基膦基)二茂鐵-二氯化鈀(II)二氯甲烷加合物(63.2mg,0.08mmol)。將反應混合物進行真空/氮迴圈3次使其完全脫氧,然後在110℃下加熱10小時。反應結束後,將反應混合物用水(10mL)稀釋,用乙酸乙酯(50mL)萃取。分離乙酸乙酯層,用硫酸鈉乾燥,減壓濃縮,得到粗產物,將其通過反相製備型高效液相色譜法(使用乙腈的水溶液作為洗脫劑)純化,得到3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮(75 mg, 0.16 mmol, 18%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.2 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.7, 1.8 Hz, 1H), 8.05-8.10 (m, 2H), 7.43-7.49 (m, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H );ESI MS (m/z) 478.95 (MH)+Example 12: 3-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6(trifluoromethyl)benzo[d][1,2,3 ] Triazine-4(3H)-one (Compound No. 182): a) Step 1 : 6-( Trifluoromethyl )-2H- benzo [d][1,3] oxazine -2, 4(1H) -Diketone: To a stirred solution of 2-amino-5-(trifluoromethyl)benzoic acid (500mg, 2.44mmol) in tetrahydrofuran (7mL) at 0°C was added triphosgene (247mg, 0.83 mmol) in tetrahydrofuran (2mL). The reaction mixture was stirred at 25°C for 4 hours. After the reaction was completed, the reaction mixture was diluted with water (20 mL) and extracted twice with ethyl acetate (50 mL). The mixed ethyl acetate layer was dried over sodium sulfate and concentrated under reduced pressure to obtain 6-(trifluoromethyl)-2H-benzo[d][1,3]oxazine-2,4(1H)-dione (500 mg, 2.16 mmol, 89% yield). 1 H-NMR (400 MHz, DMSO-d6) δ 12.08 (s, 1H), 8.13 (t, J = 0.7 Hz, 1H), 8.05-8.08 (m, 1H), 7.31 (d, J = 8.8 Hz, 1H); ESI MS (m/z) 229.85 (MH) - . b) Step 2 : 2 -Amino -N-(5- bromo- 3- fluoropyridin -2- yl) -5-( trifluoromethyl ) benzamide: To potassium tert-butoxide (3.40 g, 30.3 Add 5-bromo-3-fluoropyridin-2-amine (2.60 g, 13.63 mmol) to a suspension of tetrahydrofuran (70 mL) in tetrahydrofuran (70 mL). The reaction mixture was stirred at 25°C for 10 minutes, and then 6-(trifluoromethyl)-2H-benzo[d] [1,3]oxazine-2,4(1H)-dione ( 3.5 g, 15.14 mmol). The reaction was then stirred at 25°C for an additional hour. After the reaction was completed, the reaction mixture was diluted with water (50 mL) and extracted with ethyl acetate (200 mL). The ethyl acetate layer was separated, dried over sodium sulfate and concentrated under reduced pressure to obtain a crude product, which was purified by silica gel column chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-amino-N-( 5-Bromo-3-fluoropyridin-2-yl)-5-(trifluoromethyl)benzamide (2.8 g, 7.40 mmol, 48.9% yield). 1 H-NMR (400 MHz, DMSO-d6) δ 10.86 (s, 1H), 8.47-8.47 (m, 1H), 8.25 (dd, J = 9.4, 2.1 Hz, 1H), 8.12 (d, J = 1.0 Hz, 1H), 7.50 (dd, J = 8.9, 1.8 Hz, 1H), 7.19 (s, 2H), 6.89 (d, J = 8.6 Hz, 1H), ESI MS (m/z) 377.90 (MH) + . c) Step 3 : 3-(5- Bromo- 3- fluoropyridin -2- yl) -6-( trifluoromethyl ) benzo [d][1,2,3] triazine -4(3H) - one: to a solution of 2-amino-0 ℃ -N- (5- bromo-3-fluoropyridin-2-yl) -5- (trifluoromethyl) benzoyl-amine (2.8 g, 7.40 mmol) in 6N A solution of sodium nitrite (0.8g, 11.11mmol) in water (4mL) was added dropwise to a stirred solution of hydrochloric acid (12ml), and the reaction was stirred at 25°C for 1 hour. After the reaction was completed, the mixture was basified with saturated sodium bicarbonate solution and extracted with ethyl acetate (50 mL). The ethyl acetate layer was separated, dried over sodium sulfate, and concentrated under reduced pressure to obtain a crude product, which was purified by flash chromatography to obtain 3-(5-bromo-3-fluoropyridin-2-yl)-6-(trifluoromethyl) Yl)benzo[d][1,2,3]triazine-4(3H)-one (2.4 g, 6.17 mmol, 83% yield), as a solid. 1 H-NMR (400 MHz, DMSO-D6) δ 8.81-8.81 (m, 1H), 8.67 (dd, J = 8.8, 2.0 Hz, 1H), 8.56-8.59 (m, 2H), 8.53 (dd, J = 8.7, 1.8 Hz, 1H); ESI MS (m/z) 390.90 (MH) + . d) Step 4: 3- (5-bromo-3- (ethylthio) pyridin-2-yl) -6- (trifluoromethyl) benzo [d] [1,2,3] triazin - 4(3H) -ketone: To a stirred suspension of sodium hydride (34.5 mg, 0.86 mmol) in N,N-dimethylformamide (5 mL) was added ethyl mercaptan (0.1 mL, 0.86 mmol) at 0°C. The reaction mixture was stirred at the same temperature for 15 minutes. Subsequently, 3-(5-bromo-3-fluoropyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one ( A solution of 280 mg, 0.72 mmol) in N,N-dimethylformamide (2 mL) was added dropwise to the above reaction mixture, and the reaction was stirred at 0°C for 30 minutes. The mixture was diluted with water (10 mL) and extracted with ethyl acetate (40 mL). The ethyl acetate layer was separated, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to obtain the crude product, which was passed through silica gel column chromatography (using ethyl acetate in The solution in alkane is used as the eluent) to obtain 3-(5-bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1, 2 ,3] Triazine-4(3H)-one (240 mg, 0.56 mmol, 77% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 8.66 (d, J = 2.1 Hz, 1H), 8.58 (d, J = 8.3 Hz, 2H), 8.54 (dd, J = 8.6, 1.8 Hz, 1H) , 8.41 (d, J = 2.1 Hz, 1H), 3.10 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 432.85 (MH) + . e) Step 5 : 3-(5- Bromo- 3-( ethylsulfonyl ) pyridin -2- yl) -6-( trifluoromethyl ) benzo [d][1,2,3] tri Azin -4(3H) -one: To 3-(5-bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][ To a stirred solution of 1,2,3]triazine-4(3H)-one (120 mg, 0.28 mmol) in dichloromethane (10 mL) was added m-chloroperbenzoic acid (176 mg, 0.61 mmol). The reaction mixture was stirred at 25°C for 12 hours. After the reaction, the reaction mixture was diluted with dichloromethane (40 mL), and washed with saturated sodium bicarbonate solution (10 mL) and saturated sodium thiosulfate solution (10 mL) successively. The organic layer was separated, dried over sodium sulfate, and concentrated under reduced pressure to obtain a crude product, which was purified by silica gel column chromatography (using ethyl acetate in hexane as the eluent) to obtain 3-(5-bromo-3- (Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one (93 mg, 0.20 mmol, 72% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 9.28 (d, J = 2.4 Hz, 1H), 8.94 (d, J = 2.2 Hz, 1H), 8.60 (d, J = 8.1 Hz, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 464.85 (MH) + . f) Step 6 : 3-(3-( Ethylsulfonyl )-5-(4- fluorophenyl ) pyridin -2- yl) -6( trifluoromethyl ) benzo [d][1, 2,3] Triazine -4(3H) -one: To 3-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d ][1,2,3]triazine-4(3H)-one (400 mg, 0.86 mmol) and (4-fluorophenyl)boronic acid (181 mg, 1.29 mmol) in 1,4-dioxane (6 Add sodium acetate (133.0mg, 1.62mmol) and 1,1′-bis(diphenylphosphino)ferrocene-palladium dichloride (II) dichloride to the stirred solution of a mixture of mL) and water (1 mL) Methane adduct (63.2mg, 0.08mmol). The reaction mixture was vacuum/nitrogen looped 3 times to completely deoxygenate, and then heated at 110°C for 10 hours. After the reaction, the reaction mixture was diluted with water (10 mL) and extracted with ethyl acetate (50 mL). The ethyl acetate layer was separated, dried over sodium sulfate, and concentrated under reduced pressure to obtain a crude product, which was purified by reverse-phase preparative high performance liquid chromatography (using an aqueous solution of acetonitrile as an eluent) to obtain 3-(3-( Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H) -Ketone (75 mg, 0.16 mmol, 18% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.2 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.7, 1.8 Hz, 1H), 8.05-8.10 (m, 2H), 7.43-7.49 (m, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H ); ESI MS (m/z) 478.95 (MH) + .

例13:2-(4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮:(化合物173號)的合成:a) 1 步: 3- -6-(3-( 三氟甲基 ) 苯基 ) 噠嗪的合成: 向3,6-二氯噠嗪(5.0 g,33.2 mmol)的1,4-二噁烷(45 mL)和水(5.00 ml)的攪拌溶液中加入碳酸鉀(11.48 g,83.0 mmol )和(3-(三氟甲基)苯基)硼酸(5.05 g,26.6 mmol)。通過真空/氮氣循環3次使反應混合物完全脫氧,然後加入[1,1'-雙(二苯基膦基)二茂鐵]二氯鈀(II)(1.35g,1.66mmol)。將反應混合物在90℃下加熱2小時。反應完成後,將水(50mL)加入到反應混合物中,並用乙酸乙酯(150mL)萃取。分離乙酸乙酯層,經硫酸鈉乾燥,在減壓下濃縮。粗產物通過矽膠快速柱色譜(使用20%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到3-氯-6-(3-(三氟甲基)苯基)噠嗪(5.0 g, 19.33 mmol, 58%產率),為白色固體。1 H-NMR (400 MHz, DMSO-D6) δ 8.43-8.49 (m, 2H), 8.06-8.10 (m, 1H), 8.03 (d, J = 4.0 Hz, 1H), 7.91-7.95 (m, 1H ), 7.79-7.86 (m, 1H);ESI-MS (M/Z) 259.00 (MH)+b) 2 步: 6-(3-( 三氟甲基 ) 苯基 ) 噠嗪 -3(2H)- 酮的合成: 將3-氯-6-(3-(三氟甲基)苯基)噠嗪(5.0 g,19.33 mmol)的乙酸(45 mL)溶液在115℃下加熱12小時。反應完成後,將反應混合物冷卻至25℃,並在真空壓力下除去乙酸。向殘餘物中加入冰冷的水(50mL),將由此分離的固體過濾並真空乾燥,得到6-(3 (三氟甲基)苯基)噠嗪-3(2H)-酮(3.5 g, 14.57 mmol, 75%產率),為白色固體。1 H-NMR (400 MHz, DMSO-D6) δ 13.1 (s, 1H), 8.13-8.17 (m, 3H), 7.79 (d, J = 7.6 Hz, 1H), 7.72 (t, J = 8.1 Hz, 1H), 7.02 (d, J = 10.1 Hz, 1H);ESI-MS (M/Z) 241.05 (MH)+c) 3 步: 4- -6-(3-( 三氟甲基 ) 苯基 ) 噠嗪 -3(2H)- 酮: 在25°C下向6-(3-(三氟甲基)苯基)噠嗪-3(2H)-酮(3.5 g, 14.57 mmol)的水(87.5 ml)攪拌溶液中加入乙酸鉀(2.15 g,21.86 mmol )和溴化鉀(5.20 g,43.7 mmol)。然後在0℃下將溴(2.3mL,43.7mmol)滴加到該反應混合物中,將該反應在100°C下加熱12小時。反應完成後,通過在0℃下加入飽和亞硫酸鈉溶液(50mL)淬滅反應混合物,然後用乙酸乙酯(150mL)萃取。分離乙酸乙酯層,經硫酸鈉乾燥,在減壓下濃縮。粗產物通過矽膠快速柱色譜法(使用25%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到4-溴-6-(3-(三氟甲基)苯基)噠嗪-3( 2H)-酮(4.0 g, 12.54 mmol, 86%產率),為白色固體物質。1 H-NMR (400 MHz, DMSO-D6) δ 13.67 (s, 1H), 8.77 (s, 1H), 8.19-8.22 (m, 2H), 7.81 (d, J = 7.6 Hz, 1H), 7.72 ( t, J = 7.8 Hz, 1H);ESI MS (m/z) 316.85, 318.85 [(MH)+ Br79, 81 ]。d) 4 步: 4-( 乙硫基 )-6-(3-( 三氟甲基 ) 苯基 ) 噠嗪 -3(2H)- 酮: 在0℃下,向乙硫醇(1.1mL,15.04mmol)的N,N-二甲基甲酰胺(10mL)攪拌溶液中加入氫化鈉(0.5g,12.54mmol),將反應攪拌15分鐘。然後在0℃加入4-溴-6-(3-(三氟甲基) 苯基) 噠嗪-3(2H)-酮(4.0 g, 12.54 mmol)的N,N-二甲基甲酰胺(10 mL),將反應在25℃下繼續攪拌16小時。反應完成後,將反應混合物冷卻至0℃,並通過逐滴加入水(20mL)淬滅反應,並用乙酸乙酯(50mL)稀釋。分離乙酸乙酯層,經硫酸鈉乾燥,在減壓下濃縮。將粗產物通過矽膠快速柱色譜法(使用25%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到4-(乙硫基)-6-(3-(三氟甲基)苯基)噠嗪-3(2H)-酮(2.0 g, 6.66 mmol, 53%產率),為白色固體。1 H-NMR (400 MHz, DMSO-D6) δ 13.27 (s, 1H), 8.20-8.23 (m, 2H), 7.79-7.81 (m, 1H), 7.72 (t, J = 7.7 Hz, 1H), 7.65 (s, 1H), 3.10 (q, J = 7.3 Hz, 2H), 1.32 (t, J = 7.3 Hz, 3H);ESI-MS (M/Z) 301.00 (MH)+e) 5 步: 3- -4-( 乙硫基 )-6-(3-( 三氟甲基 ) 苯基 ) 噠嗪: 將4-(乙硫基)-6-(3-(三氟甲基)苯基)噠嗪-3(2H)-酮(2.0 g, 6.66 mmol)的三氯氧磷(6.5 mL,69.9 mmol)攪拌溶液在110℃下加熱4小時。反應完成後,將反應混合物在減壓下濃縮。通過滴加飽和碳酸氫鈉溶液(25 mL)仔細處理得到的固體殘渣,並用乙酸乙酯(150 mL)萃取兩次。混合的乙酸乙酯層經硫酸鈉乾燥並在減壓下濃縮。粗產物通過矽膠快速柱色譜(使用15%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到3-氯-4-(乙硫基)-6-(3-(三氟甲基)苯基)噠嗪(2.0 g, 6.27 mmol, 94%產率),為白色固體。1 H-NMR (400 MHz, DMSO-D6) δ 8.45-8.47 (m, 2H), 8.06 (s, 1H), 7.92 (dd, J = 8.4, 0.6 Hz, 1H), 7.81 (t, J = 7.8 Hz, 1H), 3.34 (t, J = 7.3 Hz, 2H), 1.36 (t, J = 7.3 Hz, 3H);ESI-MS (M/Z) 318.90 (MH)+f) 6 步: 3- -4-( 乙基磺醯基 )-6-(3-( 三氟甲基 ) 苯基 ) 噠嗪: 在0℃下向3-氯-4-(乙硫基)-6-(3-(三氟甲基)苯基)噠嗪(2.0 g, 6.27 mmol)的二氯甲烷(20 mL)攪拌溶液中加入3-氯過氧苯甲酸(5.4 g,18.82 mmol)。將反應在25℃下攪拌16小時。反應完成後,通過滴加飽和碳酸氫鈉溶液(10mL)淬滅反應混合物,並用二氯甲烷(100mL)萃取。減壓濃縮有機層,得到粗產物。粗產物通過矽膠快速柱色譜法(使用10%乙酸乙酯的己烷溶液)作為洗脫劑純化,得到3-氯-4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪(2.0 g, 5.70 mmol, 91%產率),為白色固體。1 H-NMR (400 MHz, DMSO-D6) δ 8.70 (s, 1H), 8.54 (t, J = 7.6 Hz, 2H), 7.99 (dd, J = 7.8, 0.7 Hz, 1H), 7.83-7.89 ( m, 1H), 3.69 (q, J = 7.4 Hz, 2H), 1.21-1.27 (m, 3H);ESI-MS (M/Z) 350.95 (MH)+g) 7 步: 2-(4-( 乙基磺醯基 )-6-(3-( 三氟甲基 ) 苯基 ) 噠嗪 -3- )-7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 在0℃下向7-(三氟甲基)酞嗪-1(2H)-酮(0.120 g, 0.56 mmol)的N,N-二甲基甲酰胺(10 mL)的攪拌溶液中加入碳酸鉀(0.116 g,0.84 mmol),將反應攪拌5分鐘。然後向反應混合物中加入3-氯-4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪(0.24 g, 0.67 mmol),將反應在25℃下攪拌16小時。反應完成後,將反應混合物用冷水(5mL)稀釋並用乙酸乙酯(50mL)萃取。用硫酸鈉乾燥乙酸乙酯層,並減壓濃縮,得到粗產物。將粗產物通過矽膠快速柱色譜法(使用20%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮(135 mg, 0.25 mmol, 46%產率),為米白色固體。1 H-NMR (400 MHz, DMSO-D6) δ 9.09 (d, J = 19.6 Hz, 1H), 8.89 (d, J = 0.6 Hz, 1H), 8.58-8.71 (m, 3H), 8.48 (dd, J = 8.3, 1.5 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.05 (d, J = 7.8 Hz, 1H), 7.92 (t, J = 7.8 Hz, 1H), 3.75 (q, J = 7.2 Hz, 2H), 1.22 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 528.85 (MH)+Example 13: 2-(4-(Ethylsulfonyl)-6-(3-(trifluoromethyl)phenyl)pyridazin-3-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-Kone: Synthesis of (Compound No. 173): a) Step 1 : Synthesis of 3- chloro -6-(3-( trifluoromethyl ) phenyl ) pyridazine: To 3,6-dichloro To a stirred solution of pyridazine (5.0 g, 33.2 mmol) in 1,4-dioxane (45 mL) and water (5.00 ml) was added potassium carbonate (11.48 g, 83.0 mmol) and (3-(trifluoromethyl) ) Phenyl)boronic acid (5.05 g, 26.6 mmol). The reaction mixture was completely deoxygenated by vacuum/nitrogen cycle 3 times, and then [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium(II) (1.35g, 1.66mmol) was added. The reaction mixture was heated at 90°C for 2 hours. After the reaction was completed, water (50 mL) was added to the reaction mixture, and it was extracted with ethyl acetate (150 mL). The ethyl acetate layer was separated, dried over sodium sulfate, and concentrated under reduced pressure. The crude product was purified by silica gel flash column chromatography (using 20% ethyl acetate in hexane as the eluent) to give 3-chloro-6-(3-(trifluoromethyl)phenyl)pyridazine (5.0 g, 19.33 mmol, 58% yield), as a white solid. 1 H-NMR (400 MHz, DMSO-D6) δ 8.43-8.49 (m, 2H), 8.06-8.10 (m, 1H), 8.03 (d, J = 4.0 Hz, 1H), 7.91-7.95 (m, 1H) ), 7.79-7.86 (m, 1H); ESI-MS (M/Z) 259.00 (MH) + . b) Step 2 : Synthesis of 6-(3-( trifluoromethyl ) phenyl ) pyridazin -3(2H) -one: Add 3-chloro-6-(3-(trifluoromethyl)phenyl ) A solution of pyridazine (5.0 g, 19.33 mmol) in acetic acid (45 mL) was heated at 115°C for 12 hours. After the reaction was completed, the reaction mixture was cooled to 25°C, and the acetic acid was removed under vacuum pressure. Ice-cold water (50 mL) was added to the residue, and the solid thus separated was filtered and dried in vacuo to obtain 6-(3 (trifluoromethyl)phenyl)pyridazine-3(2H)-one (3.5 g, 14.57) mmol, 75% yield), a white solid. 1 H-NMR (400 MHz, DMSO-D6) δ 13.1 (s, 1H), 8.13-8.17 (m, 3H), 7.79 (d, J = 7.6 Hz, 1H), 7.72 (t, J = 8.1 Hz, 1H), 7.02 (d, J = 10.1 Hz, 1H); ESI-MS (M/Z) 241.05 (MH) + . c) Step 3 : 4- Bromo -6-(3-( trifluoromethyl ) phenyl ) pyridazine -3(2H) -one: To 6-(3-(trifluoromethyl) at 25°C )Phenyl)pyridazine-3(2H)-one (3.5 g, 14.57 mmol) in water (87.5 ml) was stirred with potassium acetate (2.15 g, 21.86 mmol) and potassium bromide (5.20 g, 43.7 mmol) . Then bromine (2.3 mL, 43.7 mmol) was added dropwise to the reaction mixture at 0°C, and the reaction was heated at 100°C for 12 hours. After the reaction was completed, the reaction mixture was quenched by adding saturated sodium sulfite solution (50 mL) at 0°C, and then extracted with ethyl acetate (150 mL). The ethyl acetate layer was separated, dried over sodium sulfate, and concentrated under reduced pressure. The crude product was purified by silica gel flash column chromatography (using 25% ethyl acetate in hexane as the eluent) to give 4-bromo-6-(3-(trifluoromethyl)phenyl)pyridazine-3( 2H)-ketone (4.0 g, 12.54 mmol, 86% yield), a white solid substance. 1 H-NMR (400 MHz, DMSO-D6) δ 13.67 (s, 1H), 8.77 (s, 1H), 8.19-8.22 (m, 2H), 7.81 (d, J = 7.6 Hz, 1H), 7.72 ( t, J = 7.8 Hz, 1H); ESI MS (m/z) 316.85, 318.85 [(MH) + Br 79, 81 ]. d) Step 4 : 4-( Ethylthio )-6-(3-( trifluoromethyl ) phenyl ) pyridazine -3(2H) -one: At 0℃, add ethanethiol (1.1mL , 15.04mmol) of N,N-dimethylformamide (10mL) was added sodium hydride (0.5g, 12.54mmol) into the stirring solution, and the reaction was stirred for 15 minutes. Then add 4-bromo-6-(3-(trifluoromethyl)phenyl)pyridazine-3(2H)-one (4.0 g, 12.54 mmol) in N,N-dimethylformamide ( 10 mL), the reaction was stirred at 25°C for 16 hours. After the completion of the reaction, the reaction mixture was cooled to 0°C, and the reaction was quenched by the dropwise addition of water (20 mL) and diluted with ethyl acetate (50 mL). The ethyl acetate layer was separated, dried over sodium sulfate, and concentrated under reduced pressure. The crude product was purified by silica gel flash column chromatography (using 25% ethyl acetate in hexane as the eluent) to obtain 4-(ethylthio)-6-(3-(trifluoromethyl)phenyl) Pyridazine-3(2H)-one (2.0 g, 6.66 mmol, 53% yield) as a white solid. 1 H-NMR (400 MHz, DMSO-D6) δ 13.27 (s, 1H), 8.20-8.23 (m, 2H), 7.79-7.81 (m, 1H), 7.72 (t, J = 7.7 Hz, 1H), 7.65 (s, 1H), 3.10 (q, J = 7.3 Hz, 2H), 1.32 (t, J = 7.3 Hz, 3H); ESI-MS (M/Z) 301.00 (MH) + . e) Step 5 : 3- Chloro- 4-( ethylthio )-6-(3-( trifluoromethyl ) phenyl ) pyridazine: Add 4-(ethylthio)-6-(3-( A stirred solution of trifluoromethyl)phenyl)pyridazine-3(2H)-one (2.0 g, 6.66 mmol) in phosphorus oxychloride (6.5 mL, 69.9 mmol) was heated at 110°C for 4 hours. After the completion of the reaction, the reaction mixture was concentrated under reduced pressure. The resulting solid residue was carefully treated by dropwise addition of saturated sodium bicarbonate solution (25 mL) and extracted twice with ethyl acetate (150 mL). The combined ethyl acetate layer was dried over sodium sulfate and concentrated under reduced pressure. The crude product was purified by silica gel flash column chromatography (using 15% ethyl acetate in hexane as the eluent) to obtain 3-chloro-4-(ethylthio)-6-(3-(trifluoromethyl)benzene Pyridazine (2.0 g, 6.27 mmol, 94% yield) as a white solid. 1 H-NMR (400 MHz, DMSO-D6) δ 8.45-8.47 (m, 2H), 8.06 (s, 1H), 7.92 (dd, J = 8.4, 0.6 Hz, 1H), 7.81 (t, J = 7.8 Hz, 1H), 3.34 (t, J = 7.3 Hz, 2H), 1.36 (t, J = 7.3 Hz, 3H); ESI-MS (M/Z) 318.90 (MH) + . f) Step 6 : 3- chloro- 4-( ethylsulfonyl )-6-(3-( trifluoromethyl ) phenyl ) pyridazine: to 3-chloro-4-(ethyl Sulfuryl)-6-(3-(trifluoromethyl)phenyl)pyridazine (2.0 g, 6.27 mmol) in dichloromethane (20 mL) was added to a stirred solution of 3-chloroperoxybenzoic acid (5.4 g, 18.82 mmol). The reaction was stirred at 25°C for 16 hours. After the reaction was completed, the reaction mixture was quenched by dropwise addition of saturated sodium bicarbonate solution (10 mL), and extracted with dichloromethane (100 mL). The organic layer was concentrated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash column chromatography (using 10% ethyl acetate in hexane) as the eluent to obtain 3-chloro-4-(ethylsulfonyl)-6-(3-(trifluoromethyl) (Yl)phenyl)pyridazine (2.0 g, 5.70 mmol, 91% yield) as a white solid. 1 H-NMR (400 MHz, DMSO-D6) δ 8.70 (s, 1H), 8.54 (t, J = 7.6 Hz, 2H), 7.99 (dd, J = 7.8, 0.7 Hz, 1H), 7.83-7.89 ( m, 1H), 3.69 (q, J = 7.4 Hz, 2H), 1.21-1.27 (m, 3H); ESI-MS (M/Z) 350.95 (MH) + . g) Step 7 : 2-(4-( Ethylsulfonyl )-6-(3-( trifluoromethyl ) phenyl ) pyridazin- 3 -yl )-7-( trifluoromethyl ) phthalein Azin -1(2H) -one: To 7-(trifluoromethyl)phthalazine-1(2H)-one (0.120 g, 0.56 mmol) in N,N-dimethylformamide (10 Add potassium carbonate (0.116 g, 0.84 mmol) to the stirring solution in mL), and stir the reaction for 5 minutes. Then 3-chloro-4-(ethylsulfonyl)-6-(3-(trifluoromethyl)phenyl)pyridazine (0.24 g, 0.67 mmol) was added to the reaction mixture, and the reaction was carried out at 25°C. Stir for 16 hours. After the reaction was completed, the reaction mixture was diluted with cold water (5 mL) and extracted with ethyl acetate (50 mL). The ethyl acetate layer was dried with sodium sulfate and concentrated under reduced pressure to obtain a crude product. The crude product was purified by silica gel flash column chromatography (using 20% ethyl acetate in hexane as the eluent) to obtain 2-(4-(ethylsulfonyl)-6-(3-(trifluoromethyl) (Phenyl)phenyl)pyridazin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (135 mg, 0.25 mmol, 46% yield), as an off-white solid. 1 H-NMR (400 MHz, DMSO-D6) δ 9.09 (d, J = 19.6 Hz, 1H), 8.89 (d, J = 0.6 Hz, 1H), 8.58-8.71 (m, 3H), 8.48 (dd, J = 8.3, 1.5 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.05 (d, J = 7.8 Hz, 1H), 7.92 (t, J = 7.8 Hz, 1H), 3.75 (q, J = 7.2 Hz, 2H), 1.22 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.85 (MH) + .

例14:2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮(化合物131號)的合成:a) 1 步: 2-(5- -3-( 乙基磺醯基 ) 吡啶 -2- 基) -4- 甲基 -7-( 三氟甲基 ) 酞嗪 -1(2H)- 向2-乙酰基-5-(三氟甲基)苯甲酸(200 mg,0.86 mmol)的乙酸(6 mL)攪拌溶液中加入5-溴-3-(乙基磺醯基)-2-肼吡啶鹽酸鹽(265mg, 0.95 mmol)[按照(WO2018008727)中所述的步驟製備]。將反應混合物在120℃下加熱4小時。反應完成後,將反應混合物降溫至25℃,用水(50mL)稀釋,並用乙酸乙酯(100mL)萃取兩次。混合的乙酸乙酯層用鹽水(50mL)洗滌,用硫酸鈉乾燥並濃縮,得到粗產物,將其通過矽膠柱色譜法(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮(200 mg, 0.42 mmol, 49%產率);1 H-NMR (400 MHz, DMSO-D6) δ 9.17 (s, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.41 (d, J = 8.9 Hz , 1H), 8.31 (d, J = 8.9 Hz, 1H), 3.44-3.52 (m, 2H), 2.64 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H);ESI MS (m/z ) 475.55, 477.65 [(MH)+ Br79, 81 ]。b) 2 步: 2-(3-( 乙基磺醯基 )-5-(4- 氟苯基 ) 吡啶 -2- 基) -4- 甲基 -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮( 160 mg, 0.34 mmol)和(4-氟苯基)硼酸(70.5 mg,0.50 mmol)的1,4-二噁烷(6 mL)和水(1.5 mL)的攪拌溶液中加入碳酸氫鉀(116 mg,0.84 mmol)和1,1'-雙(二苯基膦基)二茂鐵-二氯化鈀(II)二氯甲烷加合物(27.4 mg,0.034 mmol)。將反應混合物進行真空/氮迴圈三次,使其徹底脫氧,然後在110℃下加熱3小時,反應完成後,將反應混合物用乙酸乙酯(50mL)和水(10mL)稀釋,分離乙酸乙酯層,用硫酸鈉乾燥並減壓濃縮。得到粗產物,將其通過矽膠柱色譜(使用40%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮(120 mg, 0.24 mmol, 72.7%產率);1 H-NMR (400 MHz , DMSO-D6) δ 9.28 (d, J = 2.1 Hz, 1H), 8.70 (d, J = 2.4 Hz, 1H), 8.55 (s, 1H), 8.41 (dd, J = 8.6, 1.8 Hz, 1H) , 8.32 (d, J = 8.3 Hz, 1H), 8.02 (dd, J = 8.6, 5.5 Hz, 2H), 7.44 (t, J = 8.7 Hz, 2H), 3.47-3.52 (m, 2H), 2.66 ( s, 3H), 1.17 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 492.10 (MH)+Example 14: 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1( Synthesis of 2H)-one (Compound No. 131): a) Step 1 : 2-(5- Bromo- 3-( ethylsulfonyl ) pyridin -2- yl) -4 -methyl -7-( fluoro-methyl) phthalazin--1 (2H) - one to a solution of 2-acetyl-5- (trifluoromethyl) benzoic acid (200 mg, 0.86 mmol) in acetic acid (6 mL) was added 5-bromo - 3-(Ethylsulfonyl)-2-hydrazinepyridine hydrochloride (265 mg, 0.95 mmol) [prepared according to the procedure described in (WO2018008727)]. The reaction mixture was heated at 120°C for 4 hours. After the reaction was completed, the reaction mixture was cooled to 25°C, diluted with water (50 mL), and extracted twice with ethyl acetate (100 mL). The mixed ethyl acetate layer was washed with brine (50 mL), dried over sodium sulfate and concentrated to obtain the crude product, which was purified by silica gel column chromatography (using 40% ethyl acetate in hexane as the eluent) to obtain 2-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one (200 mg, 0.42 mmol, 49% yield); 1 H-NMR (400 MHz, DMSO-D6) δ 9.17 (s, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.41 (d, J = 8.9 Hz , 1H), 8.31 (d, J = 8.9 Hz, 1H), 3.44-3.52 (m, 2H), 2.64 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z ) 475.55, 477.65 [(MH) + Br 79, 81 ]. b) Step 2 : 2-(3-( Ethylsulfonyl )-5-(4- fluorophenyl ) pyridin -2- yl) -4 -methyl -7-( trifluoromethyl ) phthalazine -1(2H) -one: To 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1( Add 2H)-ketone (160 mg, 0.34 mmol) and (4-fluorophenyl)boronic acid (70.5 mg, 0.50 mmol) to a stirred solution of 1,4-dioxane (6 mL) and water (1.5 mL) Potassium bicarbonate (116 mg, 0.84 mmol) and 1,1'-bis(diphenylphosphino)ferrocene-palladium(II) dichloride dichloromethane adduct (27.4 mg, 0.034 mmol). The reaction mixture was vacuum/nitrogen looped three times to completely deoxygenate, and then heated at 110°C for 3 hours. After the reaction was completed, the reaction mixture was diluted with ethyl acetate (50 mL) and water (10 mL), and the ethyl acetate was separated. The layer was dried over sodium sulfate and concentrated under reduced pressure. The crude product was obtained, which was purified by silica gel column chromatography (using 40% ethyl acetate in hexane as the eluent) to obtain 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl) )Pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one (120 mg, 0.24 mmol, 72.7% yield); 1 H-NMR (400 MHz , DMSO-D6) δ 9.28 (d, J = 2.1 Hz, 1H), 8.70 (d, J = 2.4 Hz, 1H), 8.55 (s, 1H), 8.41 (dd, J = 8.6, 1.8 Hz, 1H) , 8.32 (d, J = 8.3 Hz, 1H), 8.02 (dd, J = 8.6, 5.5 Hz, 2H), 7.44 (t, J = 8.7 Hz, 2H), 3.47-3.52 (m, 2H), 2.66 ( s, 3H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 492.10 (MH) + .

例15:2-(6-溴-3-(乙硫基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(化合物234號)的合成:a) 1 步: 2-(6- -3- 硝基咪唑並 [1,2-a] 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向7-(三氟甲基)酞嗪-1(2H)-酮(2.5 g, 11.67 mmol)的N,N-二甲基甲酰胺(20 mL)攪拌溶液中加入碳酸銫(7.6 g, 23.35 mmol)和6-溴-2-氯-3-硝基咪唑並[1,2-a]吡啶(3.20g, 11.67 mmol)。將反應混合物在25℃下攪拌5小時。反應完成後,將水(50mL)加入到反應混合物中,然後用乙酸乙酯(100mL)萃取兩次。合併的有機層經硫酸鈉乾燥,過濾並濃縮,得到粗產物,將其通過矽膠快速色譜(使用己烷中的乙酸乙酯作為洗脫劑)純化,得到2-(6-溴-3-硝基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(3.1 g, 6.83 mmol, 58%產率),為固體。ESI MS (m/z) 455.80 (MH)+b) 2 步: 2-(3- 氨基 -6- 溴咪唑並 [1,2-a] 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向2-(6-溴-3-硝基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(5 g, 11.01 mmol)的乙酸(100mL)攪拌懸浮液中加入鐵粉(3.07g,55.0mmol),將反應混合物在90℃加熱6小時,反應結束後,將反應混合物通過矽藻土過濾,用乙酸乙酯(150mL)稀釋,用水(50mL)和飽和碳酸鈉溶液洗滌乙酸乙酯層。將有機層用硫酸鈉乾燥,過濾並減壓蒸發,得到2-(3-氨基-6-溴咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(3.4 g, 8.02 mmol, 73%產率)。ESI MS (m/z) 425.85 (MH)+c) 3 步: 2-(6- -3-( 乙硫基 ) 咪唑並 [1,2-a] 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 在25℃下向二乙基二硫(0.1mL,0.57mmol)的乙腈(5mL)攪拌溶液中滴加亞硝酸叔丁酯(0.05mL,0.71mmol),並將得到的混合物在相同溫度下攪拌30分鐘。隨後,在25℃下將2-(3-氨基-6-溴咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(200 mg, 0.47 mmol)滴入,將反應混合物在25℃下攪拌4小時,反應完成後,將反應混合物用水(30mL)稀釋,用乙酸乙酯(50mL)萃取兩次。用硫酸鈉乾燥,過濾並減壓蒸發,得到粗產物,將其通過矽膠快速色譜法(使用乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(6-溴-3-(乙硫基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(110 mg, 0.23 mmol, 50%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 8.86 (q, J = 0.8 Hz, 1H), 8.76 (d, J = 8.9 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.4, 2.0 Hz, 1H), 8.31 (d, J = 8.6 Hz, 1H), 7.71-7.75 (m, 1H), 7.64-7.68 (m, 1H), 2.74 (q, J = 7.3 Hz, 2H), 1.05 (t, J = 24.7, 7.1 Hz, 3H);ESI MS (m/z) 468.90 (MH)+Example 15: 2-(6-Bromo-3-(ethylthio)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one Synthesis of (Compound No. 234): a) Step 1 : 2-(6- Bromo- 3 -nitroimidazo [1,2-a] pyridin -2- yl) -7-( trifluoromethyl ) phthalein Azin -1(2H) -one: To 7-(trifluoromethyl)phthalazine-1(2H)-one (2.5 g, 11.67 mmol) in N,N-dimethylformamide (20 mL) stirred solution Add cesium carbonate (7.6 g, 23.35 mmol) and 6-bromo-2-chloro-3-nitroimidazo[1,2-a]pyridine (3.20 g, 11.67 mmol). The reaction mixture was stirred at 25°C for 5 hours. After the reaction was completed, water (50 mL) was added to the reaction mixture, and then extracted twice with ethyl acetate (100 mL). The combined organic layer was dried over sodium sulfate, filtered and concentrated to obtain the crude product, which was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-(6-bromo-3-nitro Imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (3.1 g, 6.83 mmol, 58% yield), as a solid. ESI MS (m/z) 455.80 (MH) + . b) Step 2 : 2-(3- Amino -6- bromoimidazo [1,2-a] pyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H) -one: To 2-(6-bromo-3-nitroimidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (5 g, 11.01 mmol) of acetic acid (100 mL) was added to the stirring suspension of iron powder (3.07g, 55.0mmol), the reaction mixture was heated at 90 ℃ for 6 hours, after the completion of the reaction, the reaction mixture was filtered through diatomaceous earth, with ethyl acetate ( 150mL), and the ethyl acetate layer was washed with water (50mL) and saturated sodium carbonate solution. The organic layer was dried over sodium sulfate, filtered and evaporated under reduced pressure to obtain 2-(3-amino-6-bromoimidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalein Ozin-1(2H)-one (3.4 g, 8.02 mmol, 73% yield). ESI MS (m/z) 425.85 (MH) + . c) Step 3 : 2-(6- Bromo- 3-( ethylthio ) imidazo [1,2-a] pyridin -2- yl) -7-( trifluoromethyl ) phthalazine -1(2H ) -Ketone: Add tert-butyl nitrite (0.05 mL, 0.71 mmol) dropwise to a stirred solution of diethyl disulfide (0.1 mL, 0.57 mmol) in acetonitrile (5 mL) at 25°C, and place the resulting mixture in Stir at the same temperature for 30 minutes. Subsequently, 2-(3-amino-6-bromoimidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (200 mg, 0.47 mmol) was added dropwise, and the reaction mixture was stirred at 25° C. for 4 hours. After the reaction was completed, the reaction mixture was diluted with water (30 mL) and extracted twice with ethyl acetate (50 mL). Dry over sodium sulfate, filter and evaporate under reduced pressure to obtain the crude product, which was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-(6-bromo-3-(ethyl) Thio)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (110 mg, 0.23 mmol, 50% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 8.86 (q, J = 0.8 Hz, 1H), 8.76 (d, J = 8.9 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.4, 2.0 Hz, 1H), 8.31 (d, J = 8.6 Hz, 1H), 7.71-7.75 (m, 1H), 7.64-7.68 (m, 1H), 2.74 (q, J = 7.3 Hz, 2H), 1.05 (t, J = 24.7, 7.1 Hz, 3H); ESI MS (m/z) 468.90 (MH) + .

例16:2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(化合物232號)的合成:a) 1 步: 2-(6- -3-( 乙基磺醯基 ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1(2H)- 酮: 向3-羥基-6-(三氟甲基)異苯並呋喃-1(3H)-酮(200 mg, 0.92 mmol)的乙酸(5 mL)攪拌溶液中加入5-氯-3- (乙基磺醯基)-2-肼吡啶鹽酸鹽(216 mg, 0.92 mmol)。將反應混合物在115℃下加熱2小時。反應完成後,將反應混合物冷卻至25℃,用水(20mL)稀釋,然後用乙酸乙酯(50mL)萃取兩次。混合的乙酸乙酯層用鹽水(20mL)和水(20mL)洗滌,用硫酸鈉乾燥並濃縮,得到粗產物,將其通過矽膠柱色譜法(使用30%乙酸乙酯的己烷溶液作為洗脫劑)純化,得到2-(5-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(135 mg, 0.323 mmol, 35%產率)。1 H-NMR (400 MHz, DMSO-D6) δ 9.11 (d, J = 2.4 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.71 (d, J = 2.4 Hz, 1H), 8.52 (d, J = 1.2 Hz, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 418.05(MH)+b) 2 步: 2-(3-( 乙基磺醯基 )-6-(1H-1,2,4- 三唑 -1- ) 吡啶 -2- 基) -7-( 三氟甲基 ) 酞嗪 -1 (2H)- 酮: 向2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(150 mg, 0.36 mmol)的N,N-二甲基甲酰胺(5 mL)攪拌溶液中加入碳酸銫(292 mg,0.89 mmol)和1H-1,2,4-三唑(37.2 mg,0.540 mmol)。將反應在25℃下攪拌5 小時。反應完成後,向反應混合物中加入水(50 mL)並用乙酸乙酯(100 mL)萃取兩次,合併的有機層用硫酸鈉乾燥,過濾並濃縮,得到粗產物。將粗產物經矽膠快速色譜(用己烷中的乙酸乙酯作為洗脫劑)純化,得到2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮(135 mg, 0.30 mmol, 83 %產率)。1 H-NMR (400 MHz, DMSO-D6) δ 9.44 (s, 1H), 8.80-8.82 (m, 2H), 8.54 (d, J = 0.9 Hz, 1H), 8.44 (dd, J = 7.9, 1.8 Hz, 2H), 8.33-8.37 (m, 2H), 3.41-3.46 (q, 2H), 1.15 (t, J = 7.5 Hz, 3H);ESI MS (m/z) 450.95 (MH)+Example 16: 2-(3-(Ethylsulfonyl)-6-(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Synthesis of azin-1(2H)-one (Compound No. 232): a) Step 1 : 2-(6- Chloro- 3-( ethylsulfonyl ) pyridin -2- yl) -7-( trifluoro Methyl ) phthalazine -1(2H) -one: To 3-hydroxy-6-(trifluoromethyl)isobenzofuran-1(3H)-one (200 mg, 0.92 mmol) in acetic acid (5 mL) 5-chloro-3-(ethylsulfonyl)-2-hydrazinepyridine hydrochloride (216 mg, 0.92 mmol) was added to the stirred solution. The reaction mixture was heated at 115°C for 2 hours. After the reaction was completed, the reaction mixture was cooled to 25°C, diluted with water (20 mL), and then extracted twice with ethyl acetate (50 mL). The mixed ethyl acetate layer was washed with brine (20 mL) and water (20 mL), dried over sodium sulfate and concentrated to obtain a crude product, which was subjected to silica gel column chromatography (using 30% ethyl acetate in hexane as the elution Reagent) to obtain 2-(5-chloro-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (135 mg, 0.323 mmol, 35% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 9.11 (d, J = 2.4 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.71 (d, J = 2.4 Hz, 1H), 8.52 (d, J = 1.2 Hz, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 418.05(MH) + . b) Step 2 : 2-(3-( Ethylsulfonyl )-6-(1H-1,2,4- triazol- 1 -yl ) pyridin -2- yl) -7-( trifluoromethyl yl) phthalazine -1 (2H) - one: to a 2- (6-chloro-3- (sulfo acyl-ethyl) pyridin-2-yl) -7- (trifluoromethyl) phthalazine -1 (2H )-Ketone (150 mg, 0.36 mmol) in N,N-dimethylformamide (5 mL) was added cesium carbonate (292 mg, 0.89 mmol) and 1H-1,2,4-triazole (37.2 mg, 0.540 mmol). The reaction was stirred at 25°C for 5 hours. After the reaction was completed, water (50 mL) was added to the reaction mixture and extracted twice with ethyl acetate (100 mL). The combined organic layer was dried over sodium sulfate, filtered and concentrated to obtain a crude product. The crude product was purified by silica gel flash chromatography (using ethyl acetate in hexane as the eluent) to obtain 2-(3-(ethylsulfonyl)-6-(1H-1,2,4-triazole) -1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one (135 mg, 0.30 mmol, 83% yield). 1 H-NMR (400 MHz, DMSO-D6) δ 9.44 (s, 1H), 8.80-8.82 (m, 2H), 8.54 (d, J = 0.9 Hz, 1H), 8.44 (dd, J = 7.9, 1.8 Hz, 2H), 8.33-8.37 (m, 2H), 3.41-3.46 (q, 2H), 1.15 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 450.95 (MH) + .

下列化合物(表1)是使用合適的起始原料並按照方案1-9或實施例1至16中所述的類似方法獲得的 表-1 貨號    化合物名稱 分析數據 1 2-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.02 (dd, J = 4.9, 1.7 Hz, 1H), 8.74 (s, 1H), 8.61 (dd, J = 7.8, 1.7 Hz, 2H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.3, 1.5 Hz, 1H), 7.90-7.99 (m, 1H), 3.40 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 384.1 (MH)+. 2 2-(3-(乙硫基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.69 (d, J = 7.8 Hz, 1H), 8.55 (s, 1H), 8.49 (d, J = 8.3 Hz, 1H), 8.41 (dd, J = 4.6, 1.5 Hz, 1H), 8.23 (dd, J = 8.4, 1.6 Hz, 1H), 8.03-8.08 (m, 1H), 7.58 (dd, J = 8.1, 4.6 Hz, 1H), 2.96 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 352.1 (MH)+ 3 2-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.74 (d, J = 0.7 Hz, 1H), 8.57 (t, J = 2.4 Hz, 2H), 8.52 (d, J = 8.3 Hz, 1H), 8.30 (d, J = 2.2 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 3.08 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 430, 432 [(MH)+ Br79, 81]. 4 2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.20 (d, J = 2.4 Hz, 1H), 8.81 (d, J = 2.2 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.7, 1.6 Hz, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.19 ( t, J = 7.5 Hz, 3H); ESI MS (m/z) 462.0, 464.0 [(MH)+ Br79, 81]. 5 2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (d, J = 2.4 Hz, 1H), 8.60-8.65 (m, 2H), 8.51 (d, J = 8.3 Hz, 1H), 8.28-8.32 (m, 1H), 8.12-8.14 (m, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.13-1.24 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 417.85 (MH)+. 6 2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.61 ( m, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.29 (dd, J = 8.7, 1.6 Hz, 1H), 8.14 (d, J = 2.0 Hz, 2H), 7.82 (t, J = 1.8 Hz, 1H), 3.53 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 527.9, 529.9 [(MH)+ Cl35, 37]. 7 2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.2 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.61 (s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.29 (dd, J = 8.3, 1.5 Hz, 1H), 7.83-7.88 (m, 2H), 7.47 (tt, J = 9.3, 2.3 Hz, 1H), 3.53 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 496.10 (MH)+. 8 2-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.62 (s, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.29 (d, J = 6.8 Hz, 1H), 8.22 (d, J = 8.3 Hz, 2H), 7.98 (d, J = 8.1 Hz, 2H), ), 3.50 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 527.95 (MH)+. 9 2-(3-(乙硫基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6DMSO-d6) δ 8.86 (q, J = 1.0 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.60 (s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.41 (d, J = 1.7 Hz, 1H), 8.29 (dd, J = 8.3, 1.5 Hz, 1H), 3.15 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 420 (MH)+ 10 2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.51 (q, J = 1.1 Hz, 1H), 8.94-8.95 (m, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.62 (s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.30 (dd, J = 8.3, 1.5 Hz, 1H), 3.55 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 451.95 (MH)+. 11 2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.47 (d, J = 1.0 Hz, 1H), 8.83 (d, J = 8.6 Hz, 1H), 8.80 (d, J = 2.0 Hz, 1H), 8.62 (d, J = 4.6 Hz, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.47 (d, J = 1.2 Hz, 1H), 8.34-8.37 (m, 1H), 8.29-8.32 (m, 1H), 3.45 ( q, J = 7.4 Hz, 2H), 1.15 ( t, J = 7.4 Hz, 3H); ESI MS (m/z) 451.15 (MH)+. 12 2-(3-(乙基磺醯基)-6-(5-甲基-3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.77-8.79 (m, 2H), 8.61 (s, 1H), 8.55 (d, J = 8.3 Hz, 1H), 8.36 (d, J = 8.6 Hz, 1H), 8.30 (d, J = 8.3 Hz, 1H), 6.94 (s, 1H), 3.49 (q, J = 7.4 Hz, 2H), 2.62 (s, 3H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 531.95 (MH)+. 13 2-(3-(乙基磺醯基)-6-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.83 (q, J = 1.2 Hz, 1H), 8.74-8.76 (m, 2H), 8.58 (s, 1H), 8.49 (d, J = 8.3 Hz, 1H), 8.39 (d, J = 8.6 Hz, 1H), 8.26 (dd, J = 8.3, 1.5 Hz, 1H), 7.12 (d, J = 2.8 Hz, 1H), 3.40 (q, J = 7.4 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 518.15 (MH)+. 14 2-(3-(乙基磺醯基)-6-(3-(三氟甲基)-1H-1,2,4-三唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.78 (d, J = 0.7 Hz, 1H), 8.89 (d, J = 8.6 Hz, 1H), 8.81 (s, 1H), 8.63 (s, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.43 (d, J = 8.6 Hz, 1H), 8.30-8.32 (m, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.16-1.24 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 519.1 (MH)+. 15 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.29 (d, J = 2.2 Hz, 1H), 8.71-8.74 (m, 2H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.26-8.28 (m, 1H), 8.01-8.04 (m, 2H), 7.42-7.47 (m, 2H), 3.49 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.9 (MH)+. 16 2-(5-(乙硫基)-6'-氟代-[3,3'-二吡啶]-6-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.77 (d, J = 2.8 Hz, 1H), 8.76 (d, J = 2.1 Hz, 1H), 8.74 (s, 1H), 8.57 (s, 1H), 8.52 (td, J = 8.0, 3.0 Hz, 2H), 8.31 (d, J = 2.1 Hz, 1H), 8.26 (dd, J = 8.6, 1.5 Hz, 1H), 7.40 (dd, J = 8.6, 2.8 Hz, 1H), 3.12 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz,, 3H); ESI MS (m/z) 447.1 (MH)+ 17 2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.30 (d, J = 2.1 Hz, 1H), 8.72-8.73 (m, 2H), 8.57 (s, 1H), 8.48 (d, J = 8.3 Hz, 1H), 8.24 (dd, J = 8.5, 1.3 Hz, 1H), 8.05-8.09 (m, 2H), 7.57 (d, J = 7.9 Hz, 2H), 3.46 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.2(MH)+. 18 2-(5-(乙基磺醯基)-6'-氟代-[3,3'-二吡啶]-6-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.1 Hz, 1H), 8.75 (s, 1H), 8.50-8.63 (m, 3H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.43 (td, J = 8.9, 2.6 Hz, 1H), 3.49 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 479.0 (MH)+. 19 7-(5-溴-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.53 (d, J = 2.2 Hz, 1H), 9.22 (d, J = 2.1 Hz, 1H), 9.09 (d, J = 1.5 Hz, 1H), 8.83 (d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 3.45-3.51 (q, J= 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 462.7, 464.7 [(MH)+ Br79, 81]. 20 7-(3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.53 (d, J = 1.7 Hz, 1H), 9.10 (t, J = 1.1 Hz, 1H), 9.03 (dd, J = 4.9, 1.7 Hz, 1H), 8.74 (s, 1H), 8.62 (dd, J = 7.8, 1.7 Hz, 1H), 7.99 (dd, J = 7.9, 4.8 Hz, 1H), 3.40 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 384.8 (MH)+. 21 7-(6-氯-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (dd, J = 2.2, 0.5 Hz, 1H), 9.10 (q, J = 1.0 Hz, 1H), 8.76 (s, 1H), 8.66 (d, J = 8.3 Hz, 1H), 8.15 (d, J = 8.3 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 419.1 (MH)+. 22 7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.2 Hz, 1H), 9.32-9.35 (m, 1H), 9.11 (t, J = 1.1 Hz, 1H), 8.75 (t, J = 2.1 Hz, 2H), 8.03-8.07 (m, 2H), 7.44-7.50 (m, 2H), 3.52 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 479.5 (MH)+. 23 7-(3-(乙基磺醯基)-5-(3-氟代-4-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.2 Hz, 1H), 9.43 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.5 Hz, 1H), 8.90 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.27 (d, J = 12.0 Hz, 1H), 8.01-8.07 (m, 2H), 3.5 (q, J = 7.3 Hz, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 547 (MH)+ 24 7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.55 (d, J = 2.2 Hz, 1H), 9.52 (d, J = 4.6 Hz, 1H), 9.11 (s, 1H), 8.97 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 1.7 Hz, 1H), 3.56 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 452.8 (MH)+. 25 7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 1.8 Hz, 1H), 9.34 (d, J = 2.4 Hz, 1H), 9.09 (d, J = 1.5 Hz, 1H), 8.77 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.10 (dt, J = 9.4, 2.5 Hz, 2H), 7.60 (d, J = 7.9 Hz, 2H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 545.2 (MH)+. 26 7-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 1.8 Hz, 1H), 9.37 (d, J = 2.4 Hz, 1H), 9.09 (d, J = 1.5 Hz, 1H), 8.86 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.34-8.39 (m, 2H), 7.74-7.79 (m, 1H), 3.46-3.53 (q, J = 7.6 Hz 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 546.9 (MH)+. 27 7-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 2.1 Hz, 1H), 9.09 (t, J = 1.1 Hz, 1H), 8.75 (s, 1H), 8.63 (t, J = 4.1 Hz, 1H), 8.51 (d, J = 8.6 Hz, 1H), 8.23-8.28 (m, 2H), 7.37-7.43 (m, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 479.0 (MH)+. 28 7-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 2.2 Hz, 1H), 9.39-9.40 (m, 1H), 9.09 (s, 1H), 8.86-8.86 (m, 1H), 8.75 (d, J = 1.0 Hz, 1H), 8.35 (d, J = 4.6 Hz, 1H), 8.26-8.29 (m, 1H), 7.80-7.93 (m, 2H), 3.52 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 529.2 (MH)+. 29 4-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)苯並腈 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 1.6 Hz, 1H), 9.41 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.6 Hz, 1H), 8.86 (d, J = 2.0 Hz, 1H), 8.77 (s, 1H), 8.20-8.23 (m, 2H), 8.09-8.12 (m, 2H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 485.8 (MH)+. 30 7-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 1.6 Hz, 1H), 9.11 (t, J = 1.1 Hz, 1H), 8.78 (s, 1H), 8.69 (d, J = 8.3 Hz, 1H), 8.57 (d, J = 8.6 Hz, 1H), 8.33 (dt, J = 9.5, 2.6 Hz, 2H), 7.58 (d, J = 8.1 Hz, 2H), 3.45 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 545.0 (MH)+. 31 7-(3-(乙基磺醯基)-5-苯基吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 1.7 Hz, 1H), 9.34 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.5 Hz, 1H), 8.76 (t, J = 2.1 Hz, 2H), 7.97-7.99 (m, 2H), 7.57-7.65 (m, 3H), 3.52 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.0 (MH)+. 32 7-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (s, 1H), 9.39 (d, J = 2.4 Hz, 1H), 9.11 (s, 1H), 8.85 (d, J = 2.0 Hz, 1H), 8.76 (s, 1H), 7.85 (d, J = 6.8 Hz, 2H), 7.46 (t, J = 9.2 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 497.0 (MH)+. 33 7-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.0 Hz, 1H), 9.40 (d, J = 2.2 Hz, 1H), 9.11 (d, J = 1.6 Hz, 1H), 8.87 (d, J = 2.3 Hz, 1H), 8.76 (s, 1H), 8.15 (d, J = 1.6 Hz, 2H), 7.82 (t, J = 2.0 Hz, 1H), 3.54 (q, J = 7.3 Hz, 2H), 1.20 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 529.0, 531.0 [(MH)+ Cl35, 37]. 34 7-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.56 (d, J = 2.4 Hz, 1H), 9.52 (d, J = 1.8 Hz, 1H), 9.09 (d, J = 1.8 Hz, 2H), 8.94 (d, J = 2.1 Hz, 1H), 8.76 (s, 1H), 7.24 (d, J = 2.8 Hz, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.6 Hz, 3H); ESI MS (m/z) 519.0 (MH)+. 35 7-(3-(乙基磺醯基)-6-(3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.41 (d, J = 1.7 Hz, 1H), 8.58 (d, J = 8.1 Hz, 1H), 8.47-8.49 (m, 2H), 8.40 (s, 1H), 8.29 (d, J = 7.8 Hz, 1H), 8.18 (d, J = 8.1 Hz, 1H), 7.80 (d, J = 7.8 Hz, 1H), 7.67 (t, J = 7.8 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.38 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.8 (MH)+. 36 7-(6-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.8 Hz, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.46 (d, J = 1.2 Hz, 1H), 8.45 (s, 1H), 8.08 (d, J = 8.3 Hz, 1H), 7.98 (d, J = 1.8 Hz, 2H), 7.49-7.52 (m, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 528.9 ,530.9[(MH)+ Cl35, 37] 37 3-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.04-9.08 (m, 1H), 8.71 (s, 1H), 8.65 (dd, J = 8.1, 1.7 Hz, 1H), 8.42-8.50 (m, 1H), 8.17-8.30 (m, 1H), 7.97-8.04 (m, 2H), 3.36-3.46 (m, 2H), 1.18 (t ,J = 7.3 Hz,, 3H); ESI MS (m/z) 384 (MH)+ 38 3-(3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.05 (dd, J = 4.9, 1.7 Hz, 1H), 8.68 (s, 1H), 8.65 (dd, J = 8.1, 1.7 Hz, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.17 (s, 1H), 8.02 (dd, J = 7.9, 4.8 Hz, 1H), 7.97 (dd, J = 8.4, 1.6 Hz, 1H), 3.36 3.38 (m, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 383.6 (MH)+ 39 3-(3-(乙硫基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 8.67-8.69 (m, 2H), 8.14 (s, 1H), 8.00-8.07 (m, 2H), 7.91-7.95 (m, 1H), 2.95-3.10 (m, 2H), 1.33 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 420 (MH)+ 40 7-(3-(乙基磺醯基)-6-(3-甲基-1H-1,2,4-三唑-1-基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.37 (d, J = 1.5 Hz, 1H), 9.00 (s, 1H), 8.60 (dd, J = 8.6, 2.4 Hz, 1H), 8.41-8.45 (m, 2H), 8.20 (d, J = 8.6 Hz, 1H), 3.40 (q, J = 7.4 Hz, 2H), 2.52 (s, 3H), 1.33 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 465.8 (MH)+. 41 7-(3-(乙基磺醯基)-6-(3-氟代-4-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.41 (d, J = 1.7 Hz, 1H), 8.60 (d, J = 8.3 Hz, 1H), 8.48-8.50 (m, 2H), 8.16 (d, J = 8.1 Hz, 1H), 7.99 (t, J = 8.0 Hz, 2H), 7.78 (t, J = 7.7 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.38 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 547.0 (MH)+. 42 4-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-2-基)苯並腈 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.2 Hz, 1H), 8.57 (d, J = 8.3 Hz, 1H), 8.45 (d, J = 9.8 Hz, 2H), 8.21 (d, J = 8.3 Hz, 2H), 8.15 (d, J = 8.3 Hz, 1H), 7.81 (d, J = 8.3 Hz, 2H), 3.44 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 485.8 (MH)+. 43 7-(3-(乙基磺醯基)-6-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.5 Hz, 1H), 8.55 (d, J = 8.3 Hz, 1H), 8.45-8.47 (m, 2H), 8.39 (dd, J = 6.7, 1.8 Hz, 1H), 8.27-8.31 (m, 1H), 8.11 (d, J = 8.3 Hz, 1H), 7.35 (t, J = 9.2 Hz, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 546.8 (MH)+. 44 3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 8.98 (d, J = 2.4 Hz, 1H), 8.64 (d, J = 2.4 Hz, 1H), 8.63 (q, J = 0.7 Hz, 1H), 8.13 (t, J = 6.1 Hz, 1H), 8.07 (dd, J = 8.6, 1.7 Hz, 1H), 7.96 (d, J = 8.6 Hz, 1H), 3.35-3.46 (m, 2H), 1.40 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.95, 463.95 [(MH)+ Br79, 81]. 45 3-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.55 (q, J = 1.1 Hz, 1H), 9.02-9.02 (m, 1H), 8.70 (s, 1H), 8.48 (q, J = 0.7 Hz, 1H), 8.30 (dd, J = 8.7, 2.1 Hz, 1H), 8.04 (d, J = 8.6 Hz, 1H), 3.47-3.61 (m, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 451.8 (MH)+. 46 3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (d, J = 2.4 Hz, 1H), 8.93 (d, J = 2.2 Hz, 1H), 8.73 (s, 1H), 8.48 (t, J = 1.1 Hz, 1H), 8.29 (dd, J = 8.6, 2.0 Hz, 1H), 8.16 (d, J = 2.0 Hz, 2H), 8.04 (t, J = 4.3 Hz, 1H), 7.83 (t, J = 1.8 Hz, 1H), 3.48-3.62 (m, 2H), 1.18-1.24 (t,J=7.3Hz, 3H); ESI MS (m/z) 528.00, 530.00 [(MH)+ Cl35, 37]. 47 3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.1 Hz, 1H), 8.78 (d, J = 2.1 Hz, 1H), 8.72 (s, 1H), 8.46 (d, J = 2.1 Hz, 1H), 8.27 (dd, J = 8.6, 2.1 Hz, 1H), 8.01-8.06 (m, 3H), 7.43-7.48 (m, 2H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.7 (MH)+. 48 3-(3-(乙基磺醯基)-5-苯基吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.1 Hz, 1H), 8.73 (s, 1H), 8.46 (d, J = 2.1 Hz, 1H), 8.27 (dd, J = 8.9, 2.1 Hz, 1H), 8.02 (d, J = 8.6 Hz, 1H), 7.96-7.98 (m, 2H), 7.54-7.64 (m, 3H), 3.43-3.60 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 459.75 (MH)+. 49 3-(3-(乙基磺醯基)-5-(4-甲氧基苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.74 (t, J = 2.4 Hz, 2H), 8.48 (d, J = 2.2 Hz, 1H), 8.29 (dd, J = 8.7, 2.1 Hz, 1H), 8.04 (d, J = 8.6 Hz, 1H), 7.94-7.97 (m, 2H), 7.18 (dd, J = 6.8, 2.0 Hz, 2H), 3.87 (s, 3H), 3.43-3.60 (m, 2H), 1.2 ( t, J = 7.3 Hz, 3H); ESI MS (m/z) 490.00 (MH)+. 50 3-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (d, J = 2.2 Hz, 1H), 8.90 (d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 8.48 (s, 1H), 8.29 (dd, J = 8.6, 2.2 Hz, 1H), 8.23 (d, J = 8.1 Hz, 2H), 8.04 (d, J = 8.6 Hz, 1H), 7.99 (d, J = 8.3 Hz, 2H), 3.46-3.59 (m, 2H), 1.21 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 527.85 (MH)+. 51 7-(3-(乙基磺醯基)-6-苯基吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.37 (d, J = 1.5 Hz, 1H), 8.49 (d, J = 8.3 Hz, 1H), 8.44 (d, J = 7.0 Hz, 2H), 8.07-8.11 (m, 3H), 7.47-7.52 (m, 3H), 3.43 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.2 (MH)+. 52 7-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.5 Hz, 1H), 9.06 (q, J = 1.1 Hz, 1H), 8.61 (q, J = 1.1 Hz, 1H), 8.45-8.46 (m, 2H), 7.61 (t, J = 8.6 Hz, 1H), 7.19-7.24 (m, 2H), 3.48 (q, J = 7.3 Hz, 2H), 1.36 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 563.1 (MH)+. 53 7-(5-(2,2-二氟苯並[d][1,3]二氧雜環戊烯-5-基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (s, 1H), 9.05 (d, J = 2.1 Hz, 1H), 8.55 (d, J = 2.1 Hz, 1H), 8.45 (d, J = 4.3 Hz, 2H), 7.40-7.42 (m, 2H), 7.28 (s, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.37 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 540.9 (MH)+. 54 7-(6-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.5 Hz, 1H), 8.54 (t, J = 4.1 Hz, 1H), 8.46 (d, J = 1.2 Hz, 1H), 8.44 (s, 1H), 8.07 (d, J = 8.3 Hz, 1H), 7.61-7.67 (m, 2H), 6.93-7.00 (m, 1H), 3.44 (q, J = 7.3 Hz, 2H), 1.35 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 497.0 (MH)+. 55 7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.2 Hz, 1H), 9.35 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.6 Hz, 1H), 8.79 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.09 (dd, J = 6.6, 2.2 Hz, 2H), 7.53 (d, J = 8.6 Hz, 2H),6.88 (tt, J = 52.0, 2.9 Hz, 1H), 3.52 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 577.0 (MH)+. 56 3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.46-9.47 (m, 1H), 8.94 (q, J = 1.1 Hz, 1H), 8.74 (d, J = 1.0 Hz, 1H), 8.48 (d, J = 4.4 Hz, 1H), 8.38 (d, J = 4.9 Hz, 1H), 8.28-8.32 (m, 2H), 8.04 (dd, J = 8.6, 2.4 Hz, 1H), 7.93-7.96 (m, 1H), 7.84-7.89 (m, 1H),3.73 (q, J = 7.4 Hz, 2H), 1.26 (t, J = 7.5 Hz, 3H) 57 4-(5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)喹唑啉-3(4H)-基)吡啶-3-基)苯並腈 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (d, J = 2.2 Hz, 1H), 8.91 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.48 (q, J = 0.7 Hz, 1H), 8.29 (dd, J = 8.7, 2.1 Hz, 1H), 8.22 (dd, J = 6.8, 2.0 Hz, 2H), 8.11 (dd, J = 6.6, 2.0 Hz, 2H), 8.04 (d, J = 8.6 Hz, 1H), 3.46-3.63 (m, 2H), 1.26 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 485.05 (MH)+. 58 3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (t, J = 2.2 Hz, 1H), 8.84 (d, J = 2.2 Hz, 1H), 8.74 (s, 1H), 8.49 (d, J = 7.1 Hz, 1H), 8.29 (dd, J = 8.7, 2.1 Hz, 1H), 8.12-8.15 (m, 2H), 8.04 (d, J = 8.6 Hz, 1H), 7.62-7.66 (m, 2H), 3.53 (q, J = 7.3 Hz, 3H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 544.05 (MH)+. 59 3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (t, J = 2.1 Hz, 1H), 8.90 (d, J = 2.2 Hz, 1H), 8.74 (d, J = 1.7 Hz, 1H), 8.47 (d, J = 1.7 Hz, 1H), 8.29 (dd, J = 8.6, 2.2 Hz, 1H), 8.04 (d, J = 8.6 Hz, 1H), 7.85-7.89 (m, 2H), 7.48 (tt, J = 9.3, 2.2 Hz, 1H), 3.55 (q, J = 7.3 Hz, 2H), 1.21 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 496.05 (MH)+. 60 3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.2 Hz, 1H), 8.83 (t, J = 2.6 Hz, 1H), 8.73 (d, J = 2.0 Hz, 1H), 8.48 (d, J = 5.4 Hz, 1H), 8.27-8.30 (m, 1H), 8.03-8.05 (m, 3H), 7.68-7.71 (m, 2H), 3.53 (q, J = 7.2 Hz, 2H), 1.20 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 493.95 (MH)+. 61 3-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (t, J = 2.1 Hz, 1H), 8.94 (t, J = 2.2 Hz, 1H), 8.74 (d, J = 2.0 Hz, 1H), 8.49 (d, J = 5.1 Hz, 1H), 8.38 (d, J = 4.9 Hz, 1H), 8.28-8.32 (m, 2H), 8.04 (d, J = 8.6 Hz, 1H), 7.94 (d, J = 8.1 Hz, 1H), 7.86 (t, J = 7.7 Hz, 1H), 3.47-3.64 (m, 2H), 1.22 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 528.00 (MH)+. 62 3-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.30 (t, J = 1.7 Hz, 1H), 8.84 (d, J = 0.9 Hz, 1H), 8.76 (s, 1H), 8.46 (s, 1H), 8.28 (dd, J = 8.6, 2.1 Hz, 1H), 8.10 (t, J = 7.9 Hz, 1H), 7.99-8.04 (m, 2H), 7.84 (d, J = 8.3 Hz, 1H), 3.40-3.53 (m, 2H), 1.18 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 546.05 (MH)+. 63 3-(5-(3-氯-4-(三氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.1 Hz, 1H), 8.92 (d, J = 2.4 Hz, 1H), 8.65-8.69 (m, 1H), 8.43 (t, J = 1.1 Hz, 1H), 8.38 (d, J = 2.1 Hz, 1H), 8.25 (td, J = 8.9, 2.1 Hz, 2H), 7.99 (d, J = 8.6 Hz, 1H), 7.94 (d, J = 8.6 Hz, 1H), 3.42-3.58 (m, 2H), 1.15-1.22 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 561.70 (MH)+. 64 3-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.22-9.26 (m, 1H), 8.79 (t, J = 1.1 Hz, 1H), 8.76 (s, 1H), 8.46 (d, J = 1.8 Hz, 1H), 8.28 (dd, J = 8.6, 2.1 Hz, 1H), 7.99-8.03 (m, 2H), 7.71 (dd, J = 10.9, 1.7 Hz, 1H), 7.50 (d, J = 8.9 Hz, 1H), 3.41-3.53 (m, 2H), 1.11-1.19(t, J = 7.4 Hz, 3H); ESI MS (m/z) 561.75 (MH)+. 65 3-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.1 Hz, 1H), 8.92 (d, J = 2.4 Hz, 1H), 8.71 (s, 1H), 8.46 (d, J = 1.8 Hz, 1H), 8.34-8.39 (m, 2H), 8.27 (dd, J = 8.9, 2.1 Hz, 1H), 8.02 (d, J = 8.6 Hz, 1H), 7.75-7.80 (m, 1H), 3.44-3.60 (m, 2H), 1.16-1.21( t, J = 7.5 Hz, 3H); ESI MS (m/z) 543.95 (MH)+. 66 3-(3-(乙基磺醯基)-5-(2-氟代-5-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.27 (t, J = 1.8 Hz, 1H), 8.81 (t, J = 1.1 Hz, 1H), 8.75 (s, 1H), 8.46-8.48 (m, 1H), 8.28 (dd, J = 8.6, 2.1 Hz, 1H), 7.99-8.03 (m, 2H), 7.61-7.65 (m, 2H), 3.40-3.56 (m, 2H), 1.11-1.20 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 561.70 (MH)+. 67 2-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.2 Hz, 1H), 8.86 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.61 (s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.35-8.40 (m, 2H), 8.29 (dd, J = 8.6, 1.7 Hz, 1H), 7.76-7.80 (m, 1H), 3.52 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 545.7 (MH)+. 68 2-(3-(乙基磺醯基)-5-(4-氟代-3-甲氧基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.07 (d, J = 2.4 Hz, 1H), 8.65 (d, J = 8.1 Hz, 1H), 8.60 (d, J = 2.3 Hz, 1H), 8.42 (s, 1H), 8.12 (s, 1H), 8.08 (d, J = 8.6 Hz, 1H), 7.29 (d, J = 3.2 Hz, 1H), 7.23-7.25 (m, 2H), 4.03 (s, 3H), 3.43 (q, J = 7.4 Hz, 2H), 1.37 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 507.7 (MH)+. 69 2-(5-(2,4-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.18 (q, J = 1.2 Hz, 1H), 8.75 (s, 1H), 8.68 (q, J = 1.1 Hz, 1H), 8.60 (s, 1H), 8.52 (d, J = 8.6 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.94 (td, J = 8.9, 6.4 Hz, 1H), 7.52-7.58 (m, 1H), 7.36 (td, J = 8.6, 2.1 Hz, 1H), 3.46 (q, J = 7.6 Hz, 2H), 1.15 (t, J = 7.6 Hz, 3H); ESI MS (m/z) 495.7 (MH)+. 70 2-(3-(乙基磺醯基)-5-(4-氟代-3-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.28 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.71 (d, J = 2.4 Hz, 1H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.93 (dd, J = 7.2, 2.0 Hz, 1H), 7.81-7.85 (m, 1H), 7.37 (t, J = 9.0 Hz, 1H), 3.48 (q, J = 7.3 Hz, 2H), 2.36 (d, J = 1.5 Hz, 3H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 491.7 (MH)+. 71 2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.1 Hz, 1H), 8.74 (d, J = 2.4 Hz, 2H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.99-8.02 (m, 2H), 7.67 (dd, J = 6.7, 2.1 Hz, 2H), 3.49 (q, J = 7.7 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 493.7 (MH)+. 72 2-(5-環丙基-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (d, J = 2.2 Hz, 1H), 8.71 (s, 1H), 8.58 (s, 1H), 8.50 (d, J = 8.3 Hz, 1H), 8.26 (dd, J = 8.4, 1.6 Hz, 1H), 8.17 (d, J = 2.2 Hz, 1H), 3.39 (q, J = 7.4 Hz, 2H), 2.24-2.31 (m, 1H), 1.17-1.22 (m, 2H), 1.13 (t, J = 7.5 Hz, 3H), 1.00-1.04 (m, 2H); ESI MS (m/z) 424.0 (MH)+. 73 2-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (s, 1H), 8.60-8.62 (m, 2H), 8.50 (dd, J = 8.3, 5.5 Hz, 2H), 8.23-8.28 (m, 3H), 7.36-7.42 (m, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.7 (MH)+. 74 2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.55 (d, J = 2.8 Hz, 1H), 9.09 (t, J = 1.4 Hz, 1H), 8.93 (d, J = 2.8 Hz, 1H), 8.76 (s, 1H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.6, 1.5 Hz, 1H), 7.24 (d, J = 2.8 Hz, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 517.7 (MH)+. 75 2-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.67 (d, J = 8.3 Hz, 1H), 8.61 (s, 1H), 8.54 (t, J = 8.7 Hz, 2H), 8.28-8.35 (m, 3H), 7.56-7.58 (m, 2H), 3.44 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.1 (MH)+. 76 3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.2 Hz, 1H), 8.83 (d, J = 2.2 Hz, 1H), 8.74 (s, 1H), 8.48 (d, J = 2.2 Hz, 1H), 8.28-8.31 (m, 1H), 8.09-8.11 (m, 2H), 8.05 (d, J = 8.4 Hz, 1H), 7.54 (d, J = 8.6 Hz, 2H), 7.04-6.72 (m, 1H), 3.53 (dd, J = 16.7, 7.5 Hz, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 576.05 (MH)+. 77 2-(6-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.61-8.70 (m, 2H), 8.53 (q, J = 4.2 Hz, 2H), 8.29 (dd, J = 8.4, 1.6 Hz, 1H), 8.23 (dd, J = 6.8, 2.0 Hz, 2H), 7.65 (dd, J = 6.8, 2.0 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 494.0 (MH)+. 78 2-(5-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.10 (d, J = 2.2 Hz, 1H), 8.78 (s, 1H), 8.65 (d, J = 2.2 Hz, 1H), 8.62 (s, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.29 (dd, J = 8.4, 1.6 Hz, 1H), 7.84 (dd, J = 8.8, 6.1 Hz, 1H), 7.76 (dd, J = 8.9, 2.6 Hz, 1H), 7.47-7.52 (m, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 511.9 (MH)+. 79 2-(3-(乙基磺醯基)-5-(3,4,5-三氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.1 Hz, 1H), 8.81 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.3, 1.5 Hz, 1H), 8.10 (dd, J = 9.3, 6.6 Hz, 2H), 3.50 (q, J = 7.6 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 513.7 (MH)+. 80 2-(3-(乙基磺醯基)-5-(4-氟代-2-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.03 (d, J = 2.2 Hz, 1H), 8.77 (s, 1H), 8.62 (s, 1H), 8.52-8.55 (m, 2H), 8.28-8.30 (m, 1H), 7.56 (dd, J = 8.4, 6.0 Hz, 1H), 7.33 (dd, J = 10.0, 2.4 Hz, 1H), 7.25 (td, J = 8.7, 2.8 Hz, 1H), 3.49 (q, J = 7.4 Hz, 2H), 2.36 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 491.8 (MH)+. 81 2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.62 (d, J = 8.6 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.12 (d, J = 8.3 Hz, 1H), 3.42 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 418.0 (MH)+. 82 2-(3-(乙基磺醯基)-6-(4-氟代-2-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.74 (s, 1H), 8.62 (d, J = 8.3 Hz, 1H), 8.58 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.26 (dd, J = 8.4, 1.7 Hz, 1H), 8.09 (d, J = 8.3 Hz, 1H), 7.62 (dd, J = 8.6, 6.1 Hz, 1H), 7.18-7.25 (m, 2H), 3.45 (q, J = 7.3 Hz, 2H), 2.40 (s, 3H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 491.7 (MH)+. 83 2-(6-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (s, 1H), 8.68 (d, J = 7.9 Hz, 1H), 8.59 (s, 1H), 8.50 (d, J = 8.6 Hz, 1H), 8.24-8.28 (m, 2H), 7.76 (dd, J = 8.9, 6.1 Hz, 1H), 7.68 (dd, J = 8.9, 2.4 Hz, 1H), 7.41 (td, J = 8.5, 2.5 Hz, 1H), 3.45 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 511.7 (MH)+. 84 2-(3-(乙基磺醯基)-6-(3,4,5-三氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (s, 1H), 8.69 (d, J = 8.3 Hz, 1H), 8.60 (t, J = 4.3 Hz, 2H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 8.17 (dd, J = 9.2, 6.7 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 513.7 (MH)+. 85 2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.19 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.52 (d, J = 0.9 Hz, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.6 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.55, 463.55 [(MH)+ Br79, 81]. 86 3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.44 (d, J = 2.4 Hz, 1H), 8.91 (d, J = 2.4 Hz, 1H), 8.68 (s, 1H), 8.42 (d, J = 8.3 Hz, 1H), 8.15 (t, J = 2.1 Hz, 3H), 7.96 (dd, J = 8.5, 1.6 Hz, 1H), 7.82 (t, J = 1.8 Hz, 1H), 3.53 (q, J = 7.2 Hz, 2H), 1.14-1.22 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 528.05, 530.05 [(MH)+ Cl35, 37]. 87 3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.2 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.15 (s, 1H), 8.02-8.06 (m, 2H), 7.96 (dd, J = 8.4, 1.6 Hz, 1H), 7.42-7.48 (m, 2H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.95 (MH)+. 88 3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.4 Hz, 1H), 8.71 (s, 1H), 8.45 (d, J = 8.3 Hz, 1H), 8.17 (s, 1H), 8.11-8.15 (m, 2H), 7.98 (dd, J = 8.3, 1.7 Hz, 1H), 7.63 (d, J = 7.8 Hz, 2H), 3.52 (q, J = 7.5 Hz, 2H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.10 (MH)+. 89 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.30 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.72 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.01-8.05 (m, 2H), 7.44 (t, J = 8.9 Hz, 2H), 3.50 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.7 (MH)+. 90 2-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.62 (d, J = 8.3 Hz, 1H), 8.54 (s, 1H), 8.50 (d, J = 8.6 Hz, 1H), 8.42 (dd, J = 8.4, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.23-8.27 (m, 2H), 7.36-7.42 (m, 2H), 3.42 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 477.9 (MH)+. 91 2-(6-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (s, 1H), 8.66 (d, J = 8.3 Hz, 1H), 8.54 (d, J = 8.6 Hz, 2H), 8.44 (dd, J = 8.3, 1.7 Hz, 1H), 8.36 (d, J = 8.3 Hz, 1H), 8.23 (dt, J = 9.1, 2.3 Hz, 2H), 7.63-7.68 (m, 2H), 3.44 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 493.9(MH)+. 92 3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.1 Hz, 1H), 8.88 (d, J = 2.4 Hz, 1H), 8.69 (s, 1H), 8.42 (d, J = 8.3 Hz, 1H), 8.16 (s, 1H), 7.96 (dd, J = 8.6, 1.5 Hz, 1H), 7.86 (dd, J = 8.7, 2.0 Hz, 2H), 7.44-7.49 (m, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 496.05 MH)+. 93 3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.41 (d, J = 2.1 Hz, 1H), 8.86 (d, J = 2.1 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.6 Hz, 1H), 8.16 (s, 1H), 8.06 (s, 1H), 8.03 (d, J = 7.9 Hz, 1H), 7.96 (dd, J = 8.3, 1.5 Hz, 1H), 7.75 (t, J = 8.1 Hz, 1H), 7.57 (d, J = 8.3 Hz, 1H), 3.44-3.61 (m, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 544.05 (MH)+. 94 4-(5-(乙基磺醯基)-6-(4-氧代-7-(三氟甲基)喹唑啉-3(4H)-基)吡啶-3-基)苯並腈 1H-NMR (400 MHz, DMSO-d6) δ 9.44 (d, J = 2.1 Hz, 1H), 8.89 (d, J = 2.1 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.20 (d, J = 8.3 Hz, 2H), 8.16 (s, 1H), 8.09 (d, J = 8.6 Hz, 2H), 7.95-7.97 (m, 1H), 3.44-3.60 (m, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 485.05 (MH)+. 95 3-(3-(乙基磺醯基)-5-(4-甲氧基苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.1 Hz, 1H), 8.72 (d, J = 2.1 Hz, 1H), 8.68 (s, 1H), 8.42 (d, J = 8.3 Hz, 1H), 8.15 (s, 1H), 7.92-7.97 (m, 3H), 7.15-7.17 (m, 2H), 3.85 (s, 3H), 3.41-3.57 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H; ESI MS (m/z) 494.00 (MH)+. 96 3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.37 (d, J = 2.1 Hz, 1H), 8.81 (d, J = 2.1 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 7.9 Hz, 1H), 8.15 (s, 1H), 8.02 (dt, J = 9.1, 2.4 Hz, 2H), 7.96 (dd, J = 8.4, 1.7 Hz, 1H), 7.68 (dt, J = 8.9, 2.3 Hz, 2H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H) 97 2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.76 (d, J = 2.2 Hz, 1H), 8.55 (s, 1H), 8.44 (dd, J = 8.4, 1.6 Hz, 1H), 8.36 (d, J = 8.3 Hz, 1H), 8.02 (dd, J = 6.6, 2.0 Hz, 2H), 7.69 (dd, J = 6.7, 2.1 Hz, 2H), 3.52 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 494.0(MH)+. 98 2-(3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.00 (dd, J = 4.7, 1.7 Hz, 1H), 8.75 (s, 1H), 8.59 (dd, J = 7.9, 1.5 Hz, 1H), 8.52 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.96 (dd, J = 7.9, 4.6 Hz, 1H), 3.38 (q, J = 7.3 Hz, 2H), 1.13 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 383.9 (MH)+. 99 2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.50 (d, J = 1.5 Hz, 1H), 8.93 (d, J = 2.4 Hz, 1H), 8.81 (s, 1H), 8.53 (s, 1H), 8.44 (dd, J = 8.3, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.54 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 452.0 (MH)+. 100 3-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.4 Hz, 1H), 8.88 (d, J = 2.1 Hz, 1H), 8.70 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.21 (d, J = 8.3 Hz, 2H), 8.16 (s, 1H), 7.96-7.99 (m, 3H), 3.45-3.58 (m, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 527.75 (MH)+. 101 3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36-9.38 (m, 1H), 8.80-8.82 (m, 1H), 8.68-8.71 (m, 1H), 8.42 (t, J = 8.3 Hz, 1H), 8.16 (s, 1H), 8.08 (dt, J = 9.4, 2.5 Hz, 2H), 7.96 (dd, J = 8.6, 1.5 Hz, 1H), 7.52 (d, J = 8.6 Hz, 2H), 6.7-7.0 (m, 1H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 576.15 (MH)+. 102 2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.75 (d, J = 2.1 Hz, 2H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 8.05-8.08 (m, 2H), 7.51 (d, J = 8.6 Hz, 2H), 6.74-7.00 (m, 1H), 3.49 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 575.7 (MH)+. 103 2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.75-8.78 (m, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.07 (dd, J = 6.7, 2.1 Hz, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.74-7.00 (m, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 576.05 (MH)+ 104 2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.76 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.10 (dt, J = 9.4, 2.5 Hz, 2H), 7.60 (d, J = 8.3 Hz, 2H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.0 (MH)+. 105 2-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.79 (s, 1H), 8.66 (d, J = 8.3 Hz, 1H), 8.54 (t, J = 4.1 Hz, 2H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.30-8.36 (m, 3H), 7.55 (d, J = 7.9 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ; ESI MS (m/z) 543.9 (MH)+. 106 3-(5-(4-溴苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.3 Hz, 1H), 8.82 (d, J = 2.2 Hz, 1H), 8.70 (s, 1H), 8.43-8.46 (m, 1H), 8.17 (d, J = 3.9 Hz, 1H), 7.96-7.99 (m, 3H), 7.82-7.84 (m, 2H), 3.46-3.57 (m, 2H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 538.00, 540.00 [(MH)+ Br79, 81]. 107 3-(3-(乙基磺醯基)-5-(3-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.2 Hz, 1H), 8.89 (d, J = 2.2 Hz, 1H), 8.71 (s, 1H), 8.44 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 11.5, 2.2 Hz, 1H), 8.17 (s, 1H), 7.98 (d, J = 8.6 Hz, 2H), 7.84 (t, J = 7.8 Hz, 1H), 3.47-3.59 (m, 2H), 1.21 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 562.05 (MH)+. 108 3-(3-(乙基磺醯基)-5-(4-(2,2,2-三氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 2.4 Hz, 1H), 8.70 (s, 1H), 8.44 (d, J = 8.3 Hz, 1H), 8.17 (s, 1H), 7.96-8.02 (m, 3H), 7.31 (dd, J = 6.8, 2.0 Hz, 2H), 4.91 (q, J = 8.9 Hz, 2H), 3.45-3.58 (m, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 558.10 (MH)+. 109 3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.24 (t, J = 2.2 Hz, 2H), 8.88 (d, J = 2.2 Hz, 1H), 8.69-8.73 (m, 2H), 3.39-3.54 (m, 2H), 1.05-1.22 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 462.80, 464.80 [(MH)+ Br79, 81]. 110 3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.37-9.38 (m, 1H), 9.24 (t, J = 2.0 Hz, 1H), 8.69-8.82 (m, 3H), 7.99-8.03 (m, 2H), 7.67-7.69 (m, 2H), 3.51 (ddd, J = 34.1, 14.1, 7.4 Hz, 2H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 495.0 (MH)+. 111 3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.2 Hz, 1H), 9.24 (d, J = 1.7 Hz, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.70 (d, J = 1.5 Hz, 1H), 8.03-8.07 (m, 2H), 7.44-7.48 (m, 2H), 3.41-3.60 (m, 2H), 1.19 (q, J = 7.7 Hz, 3H); ESI MS (m/z) 479.0 (MH)+. 112 3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 9.25 (d, J = 1.7 Hz, 1H), 8.86 (dd, J = 19.0, 2.3 Hz, 1H), 8.79 (s, 1H), 8.71 (t, J = 1.0 Hz, 1H), 8.07-8.10 (m, 2H), 7.53 (d, J = 8.6 Hz, 2H), 6.87 (tt, J = 51.9, 3.0 Hz, 1H), 3.43-3.61 (m, 2H), 1.21 (q, J = 7.7 Hz, 3H); ESI MS (m/z) 577.0 (MH)+. 113 3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.40-9.42 (m, 1H), 9.22-9.24 (m, 1H), 8.87 (d, J = 2.2 Hz, 1H), 8.76-8.77 (m, 1H), 8.65-8.71 (m, 1H), 7.99-8.10 (m, 2H), 7.68-7.77 (m, 1H), 7.54-7.58 (m, 1H), 3.44-3.62 (m, 2H), 1.21(q, J = 7.7 Hz, 3H); ESI MS (m/z) 545.05 (MH)+. 114 2-(3-(乙基磺醯基)-5-(4-(全氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.77 (t, J = 2.3 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.4, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.09-8.12 (m, 2H), 7.60 (d, J = 8.6 Hz, 2H), 3.50 (q, J = 7.2 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 594.10 (MH)+ 115 2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.2 Hz, 1H), 8.78 (s, 1H), 8.53 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.6 Hz, 1H), 7.84 (dd, J = 8.8, 2.2 Hz, 2H), 7.43-7.48 (m, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 495.90 (MH)+. 116 2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 0.5 Hz, 1H), 8.53 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.12 (d, J = 2.0 Hz, 2H), 7.79 (t, J = 1.8 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 527.85 (MH)+. 117 2-(3-(乙基磺醯基)-5-(4-(全氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.47 (dd, J = 8.3, 1.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.13 (dd, J = 6.7, 2.1 Hz, 2H), 7.60 (d, J = 8.9 Hz, 2H), 3.46-3.60 (m, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 610.05 (MH)+ 118 2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.4 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.47 (dd, J = 8.3, 1.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.09 (d, J = 8.6 Hz, 2H), 7.51 (d, J = 8.6 Hz, 2H), 6.73-6.99 (m, 1H), 3.46-3.60 (m, 2H), 1.15 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 591..90 (MH)+ 119 2-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.6 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34-8.36 (m, 2H), 8.27 (d, J = 7.8 Hz, 1H), 7.91 (d, J = 7.8 Hz, 1H), 7.83 (t, J = 7.7 Hz, 1H), 3.52 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 527.95 (MH)+. 120 2-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.6, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.05 (s, 1H), 8.01 (d, J = 7.8 Hz, 1H), 7.74 (t, J = 8.1 Hz, 1H), 7.56 (d, J = 8.3 Hz, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H). ESI MS (m/z) 544.00 (MH)+. 121 4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯並腈 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.19 (dd, J = 6.6, 2.0 Hz, 2H), 8.08 (dd, J = 6.6, 2.0 Hz, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.15-1.19 (m, 3H) ESI MS (m/z) 484.95 (MH)+. 122 2-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.2, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.20 (d, J = 8.1 Hz, 2H), 7.96 (d, J = 8.3 Hz, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16-1.19 (m, 3H) ESI MS (m/z) 527.95 (MH)+. 123 2-(5-(3,4-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮  1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.2 Hz, 1H), 8.77-8.78 (m, 2H), 8.54 (s, 1H), 8.43 (dd, J = 8.3, 2.0 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.19 (ddd, J = 11.7, 7.8, 2.2 Hz, 1H), 7.84-7.87 (m, 1H), 7.65-7.72 (m, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 495.75 (MH)+. 124 2-(5-環丙基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (d, J = 2.4 Hz, 1H), 8.72 (s, 1H), 8.51 (s, 1H), 8.40 (d, J = 9.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 8.16 (d, J = 2.4 Hz, 1H), 3.35-3.41 (m, 2H), 2.24-2.32 (m, 1H), 1.15-1.20 (m, 2H), 1.11 (t, J = 7.3 Hz, 3H), 0.99-1.02 (m, 2H) ESI MS (m/z) 423.95 (MH)+. 125 1-(4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯基)環丙烷-1-甲腈  1H-NMR (400 MHz, DMSO-d6) δ 9.29 (d, J = 2.4 Hz, 1H), 8.75 (s, 1H), 8.70 (d, J = 2.2 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.4, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 7.96 (dd, J = 6.6, 2.0 Hz, 2H), 7.52 (dd, J = 6.6, 2.0 Hz, 2H), 3.46 (t, J = 7.5 Hz, 2H), 1.82 (dd, J = 7.7, 4.8 Hz, 2H), 1.60 (dd, J = 8.2, 5.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 524.95 (MH)+. 126 2-(5-(4-(二氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.2 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.4, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.11 (d, J = 8.3 Hz, 2H), 7.79 (d, J = 8.1 Hz, 2H), 7.15 (t, J = 55.8 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 509.95 (MH)+. 127 2-(5-(乙基磺醯基)-6'-氟代-[3,3'-二吡啶]-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.84 (dd, J = 8.7, 2.6 Hz, 2H), 8.78 (d, J = 0.5 Hz, 1H), 8.60 (td, J = 8.2, 2.4 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.4, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.44 (dd, J = 8.6, 2.2 Hz, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 478.95 (MH)+. 128 2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (dd, J = 6.4, 2.1 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.81 (d, J = 2.1 Hz, 1H), 8.47 (dd, J = 8.3, 1.5 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.09-8.13 (m, 2H), 7.60 (d, J = 7.9 Hz, 2H), 3.44-3.61 (m, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 560 (MH)+ 129 2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.17 (s, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.41 (d, J = 8.9 Hz, 1H), 8.31 (d, J = 8.9 Hz, 1H), 3.44-3.52 (m, 2H), 2.64 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 475.55, 477.65 [(MH)+ Br79, 81] 130 2-(3-(乙基磺醯基)-5-(4-(甲硫基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.29-9.30 (m, 1H), 8.77 (s, 1H), 8.70 (d, J = 2.2 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.89-7.92 (m, 2H), 7.46 (dd, J = 6.7, 1.8 Hz, 2H), 3.49 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 505.75 (MH)+. 131 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.28 (d, J = 2.1 Hz, 1H), 8.70 (d, J = 2.4 Hz, 1H), 8.55 (s, 1H), 8.41 (dd, J = 8.6, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.02 (dd, J = 8.6, 5.5 Hz, 2H), 7.44 (t, J = 8.7 Hz, 2H), 3.47-3.52 (m, 2H), 2.66 (s, 3H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 492.10 (MH)+ 132 2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (dd, J = 7.0, 2.4 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.77-8.79 (m, 1H), 8.43-8.48 (m, 1H), 8.39 (d, J = 8.3 Hz, 1H), 7.99-8.03 (m, 2H), 7.66 (dd, J = 6.7, 1.8 Hz, 2H), 3.44-3.62 (m, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 509.80 (MH)+ 133 2-(5-(3,4-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.2 Hz, 1H), 8.81 (d, J = 2.1 Hz, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.42 (d, J = 6.8 Hz, 1H), 8.33-8.35 (m, 2H), 7.98 (dd, J = 8.3, 2.2 Hz, 1H), 7.86 (d, J = 8.6 Hz, 1H), 3.51 (d, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H)ESI MS (m/z) 527.90 (MH)+. 134 2-(5-(3-氯-5-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.2 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.55 (s, 1H), 8.44 (dd, J = 8.3, 1.5 Hz, 1H), 8.36 (d, J = 8.1 Hz, 1H), 8.03 (t, J = 1.6 Hz, 1H), 7.96 (dt, J = 9.6, 2.0 Hz, 1H), 7.65 (dt, J = 8.6, 2.0 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 511.85 (MH)+. 135 2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.2 Hz, 1H), 8.75 (d, J = 2.4 Hz, 1H), 8.58 (s, 1H), 8.33-8.45 (m, 2H), 8.08 (dd, J = 6.6, 2.2 Hz, 2H), 7.53 (d, J = 8.8 Hz, 2H), 6.75-7.01 (m, 1H), 3.52 (q, J = 7.5 Hz, 2H), 2.68 (s, 3H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 590.10 (MH)+ 136 2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.4 Hz, 1H), 8.74 (d, J = 2.4 Hz, 1H), 8.56 (s, 1H), 8.40-8.43 (m, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.09 (dd, J = 6.7, 2.1 Hz, 2H), 7.60 (d, J = 7.9 Hz, 2H), 3.50 (q, J = 7.5 Hz, 2H), 2.66 (s, 3H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 557.75 (MH)+ 137 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32-9.34 (m, 1H), 9.14 (s, 1H), 8.99 (s, 1H), 8.79 (d, J = 2.4 Hz, 1H), 8.48 (dd, J = 8.3, 1.7 Hz, 1H), 8.41 (d, J = 8.3 Hz, 1H), 8.05-8.09 (m, 2H), 7.43-7.48 (m, 2H), 3.46-3.63 (m, 3H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 493.90 (MH)+ 138 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)煙腈 1H-NMR (400 MHz, DMSO-d6) δ 9.47 (d, J = 2.2 Hz, 1H), 9.14 (d, J = 2.0 Hz, 1H), 8.80 (d, J = 0.7 Hz, 1H), 8.52 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.15 (t = 7.3 Hz, 3H); ESI MS (m/z) 408.70 (MH)+ 139 2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.4 Hz, 1H), 8.58 (s, 1H), 8.43 (dd, J = 8.7, 1.8 Hz, 1H), 8.34 (d, J = 8.6 Hz, 1H), 8.13 (d, J = 1.7 Hz, 2H), 7.81 (t, J = 1.8 Hz, 1H), 3.54 (q, J = 7.1 Hz, 2H), 2.68 (s, 3H), 1.19 (t = 7.3 Hz, 3H); ); ESI MS (m/z) 541.75, 543.75 [(MH)+ Cl35 140 2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (t, J = 2.1 Hz, 1H), 8.74 (t, J = 2.1 Hz, 1H), 8.57 (s, 1H), 8.33-8.45 (m, 2H), 8.00-8.02 (m, 2H), 7.62-7.69 (m, 2H), 3.54 (q, J = 7.1 Hz, 2H), 2.68 (s, 3H), 1.19 (t = 7.3 Hz, 3H); ESI MS (m/z) 507.70 (MH)+ 141 2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.2 Hz, 1H), 8.81 (d, J = 2.2 Hz, 1H), 8.59 (d, J = 9.0 Hz, 1H), 8.33-8.45 (m, 2H), 7.82-7.87 (m, 2H), 7.46 (tt, J = 9.3, 2.3 Hz, 1H), 3.51-3.58 (m, 2H), 2.68 (s, 3H), 1.19 (q, J = 7.3 Hz, 3H); ESI MS (m/z) 510.10 (MH)+ 142 2-(5-(4-氯-3-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.6 Hz, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.16 (dd, J = 10.6, 2.1 Hz, 1H), 7.87 (dd, J = 8.6, 2.0 Hz, 1H), 7.82 (t, J = 7.9 Hz, 1H), 3.50 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 511.65 (MH)+. 143 2-(5-(2-氯-5-(三氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.15 (d, J = 2.2 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.73 (d, J = 2.2 Hz, 1H), 8.55 (d, J = 1.0 Hz, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.19 (t, J = 1.0 Hz, 1H), 7.92-7.97 (m, 2H), 3.47 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 561.90 (MH)+. 144 3-氯-5-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯並腈 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (d, J = 2.2 Hz, 1H), 8.91 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.54 (t, J = 1.6 Hz, 2H), 8.49 (t, J = 1.8 Hz, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.21 (dd, J = 1.8, 1.3 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.2 Hz, 3H) ESI MS (m/z) 518.70 (MH)+. 145 2-(3-(乙基磺醯基)-5-(2-氟代-5-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.22 (t, J = 1.8 Hz, 1H), 8.79 (s, 1H), 8.75 (q, J = 1.1 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.2, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.00-8.02 (m, 1H), 7.62-7.64 (m, 2H), 3.48 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 561.75(MH)+. 146 2-(5-(4-氯-2-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.19 (q, J = 1.3 Hz, 1H), 8.79 (s, 1H), 8.71 (q, J = 1.1 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.4, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.92 (t, J = 8.4 Hz, 1H), 7.73 (dd, J = 10.6, 2.1 Hz, 1H), 7.55 (dd, J = 8.3, 2.4 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 511.90 (MH)+. 147 2-(5-(4-溴苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.74 (d, J = 2.2 Hz, 1H), 8.54 (s, 1H), 8.41-8.43 (m, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.92-7.94 (m, 2H), 7.80 (dd, J = 6.7, 2.1 Hz, 2H), 3.50 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 539.90(MH)+. 148 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙酸乙酯 1H-NMR (400 MHz, DMSO-d6) δ 8.73 (s, 1H), 8.59 (d, J = 2.8 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 2.8 Hz, 1H), 4.22 (q, J = 7.0 Hz, 2H), 3.39 (q, J = 7.3 Hz, 2H), 1.67 (d, J = 14.7 Hz, 6H), 1.20 (t, J = 7.2 Hz, 3H), 1.11 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 514.05 (MH)+. 149 2-(4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯氧基)-2,2-二氟-N,N-二甲基乙醯胺 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.1 Hz, 1H), 8.78 (s, 1H), 8.74 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.05 (dt, J = 9.4, 2.5 Hz, 2H), 7.51 (d, J = 8.6 Hz, 2H), 3.46-3.52 (m, 2H), 3.26 (d, J = 8.3 Hz, 3H), 2.98 (s, 3H), 1.13-1.18 (m, 4H) ESI MS (m/z) 597.05 (MH)+. 150 2-(3-(乙基磺醯基)-5-(3,3,3-三氟丙基-1-烯-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.14 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.53-8.55 (m, 2H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.62 (t, J = 1.5 Hz, 1H), 6.50 (d, J = 1.2 Hz, 1H), 3.44-3.53 (m, 2H), 1.10-1.19 (m, 3H) ESI MS (m/z) 477.95 (MH)+. 151 2-(3-(乙基磺醯基)-5-(4-(2,2,3,3,3-五氟丙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.29 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.70 (d, J = 2.4 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.97 (dd, J = 6.9, 2.0 Hz, 2H), 7.29 (d, J = 8.9 Hz, 2H), 4.97 (t, J = 13.3 Hz, 2H), 3.49 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 608.00 (MH)+. 152 2-(5-(2,2-二氟苯並[d][1,3]二氧雜環戊烯-5-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.6, 2.0 Hz, 1H), 8.35 (d, J = 8.6 Hz, 1H), 7.79 (dd, J = 8.1, 1.0 Hz, 1H), 7.59 (dd, J = 8.1, 1.0 Hz, 1H), 7.44 (t, J = 8.1 Hz, 1H), 3.46-3.51 (m, 3H), 1.22 (s, 0H), 1.17 (t, J = 7.5 Hz, 4H) ESI MS (m/z) 539.80 (MH)+. 153 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)乙腈 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 3.1 Hz, 1H), 8.74 (s, 1H), 8.51 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.21 (d, J = 2.8 Hz, 1H), 5.52 (s, 2H), 3.36-3.44 (m, 2H), 1.11 (dt, J = 23.8, 7.2 Hz, 3H) ESI MS (m/z) 438.70 (MH)+. 154 2-(3-(乙基磺醯基)-5-(1,1,2,3,3,3-六氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.09 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.52 (s, 1H), 8.50 (d, J = 2.8 Hz, 1H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.63 (dq, J = 41.3, 6.1 Hz, 1H), 3.46-3.53 (m, 2H), 1.15 (q, J = 7.3 Hz, 3H) ESI MS (m/z) 549.75 (MH)+. 155 2-(3-(乙基磺醯基)-5-(4-羥基苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.94 (s, 1H), 9.22 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.61 (d, J = 2.4 Hz, 1H), 8.53 (s, 1H), 8.41 (dd, J = 8.4, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.79 (d, J = 8.6 Hz, 2H), 6.95-6.97 (m, 2H), 3.47 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 475.75 (MH)+. 156 2-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 11.36 (s, 1H), 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 2.8 Hz, 1H), 3.37 (q, J = 6.8 Hz, 2H), 1.06-1.13 (m, 4H) ESI MS (m/z) 399.95 (MH)+. 157 2-(5-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.09 (d, J = 2.1 Hz, 1H), 8.79 (s, 1H), 8.63 (d, J = 2.4 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.4, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.82 (dd, J = 8.6, 6.1 Hz, 1H), 7.74 (dd, J = 8.9, 2.8 Hz, 1H), 7.47 (td, J = 8.5, 2.5 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 511.95 (MH)+. 158 2-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.31-9.35 (m, 1H), 8.78 (d, J = 2.0 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.96 (d, J = 7.8 Hz, 1H), 7.90 (d, J = 2.0 Hz, 1H), 7.71 (t, J = 7.9 Hz, 1H), 7.48 (d, J = 8.3 Hz, 1H), 6.86 (tt, J = 51.8, 3.0 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 576.05 (MH)+. 159 5'-(乙基磺醯基)-6'-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-[2,3'-二吡啶]-5-甲腈 1H-NMR (400 MHz, DMSO-d6) δ 9.71 (d, J = 2.2 Hz, 1H), 9.26 (q, J = 1.0 Hz, 1H), 9.19 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 8.6 Hz, 1H), 8.57-8.60 (m, 2H), 8.53 (d, J = 8.8 Hz, 1H), 8.42-8.45 (m, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.44-3.52 (m, 2H), 1.11-1.18 (m, 3H) ESI MS (m/z) 486.05 (MH)+. 160 2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)嘧啶-5-甲腈 1H-NMR (400 MHz, DMSO-d6) δ 9.85 (d, J = 2.2 Hz, 1H), 9.55 (d, J = 5.4 Hz, 2H), 9.33 (d, J = 2.2 Hz, 1H), 8.81 (s, 1H), 8.54 (s, 1H), 8.44 (dd, J = 8.4, 1.8 Hz, 1H), 8.36 (d, J = 8.3 Hz, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 487.00 (MH)+. 161 2-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 3.1 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.2, 1.9 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.20 (d, J = 3.1 Hz, 1H), 5.16 (q, J = 8.8 Hz, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 481.95 (MH)+ 162 2-(3-(乙基磺醯基)-5-(2,2,3,3,3-五氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (d, J = 3.1 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.39-8.42 (m, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.22 (d, J = 3.1 Hz, 1H), 5.26 (t, J = 13.8 Hz, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 531.95 (MH)+ 163 2-(3-(乙基磺醯基)-5-(3-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 2.2 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.6, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.91 (dt, J = 10.2, 2.1 Hz, 1H), 7.82 (dq, J = 7.8, 0.8 Hz, 1H), 7.64 (td, J = 8.0, 6.2 Hz, 1H), 7.37-7.42 (m, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 478.05 (MH)+. 164 2-(3-(乙基磺醯基)-5-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.25 (d, J = 2.2 Hz, 1H), 8.78 (d, J = 2.4 Hz, 2H), 8.54 (s, 1H), 8.43 (dd, J = 8.2, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.36 (s, 1H), 4.08 (s, 3H), 3.48 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 532.00 (MH)+. 165 2-(3-(乙基磺醯基)-5-(嘧啶-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.2 Hz, 1H), 9.40 (s, 2H), 9.33 (s, 1H), 8.95 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.2, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.50 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 462.00 (MH)+. 166 2-(3-(乙基磺醯基)-5-甲基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 1.5 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.39-8.41 (m, 2H), 8.32 (d, J = 8.6 Hz, 1H), 3.36 (q, J = 7.3 Hz, 2H), 2.53 (s, 3H), 1.06-1.13 (t, 3H) ESI MS (m/z) 397.95 (MH)+. 167 2-(3-(乙基磺醯基)-5-((甲硫基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.72 (d, J = 2.8 Hz, 2H), 8.51 (s, 1H), 8.40 (d, J = 8.3 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.12 (d, J = 2.8 Hz, 1H), 5.62 (s, 2H), 3.34-3.42 (m, 2H), 2.23-2.27 (m, 3H), 1.13 (t, J = 7.3 Hz, 3H), 1.06 (s, 0H) ESI MS (m/z) 460.00 (MH)+. 168 2-(5-(環丙基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.71 (s, 1H), 8.66 (d, J = 2.8 Hz, 1H), 8.50 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.97 (d, J = 3.1 Hz, 1H), 4.14 (d, J = 7.0 Hz, 2H), 3.35-3.42 (m, 2H), 1.26-1.33 (m, 1H), 1.12 (t, J = 7.5 Hz, 3H), 0.61-0.65 (m, 2H), 0.41 (td, J = 5.3, 3.9 Hz, 2H) ESI MS (m/z) 454.00 (MH)+. 169 3-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.66 (d, J = 2.1 Hz, 1H), 8.58 (d, J = 8.3 Hz, 2H), 8.54 (dd, J = 8.6, 1.8 Hz, 1H), 8.41 (d, J = 2.1 Hz, 1H), 3.10 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 432.85 (MH)+. 170 3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.28 (d, J = 2.4 Hz, 1H), 8.94 (d, J = 2.2 Hz, 1H), 8.60 (d, J = 8.1 Hz, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.4 Hz, 3H) ESI MS (m/z) 464.85 (MH)+. 171 2-(5-((二甲基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.44 (d, J = 2.7 Hz, 1H), 8.39 (dd, J = 8.4, 1.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.88 (d, J = 2.7 Hz, 1H), 3.41-3.46 (m, 6H), 3.36 (q, J = 7.2 Hz, 2H), 1.12 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 474.95 (MH)+. 172 2-(3-(乙基磺醯基)-5-((甲基磺醯基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.86 (d, J = 2.9 Hz, 1H), 8.73 (d, J = 0.5 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 2.9 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 5.71 (s, 2H), 3.40 (q, J = 7.3 Hz, 2H), 3.17 (s, 3H), 1.11-1.16 (t, 3H) ESI MS (m/z) 491.70 (MH)+. 173 2-(4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.09 (d, J = 19.6 Hz, 1H), 8.89 (d, J = 0.6 Hz, 1H), 8.58-8.71 (m, 3H), 8.48 (dd, J = 8.3, 1.5 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.05 (d, J = 7.8 Hz, 1H), 7.92 (t, J = 7.8 Hz, 1H), 3.75 (q, J = 7.2 Hz, 2H), 1.22 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.85 (MH)+ 174 2-(3-(乙基磺醯基)-5-(氧雜環丁烷-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.68-9.02 (m, 1H), 8.59-8.62 (m, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.87-7.98 (m, 1H), 5.64-5.69 (m, 1H), 4.90-5.04 (m, 2H), 4.68 (dd, J = 7.8, 4.4 Hz, 2H), 3.42 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 456.05 (MH)+ 175 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙醯胺 1H-NMR (400 MHz, DMSO-d6) δ 10.60 (s, 1H), 9.27 (d, J = 2.7 Hz, 1H), 9.02 (d, J = 2.4 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.4, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 5.91 (s, 1H), 3.35 (q, J = 7.4 Hz, 2H), 1.40 (s, 6H), 1.13 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 485.05 (MH)+. 176 2-(3-(乙基磺醯基)-6-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.79 (d, J = 0.5 Hz, 1H), 8.61-8.66 (m, 1H), 8.51-8.54 (m, 2H), 8.43 (dd, J = 8.4, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.29 (dt, J = 9.5, 2.5 Hz, 2H), 7.47 (d, J = 8.8 Hz, 2H), 6.84 (tt, J = 51.8, 2.9 Hz, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 576.00 (MH)+. 177 2-(5-((二乙基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.7 Hz, 1H), 8.39 (dd, J = 8.3, 1.7 Hz, 1H), 8.30 (d, J = 8.3 Hz, 1H), 7.92 (d, J = 2.7 Hz, 1H), 3.51 (q, J = 7.4 Hz, 4H), 3.35 (t, J = 7.3 Hz, 2H), 1.32 (t, J = 7.3 Hz, 6H), 1.11 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 502.80 (MH)+. 178 2-(5'-(乙基磺醯基)-4-(三氟甲基)-[2,3'-二吡啶]-6'-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.75 (d, J = 2.4 Hz, 1H), 9.24 (d, J = 2.2 Hz, 1H), 9.09 (d, J = 5.1 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.76 (s, 1H), 8.56 (d, J = 10.0 Hz, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.95 (dd, J = 5.0, 0.9 Hz, 1H), 3.49 (q, J = 7.3 Hz, 2H), 1.14-1.19 (m, 3H) ESI MS (m/z) 528.80 (MH)+. 179 2-(5'-(乙基磺醯基)-5-(三氟甲基)-[2,3'-二吡啶]-6'-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.72 (d, J = 2.2 Hz, 1H), 9.20-9.22 (m, 2H), 8.80 (s, 1H), 8.59 (d, J = 8.3 Hz, 1H), 8.54 (s, 1H), 8.50 (dd, J = 8.6, 2.2 Hz, 1H), 8.43 (dd, J = 8.4, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.49 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 528.95 (MH)+. 180 2-(5-(3-(苄氧基)環丁氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.73 (s, 1H), 8.61 (dd, J = 7.1, 2.9 Hz, 1H), 8.52 (s, 1H), 8.40-8.43 (m, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.88 (dd, J = 12.5, 2.9 Hz, 1H), 7.31-7.38 (m, 5H), 4.85-5.24 (m, 1H), 4.46 (s, 2H), 3.85-4.35(m, 1H), 3.4 (m, 2H), 2.9 ( m, 1H), 2.45 -2.65(m, 2H) 2.06 (m, 1H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 560.10 (MH)+ 181 2-(5-(3-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.77-8.79 (m, 2H), 8.53 (d, J = 1.0 Hz, 1H), 8.42 (dd, J = 8.4, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.30 (dd, J = 7.0, 2.3 Hz, 1H), 8.01 (qd, J = 4.4, 2.4 Hz, 1H), 7.65 (t, J = 8.9 Hz, 1H), 3.50 (q, J = 7.4 Hz, 2H), 1.15-1.19 (t, 3H) ESI MS (m/z) 512.05 (MH)+. 182 3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.2 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.7, 1.8 Hz, 1H), 8.05-8.10 (m, 2H), 7.43-7.49 (m, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 478.95 (MH)+. 183 2-(3-(乙基磺醯基)-5-(2-甲氧基嘧啶-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 9.20 (s, 2H), 8.86 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 0.7 Hz, 1H), 8.53 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 4.01 (s, 3H), 3.48 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 492.05 (MH)+. 184 2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)乙腈 1H-NMR (400 MHz, DMSO-d6) δ 8.98 (d, J = 2.2 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.58 (d, J = 2.2 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 4.38 (s, 2H), 3.36-3.43 (m, 2H), 1.13 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 423 (MH)+. 185 2-(5-溴-3-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (d, J = 0.5 Hz, 1H), 8.55 (d, J = 2.0 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.2, 1.6 Hz, 1H), 8.29-8.32 (m, 2H), 3.06 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 429.85 (MH)+. 186 3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.2 Hz, 1H), 8.88 (d, J = 2.4 Hz, 1H), 8.60-8.63 (m, 2H), 8.55-8.57 (m, 1H), 8.14 (d, J = 8.8 Hz, 2H), 7.62 (d, J = 8.1 Hz, 2H), 3.51 (q, J = 7.5 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 545.00 (MH)+. 187 3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.2 Hz, 1H), 8.88 (d, J = 2.2 Hz, 1H), 8.61 (dd, J = 5.1, 3.4 Hz, 2H), 8.56 (dd, J = 8.7, 1.8 Hz, 1H), 8.11 (dt, J = 9.3, 2.6 Hz, 2H), 7.52 (d, J = 8.8 Hz, 2H), 6.73-7.00 (m, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H);ESI MS (m/z) 577.00 (MH)+ 188 3-(3-(乙硫基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (d, J = 2.2 Hz, 1H), 8.58-8.61 (m, 2H), 8.55 (dd, J = 8.7, 2.1 Hz, 1H), 8.32 (d, J = 2.2 Hz, 1H), 7.96-7.99 (m, 2H), 7.39-7.43 (m, 2H), 3.15 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 447.00 (MH)+ 189 3-(5-(4-氯苯基)-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 2.2 Hz, 1H), 8.60 (d, J = 10.8 Hz, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 8.34 (d, J = 2.2 Hz, 1H), 7.95 (dd, J = 6.6, 2.0 Hz, 2H), 7.64 (dd, J = 6.6, 2.2 Hz, 2H), 3.16 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 463.00 (MH)+ 190 2-(5-(2-溴-1,1,2,2-四氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.17 (d, J = 2.7 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.59 (d, J = 2.7 Hz, 1H), 8.52 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 579.90 (MH)+. 191 3-(3-(乙硫基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.82 (d, J = 2.2 Hz, 1H), 8.59-8.62 (m, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 8.36 (d, J = 2.2 Hz, 1H), 8.03-8.06 (m, 2H), 7.56-7.58 (m, 2H), 3.16 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 513.00 (MH)+ 192 3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.41 (d, J = 2.1 Hz, 1H), 8.87 (d, J = 2.1 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.6, 1.8 Hz, 1H), 8.05 (dd, J = 6.6, 2.0 Hz, 2H), 7.68 (dd, J = 6.7, 2.1 Hz, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 494.94 (MH)+ 193 3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (d, J = 2.4 Hz, 1H), 8.96 (d, J = 2.4 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.6, 1.8 Hz, 1H), 8.16 (d, J = 1.8 Hz, 2H), 7.82 (t, J = 1.8 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 528.85 (MH)+ 194 3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (d, J = 2.2 Hz, 1H), 8.94 (d, J = 2.2 Hz, 1H), 8.61 (dd, J = 5.3, 3.3 Hz, 2H), 8.56 (dd, J = 8.8, 1.7 Hz, 1H), 7.85-7.90 (m, 2H), 7.47 (tt, J = 9.3, 2.3 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H);ESI MS (m/z) 496.90 (MH)+ 195 3-(5-(3-氯-5-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (d, J = 2.2 Hz, 1H), 8.95 (d, J = 2.2 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.6, 1.7 Hz, 1H), 8.05 (d, J = 1.7 Hz, 1H), 7.99 (dt, J = 9.5, 1.8 Hz, 1H), 7.65 (dt, J = 8.6, 2.1 Hz, 1H), 3.53 (q, J = 7.2 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 512.90 (MH)+ 196 3-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.48 (d, J = 2.2 Hz, 1H), 8.98 (d, J = 2.4 Hz, 1H), 8.61-8.63 (m, 2H), 8.56 (dd, J = 8.6, 2.0 Hz, 1H), 8.39 (s, 1H), 8.31 (d, J = 7.8 Hz, 1H), 7.93 (d, J = 7.8 Hz, 1H), 7.85 (t, J = 7.8 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 528.95 (MH)+ 197 2-(5-((4,4-二氟but-3-烯-1-基)氧)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.71 (s, 1H), 8.67 (d, J = 2.9 Hz, 1H), 8.50 (s, 1H), 8.40 (dd, J = 8.4, 1.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 8.00 (d, J = 2.9 Hz, 1H), 4.67 (dtd, J = 26.8, 7.8, 2.5 Hz, 1H), 4.32 (t, J = 6.2 Hz, 2H), 3.40 (q, J = 7.4 Hz, 2H), 2.52 (s, 1H), 2.45 (s, 1H), 1.12 (t, J = 7.5 Hz, 3H), ESI MS (m/z) 490 (MH)+ 198 2-(3-(乙硫基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (s, 1H), 8.71 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.3, 1.5 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.25 (d, J = 2.1 Hz, 1H), 7.96-7.99 (m, 2H), 7.46 (d, J = 8.6 Hz, 2H), 6.72-6.99 (m, 1H), 3.12 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 544.05 (MH)+ 199 2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.20 (d, J = 2.1 Hz, 1H), 8.78 (s, 1H), 8.67 (d, J = 2.1 Hz, 1H), 8.54 (d, J = 0.9 Hz, 1H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.61 (d, J = 1.8 Hz, 1H), 6.83 (d, J = 1.8 Hz, 1H), 4.01 (s, 3H), 3.49 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 464.05 (MH)+ 200 2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.21 (d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 8.63 (d, J = 2.2 Hz, 1H), 8.56 (s, 1H), 8.52 (s, 1H), 8.41 (d, J = 8.3 Hz, 1H), 8.33 (d, J = 8.1 Hz, 1H), 8.22 (s, 1H), 3.92 (s, 3H), 3.43 (q, J = 7.6 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 464.00 (MH)+ 201 2-(3-(乙基磺醯基)-5-(3-氟代-5-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.41 (d, J = 2.2 Hz, 1H), 8.90 (d, J = 2.2 Hz, 1H), 8.78 (s, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.25-8.28 (m, 2H), 7.88 (d, J = 8.6 Hz, 1H), 3.52 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 546.00 (MH)+ 202 1-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈 1H-NMR (400 MHz, DMSO-d6) δ 8.93 (d, J = 2.4 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.51 (s, 1H), 8.40-8.42 (m, 2H), 8.33 (d, J = 8.3 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.95-1.99 (m, 2H), 1.88-1.93 (m, 2H), 1.12-1.16 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 449.05(MH)+ 203 2-(3-(乙基磺醯基)-5-(4-(甲基磺醯基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.1 Hz, 1H), 8.79 (s, 1H), 8.54 (d, J = 0.9 Hz, 1H), 8.43 (dd, J = 8.4, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.23-8.26 (m, 2H), 8.11-8.14 (m, 2H), 3.46-3.54 (m, 2H), 3.35 (s, 3H), 1.18 (t, J = 7.5 Hz, 3H);ESI MS (m/z) 537.95(MH)+ 204 2-(3-(乙硫基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (s, 1H), 8.67-8.69 (m, 1H), 8.54 (d, J = 1.2 Hz, 1H), 8.41 (dd, J = 8.4, 1.8 Hz, 1H), 8.31-8.33 (m, 1H), 8.21 (d, J = 2.2 Hz, 1H), 7.91-7.98 (m, 2H), 7.36-7.42 (m, 2H), 3.11 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 446.05 (MH)+ 205 (5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基) 乙基膦酸乙酯 1H-NMR (400 MHz, DMSO-d6) δ 8.91 (q, J = 1.3 Hz, 1H), 8.76 (s, 1H), 8.52 (s, 1H), 8.40-8.43 (m, 2H), 8.33 (d, J = 8.3 Hz, 1H), 4.18-4.28 (m, 2H), 3.43 (q, J = 7.3 Hz, 2H), 2.08-2.18 (m, 2H), 1.29 (t, J = 7.1 Hz, 3H), 1.12-1.22 (m, 6H) ESI MS (m/z) 520 (MH)+ 206 2-(5-(二甲基磷醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (dd, J = 5.4, 2.0 Hz, 1H), 8.83 (dd, J = 10.0, 2.0 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.53 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.90 (s, 3H), 1.87 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 460 (MH)+ 207 2-(3-(乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.23 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.69 (d, J = 2.1 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 8.01-8.04 (m, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.86 (tt, J = 52.0, 2.9 Hz, 1H), 4.61 (d, J = 38.8 Hz, 1H), 3.27 (q, J = 6.7 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 575.10 (MH)+ 208 2-(3-(乙基磺醯基)-5-((S-甲基磺醯亞胺基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.85 (dd, J = 7.1, 2.9 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.30-8.33 (m, 2H), 5.54 (d, J = 12.2 Hz, 1H), 5.45 (d, J = 12.0 Hz, 1H), 4.09 (s, 1H), 3.36-3.42 (q, J = 7.2 Hz, 2H), 3.02 (s, 3H), 1.08-1.18 (t, J = 7.3 HZ, 3H) ESI MS (m/z) 490.90 (MH)+ 209 2-(3-(乙基磺醯亞胺基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.20 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.66 (d, J = 2.4 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.95-8.00 (m, 2H), 7.41-7.47 (m, 2H), 4.60 (d, J = 41.9 Hz, 1H), 3.28 (q, J = 7.3 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 477.10 (MH)+ 210 2-(3-(乙基磺醯基)-5-(1,1,2,2-四氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.10 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.6 Hz, 1H), 8.53 (d, J = 2.4 Hz, 2H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.98 (tt, J = 51.6, 3.0 Hz, 1H), 3.49 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 500.00 (MH)+ 211 2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 2H), 8.55 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.35 (d, J = 8.1 Hz, 1H), 6.94 (s, 1H), 3.50 (q, J = 7.4 Hz, 2H), 2.55 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 532.00 (MH)+ 212 3-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 11.63 (s, 1H), 8.56-8.59 (m, 2H), 8.52-8.54 (m, 2H), 7.89 (d, J = 2.8 Hz, 1H), 3.34 (q, J = 7.3 Hz, 2H), 1.11 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 401.00 (MH)+ 213 3-(3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.58 (d, J = 8.9 Hz, 2H), 8.53 (td, J = 4.6, 1.5 Hz, 2H), 8.19 (dd, J = 8.1, 1.4 Hz, 1H), 7.70 (dd, J = 8.1, 4.7 Hz, 1H), 3.02 (q, J = 7.2 Hz, 2H), 1.15 (t, J = 7.1 Hz, 3H);ESI MS (m/z) 352.95 (MH)+ 214 3-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.10 (dd, J = 4.9, 1.7 Hz, 1H), 8.71 (dd, J = 8.1, 1.7 Hz, 1H), 8.59-8.61 (m, 2H), 8.54-8.56 (m, 1H), 8.07 (dd, J = 7.9, 4.8 Hz, 1H), 3.38 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.4 Hz, 3H);ESI MS (m/z) 384.95 (MH)+ 215 3-(5-((二乙基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.57 (dd, J = 5.3, 3.3 Hz, 2H), 8.51-8.54 (m, 2H), 7.98 (d, J = 2.7 Hz, 1H), 3.55 (q, J = 7.3 Hz, 4H), 3.34 (q, J = 7.3 Hz, 2H), 1.32-1.37 (m, 6H), 1.12 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 504.00 (MH)+ 216 2-(3-(乙基磺醯基)-5-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.87 (d, J = 2.1 Hz, 1H), 8.74 (s, 1H), 8.51 (d, J = 0.9 Hz, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.32 (q, J = 2.8 Hz, 2H), 3.42 (q, J = 7.4 Hz, 2H), 3.27 (q, J = 7.3 Hz, 2H), 1.33 (t, J = 7.3 Hz, 3H), 1.13 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 443.95 (MH)+ 217 2-(5-(4-氟苯基)-3-(N-甲基乙基磺醯亞胺基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.22 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.53 (s, 2H), 8.41 (d, J = 8.3 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.99 (dd, J = 8.8, 5.4 Hz, 2H), 7.44 (t, J = 8.8 Hz, 2H), 3.35-3.44 (m, 2H), 2.43 (s, 3H), 1.09-1.14 (m, 3H) ESI MS (m/z) 491.10 (MH)+ 218 (5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氨基甲酸叔丁酯 1H-NMR (400 MHz, DMSO-d6) δ 10.30 (s, 1H), 8.87 (d, J = 2.4 Hz, 1H), 8.72 (d, J = 0.5 Hz, 1H), 8.68 (d, J = 2.4 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 3.35 (q, J = 7.3 Hz, 2H), 1.52 (s, 9H), 1.12 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 499.00 (MH)+ 219 2-(5-((乙基(甲基)((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.7 Hz, 1H), 8.38-8.40 (m, 1H), 8.31 (d, J = 8.6 Hz, 1H), 7.90 (d, J = 2.7 Hz, 1H), 3.52-3.58 (m, 2H), 3.34-3.38 (m, 5H), 1.36 (t, J = 7.3 Hz, 3H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 488.95 (MH)+ 220 3-(5-((乙基(異丙基)((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.53-8.60 (m, 4H), 8.03 (d, J = 2.7 Hz, 1H), 3.74-3.81 (m, 1H), 3.55 (dd, J = 15.5, 7.2 Hz, 2H), 3.33-3.35 (m, 2H), 1.44 (d, J = 6.6 Hz, 3H), 1.39 (d, J = 6.6 Hz, 3H), 1.35 (t, J = 7.3 Hz, 3H), 1.12 (t, J = 7.2 hz, 3H); ESI MS (m/z) 518.05 (MH)+ 221 5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基 氨基磺酸二甲酯 1H-NMR (400 MHz, DMSO-d6) δ 9.16 (d, J = 2.7 Hz, 1H), 8.67-8.72 (m, 1H), 8.61 (d, J = 8.8 Hz, 2H), 8.56 (dd, J = 8.4, 2.1 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 3.06 (s, 6H), 1.14 (t, J = 7.3 Hz, 3H);ESI MS (m/z) 507.95 (MH)+ 222 2-((5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基)氧)乙腈 1H-NMR (400 MHz, DMSO-d6) δ 8.90 (d, J = 2.9 Hz, 1H), 8.58-8.60 (m, 2H), 8.54 (dd, J = 8.6, 2.0 Hz, 1H), 8.33 (d, J = 2.9 Hz, 1H), 5.54 (s, 2H), 3.42 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H)ESI MS (m/z) 439.95 (MH)+ 223 3-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.90 (d, J = 2.8 Hz, 1H), 8.58-8.60 (m, 2H), 8.54 (dd, J = 8.7, 2.0 Hz, 1H), 8.33 (d, J = 2.8 Hz, 1H), 5.19 (q, J = 8.7 Hz, 2H), 3.43 ( q, J = 7.3 Hz, 2H), 1.13 ( t, J = 7.3 Hz, 3H) ESI MS (m/z) 482.95 (MH)+ 224 3-(5-(環丙基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (d, J = 2.9 Hz, 1H), 8.57-8.59 (m, 2H), 8.53 (dd, J = 8.8, 1.7 Hz, 1H), 8.09 (d, J = 2.9 Hz, 1H), 4.17 (d, J = 7.1 Hz, 2H), 3.39 ( q, J = 7.5 Hz, 2H), 1.28-1.34 (m, 1H), 1.12 (t, J = 7.5 Hz, 3H), 0.62-0.67 (m, 2H), 0.40-0.43 (m, 2H) ESI MS (m/z) 454.95 (MH)+ 225 3-(3-(乙基磺醯基)-5-(甲氧基甲氧基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (t, J = 2.8 Hz, 1H), 8.58-8.60 (m, 2H), 8.54 (dd, J = 8.6, 1.8 Hz, 1H), 8.23 (dd, J = 11.8, 2.9 Hz, 1H), 5.53 (s, 2H), 3.47 (d, J = 7.9 Hz, 3H), 3.39 (q, J = 7.2 Hz, 2H), 1.13 ( t, J = 7.2 Hz, 3H) ESI MS (m/z) 444.95 (MH)+ 226 3-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.03 (d, J = 2.7 Hz, 1H), 8.59-8.62 (m, 2H), 8.54-8.57 (m, 1H), 8.50 (d, J = 2.7 Hz, 1H), 7.63 (t, J = 72.3 Hz, 1H), 3.46 ( q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 450.95 (MH)+ 227 2-((5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基)氧)-2-甲基丙醯胺 1H-NMR (400 MHz, DMSO-d6) δ 10.69 (s, 1H), 9.37 (d, J = 2.4 Hz, 1H), 9.10 (d, J = 2.4 Hz, 1H), 8.53-8.60 (m, 3H), 5.95 (s, 1H), 3.35 (q, J = 7.3 Hz, 2H), 1.41 (s, 6H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 486.00 (MH)+ 228 2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2-甲基丙腈 1H-NMR (400 MHz, DMSO-d6) δ 9.19 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.60 (d, J = 2.4 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 3.45 (q, J = 7.3 Hz, 2H), 1.88 (s, 6H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 451.00 (MH)+ 229 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基氨基磺酸二甲酯 1H-NMR (400 MHz, DMSO-d6) δ 9.07 (d, J = 2.7 Hz, 1H), 8.78 (s, 1H), 8.53 (d, J = 2.7 Hz, 2H), 8.43 (d, J = 8.3 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 3.04 (s, 6H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 506.95 (MH)+ 230 2-(5-氨基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.66 (s, 1H), 8.49 (d, J = 0.9 Hz, 1H), 8.37 (dd, J = 8.4, 1.7 Hz, 1H), 8.29 (d, J = 8.3 Hz, 1H), 8.12-8.14 (m, 1H), 7.57 (d, J = 2.8 Hz, 1H), 6.31 (s, 2H), 3.21-3.29 (q, J = 7.3 Hz, 2H), 1.09 (t, J = 7.6 Hz, 3H) ESI MS (m/z) 399.00 (MH)+ 231 2-(5-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.11 (d, J = 2.4 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.71 (d, J = 2.4 Hz, 1H), 8.52 (d, J = 1.2 Hz, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 418.05(MH)+ 232 2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 9.44 (s, 1H), 8.80-8.82 (m, 2H), 8.54 (d, J = 0.9 Hz, 1H), 8.44 (dd, J = 7.9, 1.8 Hz, 2H), 8.33-8.37 (m, 2H), 3.41-3.46 (q, 7.5 Hz, 2H), 1.15 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 450.95 (MH)+ 233 2-(3-(乙基磺醯基)-5-((4-氧負離子基-1,4l6-氧雜蒽-4-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.71 (d, J = 0.7 Hz, 1H), 8.53 (d, J = 2.7 Hz, 1H), 8.50 (s, 1H), 8.39 (dd, J = 8.3, 1.5 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.94 (d, J = 2.7 Hz, 1H), 4.14 (td, J = 8.6, 3.8 Hz, 2H), 3.99-4.05 (m, 2H), 3.68-3.72 (m, 2H), 3.57-3.63 (m, 2H), 3.33-3.40 (q, 2H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 517.05(MH)+ 234 2-(6-溴-3-(乙硫基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.86 (q, J = 0.8 Hz, 1H), 8.76 (d, J = 8.9 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.4, 2.0 Hz, 1H), 8.31 (d, J = 8.6 Hz, 1H), 7.71-7.75 (m, 1H), 7.64-7.68 (m, 1H), 2.74 (q, J = 7.3 Hz, 2H), 1.05 (t, J = 24.7, 7.1 Hz, 3H) ESI MS (m/z) 468.90 (MH)+ 235 2-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.94 (d, J = 2.7 Hz, 1H), 8.76 (s, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.2, 1.6 Hz, 1H), 8.37 (d, J = 2.9 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.60 (t, J = 72.5 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 450.00(MH)+ 236 1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺 1H-NMR (400 MHz, DMSO-d6) δ 10.80 (s, 1H), 9.16 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 2.8 Hz, 1H), 8.74 (s, 1H), 8.52 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 3.37 (q, J = 7.3 Hz, 2H), 1.79 (d, J = 4.3 Hz, 4H), 1.13 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 492.00(MH)+ 237 2-(3-(乙基磺醯基)-6-(5-甲基-3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (s, 1H), 8.76 (d, J = 8.6 Hz, 1H), 8.55 (s, 1H), 8.42-8.44 (m, 1H), 8.35 (d, J = 8.6 Hz, 2H), 6.92 (s, 1H), 3.47 (q, J = 7.4 Hz, 2H), 2.60 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 532.00 (MH)+ *使用Chemdraw Professional 18.1生成的化合物名稱The following compounds (Table 1) are obtained by using suitable starting materials and following the similar methods described in Schemes 1-9 or Examples 1-16. Table-1 Item No. Compound name analyze data 1 2-(3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.02 (dd, J = 4.9, 1.7 Hz, 1H), 8.74 (s, 1H), 8.61 (dd, J = 7.8, 1.7 Hz, 2H), 8.51 (d , J = 8.3 Hz, 1H), 8.28 (dd, J = 8.3, 1.5 Hz, 1H), 7.90-7.99 (m, 1H), 3.40 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 384.1 (MH)+. 2 2-(3-(Ethylthio)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.69 (d, J = 7.8 Hz, 1H), 8.55 (s, 1H), 8.49 (d, J = 8.3 Hz, 1H), 8.41 (dd, J = 4.6 , 1.5 Hz, 1H), 8.23 (dd, J = 8.4, 1.6 Hz, 1H), 8.03-8.08 (m, 1H), 7.58 (dd, J = 8.1, 4.6 Hz, 1H), 2.96 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 352.1 (MH)+ 3 2-(5-Bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.74 (d, J = 0.7 Hz, 1H), 8.57 (t, J = 2.4 Hz, 2H), 8.52 (d, J = 8.3 Hz, 1H), 8.30 ( d, J = 2.2 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 3.08 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 430, 432 [(MH)+ Br79, 81]. 4 2-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.20 (d, J = 2.4 Hz, 1H), 8.81 (d, J = 2.2 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.60 ( s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.7, 1.6 Hz, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 462.0, 464.0 [(MH)+ Br79, 81]. 5 2-(6-Chloro-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (d, J = 2.4 Hz, 1H), 8.60-8.65 (m, 2H), 8.51 (d, J = 8.3 Hz, 1H), 8.28-8.32 (m , 1H), 8.12-8.14 (m, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.13-1.24 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 417.85 (MH) +. 6 2-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.61 (m, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.29 (dd, J = 8.7, 1.6 Hz, 1H), 8.14 (d, J = 2.0 Hz, 2H), 7.82 (t, J = 1.8 Hz, 1H), 3.53 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 527.9, 529.9 [(MH)+ Cl35, 37]. 7 2-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.2 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.61 ( s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.29 (dd, J = 8.3, 1.5 Hz, 1H), 7.83-7.88 (m, 2H), 7.47 (tt, J = 9.3, 2.3 Hz , 1H), 3.53 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 496.10 (MH)+. 8 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.62 (s, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.29 (d, J = 6.8 Hz, 1H), 8.22 (d, J = 8.3 Hz, 2H), 7.98 (d, J = 8.1 Hz, 2H), ), 3.50 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 527.95 (MH)+. 9 2-(3-(Ethylthio)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6DMSO-d6) δ 8.86 (q, J = 1.0 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.60 (s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.41 (d, J = 1.7 Hz, 1H), 8.29 (dd, J = 8.3, 1.5 Hz, 1H), 3.15 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 420 (MH)+ 10 2-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.51 (q, J = 1.1 Hz, 1H), 8.94-8.95 (m, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.62 (s, 1H ), 8.53 (d, J = 8.3 Hz, 1H), 8.30 (dd, J = 8.3, 1.5 Hz, 1H), 3.55 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H ); ESI MS (m/z) 451.95 (MH)+. 11 2-(3-(Ethylsulfonyl)-6-(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1 (2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.47 (d, J = 1.0 Hz, 1H), 8.83 (d, J = 8.6 Hz, 1H), 8.80 (d, J = 2.0 Hz, 1H), 8.62 ( d, J = 4.6 Hz, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.47 (d, J = 1.2 Hz, 1H), 8.34-8.37 (m, 1H), 8.29-8.32 (m, 1H) ), 3.45 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 451.15 (MH)+. 12 2-(3-(Ethylsulfonyl)-6-(5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-6-(three Fluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.77-8.79 (m, 2H), 8.61 (s, 1H), 8.55 (d, J = 8.3 Hz, 1H), 8.36 (d, J = 8.6 Hz, 1H ), 8.30 (d, J = 8.3 Hz, 1H), 6.94 (s, 1H), 3.49 (q, J = 7.4 Hz, 2H), 2.62 (s, 3H), 1.19 (t, J = 7.3 Hz, 3H ); ESI MS (m/z) 531.95 (MH)+. 13 2-(3-(Ethylsulfonyl)-6-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalein Oxazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.83 (q, J = 1.2 Hz, 1H), 8.74-8.76 (m, 2H), 8.58 (s, 1H), 8.49 (d, J = 8.3 Hz, 1H) ), 8.39 (d, J = 8.6 Hz, 1H), 8.26 (dd, J = 8.3, 1.5 Hz, 1H), 7.12 (d, J = 2.8 Hz, 1H), 3.40 (q, J = 7.4 Hz, 2H ), 1.12 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 518.15 (MH)+. 14 2-(3-(Ethylsulfonyl)-6-(3-(trifluoromethyl)-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-6-( Trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.78 (d, J = 0.7 Hz, 1H), 8.89 (d, J = 8.6 Hz, 1H), 8.81 (s, 1H), 8.63 (s, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.43 (d, J = 8.6 Hz, 1H), 8.30-8.32 (m, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.16-1.24 (t , J = 7.4 Hz, 3H); ESI MS (m/z) 519.1 (MH)+. 15 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.29 (d, J = 2.2 Hz, 1H), 8.71-8.74 (m, 2H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H) ), 8.26-8.28 (m, 1H), 8.01-8.04 (m, 2H), 7.42-7.47 (m, 2H), 3.49 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.9 (MH)+. 16 2-(5-(Ethylthio)-6'-fluoro-[3,3'-dipyridine]-6-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.77 (d, J = 2.8 Hz, 1H), 8.76 (d, J = 2.1 Hz, 1H), 8.74 (s, 1H), 8.57 (s, 1H), 8.52 (td, J = 8.0, 3.0 Hz, 2H), 8.31 (d, J = 2.1 Hz, 1H), 8.26 (dd, J = 8.6, 1.5 Hz, 1H), 7.40 (dd, J = 8.6, 2.8 Hz , 1H), 3.12 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz,, 3H); ESI MS (m/z) 447.1 (MH)+ 17 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.30 (d, J = 2.1 Hz, 1H), 8.72-8.73 (m, 2H), 8.57 (s, 1H), 8.48 (d, J = 8.3 Hz, 1H) ), 8.24 (dd, J = 8.5, 1.3 Hz, 1H), 8.05-8.09 (m, 2H), 7.57 (d, J = 7.9 Hz, 2H), 3.46 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.2(MH)+. 18 2-(5-(Ethylsulfonyl)-6'-fluoro-[3,3'-dipyridine]-6-yl)-6-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.1 Hz, 1H), 8.75 ( s, 1H), 8.50-8.63 (m, 3H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.43 (td, J = 8.9, 2.6 Hz, 1H), 3.49 (q, J = 7.4 Hz , 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 479.0 (MH)+. 19 7-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.53 (d, J = 2.2 Hz, 1H), 9.22 (d, J = 2.1 Hz, 1H), 9.09 (d, J = 1.5 Hz, 1H), 8.83 ( d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 3.45-3.51 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 462.7, 464.7 [(MH)+ Br79, 81]. 20 7-(3-(Ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.53 (d, J = 1.7 Hz, 1H), 9.10 (t, J = 1.1 Hz, 1H), 9.03 (dd, J = 4.9, 1.7 Hz, 1H), 8.74 (s, 1H), 8.62 (dd, J = 7.8, 1.7 Hz, 1H), 7.99 (dd, J = 7.9, 4.8 Hz, 1H), 3.40 (q, J = 7.4 Hz, 2H), 1.14 (t , J = 7.3 Hz, 3H); ESI MS (m/z) 384.8 (MH)+. twenty one 7-(6-Chloro-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (dd, J = 2.2, 0.5 Hz, 1H), 9.10 (q, J = 1.0 Hz, 1H), 8.76 (s, 1H), 8.66 (d, J = 8.3 Hz, 1H), 8.15 (d, J = 8.3 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 419.1 (MH)+. twenty two 7-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.2 Hz, 1H), 9.32-9.35 (m, 1H), 9.11 (t, J = 1.1 Hz, 1H), 8.75 (t, J = 2.1 Hz, 2H), 8.03-8.07 (m, 2H), 7.44-7.50 (m, 2H), 3.52 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 479.5 (MH)+. twenty three 7-(3-(Ethylsulfonyl)-5-(3-fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[ 2,3-d)pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.2 Hz, 1H), 9.43 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.5 Hz, 1H), 8.90 ( d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.27 (d, J = 12.0 Hz, 1H), 8.01-8.07 (m, 2H), 3.5 (q, J = 7.3 Hz, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 547 (MH)+ twenty four 7-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.55 (d, J = 2.2 Hz, 1H), 9.52 (d, J = 4.6 Hz, 1H), 9.11 (s, 1H), 8.97 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 1.7 Hz, 1H), 3.56 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 452.8 ( MH)+. 25 7-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3- d)Pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 1.8 Hz, 1H), 9.34 (d, J = 2.4 Hz, 1H), 9.09 (d, J = 1.5 Hz, 1H), 8.77 ( d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.10 (dt, J = 9.4, 2.5 Hz, 2H), 7.60 (d, J = 7.9 Hz, 2H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 545.2 (MH)+. 26 7-(3-(Ethylsulfonyl)-5-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[ 2,3-d)pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 1.8 Hz, 1H), 9.37 (d, J = 2.4 Hz, 1H), 9.09 (d, J = 1.5 Hz, 1H), 8.86 ( d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.34-8.39 (m, 2H), 7.74-7.79 (m, 1H), 3.46-3.53 (q, J = 7.6 Hz 2H), 1.17 ( t, J = 7.3 Hz, 3H); ESI MS (m/z) 546.9 (MH)+. 27 7-(3-(Ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 2.1 Hz, 1H), 9.09 (t, J = 1.1 Hz, 1H), 8.75 (s, 1H), 8.63 (t, J = 4.1 Hz, 1H), 8.51 (d, J = 8.6 Hz, 1H), 8.23-8.28 (m, 2H), 7.37-7.43 (m, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.16 (t , J = 7.3 Hz, 3H); ESI MS (m/z) 479.0 (MH)+. 28 7-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d ]Pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.52 (d, J = 2.2 Hz, 1H), 9.39-9.40 (m, 1H), 9.09 (s, 1H), 8.86-8.86 (m, 1H), 8.75 (d, J = 1.0 Hz, 1H), 8.35 (d, J = 4.6 Hz, 1H), 8.26-8.29 (m, 1H), 7.80-7.93 (m, 2H), 3.52 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 529.2 (MH)+. 29 4-(5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)benzonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 1.6 Hz, 1H), 9.41 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.6 Hz, 1H), 8.86 ( d, J = 2.0 Hz, 1H), 8.77 (s, 1H), 8.20-8.23 (m, 2H), 8.09-8.12 (m, 2H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t , J = 7.2 Hz, 3H); ESI MS (m/z) 485.8 (MH)+. 30 7-(3-(Ethylsulfonyl)-6-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3- d)Pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 1.6 Hz, 1H), 9.11 (t, J = 1.1 Hz, 1H), 8.78 (s, 1H), 8.69 (d, J = 8.3 Hz, 1H), 8.57 (d, J = 8.6 Hz, 1H), 8.33 (dt, J = 9.5, 2.6 Hz, 2H), 7.58 (d, J = 8.1 Hz, 2H), 3.45 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 545.0 (MH)+. 31 7-(3-(Ethylsulfonyl)-5-phenylpyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 1.7 Hz, 1H), 9.34 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.5 Hz, 1H), 8.76 ( t, J = 2.1 Hz, 2H), 7.97-7.99 (m, 2H), 7.57-7.65 (m, 3H), 3.52 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H ); ESI MS (m/z) 461.0 (MH)+. 32 7-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridine Oxazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (s, 1H), 9.39 (d, J = 2.4 Hz, 1H), 9.11 (s, 1H), 8.85 (d, J = 2.0 Hz, 1H), 8.76 (s, 1H), 7.85 (d, J = 6.8 Hz, 2H), 7.46 (t, J = 9.2 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 497.0 (MH)+. 33 7-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridine Oxazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.0 Hz, 1H), 9.40 (d, J = 2.2 Hz, 1H), 9.11 (d, J = 1.6 Hz, 1H), 8.87 ( d, J = 2.3 Hz, 1H), 8.76 (s, 1H), 8.15 (d, J = 1.6 Hz, 2H), 7.82 (t, J = 2.0 Hz, 1H), 3.54 (q, J = 7.3 Hz, 2H), 1.20 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 529.0, 531.0 [(MH)+ Cl35, 37]. 34 7-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-3-(trifluoromethyl)pyridine And [2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.56 (d, J = 2.4 Hz, 1H), 9.52 (d, J = 1.8 Hz, 1H), 9.09 (d, J = 1.8 Hz, 2H), 8.94 ( d, J = 2.1 Hz, 1H), 8.76 (s, 1H), 7.24 (d, J = 2.8 Hz, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.6 Hz, 3H); ESI MS (m/z) 519.0 (MH)+. 35 7-(3-(Ethylsulfonyl)-6-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d ]Pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.41 (d, J = 1.7 Hz, 1H), 8.58 (d, J = 8.1 Hz, 1H), 8.47-8.49 (m, 2H), 8.40 (s, 1H) ), 8.29 (d, J = 7.8 Hz, 1H), 8.18 (d, J = 8.1 Hz, 1H), 7.80 (d, J = 7.8 Hz, 1H), 7.67 (t, J = 7.8 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.38 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.8 (MH)+. 36 7-(6-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridine Oxazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.8 Hz, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.46 (d, J = 1.2 Hz, 1H), 8.45 ( s, 1H), 8.08 (d, J = 8.3 Hz, 1H), 7.98 (d, J = 1.8 Hz, 2H), 7.49-7.52 (m, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 528.9 ,530.9[(MH)+ Cl35, 37] 37 3-(3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.04-9.08 (m, 1H), 8.71 (s, 1H), 8.65 (dd, J = 8.1, 1.7 Hz, 1H), 8.42-8.50 (m, 1H) , 8.17-8.30 (m, 1H), 7.97-8.04 (m, 2H), 3.36-3.46 (m, 2H), 1.18 (t ,J = 7.3 Hz,, 3H); ESI MS (m/z) 384 ( MH)+ 38 3-(3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.05 (dd, J = 4.9, 1.7 Hz, 1H), 8.68 (s, 1H), 8.65 (dd, J = 8.1, 1.7 Hz, 1H), 8.43 (d , J = 8.3 Hz, 1H), 8.17 (s, 1H), 8.02 (dd, J = 7.9, 4.8 Hz, 1H), 7.97 (dd, J = 8.4, 1.6 Hz, 1H), 3.36 3.38 (m, 2H ), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 383.6 (MH)+ 39 3-(3-(ethylthio)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 8.67-8.69 (m, 2H), 8.14 (s, 1H), 8.00-8.07 (m, 2H), 7.91-7.95 (m, 1H), 2.95-3.10 ( m, 2H), 1.33 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 420 (MH)+ 40 7-(3-(Ethylsulfonyl)-6-(3-methyl-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-3-(trifluoromethyl )Pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.37 (d, J = 1.5 Hz, 1H), 9.00 (s, 1H), 8.60 (dd, J = 8.6, 2.4 Hz, 1H), 8.41-8.45 (m , 2H), 8.20 (d, J = 8.6 Hz, 1H), 3.40 (q, J = 7.4 Hz, 2H), 2.52 (s, 3H), 1.33 (t, J = 7.3 Hz, 3H); ESI MS ( m/z) 465.8 (MH)+. 41 7-(3-(Ethylsulfonyl)-6-(3-fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[ 2,3-d)pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.41 (d, J = 1.7 Hz, 1H), 8.60 (d, J = 8.3 Hz, 1H), 8.48-8.50 (m, 2H), 8.16 (d, J = 8.1 Hz, 1H), 7.99 (t, J = 8.0 Hz, 2H), 7.78 (t, J = 7.7 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.38 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 547.0 (MH)+. 42 4-(5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 2-base) benzonitrile 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.2 Hz, 1H), 8.57 (d, J = 8.3 Hz, 1H), 8.45 (d, J = 9.8 Hz, 2H), 8.21 ( d, J = 8.3 Hz, 2H), 8.15 (d, J = 8.3 Hz, 1H), 7.81 (d, J = 8.3 Hz, 2H), 3.44 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 485.8 (MH)+. 43 7-(3-(Ethylsulfonyl)-6-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[ 2,3-d)pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.5 Hz, 1H), 8.55 (d, J = 8.3 Hz, 1H), 8.45-8.47 (m, 2H), 8.39 (dd, J = 6.7, 1.8 Hz, 1H), 8.27-8.31 (m, 1H), 8.11 (d, J = 8.3 Hz, 1H), 7.35 (t, J = 9.2 Hz, 1H), 3.43 (q, J = 7.4 Hz , 2H), 1.35 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 546.8 (MH)+. 44 3-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 8.98 (d, J = 2.4 Hz, 1H), 8.64 (d, J = 2.4 Hz, 1H), 8.63 (q, J = 0.7 Hz, 1H), 8.13 ( t, J = 6.1 Hz, 1H), 8.07 (dd, J = 8.6, 1.7 Hz, 1H), 7.96 (d, J = 8.6 Hz, 1H), 3.35-3.46 (m, 2H), 1.40 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.95, 463.95 [(MH)+ Br79, 81]. 45 3-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.55 (q, J = 1.1 Hz, 1H), 9.02-9.02 (m, 1H), 8.70 (s, 1H), 8.48 (q, J = 0.7 Hz, 1H ), 8.30 (dd, J = 8.7, 2.1 Hz, 1H), 8.04 (d, J = 8.6 Hz, 1H), 3.47-3.61 (m, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 451.8 (MH)+. 46 3-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (d, J = 2.4 Hz, 1H), 8.93 (d, J = 2.2 Hz, 1H), 8.73 (s, 1H), 8.48 (t, J = 1.1 Hz, 1H), 8.29 (dd, J = 8.6, 2.0 Hz, 1H), 8.16 (d, J = 2.0 Hz, 2H), 8.04 (t, J = 4.3 Hz, 1H), 7.83 (t, J = 1.8 Hz, 1H), 3.48-3.62 (m, 2H), 1.18-1.24 (t,J=7.3Hz, 3H); ESI MS (m/z) 528.00, 530.00 [(MH)+ Cl35, 37]. 47 3-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.1 Hz, 1H), 8.78 (d, J = 2.1 Hz, 1H), 8.72 (s, 1H), 8.46 (d, J = 2.1 Hz, 1H), 8.27 (dd, J = 8.6, 2.1 Hz, 1H), 8.01-8.06 (m, 3H), 7.43-7.48 (m, 2H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.7 (MH)+. 48 3-(3-(Ethylsulfonyl)-5-phenylpyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.1 Hz, 1H), 8.73 (s, 1H), 8.46 (d, J = 2.1 Hz, 1H), 8.27 (dd, J = 8.9, 2.1 Hz, 1H), 8.02 (d, J = 8.6 Hz, 1H), 7.96-7.98 (m, 2H), 7.54-7.64 (m, 3H), 3.43 -3.60 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 459.75 (MH)+. 49 3-(3-(Ethylsulfonyl)-5-(4-methoxyphenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.74 (t, J = 2.4 Hz, 2H), 8.48 (d, J = 2.2 Hz, 1H), 8.29 ( dd, J = 8.7, 2.1 Hz, 1H), 8.04 (d, J = 8.6 Hz, 1H), 7.94-7.97 (m, 2H), 7.18 (dd, J = 6.8, 2.0 Hz, 2H), 3.87 (s , 3H), 3.43-3.60 (m, 2H), 1.2 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 490.00 (MH)+. 50 3-(3-(Ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline-4(3H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (d, J = 2.2 Hz, 1H), 8.90 (d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 8.48 (s, 1H), 8.29 (dd, J = 8.6, 2.2 Hz, 1H), 8.23 (d, J = 8.1 Hz, 2H), 8.04 (d, J = 8.6 Hz, 1H), 7.99 (d, J = 8.3 Hz, 2H), 3.46-3.59 (m, 2H), 1.21 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 527.85 (MH)+. 51 7-(3-(Ethylsulfonyl)-6-phenylpyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.37 (d, J = 1.5 Hz, 1H), 8.49 (d, J = 8.3 Hz, 1H), 8.44 (d, J = 7.0 Hz, 2H), 8.07- 8.11 (m, 3H), 7.47-7.52 (m, 3H), 3.43 (q, J = 7.4 Hz, 2H), 1.35 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.2 (MH )+. 52 7-(3-(Ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido [2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.5 Hz, 1H), 9.06 (q, J = 1.1 Hz, 1H), 8.61 (q, J = 1.1 Hz, 1H), 8.45- 8.46 (m, 2H), 7.61 (t, J = 8.6 Hz, 1H), 7.19-7.24 (m, 2H), 3.48 (q, J = 7.3 Hz, 2H), 1.36 (t, J = 7.2 Hz, 3H ); ESI MS (m/z) 563.1 (MH)+. 53 7-(5-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)-3-(ethylsulfonyl)pyridin-2-yl)- 3-(Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (s, 1H), 9.05 (d, J = 2.1 Hz, 1H), 8.55 (d, J = 2.1 Hz, 1H), 8.45 (d, J = 4.3 Hz, 2H), 7.40-7.42 (m, 2H), 7.28 (s, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.37 (t, J = 7.3 Hz, 3H); ESI MS (m/ z) 540.9 (MH)+. 54 7-(6-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridine Oxazine-8(7H)-one 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.38 (d, J = 1.5 Hz, 1H), 8.54 (t, J = 4.1 Hz, 1H), 8.46 (d, J = 1.2 Hz, 1H), 8.44 ( s, 1H), 8.07 (d, J = 8.3 Hz, 1H), 7.61-7.67 (m, 2H), 6.93-7.00 (m, 1H), 3.44 (q, J = 7.3 Hz, 2H), 1.35 (t , J = 7.3 Hz, 3H); ESI MS (m/z) 497.0 (MH)+. 55 7-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl )Pyrido[2,3-d]pyridazine-8(7H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.54 (d, J = 2.2 Hz, 1H), 9.35 (d, J = 2.4 Hz, 1H), 9.11 (d, J = 1.6 Hz, 1H), 8.79 ( d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.09 (dd, J = 6.6, 2.2 Hz, 2H), 7.53 (d, J = 8.6 Hz, 2H), 6.88 (tt, J = 52.0 , 2.9 Hz, 1H), 3.52 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 577.0 (MH)+. 56 3-(3-(Ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline-4(3H )-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.46-9.47 (m, 1H), 8.94 (q, J = 1.1 Hz, 1H), 8.74 (d, J = 1.0 Hz, 1H), 8.48 (d, J = 4.4 Hz, 1H), 8.38 (d, J = 4.9 Hz, 1H), 8.28-8.32 (m, 2H), 8.04 (dd, J = 8.6, 2.4 Hz, 1H), 7.93-7.96 (m, 1H) , 7.84-7.89 (m, 1H), 3.73 (q, J = 7.4 Hz, 2H), 1.26 (t, J = 7.5 Hz, 3H) 57 4-(5-(Ethylsulfonyl)-6-(4-oxo-6-(trifluoromethyl)quinazolin-3(4H)-yl)pyridin-3-yl)benzonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (d, J = 2.2 Hz, 1H), 8.91 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.48 (q, J = 0.7 Hz, 1H), 8.29 (dd, J = 8.7, 2.1 Hz, 1H), 8.22 (dd, J = 6.8, 2.0 Hz, 2H), 8.11 (dd, J = 6.6, 2.0 Hz, 2H), 8.04 (d , J = 8.6 Hz, 1H), 3.46-3.63 (m, 2H), 1.26 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 485.05 (MH)+. 58 3-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline-4(3H )-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (t, J = 2.2 Hz, 1H), 8.84 (d, J = 2.2 Hz, 1H), 8.74 (s, 1H), 8.49 (d, J = 7.1 Hz, 1H), 8.29 (dd, J = 8.7, 2.1 Hz, 1H), 8.12-8.15 (m, 2H), 8.04 (d, J = 8.6 Hz, 1H), 7.62-7.66 (m, 2H), 3.53 (q, J = 7.3 Hz, 3H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 544.05 (MH)+. 59 3-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.45 (t, J = 2.1 Hz, 1H), 8.90 (d, J = 2.2 Hz, 1H), 8.74 (d, J = 1.7 Hz, 1H), 8.47 ( d, J = 1.7 Hz, 1H), 8.29 (dd, J = 8.6, 2.2 Hz, 1H), 8.04 (d, J = 8.6 Hz, 1H), 7.85-7.89 (m, 2H), 7.48 (tt, J = 9.3, 2.2 Hz, 1H), 3.55 (q, J = 7.3 Hz, 2H), 1.21 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 496.05 (MH)+. 60 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.2 Hz, 1H), 8.83 (t, J = 2.6 Hz, 1H), 8.73 (d, J = 2.0 Hz, 1H), 8.48 ( d, J = 5.4 Hz, 1H), 8.27-8.30 (m, 1H), 8.03-8.05 (m, 3H), 7.68-7.71 (m, 2H), 3.53 (q, J = 7.2 Hz, 2H), 1.20 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 493.95 (MH)+. 61 3-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline-4(3H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (t, J = 2.1 Hz, 1H), 8.94 (t, J = 2.2 Hz, 1H), 8.74 (d, J = 2.0 Hz, 1H), 8.49 ( d, J = 5.1 Hz, 1H), 8.38 (d, J = 4.9 Hz, 1H), 8.28-8.32 (m, 2H), 8.04 (d, J = 8.6 Hz, 1H), 7.94 (d, J = 8.1 Hz, 1H), 7.86 (t, J = 7.7 Hz, 1H), 3.47-3.64 (m, 2H), 1.22 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 528.00 (MH)+ . 62 3-(3-(Ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline -4(3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.30 (t, J = 1.7 Hz, 1H), 8.84 (d, J = 0.9 Hz, 1H), 8.76 (s, 1H), 8.46 (s, 1H), 8.28 (dd, J = 8.6, 2.1 Hz, 1H), 8.10 (t, J = 7.9 Hz, 1H), 7.99-8.04 (m, 2H), 7.84 (d, J = 8.3 Hz, 1H), 3.40-3.53 (m, 2H), 1.18 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 546.05 (MH)+. 63 3-(5-(3-chloro-4-(trifluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline- 4(3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.1 Hz, 1H), 8.92 (d, J = 2.4 Hz, 1H), 8.65-8.69 (m, 1H), 8.43 (t, J = 1.1 Hz, 1H), 8.38 (d, J = 2.1 Hz, 1H), 8.25 (td, J = 8.9, 2.1 Hz, 2H), 7.99 (d, J = 8.6 Hz, 1H), 7.94 (d, J = 8.6 Hz, 1H), 3.42-3.58 (m, 2H), 1.15-1.22 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 561.70 (MH)+. 64 3-(3-(Ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazole Lin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.22-9.26 (m, 1H), 8.79 (t, J = 1.1 Hz, 1H), 8.76 (s, 1H), 8.46 (d, J = 1.8 Hz, 1H ), 8.28 (dd, J = 8.6, 2.1 Hz, 1H), 7.99-8.03 (m, 2H), 7.71 (dd, J = 10.9, 1.7 Hz, 1H), 7.50 (d, J = 8.9 Hz, 1H) , 3.41-3.53 (m, 2H), 1.11-1.19(t, J = 7.4 Hz, 3H); ESI MS (m/z) 561.75 (MH)+. 65 3-(3-(Ethylsulfonyl)-5-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline -4(3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.1 Hz, 1H), 8.92 (d, J = 2.4 Hz, 1H), 8.71 (s, 1H), 8.46 (d, J = 1.8 Hz, 1H), 8.34-8.39 (m, 2H), 8.27 (dd, J = 8.9, 2.1 Hz, 1H), 8.02 (d, J = 8.6 Hz, 1H), 7.75-7.80 (m, 1H), 3.44 -3.60 (m, 2H), 1.16-1.21( t, J = 7.5 Hz, 3H); ESI MS (m/z) 543.95 (MH)+. 66 3-(3-(Ethylsulfonyl)-5-(2-fluoro-5-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazole Lin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.27 (t, J = 1.8 Hz, 1H), 8.81 (t, J = 1.1 Hz, 1H), 8.75 (s, 1H), 8.46-8.48 (m, 1H ), 8.28 (dd, J = 8.6, 2.1 Hz, 1H), 7.99-8.03 (m, 2H), 7.61-7.65 (m, 2H), 3.40-3.56 (m, 2H), 1.11-1.20 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 561.70 (MH)+. 67 2-(3-(Ethylsulfonyl)-5-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine- 1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.2 Hz, 1H), 8.86 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.61 (s, 1H), 8.53 (d, J = 8.3 Hz, 1H), 8.35-8.40 (m, 2H), 8.29 (dd, J = 8.6, 1.7 Hz, 1H), 7.76-7.80 (m, 1H), 3.52 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 545.7 (MH)+. 68 2-(3-(Ethylsulfonyl)-5-(4-fluoro-3-methoxyphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H )-ketone 1H-NMR (400 MHz, CHLOROFORM-D) δ 9.07 (d, J = 2.4 Hz, 1H), 8.65 (d, J = 8.1 Hz, 1H), 8.60 (d, J = 2.3 Hz, 1H), 8.42 ( s, 1H), 8.12 (s, 1H), 8.08 (d, J = 8.6 Hz, 1H), 7.29 (d, J = 3.2 Hz, 1H), 7.23-7.25 (m, 2H), 4.03 (s, 3H ), 3.43 (q, J = 7.4 Hz, 2H), 1.37 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 507.7 (MH)+. 69 2-(5-(2,4-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.18 (q, J = 1.2 Hz, 1H), 8.75 (s, 1H), 8.68 (q, J = 1.1 Hz, 1H), 8.60 (s, 1H), 8.52 (d, J = 8.6 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.94 (td, J = 8.9, 6.4 Hz, 1H), 7.52-7.58 (m, 1H), 7.36 (td, J = 8.6, 2.1 Hz, 1H), 3.46 (q, J = 7.6 Hz, 2H), 1.15 (t, J = 7.6 Hz, 3H); ESI MS (m/z) 495.7 (MH)+. 70 2-(3-(Ethylsulfonyl)-5-(4-fluoro-3-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.28 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.71 (d, J = 2.4 Hz, 1H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.93 (dd, J = 7.2, 2.0 Hz, 1H), 7.81-7.85 (m, 1H), 7.37 (t, J = 9.0 Hz, 1H), 3.48 (q, J = 7.3 Hz, 2H), 2.36 (d, J = 1.5 Hz, 3H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS ( m/z) 491.7 (MH)+. 71 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazin-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.1 Hz, 1H), 8.74 (d, J = 2.4 Hz, 2H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 7.99-8.02 (m, 2H), 7.67 (dd, J = 6.7, 2.1 Hz, 2H), 3.49 (q, J = 7.7 Hz , 2H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 493.7 (MH)+. 72 2-(5-Cyclopropyl-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (d, J = 2.2 Hz, 1H), 8.71 (s, 1H), 8.58 (s, 1H), 8.50 (d, J = 8.3 Hz, 1H), 8.26 (dd, J = 8.4, 1.6 Hz, 1H), 8.17 (d, J = 2.2 Hz, 1H), 3.39 (q, J = 7.4 Hz, 2H), 2.24-2.31 (m, 1H), 1.17-1.22 (m, 2H), 1.13 (t, J = 7.5 Hz, 3H), 1.00-1.04 (m, 2H); ESI MS (m/z) 424.0 (MH)+. 73 2-(3-(Ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (s, 1H), 8.60-8.62 (m, 2H), 8.50 (dd, J = 8.3, 5.5 Hz, 2H), 8.23-8.28 (m, 3H) , 7.36-7.42 (m, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.7 (MH)+. 74 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalein Oxazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.55 (d, J = 2.8 Hz, 1H), 9.09 (t, J = 1.4 Hz, 1H), 8.93 (d, J = 2.8 Hz, 1H), 8.76 ( s, 1H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 8.6, 1.5 Hz, 1H), 7.24 (d, J = 2.8 Hz, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 517.7 (MH)+. 75 2-(3-(Ethylsulfonyl)-6-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.67 (d, J = 8.3 Hz, 1H), 8.61 (s, 1H), 8.54 (t, J = 8.7 Hz, 2H), 8.28-8.35 (m, 3H), 7.56-7.58 (m, 2H), 3.44 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.1 (MH)+. 76 3-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl )Quazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.2 Hz, 1H), 8.83 (d, J = 2.2 Hz, 1H), 8.74 (s, 1H), 8.48 (d, J = 2.2 Hz, 1H), 8.28-8.31 (m, 1H), 8.09-8.11 (m, 2H), 8.05 (d, J = 8.4 Hz, 1H), 7.54 (d, J = 8.6 Hz, 2H), 7.04-6.72 (m, 1H), 3.53 (dd, J = 16.7, 7.5 Hz, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 576.05 (MH)+. 77 2-(6-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.61-8.70 (m, 2H), 8.53 (q, J = 4.2 Hz, 2H), 8.29 (dd, J = 8.4, 1.6 Hz , 1H), 8.23 (dd, J = 6.8, 2.0 Hz, 2H), 7.65 (dd, J = 6.8, 2.0 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 494.0 (MH)+. 78 2-(5-(2-Chloro-4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.10 (d, J = 2.2 Hz, 1H), 8.78 (s, 1H), 8.65 (d, J = 2.2 Hz, 1H), 8.62 (s, 1H), 8.54 (d, J = 8.3 Hz, 1H), 8.29 (dd, J = 8.4, 1.6 Hz, 1H), 7.84 (dd, J = 8.8, 6.1 Hz, 1H), 7.76 (dd, J = 8.9, 2.6 Hz , 1H), 7.47-7.52 (m, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.2 Hz, 3H); ESI MS (m/z) 511.9 (MH)+. 79 2-(3-(Ethylsulfonyl)-5-(3,4,5-trifluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.1 Hz, 1H), 8.81 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.59 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.3, 1.5 Hz, 1H), 8.10 (dd, J = 9.3, 6.6 Hz, 2H), 3.50 (q, J = 7.6 Hz, 2H ), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 513.7 (MH)+. 80 2-(3-(Ethylsulfonyl)-5-(4-fluoro-2-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.03 (d, J = 2.2 Hz, 1H), 8.77 (s, 1H), 8.62 (s, 1H), 8.52-8.55 (m, 2H), 8.28-8.30 (m, 1H), 7.56 (dd, J = 8.4, 6.0 Hz, 1H), 7.33 (dd, J = 10.0, 2.4 Hz, 1H), 7.25 (td, J = 8.7, 2.8 Hz, 1H), 3.49 ( q, J = 7.4 Hz, 2H), 2.36 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 491.8 (MH)+. 81 2-(6-Chloro-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.62 (d, J = 8.6 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H ), 8.34 (d, J = 8.3 Hz, 1H), 8.12 (d, J = 8.3 Hz, 1H), 3.42 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 418.0 (MH)+. 82 2-(3-(Ethylsulfonyl)-6-(4-fluoro-2-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.74 (s, 1H), 8.62 (d, J = 8.3 Hz, 1H), 8.58 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.26 (dd, J = 8.4, 1.7 Hz, 1H), 8.09 (d, J = 8.3 Hz, 1H), 7.62 (dd, J = 8.6, 6.1 Hz, 1H), 7.18-7.25 (m, 2H), 3.45 (q, J = 7.3 Hz, 2H), 2.40 (s, 3H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 491.7 (MH)+. 83 2-(6-(2-Chloro-4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (s, 1H), 8.68 (d, J = 7.9 Hz, 1H), 8.59 (s, 1H), 8.50 (d, J = 8.6 Hz, 1H), 8.24-8.28 (m, 2H), 7.76 (dd, J = 8.9, 6.1 Hz, 1H), 7.68 (dd, J = 8.9, 2.4 Hz, 1H), 7.41 (td, J = 8.5, 2.5 Hz, 1H) , 3.45 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 511.7 (MH)+. 84 2-(3-(Ethylsulfonyl)-6-(3,4,5-trifluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (s, 1H), 8.69 (d, J = 8.3 Hz, 1H), 8.60 (t, J = 4.3 Hz, 2H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 8.17 (dd, J = 9.2, 6.7 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 513.7 (MH)+. 85 2-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.19 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.52 (d, J = 0.9 Hz, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.6 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 461.55, 463.55 [(MH)+ Br79, 81]. 86 3-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.44 (d, J = 2.4 Hz, 1H), 8.91 (d, J = 2.4 Hz, 1H), 8.68 (s, 1H), 8.42 (d, J = 8.3 Hz, 1H), 8.15 (t, J = 2.1 Hz, 3H), 7.96 (dd, J = 8.5, 1.6 Hz, 1H), 7.82 (t, J = 1.8 Hz, 1H), 3.53 (q, J = 7.2 Hz, 2H), 1.14-1.22 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 528.05, 530.05 [(MH)+ Cl35, 37]. 87 3-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.2 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.15 (s, 1H), 8.02-8.06 (m, 2H), 7.96 (dd, J = 8.4, 1.6 Hz, 1H), 7.42-7.48 (m, 2H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.95 (MH)+. 88 3-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazoline-4(3H )-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.4 Hz, 1H), 8.71 (s, 1H), 8.45 (d, J = 8.3 Hz, 1H), 8.17 (s, 1H), 8.11-8.15 (m, 2H), 7.98 (dd, J = 8.3, 1.7 Hz, 1H), 7.63 (d, J = 7.8 Hz, 2H), 3.52 (q , J = 7.5 Hz, 2H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.10 (MH)+. 89 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.30 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.72 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.01-8.05 (m, 2H), 7.44 (t, J = 8.9 Hz, 2H), 3.50 (q , J = 7.4 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 477.7 (MH)+. 90 2-(3-(Ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.78 (s, 1H), 8.62 (d, J = 8.3 Hz, 1H), 8.54 (s, 1H), 8.50 (d, J = 8.6 Hz, 1H), 8.42 (dd, J = 8.4, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.23-8.27 (m, 2H), 7.36-7.42 (m, 2H), 3.42 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 477.9 (MH)+. 91 2-(6-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (s, 1H), 8.66 (d, J = 8.3 Hz, 1H), 8.54 (d, J = 8.6 Hz, 2H), 8.44 (dd, J = 8.3 , 1.7 Hz, 1H), 8.36 (d, J = 8.3 Hz, 1H), 8.23 (dt, J = 9.1, 2.3 Hz, 2H), 7.63-7.68 (m, 2H), 3.44 (q, J = 7.3 Hz , 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 493.9(MH)+. 92 3-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.1 Hz, 1H), 8.88 (d, J = 2.4 Hz, 1H), 8.69 (s, 1H), 8.42 (d, J = 8.3 Hz, 1H), 8.16 (s, 1H), 7.96 (dd, J = 8.6, 1.5 Hz, 1H), 7.86 (dd, J = 8.7, 2.0 Hz, 2H), 7.44-7.49 (m, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 496.05 MH)+. 93 3-(3-(Ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazoline-4(3H )-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.41 (d, J = 2.1 Hz, 1H), 8.86 (d, J = 2.1 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.6 Hz, 1H), 8.16 (s, 1H), 8.06 (s, 1H), 8.03 (d, J = 7.9 Hz, 1H), 7.96 (dd, J = 8.3, 1.5 Hz, 1H), 7.75 (t, J = 8.1 Hz, 1H), 7.57 (d, J = 8.3 Hz, 1H), 3.44-3.61 (m, 2H), 1.19 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 544.05 (MH )+. 94 4-(5-(Ethylsulfonyl)-6-(4-oxo-7-(trifluoromethyl)quinazolin-3(4H)-yl)pyridin-3-yl)benzonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.44 (d, J = 2.1 Hz, 1H), 8.89 (d, J = 2.1 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.20 (d, J = 8.3 Hz, 2H), 8.16 (s, 1H), 8.09 (d, J = 8.6 Hz, 2H), 7.95-7.97 (m, 1H), 3.44-3.60 (m , 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 485.05 (MH)+. 95 3-(3-(Ethylsulfonyl)-5-(4-methoxyphenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.1 Hz, 1H), 8.72 (d, J = 2.1 Hz, 1H), 8.68 (s, 1H), 8.42 (d, J = 8.3 Hz, 1H), 8.15 (s, 1H), 7.92-7.97 (m, 3H), 7.15-7.17 (m, 2H), 3.85 (s, 3H), 3.41-3.57 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H; ESI MS (m/z) 494.00 (MH)+. 96 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.37 (d, J = 2.1 Hz, 1H), 8.81 (d, J = 2.1 Hz, 1H), 8.69 (s, 1H), 8.43 (d, J = 7.9 Hz, 1H), 8.15 (s, 1H), 8.02 (dt, J = 9.1, 2.4 Hz, 2H), 7.96 (dd, J = 8.4, 1.7 Hz, 1H), 7.68 (dt, J = 8.9, 2.3 Hz , 2H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H) 97 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.76 (d, J = 2.2 Hz, 1H), 8.55 (s, 1H), 8.44 (dd, J = 8.4, 1.6 Hz, 1H), 8.36 (d, J = 8.3 Hz, 1H), 8.02 (dd, J = 6.6, 2.0 Hz, 2H), 7.69 (dd, J = 6.7, 2.1 Hz , 2H), 3.52 (q, J = 7.4 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 494.0(MH)+. 98 2-(3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.00 (dd, J = 4.7, 1.7 Hz, 1H), 8.75 (s, 1H), 8.59 (dd, J = 7.9, 1.5 Hz, 1H), 8.52 (s , 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.96 (dd, J = 7.9, 4.6 Hz, 1H), 3.38 (q, J = 7.3 Hz, 2H), 1.13 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 383.9 (MH)+. 99 2-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.50 (d, J = 1.5 Hz, 1H), 8.93 (d, J = 2.4 Hz, 1H), 8.81 (s, 1H), 8.53 (s, 1H), 8.44 (dd, J = 8.3, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.54 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 452.0 (MH)+. 100 3-(3-(Ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazoline-4(3H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.4 Hz, 1H), 8.88 (d, J = 2.1 Hz, 1H), 8.70 (s, 1H), 8.43 (d, J = 8.3 Hz, 1H), 8.21 (d, J = 8.3 Hz, 2H), 8.16 (s, 1H), 7.96-7.99 (m, 3H), 3.45-3.58 (m, 2H), 1.19 (t, J = 7.3 Hz , 3H); ESI MS (m/z) 527.75 (MH)+. 101 3-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Quazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.36-9.38 (m, 1H), 8.80-8.82 (m, 1H), 8.68-8.71 (m, 1H), 8.42 (t, J = 8.3 Hz, 1H) , 8.16 (s, 1H), 8.08 (dt, J = 9.4, 2.5 Hz, 2H), 7.96 (dd, J = 8.6, 1.5 Hz, 1H), 7.52 (d, J = 8.6 Hz, 2H), 6.7- 7.0 (m, 1H), 3.42-3.59 (m, 2H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 576.15 (MH)+. 102 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl )Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.75 (d, J = 2.1 Hz, 2H), 8.60 (s, 1H), 8.51 (d, J = 8.3 Hz, 1H), 8.27 (dd, J = 8.6, 1.5 Hz, 1H), 8.05-8.08 (m, 2H), 7.51 (d, J = 8.6 Hz, 2H), 6.74-7.00 (m, 1H), 3.49 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 575.7 (MH)+. 103 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.75-8.78 (m, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz , 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.07 (dd, J = 6.7, 2.1 Hz, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.74-7.00 (m, 1H) , 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 576.05 (MH)+ 104 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.76 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.10 (dt, J = 9.4, 2.5 Hz, 2H), 7.60 (d, J = 8.3 Hz, 2H ), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 544.0 (MH)+. 105 2-(3-(Ethylsulfonyl)-6-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.79 (s, 1H), 8.66 (d, J = 8.3 Hz, 1H), 8.54 (t, J = 4.1 Hz, 2H), 8.43 (dd, J = 8.3 , 1.8 Hz, 1H), 8.30-8.36 (m, 3H), 7.55 (d, J = 7.9 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H ); ESI MS (m/z) 543.9 (MH)+. 106 3-(5-(4-Bromophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.3 Hz, 1H), 8.82 (d, J = 2.2 Hz, 1H), 8.70 (s, 1H), 8.43-8.46 (m, 1H) ), 8.17 (d, J = 3.9 Hz, 1H), 7.96-7.99 (m, 3H), 7.82-7.84 (m, 2H), 3.46-3.57 (m, 2H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 538.00, 540.00 [(MH)+ Br79, 81]. 107 3-(3-(Ethylsulfonyl)-5-(3-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazole Lin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.43 (d, J = 2.2 Hz, 1H), 8.89 (d, J = 2.2 Hz, 1H), 8.71 (s, 1H), 8.44 (d, J = 8.3 Hz, 1H), 8.28 (dd, J = 11.5, 2.2 Hz, 1H), 8.17 (s, 1H), 7.98 (d, J = 8.6 Hz, 2H), 7.84 (t, J = 7.8 Hz, 1H), 3.47-3.59 (m, 2H), 1.21 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 562.05 (MH)+. 108 3-(3-(Ethylsulfonyl)-5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quine Oxazolin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 2.4 Hz, 1H), 8.70 (s, 1H), 8.44 (d, J = 8.3 Hz, 1H), 8.17 (s, 1H), 7.96-8.02 (m, 3H), 7.31 (dd, J = 6.8, 2.0 Hz, 2H), 4.91 (q, J = 8.9 Hz, 2H), 3.45-3.58 (m, 2H), 1.20 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 558.10 (MH)+. 109 3-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.24 (t, J = 2.2 Hz, 2H), 8.88 (d, J = 2.2 Hz, 1H), 8.69-8.73 (m, 2H), 3.39-3.54 (m , 2H), 1.05-1.22 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 462.80, 464.80 [(MH)+ Br79, 81]. 110 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidine-4( 3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.37-9.38 (m, 1H), 9.24 (t, J = 2.0 Hz, 1H), 8.69-8.82 (m, 3H), 7.99-8.03 (m, 2H) , 7.67-7.69 (m, 2H), 3.51 (ddd, J = 34.1, 14.1, 7.4 Hz, 2H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 495.0 (MH)+ . 111 3-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidine-4( 3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.2 Hz, 1H), 9.24 (d, J = 1.7 Hz, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.78 ( s, 1H), 8.70 (d, J = 1.5 Hz, 1H), 8.03-8.07 (m, 2H), 7.44-7.48 (m, 2H), 3.41-3.60 (m, 2H), 1.19 (q, J = 7.7 Hz, 3H); ESI MS (m/z) 479.0 (MH)+. 112 3-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Pyrido[3,2-d]pyrimidin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 9.25 (d, J = 1.7 Hz, 1H), 8.86 (dd, J = 19.0, 2.3 Hz, 1H), 8.79 (s, 1H), 8.71 (t, J = 1.0 Hz, 1H), 8.07-8.10 (m, 2H), 7.53 (d, J = 8.6 Hz, 2H), 6.87 (tt, J = 51.9, 3.0 Hz , 1H), 3.43-3.61 (m, 2H), 1.21 (q, J = 7.7 Hz, 3H); ESI MS (m/z) 577.0 (MH)+. 113 3-(3-(Ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2- d)Pyrimidine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.40-9.42 (m, 1H), 9.22-9.24 (m, 1H), 8.87 (d, J = 2.2 Hz, 1H), 8.76-8.77 (m, 1H) , 8.65-8.71 (m, 1H), 7.99-8.10 (m, 2H), 7.68-7.77 (m, 1H), 7.54-7.58 (m, 1H), 3.44-3.62 (m, 2H), 1.21(q, J = 7.7 Hz, 3H); ESI MS (m/z) 545.05 (MH)+. 114 2-(3-(Ethylsulfonyl)-5-(4-(perfluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.77 (t, J = 2.3 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.4 , 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.09-8.12 (m, 2H), 7.60 (d, J = 8.6 Hz, 2H), 3.50 (q, J = 7.2 Hz, 2H ), 1.17 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 594.10 (MH)+ 115 2-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.2 Hz, 1H), 8.78 (s, 1H), 8.53 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.6 Hz, 1H), 7.84 (dd, J = 8.8, 2.2 Hz, 2H), 7.43-7.48 (m, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 495.90 (MH)+. 116 2-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 0.5 Hz, 1H), 8.53 ( s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.12 (d, J = 2.0 Hz, 2H), 7.79 (t, J = 1.8 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 527.85 (MH)+. 117 2-(3-(Ethylsulfonyl)-5-(4-(perfluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -Thione 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.47 (dd, J = 8.3, 1.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.13 (dd, J = 6.7, 2.1 Hz, 2H), 7.60 (d, J = 8.9 Hz, 2H ), 3.46-3.60 (m, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 610.05 (MH)+ 118 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-thione 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.4 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.80 (d, J = 2.4 Hz, 1H), 8.47 (dd, J = 8.3, 1.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.09 (d, J = 8.6 Hz, 2H), 7.51 (d, J = 8.6 Hz, 2H), 6.73-6.99 (m, 1H), 3.46-3.60 (m, 2H), 1.15 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 591..90 (MH)+ 119 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.6 Hz, 1H), 8.54 ( s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34-8.36 (m, 2H), 8.27 (d, J = 7.8 Hz, 1H), 7.91 (d, J = 7.8 Hz, 1H ), 7.83 (t, J = 7.7 Hz, 1H), 3.52 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 527.95 (MH)+. 120 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.54 ( s, 1H), 8.42 (dd, J = 8.6, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.05 (s, 1H), 8.01 (d, J = 7.8 Hz, 1H), 7.74 (t, J = 8.1 Hz, 1H), 7.56 (d, J = 8.3 Hz, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H). ESI MS (m/z) 544.00 (MH)+. 121 4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)benzonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.19 (dd, J = 6.6, 2.0 Hz, 2H), 8.08 (dd, J = 6.6, 2.0 Hz , 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.15-1.19 (m, 3H) ESI MS (m/z) 484.95 (MH)+. 122 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.54 ( s, 1H), 8.43 (dd, J = 8.2, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.20 (d, J = 8.1 Hz, 2H), 7.96 (d, J = 8.3 Hz, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16-1.19 (m, 3H) ESI MS (m/z) 527.95 (MH)+. 123 2-(5-(3,4-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.2 Hz, 1H), 8.77-8.78 (m, 2H), 8.54 (s, 1H), 8.43 (dd, J = 8.3, 2.0 Hz , 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.19 (ddd, J = 11.7, 7.8, 2.2 Hz, 1H), 7.84-7.87 (m, 1H), 7.65-7.72 (m, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 495.75 (MH)+. 124 2-(5-Cyclopropyl-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (d, J = 2.4 Hz, 1H), 8.72 (s, 1H), 8.51 (s, 1H), 8.40 (d, J = 9.8 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 8.16 (d, J = 2.4 Hz, 1H), 3.35-3.41 (m, 2H), 2.24-2.32 (m, 1H), 1.15-1.20 (m, 2H) , 1.11 (t, J = 7.3 Hz, 3H), 0.99-1.02 (m, 2H) ESI MS (m/z) 423.95 (MH)+. 125 1-(4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenyl )Cyclopropane-1-carbonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.29 (d, J = 2.4 Hz, 1H), 8.75 (s, 1H), 8.70 (d, J = 2.2 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.4, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 7.96 (dd, J = 6.6, 2.0 Hz, 2H), 7.52 (dd, J = 6.6, 2.0 Hz , 2H), 3.46 (t, J = 7.5 Hz, 2H), 1.82 (dd, J = 7.7, 4.8 Hz, 2H), 1.60 (dd, J = 8.2, 5.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 524.95 (MH)+. 126 2-(5-(4-(Difluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 2.2 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.4 , 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.11 (d, J = 8.3 Hz, 2H), 7.79 (d, J = 8.1 Hz, 2H), 7.15 (t, J = 55.8 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 509.95 (MH)+. 127 2-(5-(Ethylsulfonyl)-6'-fluoro-[3,3'-dipyridine]-6-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.84 (dd, J = 8.7, 2.6 Hz, 2H), 8.78 (d, J = 0.5 Hz, 1H), 8.60 (td, J = 8.2, 2.4 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.4, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.44 (dd , J = 8.6, 2.2 Hz, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 478.95 (MH)+. 128 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -Thione 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (dd, J = 6.4, 2.1 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.81 (d, J = 2.1 Hz, 1H ), 8.47 (dd, J = 8.3, 1.5 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.09-8.13 (m, 2H), 7.60 (d, J = 7.9 Hz, 2H), 3.44 -3.61 (m, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 560 (MH)+ 129 2-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.17 (s, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.41 (d, J = 8.9 Hz, 1H), 8.31 (d, J = 8.9 Hz, 1H), 3.44-3.52 (m, 2H), 2.64 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 475.55, 477.65 [(MH)+ Br79, 81] 130 2-(3-(Ethylsulfonyl)-5-(4-(methylthio)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.29-9.30 (m, 1H), 8.77 (s, 1H), 8.70 (d, J = 2.2 Hz, 1H), 8.54 (s, 1H), 8.42 (dd , J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.89-7.92 (m, 2H), 7.46 (dd, J = 6.7, 1.8 Hz, 2H), 3.49 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 505.75 (MH)+. 131 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.28 (d, J = 2.1 Hz, 1H), 8.70 (d, J = 2.4 Hz, 1H), 8.55 (s, 1H), 8.41 (dd, J = 8.6 , 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.02 (dd, J = 8.6, 5.5 Hz, 2H), 7.44 (t, J = 8.7 Hz, 2H), 3.47-3.52 (m , 2H), 2.66 (s, 3H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 492.10 (MH)+ 132 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (dd, J = 7.0, 2.4 Hz, 1H), 9.13 (s, 1H), 8.97 (s, 1H), 8.77-8.79 (m, 1H), 8.43 -8.48 (m, 1H), 8.39 (d, J = 8.3 Hz, 1H), 7.99-8.03 (m, 2H), 7.66 (dd, J = 6.7, 1.8 Hz, 2H), 3.44-3.62 (m, 2H ), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 509.80 (MH)+ 133 2-(5-(3,4-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.2 Hz, 1H), 8.81 (d, J = 2.1 Hz, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.42 (d, J = 6.8 Hz, 1H), 8.33-8.35 (m, 2H), 7.98 (dd, J = 8.3, 2.2 Hz, 1H), 7.86 (d, J = 8.6 Hz, 1H), 3.51 (d , J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 527.90 (MH)+. 134 2-(5-(3-chloro-5-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.38 (d, J = 2.2 Hz, 1H), 8.85 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.55 ( s, 1H), 8.44 (dd, J = 8.3, 1.5 Hz, 1H), 8.36 (d, J = 8.1 Hz, 1H), 8.03 (t, J = 1.6 Hz, 1H), 7.96 (dt, J = 9.6 , 2.0 Hz, 1H), 7.65 (dt, J = 8.6, 2.0 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.19 (t, J = 7.5 Hz, 3H) ESI MS (m/z ) 511.85 (MH)+. 135 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-4-methyl-7- (Trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.2 Hz, 1H), 8.75 (d, J = 2.4 Hz, 1H), 8.58 (s, 1H), 8.33-8.45 (m, 2H ), 8.08 (dd, J = 6.6, 2.2 Hz, 2H), 7.53 (d, J = 8.8 Hz, 2H), 6.75-7.01 (m, 1H), 3.52 (q, J = 7.5 Hz, 2H), 2.68 (s, 3H), 1.20 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 590.10 (MH)+ 136 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine -1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.4 Hz, 1H), 8.74 (d, J = 2.4 Hz, 1H), 8.56 (s, 1H), 8.40-8.43 (m, 1H ), 8.32 (d, J = 8.3 Hz, 1H), 8.09 (dd, J = 6.7, 2.1 Hz, 2H), 7.60 (d, J = 7.9 Hz, 2H), 3.50 (q, J = 7.5 Hz, 2H ), 2.66 (s, 3H), 1.18 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 557.75 (MH)+ 137 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione 1H-NMR (400 MHz, DMSO-d6) δ 9.32-9.34 (m, 1H), 9.14 (s, 1H), 8.99 (s, 1H), 8.79 (d, J = 2.4 Hz, 1H), 8.48 (dd , J = 8.3, 1.7 Hz, 1H), 8.41 (d, J = 8.3 Hz, 1H), 8.05-8.09 (m, 2H), 7.43-7.48 (m, 2H), 3.46-3.63 (m, 3H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 493.90 (MH)+ 138 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)nicotinonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.47 (d, J = 2.2 Hz, 1H), 9.14 (d, J = 2.0 Hz, 1H), 8.80 (d, J = 0.7 Hz, 1H), 8.52 ( s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.48 (q, J = 7.4 Hz, 2H), 1.15 (t = 7.3 Hz, 3H); ESI MS (m/z) 408.70 (MH)+ 139 2-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.4 Hz, 1H), 8.58 (s, 1H), 8.43 (dd, J = 8.7 , 1.8 Hz, 1H), 8.34 (d, J = 8.6 Hz, 1H), 8.13 (d, J = 1.7 Hz, 2H), 7.81 (t, J = 1.8 Hz, 1H), 3.54 (q, J = 7.1 Hz, 2H), 2.68 (s, 3H), 1.19 (t = 7.3 Hz, 3H); ); ESI MS (m/z) 541.75, 543.75 [(MH)+ Cl35 140 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (t, J = 2.1 Hz, 1H), 8.74 (t, J = 2.1 Hz, 1H), 8.57 (s, 1H), 8.33-8.45 (m, 2H ), 8.00-8.02 (m, 2H), 7.62-7.69 (m, 2H), 3.54 (q, J = 7.1 Hz, 2H), 2.68 (s, 3H), 1.19 (t = 7.3 Hz, 3H); ESI MS (m/z) 507.70 (MH)+ 141 2-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.36 (d, J = 2.2 Hz, 1H), 8.81 (d, J = 2.2 Hz, 1H), 8.59 (d, J = 9.0 Hz, 1H), 8.33- 8.45 (m, 2H), 7.82-7.87 (m, 2H), 7.46 (tt, J = 9.3, 2.3 Hz, 1H), 3.51-3.58 (m, 2H), 2.68 (s, 3H), 1.19 (q, J = 7.3 Hz, 3H); ESI MS (m/z) 510.10 (MH)+ 142 2-(5-(4-chloro-3-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.6 Hz, 1H), 8.77 (s, 1H), 8.53 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.16 (dd, J = 10.6, 2.1 Hz, 1H), 7.87 (dd, J = 8.6, 2.0 Hz , 1H), 7.82 (t, J = 7.9 Hz, 1H), 3.50 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 511.65 (MH) +. 143 2-(5-(2-Chloro-5-(trifluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.15 (d, J = 2.2 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.73 (d, J = 2.2 Hz, 1H), 8.55 ( d, J = 1.0 Hz, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.19 (t, J = 1.0 Hz, 1H), 7.92- 7.97 (m, 2H), 3.47 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 561.90 (MH)+. 144 3-chloro-5-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)benzene Acetonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.40 (d, J = 2.2 Hz, 1H), 8.91 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.54 (t, J = 1.6 Hz, 2H), 8.49 (t, J = 1.8 Hz, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.21 (dd, J = 1.8 , 1.3 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.2 Hz, 3H) ESI MS (m/z) 518.70 (MH)+. 145 2-(3-(Ethylsulfonyl)-5-(2-fluoro-5-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.22 (t, J = 1.8 Hz, 1H), 8.79 (s, 1H), 8.75 (q, J = 1.1 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.2, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.00-8.02 (m, 1H), 7.62-7.64 (m, 2H), 3.48 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 561.75(MH)+. 146 2-(5-(4-chloro-2-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.19 (q, J = 1.3 Hz, 1H), 8.79 (s, 1H), 8.71 (q, J = 1.1 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.4, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.92 (t, J = 8.4 Hz, 1H), 7.73 (dd, J = 10.6, 2.1 Hz, 1H) ), 7.55 (dd, J = 8.3, 2.4 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 511.90 (MH) +. 147 2-(5-(4-Bromophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.31 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.74 (d, J = 2.2 Hz, 1H), 8.54 (s, 1H), 8.41-8.43 (m, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.92-7.94 (m, 2H), 7.80 (dd, J = 6.7, 2.1 Hz, 2H), 3.50 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 539.90(MH)+. 148 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2 -Ethyl methyl propionate 1H-NMR (400 MHz, DMSO-d6) δ 8.73 (s, 1H), 8.59 (d, J = 2.8 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H ), 8.32 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 2.8 Hz, 1H), 4.22 (q, J = 7.0 Hz, 2H), 3.39 (q, J = 7.3 Hz, 2H), 1.67 (d, J = 14.7 Hz, 6H), 1.20 (t, J = 7.2 Hz, 3H), 1.11 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 514.05 (MH)+. 149 2-(4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenoxy Yl)-2,2-difluoro-N,N-dimethylacetamide 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.1 Hz, 1H), 8.78 (s, 1H), 8.74 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.05 (dt, J = 9.4, 2.5 Hz, 2H), 7.51 (d, J = 8.6 Hz, 2H ), 3.46-3.52 (m, 2H), 3.26 (d, J = 8.3 Hz, 3H), 2.98 (s, 3H), 1.13-1.18 (m, 4H) ESI MS (m/z) 597.05 (MH)+ . 150 2-(3-(Ethylsulfonyl)-5-(3,3,3-trifluoropropyl-1-en-2-yl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.14 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.53-8.55 (m, 2H), 8.43 (dd, J = 8.3, 1.8 Hz , 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.62 (t, J = 1.5 Hz, 1H), 6.50 (d, J = 1.2 Hz, 1H), 3.44-3.53 (m, 2H), 1.10 -1.19 (m, 3H) ESI MS (m/z) 477.95 (MH)+. 151 2-(3-(Ethylsulfonyl)-5-(4-(2,2,3,3,3-pentafluoropropoxy)phenyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.29 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.70 (d, J = 2.4 Hz, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.97 (dd, J = 6.9, 2.0 Hz, 2H), 7.29 (d, J = 8.9 Hz, 2H ), 4.97 (t, J = 13.3 Hz, 2H), 3.49 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 608.00 (MH)+. 152 2-(5-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)-3-(ethylsulfonyl)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.4 Hz, 1H), 8.82 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 0.5 Hz, 1H), 8.54 ( s, 1H), 8.43 (dd, J = 8.6, 2.0 Hz, 1H), 8.35 (d, J = 8.6 Hz, 1H), 7.79 (dd, J = 8.1, 1.0 Hz, 1H), 7.59 (dd, J = 8.1, 1.0 Hz, 1H), 7.44 (t, J = 8.1 Hz, 1H), 3.46-3.51 (m, 3H), 1.22 (s, 0H), 1.17 (t, J = 7.5 Hz, 4H) ESI MS (m/z) 539.80 (MH)+. 153 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)acetonitrile 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 3.1 Hz, 1H), 8.74 (s, 1H), 8.51 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H ), 8.32 (d, J = 8.3 Hz, 1H), 8.21 (d, J = 2.8 Hz, 1H), 5.52 (s, 2H), 3.36-3.44 (m, 2H), 1.11 (dt, J = 23.8, 7.2 Hz, 3H) ESI MS (m/z) 438.70 (MH)+. 154 2-(3-(Ethylsulfonyl)-5-(1,1,2,3,3,3-hexafluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.09 (d, J = 2.4 Hz, 1H), 8.78 (s, 1H), 8.52 (s, 1H), 8.50 (d, J = 2.8 Hz, 1H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.63 (dq, J = 41.3, 6.1 Hz, 1H), 3.46-3.53 (m, 2H), 1.15 (q, J = 7.3 Hz, 3H) ESI MS (m/z) 549.75 (MH)+. 155 2-(3-(Ethylsulfonyl)-5-(4-hydroxyphenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.94 (s, 1H), 9.22 (d, J = 2.4 Hz, 1H), 8.76 (s, 1H), 8.61 (d, J = 2.4 Hz, 1H), 8.53 (s, 1H), 8.41 (dd, J = 8.4, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.79 (d, J = 8.6 Hz, 2H), 6.95-6.97 (m , 2H), 3.47 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 475.75 (MH)+. 156 2-(3-(Ethylsulfonyl)-5-hydroxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 11.36 (s, 1H), 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.8 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.80 (d, J = 2.8 Hz, 1H), 3.37 (q, J = 6.8 Hz, 2H), 1.06-1.13 (m, 4H ) ESI MS (m/z) 399.95 (MH)+. 157 2-(5-(2-chloro-4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.09 (d, J = 2.1 Hz, 1H), 8.79 (s, 1H), 8.63 (d, J = 2.4 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.4, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.82 (dd, J = 8.6, 6.1 Hz, 1H), 7.74 (dd, J = 8.9, 2.8 Hz , 1H), 7.47 (td, J = 8.5, 2.5 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 511.95 ( MH)+. 158 2-(3-(Ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.31-9.35 (m, 1H), 8.78 (d, J = 2.0 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz , 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.96 (d, J = 7.8 Hz, 1H), 7.90 (d, J = 2.0 Hz, 1H), 7.71 (t, J = 7.9 Hz, 1H ), 7.48 (d, J = 8.3 Hz, 1H), 6.86 (tt, J = 51.8, 3.0 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H ) ESI MS (m/z) 576.05 (MH)+. 159 5'-(Ethylsulfonyl)-6'-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)-[2,3'-dipyridine]-5 -Formonitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.71 (d, J = 2.2 Hz, 1H), 9.26 (q, J = 1.0 Hz, 1H), 9.19 (d, J = 2.4 Hz, 1H), 8.78 ( d, J = 8.6 Hz, 1H), 8.57-8.60 (m, 2H), 8.53 (d, J = 8.8 Hz, 1H), 8.42-8.45 (m, 1H), 8.35 (d, J = 8.3 Hz, 1H ), 3.44-3.52 (m, 2H), 1.11-1.18 (m, 3H) ESI MS (m/z) 486.05 (MH)+. 160 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)pyrimidine-5-methyl Nitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.85 (d, J = 2.2 Hz, 1H), 9.55 (d, J = 5.4 Hz, 2H), 9.33 (d, J = 2.2 Hz, 1H), 8.81 ( s, 1H), 8.54 (s, 1H), 8.44 (dd, J = 8.4, 1.8 Hz, 1H), 8.36 (d, J = 8.3 Hz, 1H), 3.50 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 487.00 (MH)+. 161 2-(3-(Ethylsulfonyl)-5-(2,2,2-trifluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 3.1 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.2, 1.9 Hz, 1H ), 8.32 (d, J = 8.3 Hz, 1H), 8.20 (d, J = 3.1 Hz, 1H), 5.16 (q, J = 8.8 Hz, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 481.95 (MH)+ 162 2-(3-(Ethylsulfonyl)-5-(2,2,3,3,3-pentafluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (d, J = 3.1 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.39-8.42 (m, 1H), 8.32 (d , J = 8.3 Hz, 1H), 8.22 (d, J = 3.1 Hz, 1H), 5.26 (t, J = 13.8 Hz, 2H), 3.41 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 531.95 (MH)+ 163 2-(3-(Ethylsulfonyl)-5-(3-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.34 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 2.2 Hz, 2H), 8.54 (s, 1H), 8.42 (dd, J = 8.6 , 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 7.91 (dt, J = 10.2, 2.1 Hz, 1H), 7.82 (dq, J = 7.8, 0.8 Hz, 1H), 7.64 (td , J = 8.0, 6.2 Hz, 1H), 7.37-7.42 (m, 1H), 3.51 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 478.05 (MH)+. 164 2-(3-(Ethylsulfonyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.25 (d, J = 2.2 Hz, 1H), 8.78 (d, J = 2.4 Hz, 2H), 8.54 (s, 1H), 8.43 (dd, J = 8.2 , 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.36 (s, 1H), 4.08 (s, 3H), 3.48 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 532.00 (MH)+. 165 2-(3-(Ethylsulfonyl)-5-(pyrimidin-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.2 Hz, 1H), 9.40 (s, 2H), 9.33 (s, 1H), 8.95 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.54 (s, 1H), 8.43 (dd, J = 8.2, 1.6 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.50 (q, J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 462.00 (MH)+. 166 2-(3-(Ethylsulfonyl)-5-methylpyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 1.5 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.39-8.41 (m, 2H), 8.32 (d , J = 8.6 Hz, 1H), 3.36 (q, J = 7.3 Hz, 2H), 2.53 (s, 3H), 1.06-1.13 (t, 3H) ESI MS (m/z) 397.95 (MH)+. 167 2-(3-(Ethylsulfonyl)-5-((methylthio)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.72 (d, J = 2.8 Hz, 2H), 8.51 (s, 1H), 8.40 (d, J = 8.3 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 8.12 (d, J = 2.8 Hz, 1H), 5.62 (s, 2H), 3.34-3.42 (m, 2H), 2.23-2.27 (m, 3H), 1.13 (t, J = 7.3 Hz , 3H), 1.06 (s, 0H) ESI MS (m/z) 460.00 (MH)+. 168 2-(5-(Cyclopropylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.71 (s, 1H), 8.66 (d, J = 2.8 Hz, 1H), 8.50 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H ), 8.31 (d, J = 8.3 Hz, 1H), 7.97 (d, J = 3.1 Hz, 1H), 4.14 (d, J = 7.0 Hz, 2H), 3.35-3.42 (m, 2H), 1.26-1.33 (m, 1H), 1.12 (t, J = 7.5 Hz, 3H), 0.61-0.65 (m, 2H), 0.41 (td, J = 5.3, 3.9 Hz, 2H) ESI MS (m/z) 454.00 (MH )+. 169 3-(5-Bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.66 (d, J = 2.1 Hz, 1H), 8.58 (d, J = 8.3 Hz, 2H), 8.54 (dd, J = 8.6, 1.8 Hz, 1H), 8.41 (d, J = 2.1 Hz, 1H), 3.10 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 432.85 (MH)+. 170 3-(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.28 (d, J = 2.4 Hz, 1H), 8.94 (d, J = 2.2 Hz, 1H), 8.60 (d, J = 8.1 Hz, 2H), 8.55 ( dd, J = 8.6, 2.0 Hz, 1H), 3.47 (q, J = 7.4 Hz, 2H), 1.13 (t, J = 7.4 Hz, 3H) ESI MS (m/z) 464.85 (MH)+. 171 2-(5-((Dimethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.44 (d, J = 2.7 Hz, 1H), 8.39 (dd, J = 8.4, 1.8 Hz, 1H ), 8.31 (d, J = 8.3 Hz, 1H), 7.88 (d, J = 2.7 Hz, 1H), 3.41-3.46 (m, 6H), 3.36 (q, J = 7.2 Hz, 2H), 1.12 (t , J = 7.5 Hz, 3H) ESI MS (m/z) 474.95 (MH)+. 172 2-(3-(Ethylsulfonyl)-5-((methylsulfonyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.86 (d, J = 2.9 Hz, 1H), 8.73 (d, J = 0.5 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3 , 1.5 Hz, 1H), 8.35 (d, J = 2.9 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 5.71 (s, 2H), 3.40 (q, J = 7.3 Hz, 2H), 3.17 (s, 3H), 1.11-1.16 (t, 3H) ESI MS (m/z) 491.70 (MH)+. 173 2-(4-(Ethylsulfonyl)-6-(3-(trifluoromethyl)phenyl)pyridazin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.09 (d, J = 19.6 Hz, 1H), 8.89 (d, J = 0.6 Hz, 1H), 8.58-8.71 (m, 3H), 8.48 (dd, J = 8.3, 1.5 Hz, 1H), 8.39 (d, J = 8.3 Hz, 1H), 8.05 (d, J = 7.8 Hz, 1H), 7.92 (t, J = 7.8 Hz, 1H), 3.75 (q, J = 7.2 Hz, 2H), 1.22 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.85 (MH)+ 174 2-(3-(Ethylsulfonyl)-5-(oxetan-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.68-9.02 (m, 1H), 8.59-8.62 (m, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H) , 8.33 (d, J = 8.3 Hz, 1H), 7.87-7.98 (m, 1H), 5.64-5.69 (m, 1H), 4.90-5.04 (m, 2H), 4.68 (dd, J = 7.8, 4.4 Hz , 2H), 3.42 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 456.05 (MH)+ 175 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2 -Methylpropionamide 1H-NMR (400 MHz, DMSO-d6) δ 10.60 (s, 1H), 9.27 (d, J = 2.7 Hz, 1H), 9.02 (d, J = 2.4 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.4, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 5.91 (s, 1H), 3.35 (q, J = 7.4 Hz, 2H ), 1.40 (s, 6H), 1.13 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 485.05 (MH)+. 176 2-(3-(Ethylsulfonyl)-6-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.79 (d, J = 0.5 Hz, 1H), 8.61-8.66 (m, 1H), 8.51-8.54 (m, 2H), 8.43 (dd, J = 8.4, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.29 (dt, J = 9.5, 2.5 Hz, 2H), 7.47 (d, J = 8.8 Hz, 2H), 6.84 (tt, J = 51.8, 2.9 Hz, 1H), 3.43 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 576.00 (MH)+. 177 2-(5-((Diethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.7 Hz, 1H), 8.39 (dd, J = 8.3, 1.7 Hz, 1H ), 8.30 (d, J = 8.3 Hz, 1H), 7.92 (d, J = 2.7 Hz, 1H), 3.51 (q, J = 7.4 Hz, 4H), 3.35 (t, J = 7.3 Hz, 2H), 1.32 (t, J = 7.3 Hz, 6H), 1.11 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 502.80 (MH)+. 178 2-(5'-(Ethylsulfonyl)-4-(trifluoromethyl)-[2,3'-dipyridine]-6'-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.75 (d, J = 2.4 Hz, 1H), 9.24 (d, J = 2.2 Hz, 1H), 9.09 (d, J = 5.1 Hz, 1H), 8.79 ( d, J = 0.5 Hz, 1H), 8.76 (s, 1H), 8.56 (d, J = 10.0 Hz, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.95 (dd, J = 5.0, 0.9 Hz, 1H), 3.49 (q, J = 7.3 Hz, 2H), 1.14-1.19 (m, 3H) ESI MS (m/z) 528.80 (MH) +. 179 2-(5'-(Ethylsulfonyl)-5-(trifluoromethyl)-[2,3'-dipyridine]-6'-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.72 (d, J = 2.2 Hz, 1H), 9.20-9.22 (m, 2H), 8.80 (s, 1H), 8.59 (d, J = 8.3 Hz, 1H) ), 8.54 (s, 1H), 8.50 (dd, J = 8.6, 2.2 Hz, 1H), 8.43 (dd, J = 8.4, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 3.49 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 528.95 (MH)+. 180 2-(5-(3-(benzyloxy)cyclobutoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.73 (s, 1H), 8.61 (dd, J = 7.1, 2.9 Hz, 1H), 8.52 (s, 1H), 8.40-8.43 (m, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.88 (dd, J = 12.5, 2.9 Hz, 1H), 7.31-7.38 (m, 5H), 4.85-5.24 (m, 1H), 4.46 (s, 2H), 3.85-4.35(m, 1H), 3.4 (m, 2H), 2.9 (m, 1H), 2.45 -2.65(m, 2H) 2.06 (m, 1H), 1.15 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 560.10 (MH)+ 181 2-(5-(3-chloro-4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.33 (d, J = 2.4 Hz, 1H), 8.77-8.79 (m, 2H), 8.53 (d, J = 1.0 Hz, 1H), 8.42 (dd, J = 8.4, 1.8 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 8.30 (dd, J = 7.0, 2.3 Hz, 1H), 8.01 (qd, J = 4.4, 2.4 Hz, 1H), 7.65 (t, J = 8.9 Hz, 1H), 3.50 (q, J = 7.4 Hz, 2H), 1.15-1.19 (t, 3H) ESI MS (m/z) 512.05 (MH)+. 182 3-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]tri Oxazin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.84 (d, J = 2.2 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.7, 1.8 Hz, 1H), 8.05-8.10 (m, 2H), 7.43-7.49 (m, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H) ;ESI MS (m/z) 478.95 (MH)+. 183 2-(3-(Ethylsulfonyl)-5-(2-methoxypyrimidin-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.35 (d, J = 2.4 Hz, 1H), 9.20 (s, 2H), 8.86 (d, J = 2.4 Hz, 1H), 8.77 (d, J = 0.7 Hz, 1H), 8.53 (s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 4.01 (s, 3H), 3.48 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 492.05 (MH)+. 184 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile 1H-NMR (400 MHz, DMSO-d6) δ 8.98 (d, J = 2.2 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.58 (d, J = 2.2 Hz, 1H), 8.52 ( s, 1H), 8.42 (dd, J = 8.3, 1.7 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 4.38 (s, 2H), 3.36-3.43 (m, 2H), 1.13 (t , J = 7.3 Hz, 3H) ESI MS (m/z) 423 (MH)+. 185 2-(5-Bromo-3-(ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (d, J = 0.5 Hz, 1H), 8.55 (d, J = 2.0 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.2 , 1.6 Hz, 1H), 8.29-8.32 (m, 2H), 3.06 (q, J = 7.3 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 429.85 (MH) +. 186 3-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1 ,2,3)triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.2 Hz, 1H), 8.88 (d, J = 2.4 Hz, 1H), 8.60-8.63 (m, 2H), 8.55-8.57 (m , 1H), 8.14 (d, J = 8.8 Hz, 2H), 7.62 (d, J = 8.1 Hz, 2H), 3.51 (q, J = 7.5 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H ); ESI MS (m/z) 545.00 (MH)+. 187 3-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl )Benzo[d][1,2,3]triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.42 (d, J = 2.2 Hz, 1H), 8.88 (d, J = 2.2 Hz, 1H), 8.61 (dd, J = 5.1, 3.4 Hz, 2H), 8.56 (dd, J = 8.7, 1.8 Hz, 1H), 8.11 (dt, J = 9.3, 2.6 Hz, 2H), 7.52 (d, J = 8.8 Hz, 2H), 6.73-7.00 (m, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 577.00 (MH)+ 188 3-(3-(ethylthio)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine- 4(3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (d, J = 2.2 Hz, 1H), 8.58-8.61 (m, 2H), 8.55 (dd, J = 8.7, 2.1 Hz, 1H), 8.32 (d , J = 2.2 Hz, 1H), 7.96-7.99 (m, 2H), 7.39-7.43 (m, 2H), 3.15 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ;ESI MS (m/z) 447.00 (MH)+ 189 3-(5-(4-chlorophenyl)-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine- 4(3H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (d, J = 2.2 Hz, 1H), 8.60 (d, J = 10.8 Hz, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 8.34 (d, J = 2.2 Hz, 1H), 7.95 (dd, J = 6.6, 2.0 Hz, 2H), 7.64 (dd, J = 6.6, 2.2 Hz, 2H), 3.16 (q, J = 7.3 Hz, 2H) ), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 463.00 (MH)+ 190 2-(5-(2-Bromo-1,1,2,2-tetrafluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.17 (d, J = 2.7 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H), 8.59 (d, J = 2.7 Hz, 1H), 8.52 ( s, 1H), 8.43 (dd, J = 8.3, 1.7 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.51 (q, J = 7.4 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 579.90 (MH)+. 191 3-(3-(ethylthio)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2 ,3)Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.82 (d, J = 2.2 Hz, 1H), 8.59-8.62 (m, 2H), 8.55 (dd, J = 8.6, 2.0 Hz, 1H), 8.36 (d , J = 2.2 Hz, 1H), 8.03-8.06 (m, 2H), 7.56-7.58 (m, 2H), 3.16 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H) ;ESI MS (m/z) 513.00 (MH)+ 192 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3] three Oxazin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.41 (d, J = 2.1 Hz, 1H), 8.87 (d, J = 2.1 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.6, 1.8 Hz, 1H), 8.05 (dd, J = 6.6, 2.0 Hz, 2H), 7.68 (dd, J = 6.7, 2.1 Hz, 2H), 3.51 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 494.94 (MH)+ 193 3-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2, 3) Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (d, J = 2.4 Hz, 1H), 8.96 (d, J = 2.4 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.6, 1.8 Hz, 1H), 8.16 (d, J = 1.8 Hz, 2H), 7.82 (t, J = 1.8 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.85 (MH)+ 194 3-(5-(3,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2, 3) Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (d, J = 2.2 Hz, 1H), 8.94 (d, J = 2.2 Hz, 1H), 8.61 (dd, J = 5.3, 3.3 Hz, 2H), 8.56 (dd, J = 8.8, 1.7 Hz, 1H), 7.85-7.90 (m, 2H), 7.47 (tt, J = 9.3, 2.3 Hz, 1H), 3.53 (q, J = 7.3 Hz, 2H), 1.16 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 496.90 (MH)+ 195 3-(5-(3-chloro-5-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2 ,3)Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.46 (d, J = 2.2 Hz, 1H), 8.95 (d, J = 2.2 Hz, 1H), 8.60-8.62 (m, 2H), 8.56 (dd, J = 8.6, 1.7 Hz, 1H), 8.05 (d, J = 1.7 Hz, 1H), 7.99 (dt, J = 9.5, 1.8 Hz, 1H), 7.65 (dt, J = 8.6, 2.1 Hz, 1H), 3.53 (q, J = 7.2 Hz, 2H), 1.16 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 512.90 (MH)+ 196 3-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1, 2,3]Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.48 (d, J = 2.2 Hz, 1H), 8.98 (d, J = 2.4 Hz, 1H), 8.61-8.63 (m, 2H), 8.56 (dd, J = 8.6, 2.0 Hz, 1H), 8.39 (s, 1H), 8.31 (d, J = 7.8 Hz, 1H), 7.93 (d, J = 7.8 Hz, 1H), 7.85 (t, J = 7.8 Hz, 1H ), 3.53 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 528.95 (MH)+ 197 2-(5-((4,4-Difluorobut-3-en-1-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.71 (s, 1H), 8.67 (d, J = 2.9 Hz, 1H), 8.50 (s, 1H), 8.40 (dd, J = 8.4, 1.8 Hz, 1H ), 8.31 (d, J = 8.3 Hz, 1H), 8.00 (d, J = 2.9 Hz, 1H), 4.67 (dtd, J = 26.8, 7.8, 2.5 Hz, 1H), 4.32 (t, J = 6.2 Hz , 2H), 3.40 (q, J = 7.4 Hz, 2H), 2.52 (s, 1H), 2.45 (s, 1H), 1.12 (t, J = 7.5 Hz, 3H), ESI MS (m/z) 490 (MH)+ 198 2-(3-(ethylthio)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (s, 1H), 8.71 (d, J = 2.1 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.3, 1.5 Hz, 1H ), 8.32 (d, J = 8.3 Hz, 1H), 8.25 (d, J = 2.1 Hz, 1H), 7.96-7.99 (m, 2H), 7.46 (d, J = 8.6 Hz, 2H), 6.72-6.99 (m, 1H), 3.12 (q, J = 7.3 Hz, 2H), 1.18 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 544.05 (MH)+ 199 2-(3-(Ethylsulfonyl)-5-(1-methyl-1H-pyrazol-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.20 (d, J = 2.1 Hz, 1H), 8.78 (s, 1H), 8.67 (d, J = 2.1 Hz, 1H), 8.54 (d, J = 0.9 Hz, 1H), 8.43 (dd, J = 8.3, 1.8 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 7.61 (d, J = 1.8 Hz, 1H), 6.83 (d, J = 1.8 Hz, 1H), 4.01 (s, 3H), 3.49 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 464.05 (MH)+ 200 2-(3-(Ethylsulfonyl)-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.21 (d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 8.63 (d, J = 2.2 Hz, 1H), 8.56 (s, 1H), 8.52 (s, 1H), 8.41 (d, J = 8.3 Hz, 1H), 8.33 (d, J = 8.1 Hz, 1H), 8.22 (s, 1H), 3.92 (s, 3H), 3.43 (q, J = 7.6 Hz, 2H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 464.00 (MH)+ 201 2-(3-(Ethylsulfonyl)-5-(3-fluoro-5-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.41 (d, J = 2.2 Hz, 1H), 8.90 (d, J = 2.2 Hz, 1H), 8.78 (s, 1H), 8.54 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.25-8.28 (m, 2H), 7.88 (d, J = 8.6 Hz, 1H), 3.52 (q , J = 7.4 Hz, 2H), 1.18 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 546.00 (MH)+ 202 1-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1- Formonitrile 1H-NMR (400 MHz, DMSO-d6) δ 8.93 (d, J = 2.4 Hz, 1H), 8.75 (d, J = 0.5 Hz, 1H), 8.51 (s, 1H), 8.40-8.42 (m, 2H ), 8.33 (d, J = 8.3 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.95-1.99 (m, 2H), 1.88-1.93 (m, 2H), 1.12-1.16 (t, J = 7.4 Hz, 3H); ESI MS (m/z) 449.05(MH)+ 203 2-(3-(Ethylsulfonyl)-5-(4-(methylsulfonyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.39 (d, J = 2.4 Hz, 1H), 8.83 (d, J = 2.1 Hz, 1H), 8.79 (s, 1H), 8.54 (d, J = 0.9 Hz, 1H), 8.43 (dd, J = 8.4, 1.7 Hz, 1H), 8.35 (d, J = 8.3 Hz, 1H), 8.23-8.26 (m, 2H), 8.11-8.14 (m, 2H), 3.46 -3.54 (m, 2H), 3.35 (s, 3H), 1.18 (t, J = 7.5 Hz, 3H); ESI MS (m/z) 537.95(MH)+ 204 2-(3-(Ethylthio)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.76 (s, 1H), 8.67-8.69 (m, 1H), 8.54 (d, J = 1.2 Hz, 1H), 8.41 (dd, J = 8.4, 1.8 Hz , 1H), 8.31-8.33 (m, 1H), 8.21 (d, J = 2.2 Hz, 1H), 7.91-7.98 (m, 2H), 7.36-7.42 (m, 2H), 3.11 (q, J = 7.3 Hz, 2H), 1.17 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 446.05 (MH)+ 205 (5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) ethyl phosphonate 1H-NMR (400 MHz, DMSO-d6) δ 8.91 (q, J = 1.3 Hz, 1H), 8.76 (s, 1H), 8.52 (s, 1H), 8.40-8.43 (m, 2H), 8.33 (d , J = 8.3 Hz, 1H), 4.18-4.28 (m, 2H), 3.43 (q, J = 7.3 Hz, 2H), 2.08-2.18 (m, 2H), 1.29 (t, J = 7.1 Hz, 3H) , 1.12-1.22 (m, 6H) ESI MS (m/z) 520 (MH)+ 206 2-(5-(Dimethylphosphoryl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (dd, J = 5.4, 2.0 Hz, 1H), 8.83 (dd, J = 10.0, 2.0 Hz, 1H), 8.78 (d, J = 0.5 Hz, 1H ), 8.53 (s, 1H), 8.43 (dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.90 (s , 3H), 1.87 (s, 3H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 460 (MH)+ 207 2-(3-(Ethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.23 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.69 (d, J = 2.1 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 8.01-8.04 (m, 2H), 7.51 (d, J = 8.9 Hz, 2H), 6.86 (tt , J = 52.0, 2.9 Hz, 1H), 4.61 (d, J = 38.8 Hz, 1H), 3.27 (q, J = 6.7 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m /z) 575.10 (MH)+ 208 2-(3-(Ethylsulfonyl)-5-((S-methylsulfonylimino)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 8.85 (dd, J = 7.1, 2.9 Hz, 1H), 8.73 (s, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz , 1H), 8.30-8.33 (m, 2H), 5.54 (d, J = 12.2 Hz, 1H), 5.45 (d, J = 12.0 Hz, 1H), 4.09 (s, 1H), 3.36-3.42 (q, J = 7.2 Hz, 2H), 3.02 (s, 3H), 1.08-1.18 (t, J = 7.3 HZ, 3H) ESI MS (m/z) 490.90 (MH)+ 209 2-(3-(Ethylsulfonylimino)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.20 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.66 (d, J = 2.4 Hz, 1H), 8.52 (s, 1H), 8.40 (dd, J = 8.3, 1.8 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.95-8.00 (m, 2H), 7.41-7.47 (m, 2H), 4.60 (d, J = 41.9 Hz, 1H), 3.28 (q, J = 7.3 Hz, 2H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 477.10 (MH)+ 210 2-(3-(Ethylsulfonyl)-5-(1,1,2,2-tetrafluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.10 (d, J = 2.4 Hz, 1H), 8.78 (d, J = 0.6 Hz, 1H), 8.53 (d, J = 2.4 Hz, 2H), 8.43 ( dd, J = 8.3, 1.5 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 6.98 (tt, J = 51.6, 3.0 Hz, 1H), 3.49 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 500.00 (MH)+ 211 2-(3-(Ethylsulfonyl)-5-(3-methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.32 (d, J = 2.4 Hz, 1H), 8.80 (d, J = 2.4 Hz, 2H), 8.55 (s, 1H), 8.43 (dd, J = 8.3 , 1.7 Hz, 1H), 8.35 (d, J = 8.1 Hz, 1H), 6.94 (s, 1H), 3.50 (q, J = 7.4 Hz, 2H), 2.55 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 532.00 (MH)+ 212 3-(3-(Ethylsulfonyl)-5-hydroxypyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 11.63 (s, 1H), 8.56-8.59 (m, 2H), 8.52-8.54 (m, 2H), 7.89 (d, J = 2.8 Hz, 1H), 3.34 (q, J = 7.3 Hz, 2H), 1.11 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 401.00 (MH)+ 213 3-(3-(Ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.58 (d, J = 8.9 Hz, 2H), 8.53 (td, J = 4.6, 1.5 Hz, 2H), 8.19 (dd, J = 8.1, 1.4 Hz, 1H ), 7.70 (dd, J = 8.1, 4.7 Hz, 1H), 3.02 (q, J = 7.2 Hz, 2H), 1.15 (t, J = 7.1 Hz, 3H); ESI MS (m/z) 352.95 (MH )+ 214 3-(3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.10 (dd, J = 4.9, 1.7 Hz, 1H), 8.71 (dd, J = 8.1, 1.7 Hz, 1H), 8.59-8.61 (m, 2H), 8.54 -8.56 (m, 1H), 8.07 (dd, J = 7.9, 4.8 Hz, 1H), 3.38 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.4 Hz, 3H); ESI MS (m /z) 384.95 (MH)+ 215 3-(5-((Diethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl) Benzo[d][1,2,3]triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.57 (dd, J = 5.3, 3.3 Hz, 2H), 8.51-8.54 (m, 2H), 7.98 (d, J = 2.7 Hz, 1H), 3.55 (q , J = 7.3 Hz, 4H), 3.34 (q, J = 7.3 Hz, 2H), 1.32-1.37 (m, 6H), 1.12 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 504.00 (MH)+ 216 2-(3-(Ethylsulfonyl)-5-(ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.87 (d, J = 2.1 Hz, 1H), 8.74 (s, 1H), 8.51 (d, J = 0.9 Hz, 1H), 8.40 (dd, J = 8.3 , 1.5 Hz, 1H), 8.32 (q, J = 2.8 Hz, 2H), 3.42 (q, J = 7.4 Hz, 2H), 3.27 (q, J = 7.3 Hz, 2H), 1.33 (t, J = 7.3 Hz, 3H), 1.13 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 443.95 (MH)+ 217 2-(5-(4-Fluorophenyl)-3-(N-methylethylsulfonylimino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.22 (d, J = 2.4 Hz, 1H), 8.74 (s, 1H), 8.53 (s, 2H), 8.41 (d, J = 8.3 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.99 (dd, J = 8.8, 5.4 Hz, 2H), 7.44 (t, J = 8.8 Hz, 2H), 3.35-3.44 (m, 2H), 2.43 (s , 3H), 1.09-1.14 (m, 3H) ESI MS (m/z) 491.10 (MH)+ 218 (5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) tert-butyl carbamate 1H-NMR (400 MHz, DMSO-d6) δ 10.30 (s, 1H), 8.87 (d, J = 2.4 Hz, 1H), 8.72 (d, J = 0.5 Hz, 1H), 8.68 (d, J = 2.4 Hz, 1H), 8.51 (s, 1H), 8.40 (dd, J = 8.3, 1.5 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 3.35 (q, J = 7.3 Hz, 2H), 1.52 (s, 9H), 1.12 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 499.00 (MH)+ 219 2-(5-((Ethyl(methyl)((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.70 (s, 1H), 8.50 (s, 1H), 8.45 (d, J = 2.7 Hz, 1H), 8.38-8.40 (m, 1H), 8.31 (d , J = 8.6 Hz, 1H), 7.90 (d, J = 2.7 Hz, 1H), 3.52-3.58 (m, 2H), 3.34-3.38 (m, 5H), 1.36 (t, J = 7.3 Hz, 3H) , 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 488.95 (MH)+ 220 3-(5-((Ethyl(isopropyl)((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-6-(tri Fluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.53-8.60 (m, 4H), 8.03 (d, J = 2.7 Hz, 1H), 3.74-3.81 (m, 1H), 3.55 (dd, J = 15.5, 7.2 Hz, 2H), 3.33-3.35 (m, 2H), 1.44 (d, J = 6.6 Hz, 3H), 1.39 (d, J = 6.6 Hz, 3H), 1.35 (t, J = 7.3 Hz, 3H) , 1.12 (t, J = 7.2 hz, 3H); ESI MS (m/z) 518.05 (MH)+ 221 5-(Ethylsulfonyl)-6-(4-oxo-6-(trifluoromethyl)benzo[d][1,2,3]triazine-3(4H)-yl)pyridine- Dimethyl 3-sulfamate 1H-NMR (400 MHz, DMSO-d6) δ 9.16 (d, J = 2.7 Hz, 1H), 8.67-8.72 (m, 1H), 8.61 (d, J = 8.8 Hz, 2H), 8.56 (dd, J = 8.4, 2.1 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 3.06 (s, 6H), 1.14 (t, J = 7.3 Hz, 3H); ESI MS (m/z) 507.95 (MH )+ 222 2-((5-(Ethylsulfonyl)-6-(4-oxo-6-(trifluoromethyl)benzo[d][1,2,3]triazine-3(4H)- (Yl)pyridin-3-yl)oxy)acetonitrile 1H-NMR (400 MHz, DMSO-d6) δ 8.90 (d, J = 2.9 Hz, 1H), 8.58-8.60 (m, 2H), 8.54 (dd, J = 8.6, 2.0 Hz, 1H), 8.33 (d , J = 2.9 Hz, 1H), 5.54 (s, 2H), 3.42 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 439.95 (MH) + 223 3-(3-(Ethylsulfonyl)-5-(2,2,2-trifluoroethoxy)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1 ,2,3)triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.90 (d, J = 2.8 Hz, 1H), 8.58-8.60 (m, 2H), 8.54 (dd, J = 8.7, 2.0 Hz, 1H), 8.33 (d , J = 2.8 Hz, 1H), 5.19 (q, J = 8.7 Hz, 2H), 3.43 (q, J = 7.3 Hz, 2H), 1.13 (t, J = 7.3 Hz, 3H) ESI MS (m/z ) 482.95 (MH)+ 224 3-(5-(Cyclopropylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3] Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.75 (d, J = 2.9 Hz, 1H), 8.57-8.59 (m, 2H), 8.53 (dd, J = 8.8, 1.7 Hz, 1H), 8.09 (d , J = 2.9 Hz, 1H), 4.17 (d, J = 7.1 Hz, 2H), 3.39 (q, J = 7.5 Hz, 2H), 1.28-1.34 (m, 1H), 1.12 (t, J = 7.5 Hz , 3H), 0.62-0.67 (m, 2H), 0.40-0.43 (m, 2H) ESI MS (m/z) 454.95 (MH)+ 225 3-(3-(Ethylsulfonyl)-5-(methoxymethoxy)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3] Triazine-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.81 (t, J = 2.8 Hz, 1H), 8.58-8.60 (m, 2H), 8.54 (dd, J = 8.6, 1.8 Hz, 1H), 8.23 (dd , J = 11.8, 2.9 Hz, 1H), 5.53 (s, 2H), 3.47 (d, J = 7.9 Hz, 3H), 3.39 (q, J = 7.2 Hz, 2H), 1.13 (t, J = 7.2 Hz , 3H) ESI MS (m/z) 444.95 (MH)+ 226 3-(5-(Difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3] three Oxazin-4(3H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.03 (d, J = 2.7 Hz, 1H), 8.59-8.62 (m, 2H), 8.54-8.57 (m, 1H), 8.50 (d, J = 2.7 Hz , 1H), 7.63 (t, J = 72.3 Hz, 1H), 3.46 (q, J = 7.3 Hz, 2H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 450.95 (MH) + 227 2-((5-(Ethylsulfonyl)-6-(4-oxo-6-(trifluoromethyl)benzo[d][1,2,3]triazine-3(4H)- (Yl)pyridin-3-yl)oxy)-2-methylpropanamide 1H-NMR (400 MHz, DMSO-d6) δ 10.69 (s, 1H), 9.37 (d, J = 2.4 Hz, 1H), 9.10 (d, J = 2.4 Hz, 1H), 8.53-8.60 (m, 3H ), 5.95 (s, 1H), 3.35 (q, J = 7.3 Hz, 2H), 1.41 (s, 6H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 486.00 (MH) + 228 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-2-methyl Propionitrile 1H-NMR (400 MHz, DMSO-d6) δ 9.19 (d, J = 2.4 Hz, 1H), 8.77 (s, 1H), 8.60 (d, J = 2.4 Hz, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 3.45 (q, J = 7.3 Hz, 2H), 1.88 (s, 6H), 1.15 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 451.00 (MH)+ 229 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl dimethyl sulfamate 1H-NMR (400 MHz, DMSO-d6) δ 9.07 (d, J = 2.7 Hz, 1H), 8.78 (s, 1H), 8.53 (d, J = 2.7 Hz, 2H), 8.43 (d, J = 8.3 Hz, 1H), 8.34 (d, J = 8.3 Hz, 1H), 3.47 (q, J = 7.3 Hz, 2H), 3.04 (s, 6H), 1.14 (t, J = 7.3 Hz, 3H) ESI MS ( m/z) 506.95 (MH)+ 230 2-(5-Amino-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.66 (s, 1H), 8.49 (d, J = 0.9 Hz, 1H), 8.37 (dd, J = 8.4, 1.7 Hz, 1H), 8.29 (d, J = 8.3 Hz, 1H), 8.12-8.14 (m, 1H), 7.57 (d, J = 2.8 Hz, 1H), 6.31 (s, 2H), 3.21-3.29 (q, J = 7.3 Hz, 2H), 1.09 (t, J = 7.6 Hz, 3H) ESI MS (m/z) 399.00 (MH)+ 231 2-(5-Chloro-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 9.11 (d, J = 2.4 Hz, 1H), 8.76 (d, J = 0.5 Hz, 1H), 8.71 (d, J = 2.4 Hz, 1H), 8.52 ( d, J = 1.2 Hz, 1H), 8.42 (dd, J = 8.3, 1.5 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 3.46 (q, J = 7.4 Hz, 2H), 1.14 ( t, J = 7.3 Hz, 3H) ESI MS (m/z) 418.05(MH)+ 232 2-(3-(Ethylsulfonyl)-6-(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 1H-NMR (400 MHz, DMSO-d6) δ 9.44 (s, 1H), 8.80-8.82 (m, 2H), 8.54 (d, J = 0.9 Hz, 1H), 8.44 (dd, J = 7.9, 1.8 Hz , 2H), 8.33-8.37 (m, 2H), 3.41-3.46 (q, 7.5 Hz, 2H), 1.15 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 450.95 (MH)+ 233 2-(3-(Ethylsulfonyl)-5-((4-oxoanion-1,4l6-xanthene-4-yl subunit) amino)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.71 (d, J = 0.7 Hz, 1H), 8.53 (d, J = 2.7 Hz, 1H), 8.50 (s, 1H), 8.39 (dd, J = 8.3 , 1.5 Hz, 1H), 8.31 (d, J = 8.3 Hz, 1H), 7.94 (d, J = 2.7 Hz, 1H), 4.14 (td, J = 8.6, 3.8 Hz, 2H), 3.99-4.05 (m , 2H), 3.68-3.72 (m, 2H), 3.57-3.63 (m, 2H), 3.33-3.40 (q, 2H), 1.12 (t, J = 7.3 Hz, 3H) ESI MS (m/z) 517.05 (MH)+ 234 2-(6-Bromo-3-(ethylthio)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.86 (q, J = 0.8 Hz, 1H), 8.76 (d, J = 8.9 Hz, 1H), 8.54 (s, 1H), 8.41 (dd, J = 8.4 , 2.0 Hz, 1H), 8.31 (d, J = 8.6 Hz, 1H), 7.71-7.75 (m, 1H), 7.64-7.68 (m, 1H), 2.74 (q, J = 7.3 Hz, 2H), 1.05 (t, J = 24.7, 7.1 Hz, 3H) ESI MS (m/z) 468.90 (MH)+ 235 2-(5-(Difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.94 (d, J = 2.7 Hz, 1H), 8.76 (s, 1H), 8.52 (s, 1H), 8.42 (dd, J = 8.2, 1.6 Hz, 1H ), 8.37 (d, J = 2.9 Hz, 1H), 8.33 (d, J = 8.3 Hz, 1H), 7.60 (t, J = 72.5 Hz, 1H), 3.44 (q, J = 7.4 Hz, 2H), 1.14 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 450.00(MH)+ 236 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) Cyclopropane-1-formamide 1H-NMR (400 MHz, DMSO-d6) δ 10.80 (s, 1H), 9.16 (d, J = 2.4 Hz, 1H), 8.79 (d, J = 2.8 Hz, 1H), 8.74 (s, 1H), 8.52 (s, 1H), 8.41 (dd, J = 8.3, 1.8 Hz, 1H), 8.32 (d, J = 8.3 Hz, 1H), 3.37 (q, J = 7.3 Hz, 2H), 1.79 (d, J = 4.3 Hz, 4H), 1.13 (t, J = 7.5 Hz, 3H) ESI MS (m/z) 492.00(MH)+ 237 2-(3-(Ethylsulfonyl)-6-(5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 1H-NMR (400 MHz, DMSO-d6) δ 8.80 (s, 1H), 8.76 (d, J = 8.6 Hz, 1H), 8.55 (s, 1H), 8.42-8.44 (m, 1H), 8.35 (d , J = 8.6 Hz, 2H), 6.92 (s, 1H), 3.47 (q, J = 7.4 Hz, 2H), 2.60 (s, 3H), 1.17 (t, J = 7.5 Hz, 3H) ESI MS (m /z) 532.00 (MH)+ *Use the compound name generated by Chemdraw Professional 18.1

下列化合物(表2)是使用合適的起始原料並按照方案1-9或實施例1至16中所述的類似方法獲得的 表-2 序號    化合物名稱 序號    化合物名稱 238 2-(3-(乙基磺醯基)-5-((2,2,2-三氟乙基)硫代)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 337 2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-((三氟甲基)磺醯基)酞嗪-1(2H)-酮 239 2-(3,5-雙(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 338 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-((三氟甲基)磺醯基)酞嗪-1(2H)-酮 240 2-(5-((1,1-二氟乙基)硫代)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 339 1-(5-(乙基磺醯基)-6-(1-氧代-7-((三氟甲基)磺醯基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈 241 2-(5-(乙基磺醯亞胺基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 340 7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 242 2-(5-((1,1-二氟乙基)磺醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 341 7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 243 2-(5-(4-(二甲基磷醯基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 342 7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 244 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷甲醯胺 343 2-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)乙腈 245 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙腈 344 1-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)環丙烷-1-甲腈 246 2-(3-(乙基磺醯基)-5-異丙氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 345 7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 247 2-(3-(乙基磺醯基)-5-((1,1,1-三氟-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 346 2-(3-(乙基磺醯基)-5-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 248 2-(3-(乙基磺醯基)-5-(三氟甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 347 2-(3-(乙基磺醯基)-5-((2-(三氟甲基)環丙基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 249 2-(3-(乙基磺醯基)-5-(1-氧負離子基-4,5-二氫-3H-1l6-異噻唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 348 2-(3-(乙基磺醯基)-5-(3-甲氧基雜氮環丁烷-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 250 2-(3-(乙基磺醯基)-5-((3-羥基-1-氧化四氫-1l6-噻吩-1-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 349 2-(3-(乙基磺醯基)-5-((1-甲基雜氮環丁烷-3-基)氧)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 251 2-(3-(乙基磺醯基)-5-((4-氧負離子基-1,4l6-氧雜蒽-4-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 350 2-(3-(乙基磺醯基)-5-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 252 4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯磺醯氟 351 2-(3-(乙基磺醯基)-5-(2H-1,2,3-三唑-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 253 2-(5-(4-(二甲基磷醯基)苯基)-3-(乙基磺醯亞胺基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 352 2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 254 5'-(乙基磺醯基)-6'-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-[3,3'-二吡啶]-6-磺醯氟 353 2-(3-(乙基磺醯基)-5-(4-(2-羥基-2-甲基丙基)-1H-1,2,3-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 255 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-磺醯氟 354 2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 256 2-(5-(4-(1,1-二氟乙基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 355 2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 257 2-(3-(乙基磺醯基)-5-(1-(三氟甲基)環丙基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 356 2-(5-(3,5-雙(三氟甲基)-1H-吡唑-1-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 258 2-(3-(乙基磺醯基)-5-(1,3,5-三甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 357 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(2,2,2-三氟乙氧基)酞嗪-1(2H)-酮 259 2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 358 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(2,2,3,3,3-五氟丙氧基)酞嗪-1(2H)-酮 260 2-(3-(乙基磺醯基)-5-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 359 1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]嘧啶-7-基)環丙烷-1-甲腈 261 2-(3-(乙基磺醯基)-5-(1-異丁基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 360 2-(3-(乙基磺醯基)-6-甲基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 262 2-(3-(乙基磺醯基)-5-(3-甲氧基-1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 361 2-(6-(乙基磺醯基)-2-(三氟甲基)吡唑並[1,5-a]嘧啶-5-基)-7-(三氟甲基)酞嗪-1(2H)-酮 263 2-(1'-(二氟甲基)-5-(乙基磺醯基)-6'-氧代-1',6'-二氫-[3,3'-二吡啶]-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮 362 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[2,1-b]噻唑-2-甲腈 264 2-(3-(乙基磺醯基)-5-異丙基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 363 1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]嘧啶-6-基)環丙烷-1-甲腈 265 2-(5-(3,5-二甲基異唑-4-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 364 1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡唑並[1,5-a]吡啶-5-基)環丙烷-1-甲腈 266 2-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮 365 2-(2-(乙基磺醯基)-7-甲基吡唑並[1,5-a]嘧啶-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮 267 2-(3-(乙基磺醯亞胺基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 366 2-(3-(乙基磺醯基)-1-甲基-6-(三氟甲氧基)-1H-吲哚-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 268 4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯基 氟化硫 367 2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-1H-吡咯並[2,3-b]吡啶-1-基)乙腈 269 2-(3-(乙基磺醯亞胺基)-5-((1,1,1-三氟-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 368 2-(5-(乙基磺醯基)-1-甲基-1H-吡唑並[3,4-b]吡啶-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮 270 2-((5-(乙基磺醯亞胺基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙腈 369 2-(7-環丙基-2-(乙基磺醯基)咪唑並[1,2-a]嘧啶-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮 271 2-(3-(乙基磺醯基)-5-((甲基亞磺醯基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 370 2-(3-(乙基磺醯基)咪唑並[1,2-a]吡嗪-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 272 2-(3-(乙基磺醯基)-5-(2,2,3,3-四氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 371 2-(3-(乙基磺醯基)咪唑並[1,2-b]噠嗪-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 273 2-(3-(乙基磺醯基)-5-(1,1,2-三氟-2-(三氟甲氧基)乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 372 2-(5-(溴二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 274 2-(3-(乙基磺醯基)-5-(2,2,3,4,4,4-六氟丁氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 373 2-(3-(乙基磺醯基)-5-(吡啶-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 275 2-(3-(乙基磺醯基)-5-(2,2,3,3,3-五氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 374 2-(3-(乙基磺醯基)-5-(吡啶-2-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 276 2-(5-(2,2-二氟-2-(三氟甲氧基)乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 375 2-(5-((5-溴吡啶-2-基)氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 277 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2,2-二氟環丙烷-1-甲醯胺 376 2-(3-(乙基磺醯基)-5-(嘧啶-2-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 278 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2,2-二甲基環丙烷-1-甲醯胺 377 2-(3-(乙基磺醯基)-5-((1-甲基-1H-吡唑-3-基)氧)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 279 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-氟環丙烷-1-甲醯胺 378 2-(5-(3,3-二氟環丁氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 280 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環丙烷-1-甲醯胺 379 2-(5-(2,2-二氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 281 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-N-甲基環丁烷甲醯胺 380 2-(5-((1,3-二氟丙烷-2-基)氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 282 1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺 381 2-(3-(乙基磺醯基)-5-(新戊基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 283 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3,3-二甲基環丁烷-1-甲醯胺 382 1-(((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)甲基)環丙烷-1-甲腈 284 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3,3-二氟環丁烷-1-甲醯胺 383 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丙腈 285 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丁烷甲醯胺 384 2-(3-(乙基磺醯基)-5-((1-氟代-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 286 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環丁烷-1-甲醯胺 385 2-(3-(乙基磺醯基)-5-甲氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 287 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3-甲基環丁烷-1-甲醯胺 386 2-(3-(乙基磺醯基)-5-(2-氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 288 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3-氧代環丁烷-1-甲醯胺 387 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-(甲硫基)乙腈 289 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環戊烷甲醯胺 388 2-(5-((2,2-二氟環丙基)甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 290 1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環戊烷-1-甲醯胺 389 4-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丁腈 291 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環戊烷-1-甲醯胺 390 2-(5-(環丁基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 292 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環己烷甲醯胺 391 2-(5-(2,2-二氟丙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 293 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4-甲基環己烷-1-甲醯胺 392 2-(3-(乙基磺醯基)-5-(1-氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 294 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4,4-二氟環己烷-1-甲醯胺 393 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-N,N-二甲基-2-(甲硫基)乙醯胺 295 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氮雜環丁烷-3-甲醯胺 394 2-乙基-2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丁腈 296 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基氮雜環丁烷-3-甲醯胺 395 2-(3-(乙基磺醯基)-5-異丁氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 297 1-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氮雜環丁烷-3-甲醯胺 396 2-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 298 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧雜環丁烷e-3-甲醯胺 397 2-(5-(2-溴-1,1-二氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 299 3-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧雜環丁烷e-3-甲醯胺 398 2-(5-((3-環丙基異惡唑-5-基)甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 300 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基吡咯烷-3-甲醯胺 399 2-(3-(乙基磺醯基)-5-(3-甲氧基環丁氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 301 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)四氫呋喃-3-甲醯胺 400 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基 二氟甲磺酸酯 302 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)呱啶-4-甲醯胺 401 3-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)環丁烷-1-甲腈 303 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基呱啶-4-甲醯胺 402 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基氟甲磺酸酯 304 1-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)呱啶-4-甲醯胺 403 3-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-3-甲基丁腈 305 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)四氫-2H-吡喃-4-甲醯胺 404 5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基三氟甲磺酸酯 306 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4-氟四氫-2H-吡喃-4-甲醯胺 405 2-(3-(乙基磺醯基)-5-((1-甲氧基-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 307 2-(7-溴-3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 406 2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-N,N,2-三甲基丙醯胺 308 2-(3-(乙基磺醯基)-7-(三氟甲基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 407 2-(3-(乙基磺醯基)-5-((3-甲基氧雜環丁烷-3-基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 309 2-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-基)乙腈 408 (E)-2-(3-(乙基磺醯基)-5-(2-(甲基亞氨基)丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 310 3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-甲腈 409 2-(3-(乙基磺醯基)-5-((三甲基silyl)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 311 2-(3-(乙基磺醯基)-7-甲氧基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 410 2-(3-(乙基磺醯基)-5-(2-氧丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 312 2-(3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 411 2-(3-(乙基磺醯基)-5-((2-甲基-3-氧代丁烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 313 1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-基)環丙烷-1-甲腈 412 2-(5-(烯丙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 314 2-(3-(乙基磺醯基)-7-(2,2,2-三氟乙基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 413 2-(3-(乙基磺醯基)-5-丙氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 315 2-(6-溴-3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 414 2-(5-乙氧基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 316 2-(3-(乙基磺醯基)-6-(三氟甲基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 415 2-(3-(乙基磺醯基)-5-(甲氧基甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 317 3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-甲腈 416 2-(5-環丁基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 318 2-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-基)乙腈 417 2-(5-(2,2-二氟環丙基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 319 2-(3-(乙基磺醯基)-7-(1-甲基環丙基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 418 2-(3-(乙基磺醯基)-5-(2-甲基氧雜環丁烷-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 320 2-(3-(乙基磺醯基)-7-(甲基氨基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 419 2-(3-(乙基磺醯基)-5-(3-甲基硫雜環丁烷基-3-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 321 7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 420 2-(5-(1,1-二氧負離子基硫雜環丁烷基-2-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 322 7-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 421 6-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)煙腈 323 7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 422 2-(3-(乙基磺醯基)-5-(硫雜環丁烷基-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 324 7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 423 2-(5-((1,1-二氧負離子基硫雜環丁烷基-3-基)氧)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 325 5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)煙腈 424 2-(5-((1,1-二氧負離子基硫雜環丁烷基-3-基)甲基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 326 2-(5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)乙腈 425 7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 327 1-(5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)環丙烷-1-甲腈 426 2-(3-(N-甲基乙基磺醯亞胺基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 328 2-((5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)氧)-2-甲基丙腈 427 2-(3-(N-甲基乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 329 7-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮 428 N-(乙基((氧代)(2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-3-基)-l6-亞硫烷基)氰胺 330 2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮 429 2-(3-(N-乙基乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 331 2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮 430 2-(6-溴-3-(乙基磺醯亞胺基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 332 2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮 431 2-(6-溴-3-(N-甲基乙基磺醯亞胺基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 333 5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)煙腈 432 1-(3-(乙基磺醯亞胺基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-基)環丙烷-1-甲腈 334 2-(5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)吡啶-3-基)乙腈 433 3-(乙基磺醯亞胺基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-甲腈 335 1-(5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈 434 2-(6-(環丙基氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮 336 5-(乙基磺醯基)-6-(1-氧代-7-((三氟甲基)磺醯基)酞嗪-2(1H)-基)煙腈 435 N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-2-基)環丙烷甲醯胺 *使用Chemdraw Professional 18.1生成的化合物名稱The following compounds (Table 2) are obtained by using suitable starting materials and following the similar methods described in Schemes 1-9 or Examples 1-16. Table-2 Serial number Compound name Serial number Compound name 238 2-(3-(Ethylsulfonyl)-5-((2,2,2-trifluoroethyl)thio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 337 2-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-((trifluoromethyl)sulfonyl)phthalazine-1(2H)-one 239 2-(3,5-bis(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 338 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-((trifluoromethyl)sulfonyl)phthalazine-1(2H)- ketone 240 2-(5-((1,1-Difluoroethyl)thio)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-ketone 339 1-(5-(Ethylsulfonyl)-6-(1-oxo-7-((trifluoromethyl)sulfonyl)phthalazine-2(1H)-yl)pyridin-3-yl) Cyclopropane-1-carbonitrile 241 2-(5-(Ethylsulfonylimino)-3-(ethylsulfonylimino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 340 7-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone 242 2-(5-((1,1-Difluoroethyl)sulfonyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 341 7-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl )Pyrido[2,3-d]pyridazine-8(7H)-one 243 2-(5-(4-(Dimethylphosphoryl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-ketone 342 7-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3- d)Pyridazine-8(7H)-one 244 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropanecarboxamide 343 2-(5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)acetonitrile 245 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2 -Methylpropionitrile 344 1-(5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)cyclopropane-1-carbonitrile 246 2-(3-(Ethylsulfonyl)-5-isopropoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 345 7-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H)-ketone 247 2-(3-(Ethylsulfonyl)-5-((1,1,1-trifluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(tris Fluoromethyl)phthalazine-1(2H)-one 346 2-(3-(Ethylsulfonyl)-5-(ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 248 2-(3-(Ethylsulfonyl)-5-(trifluoromethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 347 2-(3-(Ethylsulfonyl)-5-((2-(trifluoromethyl)cyclopropyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-ketone 249 2-(3-(Ethylsulfonyl)-5-(1-oxyanion-4,5-dihydro-3H-1l6-isothiazol-1-yl)pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one 348 2-(3-(Ethylsulfonyl)-5-(3-methoxyazetidine-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 250 2-(3-(Ethylsulfonyl)-5-((3-hydroxy-1-oxytetrahydro-1l6-thiophen-1-yl subunit) amino)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 349 2-(3-(Ethylsulfonyl)-5-((1-methylazacyclobutan-3-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-ketone 251 2-(3-(Ethylsulfonyl)-5-((4-oxoanion-1,4l6-xanthene-4-yl subunit) amino)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 350 2-(3-(Ethylsulfonyl)-5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 252 4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)benzenesulfonyl fluoride 351 2-(3-(Ethylsulfonyl)-5-(2H-1,2,3-triazol-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 253 2-(5-(4-(Dimethylphosphoryl)phenyl)-3-(ethylsulfonylimino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 352 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one 254 5'-(Ethylsulfonyl)-6'-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)-[3,3'-dipyridine]-6 -Sulfonyl fluoride 353 2-(3-(Ethylsulfonyl)-5-(4-(2-hydroxy-2-methylpropyl)-1H-1,2,3-triazol-1-yl)pyridine-2- Base)-7-(trifluoromethyl)phthalazine-1(2H)-one 255 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3-sulfonyl fluoride 354 2-(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one 256 2-(5-(4-(1,1-Difluoroethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 355 2-(3-(Ethylsulfonyl)-5-(3-methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 257 2-(3-(Ethylsulfonyl)-5-(1-(trifluoromethyl)cyclopropyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 356 2-(5-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Base) phthalazine-1(2H)-one 258 2-(3-(Ethylsulfonyl)-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 357 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(2,2,2-trifluoroethoxy)phthalazine-1(2H )-ketone 259 2-(3-(Ethylsulfonyl)-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 358 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(2,2,3,3,3-pentafluoropropoxy)phthalazine -1(2H)-ketone 260 2-(3-(Ethylsulfonyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 359 1-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyrimidine- 7-yl)cyclopropane-1-carbonitrile 261 2-(3-(Ethylsulfonyl)-5-(1-isobutyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 360 2-(3-(Ethylsulfonyl)-6-methylimidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 262 2-(3-(Ethylsulfonyl)-5-(3-methoxy-1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 361 2-(6-(Ethylsulfonyl)-2-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-5-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 263 2-(1'-(Difluoromethyl)-5-(ethylsulfonyl)-6'-oxo-1',6'-dihydro-[3,3'-dipyridine]-6- Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 362 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[2,1-b]thiazole-2-methan Nitrile 264 2-(3-(Ethylsulfonyl)-5-isopropylpyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 363 1-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyrimidine- 6-yl)cyclopropane-1-carbonitrile 265 2-(5-(3,5-Dimethylisoxazol-4-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 364 1-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyrazolo[1,5-a]pyridine -5-yl)cyclopropane-1-carbonitrile 266 2-(3-(Ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-4-methyl-7- (Trifluoromethyl)phthalazine-1(2H)-one 365 2-(2-(Ethylsulfonyl)-7-methylpyrazolo[1,5-a]pyrimidin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 267 2-(3-(Ethylsulfonylimino)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one 366 2-(3-(Ethylsulfonyl)-1-methyl-6-(trifluoromethoxy)-1H-indol-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 268 4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenylsulfur fluoride 367 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)-1H-pyrrolo[2,3-b ]Pyridin-1-yl)acetonitrile 269 2-(3-(Ethylsulfonylimino)-5-((1,1,1-trifluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one 368 2-(5-(Ethylsulfonyl)-1-methyl-1H-pyrazolo[3,4-b]pyridin-6-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 270 2-((5-(Ethylsulfonylimino)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy) -2-Methylpropionitrile 369 2-(7-Cyclopropyl-2-(ethylsulfonyl)imidazo[1,2-a]pyrimidin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 271 2-(3-(Ethylsulfinyl)-5-((methylsulfinyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 370 2-(3-(Ethylsulfonyl)imidazo[1,2-a]pyrazin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 272 2-(3-(Ethylsulfonyl)-5-(2,2,3,3-tetrafluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 371 2-(3-(Ethylsulfonyl)imidazo[1,2-b]pyridazin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 273 2-(3-(Ethylsulfonyl)-5-(1,1,2-trifluoro-2-(trifluoromethoxy)ethoxy)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one 372 2-(5-(Bromodifluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 274 2-(3-(Ethylsulfonyl)-5-(2,2,3,4,4,4-hexafluorobutoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one 373 2-(3-(Ethylsulfonyl)-5-(pyridin-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 275 2-(3-(Ethylsulfonyl)-5-(2,2,3,3,3-pentafluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 374 2-(3-(Ethylsulfonyl)-5-(pyridin-2-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 276 2-(5-(2,2-Difluoro-2-(trifluoromethoxy)ethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 375 2-(5-((5-Bromopyridin-2-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-ketone 277 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-2,2- Difluorocyclopropane-1-formamide 376 2-(3-(Ethylsulfonyl)-5-(pyrimidin-2-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 278 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-2,2- Dimethylcyclopropane-1-formamide 377 2-(3-(Ethylsulfonyl)-5-((1-methyl-1H-pyrazol-3-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-ketone 279 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-fluoro Propane-1-formamide 378 2-(5-(3,3-Difluorocyclobutoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 280 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Cyclopropane-1-formamide 379 2-(5-(2,2-Difluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 281 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-N-methyl Cyclobutane carboxamide 380 2-(5-((1,3-Difluoropropan-2-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 282 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) Cyclopropane-1-formamide 381 2-(3-(Ethylsulfonyl)-5-(neopentyloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 283 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3,3- Dimethylcyclobutane-1-formamide 382 1-(((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)methyl Base) cyclopropane-1-carbonitrile 284 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3,3- Difluorocyclobutane-1-carboxamide 383 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)propionitrile 285 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclobutane amine 384 2-(3-(Ethylsulfonyl)-5-((1-fluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 286 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Cyclobutane-1-formamide 385 2-(3-(Ethylsulfonyl)-5-methoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 287 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3-methyl Cyclobutane-1-formamide 386 2-(3-(Ethylsulfonyl)-5-(2-fluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 288 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3-oxo Cyclobutane-1-formamide 387 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2 -(Methylthio)acetonitrile 289 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopentanemethan amine 388 2-(5-((2,2-Difluorocyclopropyl)methoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 290 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) Cyclopentane-1-formamide 389 4-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)butyronitrile 291 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Cyclopentane-1-formamide 390 2-(5-(Cyclobutylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 292 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclohexanemethyl amine 391 2-(5-(2,2-Difluoropropoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 293 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4-methyl Cyclohexane-1-formamide 392 2-(3-(Ethylsulfonyl)-5-(1-fluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 294 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4,4- Difluorocyclohexane-1-methanamide 393 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-N ,N-Dimethyl-2-(methylthio)acetamide 295 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)azetidine -3-formamide 394 2-Ethyl-2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl ) Oxygen) Butyronitrile 296 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Azetidine-3-formamide 395 2-(3-(Ethylsulfonyl)-5-isobutoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 297 1-Ethyl-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazin-2(1H)-yl)pyridin-3-yl) Azetidine-3-formamide 396 2-(3-(Ethylsulfonyl)-5-(2,2,2-trifluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -ketone 298 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxetane e-3-formamide 397 2-(5-(2-Bromo-1,1-difluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 299 3-ethyl-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazin-2(1H)-yl)pyridin-3-yl) Oxetane e-3-formamide 398 2-(5-((3-Cyclopropylisoxazol-5-yl)methoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Oxazine-1(2H)-one 300 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Pyrrolidine-3-formamide 399 2-(3-(Ethylsulfonyl)-5-(3-methoxycyclobutoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 301 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)tetrahydrofuran-3-methyl Amide 400 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl difluoromethanesulfonate 302 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)piperidine-4- Formamide 401 3-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)cyclobutane Alkane-1-carbonitrile 303 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Pyridine-4-methamide 402 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl fluoromethanesulfonate 304 1-Ethyl-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazin-2(1H)-yl)pyridin-3-yl) Pyridine-4-methamide 403 3-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-3 -Methyl butyronitrile 305 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)tetrahydro-2H- Pyran-4-formamide 404 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl triflate 306 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4-fluorotetra Hydrogen-2H-pyran-4-methylamide 405 2-(3-(Ethylsulfonyl)-5-((1-methoxy-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 307 2-(7-Bromo-3-(ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 406 2-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-N ,N,2-Trimethylpropionamide 308 2-(3-(Ethylsulfonyl)-7-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 407 2-(3-(Ethylsulfonyl)-5-((3-methyloxetan-3-yl)methoxy)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 309 2-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine- 7-base) acetonitrile 408 (E)-2-(3-(Ethylsulfonyl)-5-(2-(methylimino)propoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-ketone 310 3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-7-methyl Nitrile 409 2-(3-(Ethylsulfonyl)-5-((trimethylsilyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 311 2-(3-(Ethylsulfonyl)-7-methoxyimidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 410 2-(3-(Ethylsulfonyl)-5-(2-oxypropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 312 2-(3-(Ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 411 2-(3-(Ethylsulfonyl)-5-((2-methyl-3-oxobutan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 313 1-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine- 7-yl)cyclopropane-1-carbonitrile 412 2-(5-(allyloxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 314 2-(3-(Ethylsulfonyl)-7-(2,2,2-trifluoroethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one 413 2-(3-(Ethylsulfonyl)-5-propoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 315 2-(6-Bromo-3-(ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 414 2-(5-Ethoxy-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 316 2-(3-(Ethylsulfonyl)-6-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 415 2-(3-(Ethylsulfonyl)-5-(methoxymethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 317 3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-6-methyl Nitrile 416 2-(5-Cyclobutyl-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 318 2-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine- 6-base) acetonitrile 417 2-(5-(2,2-Difluorocyclopropyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one 319 2-(3-(Ethylsulfonyl)-7-(1-methylcyclopropyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-ketone 418 2-(3-(Ethylsulfonyl)-5-(2-methyloxetan-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-ketone 320 2-(3-(Ethylsulfonyl)-7-(methylamino)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-ketone 419 2-(3-(Ethylsulfonyl)-5-(3-methylthietane-3-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 321 7-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl )Pyrido[2,3-d]pyridazine-8(7H)-one 420 2-(5-(1,1-Dioxanethioetanyl-2-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one 322 7-(3-(Ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl )Pyrido[2,3-d]pyridazine-8(7H)-one 421 6-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)nicotinonitrile 323 7-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3- d)Pyridazine-8(7H)-one 422 2-(3-(Ethylsulfonyl)-5-(thietanyl-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-ketone 324 7-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone 423 2-(5-((1,1-Dioxanethioetanyl-3-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one 325 5-(Ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)nicotinonitrile 424 2-(5-((1,1-dioxanylthietanyl-3-yl)methyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one 326 2-(5-(Ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)acetonitrile 425 7-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H)-ketone 327 1-(5-(Ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)cyclopropane-1-carbonitrile 426 2-(3-(N-Methylethylsulfonylimino)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one 328 2-((5-(Ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine -3-yl)oxy)-2-methylpropionitrile 427 2-(3-(N-Methylethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one 329 7-(5-(Difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone 428 N-(Ethyl((oxo)(2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)-5-(4-(1,1,2, 2-Tetrafluoroethoxy)phenyl)pyridin-3-yl)-16-sulfinyl)cyanamide 330 2-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-(perfluoroethyl)phthalazin-1(2H)-one 429 2-(3-(N-ethylethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one 331 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(perfluoroethyl)phthalazine-1(2H)-one 430 2-(6-Bromo-3-(ethylsulfonylimino)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- ketone 332 2-(3-(Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(perfluoroethyl) )Phthalazine-1(2H)-one 431 2-(6-Bromo-3-(N-methylethylsulfonylimino)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone 333 5-(Ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)nicotinonitrile 432 1-(3-(Ethylsulfonylimino)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a] (Pyridin-6-yl) cyclopropane-1-carbonitrile 334 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile 433 3-(Ethylsulfonylimino)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-6 -Formonitrile 335 1-(5-(Ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1- Formonitrile 434 2-(6-(Cyclopropylamino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one 336 5-(Ethylsulfonyl)-6-(1-oxo-7-((trifluoromethyl)sulfonyl)phthalazine-2(1H)-yl)nicotinonitrile 435 N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-2-yl)cyclopropanecarboxamide *Use the compound name generated by Chemdraw Professional 18.1

如本文所述,通式(I)化合物顯示出極高的殺蟲活性,其對許多攻擊重要農作物的害蟲有效。下列試驗將評估本發明化合物的活性:生物實例 As described herein, the compound of general formula (I) shows extremely high insecticidal activity, which is effective against many pests that attack important crops. The following tests will evaluate the activity of the compounds of the invention: biological examples :

例A:棉鈴蟲 Example A: Helicoverpa armigera

使用食物摻入法,將所需量的實驗化合物稱量並溶解在含有溶劑溶液的試管中。將試管以2000 rpm的速度渦旋90分鐘以進行適當混合,然後用水稀釋至所需的實驗濃度。當生物測定容器中的溫度達到約50o C時,將半合成飲食添加到特定溶液中。將飲食和溶液充分攪拌使其充分混合,然後冷卻30分鐘。將凝固的飲食均勻切成幾塊,然後將這些塊放到生物測定托盤的單元格。將單個三齡飢餓的幼蟲釋放到生物測定托盤的這些單元格中,每個托盤蓋上蓋子。將生物測定托盤保持在溫度為25o C,相對濕度為70%的實驗室條件下。放幼蟲96小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物  10 15 26 38 72 89 94 96 101 102 103 115 116 119 123 125 127 128 134 137 144 146 152 158 160 201 204 207 209 210和217能造成超過70%的死亡率。Using the food incorporation method, the required amount of test compound is weighed and dissolved in a test tube containing a solvent solution. The test tube was vortexed at 2000 rpm for 90 minutes for proper mixing, and then diluted with water to the desired experimental concentration. When the temperature in the bioassay container reaches about 50 o C, the semi-synthetic diet is added to the specific solution. Stir the food and solution thoroughly to mix well, and then cool for 30 minutes. Cut the solidified diet evenly into several pieces, and then place these pieces into the cells of the bioassay tray. A single third-instar hungry larva is released into these cells of the bioassay tray, and each tray is covered with a lid. Keep the bioassay tray under laboratory conditions with a temperature of 25 o C and a relative humidity of 70%. The dead, dying and alive larvae observed were recorded 96 hours after the larvae were released. The mortality was calculated by adding the dead and dying larvae, and the results were compared with an untreated control group. According to records, the compound 10 15 26 38 72 89 94 96 101 102 103 115 116 119 123 125 127 128 134 137 144 146 152 158 160 201 204 207 209 210 and 217 can cause more than 70% mortality.

例B:斜紋夜蛾 Example B: Spodoptera litura

使用食物摻入法,將所需量的實驗化合物稱量並溶解在含有溶劑溶液的試管中。將試管以2000 rpm的速度渦旋90分鐘以進行適當混合。當生物測定容器中的溫度達到約50o C時,將半合成飲食添加到特定溶液中。將飲食和溶液充分攪拌使其充分混合,然後冷卻30分鐘。將凝固的飲食均勻切成幾塊,然後將這些塊放到生物測定托盤的單元格。將單個三齡飢餓的幼蟲釋放到生物測定托盤的這些單元格中,每個托盤蓋上蓋子。將生物測定托盤保持在溫度為25o C,相對濕度為70%的實驗室條件下。放幼蟲96小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物  15 17 87 89 103 104 116 118 119 120 124 125 128 131 132 134 137 151 152 158 163 182 190 198 201 202 204 207 209 210 217和234能造成超過70%的死亡率。Using the food incorporation method, the required amount of test compound is weighed and dissolved in a test tube containing a solvent solution. The test tube was vortexed at 2000 rpm for 90 minutes for proper mixing. When the temperature in the bioassay container reaches about 50 o C, the semi-synthetic diet is added to the specific solution. Stir the food and solution thoroughly to mix well, and then cool for 30 minutes. Cut the solidified diet evenly into several pieces, and then place these pieces into the cells of the bioassay tray. A single third-instar hungry larva is released into these cells of the bioassay tray, and each tray is covered with a lid. Keep the bioassay tray under laboratory conditions with a temperature of 25 o C and a relative humidity of 70%. The dead, dying and alive larvae observed were recorded 96 hours after the larvae were released. The mortality was calculated by adding the dead and dying larvae, and the results were compared with an untreated control group. According to records, compounds 15 17 87 89 103 104 116 118 119 120 124 125 128 131 132 134 137 151 152 158 163 182 190 198 201 202 204 207 209 210 217 and 234 can cause more than 70% mortality.

例C:小菜蛾 Example C: Plutella xylostella

使用葉片浸漬法,將所需量的化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01% Triton-X溶液稀釋至所需的實驗濃度。將白菜葉浸入溶液中10秒鐘,遮陰乾燥20分鐘,然後轉移到生物測定托盤中。將單個二齡幼蟲釋放到生物測定托盤的這些單元格中,每個托盤蓋上蓋子。將生物測定托盤保持在溫度為25o C,相對濕度為70%的實驗室條件下。放幼蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物     1 2 3 4 6 8 9 10 11 14 15 16 17 18 22 23 24 25 26 27 28 29 34 37 38 41 47 52 53 55 56 57 58 59 60 62 66 67 69 71 72 74 76 77 80 85 87 88 89 90 91 92 94 96 97 98 99 100 101 102 103 104 105 107 108 109 110 111 112 113 114 115 116 117 118 119 120 121 122 123 124 125 127 128 130 131 132 134 135 137 140 141 143 144 145 147 151 152 154 157 158 159 160 161 162 163 164 165 171 175 177 178 179 181 185 186 187 190 191 193 194 198 201 202 203 204 207 209 210 213 215 216 217 218 226 228 231 232 234和235能造成超過70%的死亡率。Using the blade dipping method, weigh and dissolve the required amount of compound in a test tube containing a solvent solution, place it on a stirrer with a rotation speed of 2000 rpm for 90 minutes to mix properly, and then dilute it with 0.01% Triton-X solution. The required experimental concentration. The cabbage leaves were immersed in the solution for 10 seconds, shaded and dried for 20 minutes, and then transferred to the bioassay tray. A single second instar larva is released into these cells of the bioassay tray, and each tray is covered with a lid. Keep the bioassay tray under laboratory conditions with a temperature of 25 o C and a relative humidity of 70%. The dead, dying and alive larvae observed were recorded 72 hours after the larvae were released. The mortality was calculated by adding the dead and dying larvae, and the results were compared with an untreated control group. According to records, the compound with a concentration of 300ppm 1 2 3 4 6 8 9 10 11 14 15 16 17 18 22 23 24 25 26 27 28 29 34 37 38 41 47 52 53 55 56 57 58 59 60 62 66 67 69 71 72 74 76 77 80 85 87 88 89 90 91 92 94 96 97 98 99 100 101 102 103 104 105 107 108 109 110 111 112 113 114 115 116 117 118 119 120 121 122 123 124 125 127 128 130 131 132 134 135 137 140 141 143 144 145 147 151 152 154 157 158 159 160 161 162 163 164 165 171 175 177 178 179 181 185 186 187 190 191 193 194 198 201 202 203 204 207 209 210 213 215 216 217 218 226 228 231 232 234 and 235 Cause more than 70% mortality.

例D:煙粉蝨 Example D: Bemisia tabaci

使用葉片浸漬法,將所需量的化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01% Triton-X溶液稀釋至所需的實驗濃度。將棉葉浸入溶液中10秒鐘,陰涼乾燥20分鐘,然後將葉保存在玻璃單元中,將葉柄浸入水中。釋放已知數量的活力滿滿的羽化成蟲,並將其保存在溫度為25o C,相對濕度為70%植物生長室中。放蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物4和18能造成超過70%的死亡率。Using the blade dipping method, weigh and dissolve the required amount of compound in a test tube containing a solvent solution, place it on a stirrer with a rotation speed of 2000 rpm for 90 minutes to mix properly, and then dilute it with 0.01% Triton-X solution. The required experimental concentration. Soak the cotton leaves in the solution for 10 seconds, cool and dry for 20 minutes, then store the leaves in a glass cell, and immerse the petioles in water. Release a known number of vigorous emerging adults and store them in a plant growth room at a temperature of 25 o C and a relative humidity of 70%. The dead, dying and alive larvae observed were recorded 72 hours after the insects were released. The mortality was calculated by adding the dead and dying larvae, and the results were compared with an untreated control group. According to records, compounds 4 and 18 at a concentration of 300 ppm can cause more than 70% mortality.

例E:桃蚜 Example E: Myzus persicae

使用葉片浸漬法,將所需量的實驗化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01% Triton-X溶液稀釋至所需的實驗濃度。將辣椒葉浸入溶液中10秒鐘,陰涼乾燥20分鐘,然後將葉子的背面朝上放置在含有4 ml 1%瓊脂溶液的生物測定托盤的單元格中。釋放已知數量的三齡若蟲,並將其保存在溫度為25o C,相對濕度為70%植物生長室中。放蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物24 35 36 40 124 171 200 202 209和219能造成超過70%的死亡率。Using the blade dipping method, weigh and dissolve the required amount of test compound in a test tube containing a solvent solution, place it on a stirrer at 2000 rpm for 90 minutes to mix properly, and then dilute it with 0.01% Triton-X solution to The required experimental concentration. Soak the pepper leaves in the solution for 10 seconds, cool and dry for 20 minutes, and then place the leaves backside up in the cells of the bioassay tray containing 4 ml of 1% agar solution. Release a known number of third instar nymphs and store them in a plant growth room at a temperature of 25 o C and a relative humidity of 70%. The dead, dying and alive larvae observed were recorded 72 hours after the insects were released. The mortality was calculated by adding the dead and dying larvae, and the results were compared with an untreated control group. According to records, compounds 24 35 36 40 124 171 200 202 209 and 219 at a concentration of 300 ppm can cause more than 70% mortality.

例F:褐飛蝨 Example F: Brown planthopper

採用浸苗法進行篩選,將所需量的化合物稱量並溶解在含有溶劑溶液的試管中,放在轉速為2000 rpm的攪拌器攪拌90分鐘進行適當混合,然後用0.01%Triton-X溶液稀釋至所需的實驗濃度。將水稻幼苗浸入溶液中10秒鐘,陰涼乾燥20分鐘,然後將幼苗保存在玻璃試管,將根浸入水中,將該試管放入玻璃容器中。釋放已知數量的三齡若蟲,並將其保存在溫度為25o C,相對濕度為75%植物生長室中。放蟲72小時後記錄觀察到的死亡、瀕死和活著的幼蟲。通過將死亡的和瀕死的幼蟲相加計算死亡率,並將結果與一個未處理的對照組進行比較。根據記錄,濃度為300ppm的化合物6能造成超過70%的死亡率。The seedling immersion method is used for screening, the required amount of compound is weighed and dissolved in a test tube containing a solvent solution, placed on a stirrer with a rotation speed of 2000 rpm for 90 minutes for proper mixing, and then diluted with a 0.01% Triton-X solution To the required experimental concentration. The rice seedlings were immersed in the solution for 10 seconds, and dried for 20 minutes in a cool shade, and then the seedlings were stored in a glass test tube, the roots were immersed in water, and the test tube was placed in a glass container. Release a known number of third instar nymphs and store them in a plant growth room at a temperature of 25 o C and a relative humidity of 75%. The dead, dying and alive larvae observed were recorded 72 hours after the insects were released. The mortality was calculated by adding the dead and dying larvae, and the results were compared with an untreated control group. According to records, compound 6 at a concentration of 300 ppm can cause more than 70% mortality.

在參考某些優選實施例描述本發明後,本領域技術人員應該很熟悉其他技術參數。對於本領域技術人員而言,可以在不脫離本發明範圍的情況下實施對材料和方法的許多修改。After describing the present invention with reference to certain preferred embodiments, those skilled in the art should be familiar with other technical parameters. For those skilled in the art, many modifications to materials and methods can be implemented without departing from the scope of the present invention.

no

no

Figure 109128488-A0101-11-0002-3
Figure 109128488-A0101-11-0002-3

Claims (16)

一種式(I)化合物,
Figure 03_image035
式(I) 其中, R1 選自C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基和C3 -C8 -環烷基-C1 -C6 -烷基; Y獨立地選自O和/或NRy ; Ry 選自氫、氰基、C1 -C4 -烷基、C2 -C4 -烯基、C2 -C4 -炔基、C1 -C4 -鹵代烷基、C2 -C4 -鹵代烯基、C3 -C5 -環烷基和C3 -C5 -環烷基-C1 -C3 -烷基; Q代表5至10元雜環系統,其可任選地被一個或多個R2 基團取代; R2 選自氫、鹵素、氰基、硝基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、C1 -C6 -氰基烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、SCN、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、P(=O)(OR”)2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R2 可任選地被一個或多個R2a 基團取代; R2a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、SCN、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;或者 兩個R2a 取代基以及它們所連接的原子或其他選自C、N、O、S的原子,和任選地包括1至3個選自C(=O)、C(=S)、S(O)0-2 和Si(R”)2 的環成員一起可以形成3至7元環,其本身可任選地被一個或多個R2aa 基團取代; R2aa 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; A1 和A2 獨立地代表N或CRA ; RA 選自氫、鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C3 -C8 -環烷基、OR”和N(R”)2 ;其中每個RA 基團可任選地被一個或多個RA 基團取代; RA' 選自鹵素、氰基、C3 -C8 -環烷基、OR”和N(R”)2 ; Z代表O或S; G1 、G2 、G3 和G4 獨立地代表N或CR3 ;其中在環E中同時存在的N不超過兩個; R3 選自氫、鹵素、氰基、硝基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、SCN、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、P(=O)(OR”)2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R3 基團可任選地被一個或多個R3a 基團取代; R3a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、CR4 =NR5 、C(=O)R8 、S(O)0-2 R7 、S(O)0-1 R9 =NR10 、N=S(O)0-1 (R9 )2 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R4 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、S(O)0-2 R7 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R4 基團可任選地被R4a 基團取代; R4a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R5 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR'R”、S(O)0-2 R7 、C(=O)R8 、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R54 基團可任選地被R5a 取代; R5a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、Si(R”)3 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R6 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C1 -C6 -環烷基和C(=O)R8 ; R7 選自C1 -C6 -烷基, C2 -C6 -烯基, C2 -C6 -炔基, C1 -C6 -鹵代烷基, C2 -C6 -鹵代烯基, C3 -C8 -環烷基, NR5 R6 , C6 -C10 -芳基, C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R7 基團可任選地被一個或多個R7a 基團取代; R7a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R8 選自氫、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR4 、NR5 R6 、N=S(O)0-1 (R9 )2 、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基;其中每個R8 可任選地被一個或多個R8a 基團取代; R8a 選自鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、OR”、NR'R”、S(O)0-2 R'、C(=O)R'、C6 -C10 -芳基、C7 -C14 -芳烷基和C3 -C10 -雜環基; R9 選自C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基和C(=O)R8 ; R10 選自氫、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C1 -C6 -鹵代烷基、C2 -C6 -鹵代烯基、C3 -C8 -環烷基、Si(R”)3 、S(O)0-2 R7 和C(=O)R8 ; 或者兩個R9 取代基以及它們所連接的原子或其他選自C、N、O,和任選地包括C(=O)取代基的原子一起可以形成4至7元環,其本身可任選地被一個或多個鹵素、氰基、C1 -C6 -烷基、C1 -C6 -鹵代烷基或C1 -C6 -烷氧基基團取代; 或者R9 和R10 取代基以及它們所連接的原子或其他選自C、N、O,和任選地包括C(=O)取代基的原子一起可以形成4至7元環,其本身可任選地被一個或多個鹵素、氰基、C1 -C6 -烷基、C1 -C6 -鹵代烷基或C1 -C6 -烷氧基基團取代; R'選自氫、鹵素、氰基、C1 -C6 -烷基、C2 -C6 -烯基、C2 -C6 -炔基、C3 -C8 -環烷基、OR”、N(R”)2 、S(O)0-2 R”、C(=O)R”、C(=O)OR”和C(=O)N(R”)2 ; R”選自氫、C1 -C6 -烷基、C2 -C6 -烯基和C2 -C6 -炔基和C3 -C8 -環烷基;其中每個R”基團可任選地被鹵素取代; 每個R1 至R10 、RA 、R2a 、R2aa 、R3a 、R4a 、R5a 、R7a 和R8a 可任選地被一個或多個選自X、CN、R '、OR”、SR'、N(R')2 、COOR”和CON(R')2 的基團取代; “n”為0〜2的整數; 或其農業上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、多晶型物、金屬絡合物、N-氧化物或S-氧化物。
A compound of formula (I),
Figure 03_image035
Formula (I) wherein, R 1 is selected from C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -Haloalkenyl, C 3 -C 8 -cycloalkyl and C 3 -C 8 -cycloalkyl-C 1 -C 6 -alkyl; Y is independently selected from O and/or NR y ; R y Selected from hydrogen, cyano, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -halo Alkenyl, C 3 -C 5 -cycloalkyl and C 3 -C 5 -cycloalkyl-C 1 -C 3 -alkyl; Q represents a 5- to 10-membered heterocyclic ring system, which may optionally be substituted by one Or multiple R 2 groups; R 2 is selected from hydrogen, halogen, cyano, nitro, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, C 1 -C 6 -cyanoalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , SCN, S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , P(=O)(OR”) 2 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclic group; Wherein each R 2 may be optionally substituted by one or more R 2a groups; R 2a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2- C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , SCN, S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , Si( R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; or two R 2a substituents and the atoms to which they are connected or other options Atoms from C, N, O, S, and optionally including 1 to 3 rings selected from C(=O), C(=S), S(O) 0-2 and Si(R”) 2 The members together can form a 3 to 7 membered ring, which itself can be optionally substituted by one or more R 2aa groups; R 2aa is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6. CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; A 1 and A 2 independently represent N or CR A ; R A is selected from hydrogen, halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 3 -C 8 - cycloalkyl, oR "and N (R") 2; wherein each R a groups may optionally be substituted with one or more R a radicals; R a 'is selected from halo, cyano Group, C 3 -C 8 -cycloalkyl, OR” and N(R”) 2 ; Z represents O or S; G 1 , G 2 , G 3 and G 4 independently represent N or CR 3 ; where in the ring There are no more than two Ns present in E; R 3 is selected from hydrogen, halogen, cyano, nitro, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynes Group, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O ) R 8 , S(O) 0-2 R 7 , SCN, S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , P(=O)( OR”) 2 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclic group; wherein each R 3 group can be any Is optionally substituted with one or more R 3a groups; R 3a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , CR 4 =NR 5 , C(=O)R 8 , S(O) 0-2 R 7 , S(O) 0-1 R 9 =NR 10 , N=S(O) 0-1 (R 9 ) 2 , Si(R”) 3 , C 6 -C 10 -aryl group, C 7 -C 14 -aralkyl group and C 3 -C 10 -heterocyclic group; R 4 is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -Cycloalkyl, S(O) 0-2 R 7 , Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocycle Group; wherein each R 4 group may be optionally substituted by R 4a group; R 4a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2- C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR'R", S(O) 0- 2 R', C(=O)R', Si(R”) 3 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 5 Selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl , C 3 -C 8 -Cycloalkyl, OR 4 , NR'R”, S(O) 0-2 R 7 , C(=O)R 8 , Si(R”) 3 , C 6 -C 10- Aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; wherein each R 54 group may be optionally substituted by R 5a ; R 5a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -Cycloalkyl, OR", NR'R", S(O) 0-2 R', C(=O)R', Si(R") 3 , C 6 -C 10 -aryl, C 7- C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 6 is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 1 -C 6 -cycloalkyl and C(=O)R 8 ; R 7 is selected from C 1 -C 6 -alkyl , C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, NR 5 R 6 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; wherein each R 7 group may optionally Substituted by one or more R 7a groups; R 7a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1- C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR'R", S(O) 0-2 R', C(=O) R', C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 8 is selected from hydrogen, C 1 -C 6 -alkyl, C 2- C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR 4 , NR 5 R 6 , N=S(O) 0-1 (R 9 ) 2 , C 6 -C 10 -aryl, C 7 -C 14 -aralkyl, and C 3 -C 10 -heterocyclic group; each of them R 8 may be optionally substituted with one or more R 8a groups; R 8a is selected from halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6- Alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, OR", NR'R", S(O) 0-2 R' , C(=O)R', C 6 -C 10 -aryl, C 7 -C 14 -aralkyl and C 3 -C 10 -heterocyclyl; R 9 is selected from C 1 -C 6 -alkyl , C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl and C (=O) R 8 ; R 10 is selected from hydrogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkane Group, C 2 -C 6 -haloalkenyl, C 3 -C 8 -cycloalkyl, Si(R”) 3 , S(O) 0-2 R 7 and C(=O)R 8 ; or two The R 9 substituents and the atoms to which they are attached or other atoms selected from C, N, O, and optionally including C(=O) substituents together can form a 4- to 7-membered ring, which itself may optionally be Substituted by one or more halogen, cyano, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl or C 1 -C 6 -alkoxy groups; or R 9 and R 10 substituents and The atoms to which they are attached or other atoms selected from C, N, O, and optionally including C(=O) substituents together can form a 4- to 7-membered ring, which itself may optionally be substituted by one or more halogens. , Cyano, C 1 -C 6 -alkane Group, C 1 -C 6 -haloalkyl or C 1 -C 6 -alkoxy group; R'is selected from hydrogen, halogen, cyano, C 1 -C 6 -alkyl, C 2 -C 6- Alkenyl, C 2 -C 6 -alkynyl, C 3 -C 8 -cycloalkyl, OR”, N(R”) 2 , S(O) 0-2 R”, C(=O)R”, C(=O)OR” and C(=O)N(R”) 2 ; R” is selected from hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl and C 2 -C 6- alkynyl, and C 3 -C 8 - cycloalkyl; wherein each R "group may optionally be substituted by halogen; each R 1 to R 10, R A, R 2a , R 2aa, R 3a, R 4a , R 5a , R 7a and R 8a may optionally be selected from X, CN, R', OR", SR', N(R') 2 , COOR" and CON(R') 2 Group substitution; "n" is an integer from 0 to 2; or its agriculturally acceptable salts, isomers/structural isomers, stereoisomers, diastereomers, enantiomers, Tautomers, polymorphs, metal complexes, N-oxides or S-oxides.
如請求項1所述的式(I)化合物,其中Q選自Q1至Q14:
Figure 03_image008
; 其中,#表示與DE環的連接點,
Figure 03_image010
表示與-S(Y)n R1 基團的連接點,並且Q環可任選被一個或多個R2 基團取代; 其中每個脂族基團可以任選地被一個或多個R2a 基團取代,並且R2 的環狀基團可以任選地被一個或多個R2b 基團取代; “n”為0〜2的整數。
The compound of formula (I) as described in claim 1, wherein Q is selected from Q1 to Q14:
Figure 03_image008
; Among them, # represents the connection point with the DE ring,
Figure 03_image010
Represents the point of attachment to the -S(Y) n R 1 group, and the Q ring may be optionally substituted by one or more R 2 groups; wherein each aliphatic group may be optionally substituted by one or more R The 2a group is substituted, and the cyclic group of R 2 may be optionally substituted with one or more R 2b groups; "n" is an integer from 0 to 2.
如請求項1所述的式(I)化合物,其中DE環選自式DE-a至DE-c;
Figure 03_image038
其中G1 、G2 、 G3 和G4 獨立地代表N或CR3 ;A1 和A2 獨立地代表N或CRA ; 其中,#表示與Q環的連接點。
The compound of formula (I) as described in claim 1, wherein the DE ring is selected from formulas DE-a to DE-c;
Figure 03_image038
Wherein G 1 , G 2 , G 3 and G 4 independently represent N or CR 3 ; A 1 and A 2 independently represent N or CR A ; where # represents the connection point with the Q ring.
如請求項1所述的式(I)化合物,其中DE環選自式DE1至DE16;
Figure 03_image040
其中,#表示與Q環的連接點,並且DE環可任選被一個或多個R3 和RA 基團取代。
The compound of formula (I) as described in claim 1, wherein the DE ring is selected from formulas DE1 to DE16;
Figure 03_image040
Wherein # denotes the point of attachment of the Q ring, and the ring may DE optionally substituted with one or more substituents R 3 and R A groups.
如請求項1所述的式(I)化合物,其中所述的式(I)化合物選自2-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(5-甲基-3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(3-(三氟甲基)-1H-1,2,4-三唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙硫基)-6'-氟代-[3,3'-二吡啶]-6-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6'-氟代-[3,3'-二吡啶]-6-基)-6-(三氟甲基)酞嗪-1(2H)-酮;7-(5-溴-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(6-氯-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-氟代-4-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;4-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)苯並腈;7-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-苯基吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-6-(3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(6-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;3-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙硫基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;7-(3-(乙基磺醯基)-6-(3-甲基-1H-1,2,4-三唑-1-基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-6-(3-氟代-4-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;4-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-2-基)苯並腈;7-(3-(乙基磺醯基)-6-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-苯基吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-甲氧基苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;7-(3-(乙基磺醯基)-6-苯基吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(5-(2,2-二氟苯並[d][1,3]二氧雜環戊烯-5-基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(6-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;4-(5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)喹唑啉-3(4H)-基)吡啶-3-基)苯並腈;3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(3-氯-4-(三氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(2-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(2-氟代-5-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-3-甲氧基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,4-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-3-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-環丙基-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)喹唑啉-4(3H)-酮;2-(6-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3,4,5-三氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟代-2-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(6-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-氟代-2-甲基苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(6-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(3,4,5-三氟苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;4-(5-(乙基磺醯基)-6-(4-氧代-7-(三氟甲基)喹唑啉-3(4H)-基)吡啶-3-基)苯並腈;3-(3-(乙基磺醯基)-5-(4-甲氧基苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-(4-溴苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-氟代-4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(2,2,2-三氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)喹唑啉-4(3H)-酮;3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)吡啶並[3,2-d]嘧啶-4(3H)-酮;2-(3-(乙基磺醯基)-5-(4-(全氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(全氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯並腈;2-(3-(乙基磺醯基)-5-(4-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,4-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-環丙基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯基)環丙烷-1-甲腈;2-(5-(4-(二氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6'-氟代-[3,3'-二吡啶]-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(5-溴-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(甲硫基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;2-(5-(3,4-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3-氯-5-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-硫酮;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)煙腈;2-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯-3-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-氯-5-(三氟甲基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-氯-5-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯並腈;2-(3-(乙基磺醯基)-5-(2-氟代-5-(三氟甲氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氯-2-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-溴苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙酸乙酯;2-(4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯氧基)-2,2-二氟-N,N-二甲基乙醯胺;2-(3-(乙基磺醯基)-5-(3,3,3-三氟丙基-1-烯-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(2,2,3,3,3-五氟丙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟苯並[d][1,3]二氧雜環戊烯-5-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)乙腈;2-(3-(乙基磺醯基)-5-(1,1,2,3,3,3-六氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-羥基苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5'-(乙基磺醯基)-6'-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-[2,3'-二吡啶]-5-甲腈;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)嘧啶-5-甲腈;2-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,3,3-五氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(嘧啶-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-甲基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((甲硫基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(環丙基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-溴-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-溴-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(5-((二甲基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((甲基磺醯基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(4-(乙基磺醯基)-6-(3-(三氟甲基)苯基)噠嗪-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(氧雜環丁烷-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙醯胺;2-(3-(乙基磺醯基)-6-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((二乙基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5'-(乙基磺醯基)-4-(三氟甲基)-[2,3'-二吡啶]-6'-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5'-(乙基磺醯基)-5-(三氟甲基)-[2,3'-二吡啶]-6'-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3-(苄氧基)環丁氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3-氯-4-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(3-(乙基磺醯基)-5-(2-甲氧基嘧啶-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)乙腈;2-(5-溴-3-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙硫基)-5-(4-氟苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(5-(2-溴-1,1,2,2-四氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙硫基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(4-氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(3,5-二氯苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(3,5-二氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(3-氯-5-氟苯基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)-5-(3-(三氟甲基)苯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(5-((4,4-二氟but-3-烯-1-基)氧)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-氟代-5-(三氟甲基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈;2-(3-(乙基磺醯基)-5-(4-(甲基磺醯基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙硫基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基) 乙基膦酸乙酯;2-(5-(二甲基磷醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((S-甲基磺醯亞胺基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯亞胺基)-5-(4-氟苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1,1,2,2-四氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(3-(乙基磺醯基)-5-羥基吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙硫基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-((二乙基((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-(3-(乙基磺醯基)-5-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-氟苯基)-3-(N-甲基乙基磺醯亞胺基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮; (5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氨基甲酸叔丁酯;2-(5-((乙基(甲基)((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(5-((乙基(異丙基)((氧代)-l6-亞硫烷基)氨基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基 氨基磺酸二甲酯;2-((5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基)氧)乙腈;3-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(環丙基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(3-(乙基磺醯基)-5-(甲氧基甲氧基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;3-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-6-(三氟甲基)苯並[d][1,2,3]三嗪-4(3H)-酮;2-((5-(乙基磺醯基)-6-(4-氧代-6-(三氟甲基)苯並[d][1,2,3]三嗪-3(4H)-基)吡啶-3-基)氧)-2-甲基丙醯胺;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2-甲基丙腈;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基氨基磺酸二甲酯;2-(5-氨基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-氯-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((4-氧負離子基-1,4l6-氧雜蒽-4-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(乙硫基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺;2-(3-(乙基磺醯基)-6-(5-甲基-3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((2,2,2-三氟乙基)硫代)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3,5-雙(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氟乙基)硫代)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯亞胺基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氟乙基)磺醯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(4-(二甲基磷醯基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷甲醯胺;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙腈;2-(3-(乙基磺醯基)-5-異丙氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((1,1,1-三氟-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-氧負離子基-4,5-二氫-3H-1l6-異噻唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((3-羥基-1-氧化四氫-1l6-噻吩-1-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((4-氧負離子基-1,4l6-氧雜蒽-4-基亞基)氨基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯磺醯氟;2-(5-(4-(二甲基磷醯基)苯基)-3-(乙基磺醯亞胺基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5'-(乙基磺醯基)-6'-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-[3,3'-二吡啶]-6-磺醯氟;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-磺醯氟;2-(5-(4-(1,1-二氟乙基)苯基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-(三氟甲基)環丙基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1,3,5-三甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-甲基-3-(三氟甲基)-1H-吡唑-5-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-異丁基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲氧基-1-甲基-1H-吡唑-4-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(1'-(二氟甲基)-5-(乙基磺醯基)-6'-氧代-1',6'-二氫-[3,3'-二吡啶]-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-異丙基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-二甲基異唑-4-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-4-甲基-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯亞胺基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)苯基 氟化硫;2-(3-(乙基磺醯亞胺基)-5-((1,1,1-三氟-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯亞胺基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-甲基丙腈;2-(3-(乙基磺醯基)-5-((甲基亞磺醯基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,3-四氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1,1,2-三氟-2-(三氟甲氧基)乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,4,4,4-六氟丁氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,3,3,3-五氟丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟-2-(三氟甲氧基)乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2,2-二氟環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-2,2-二甲基環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-氟環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-N-甲基環丁烷甲醯胺;1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3,3-二甲基環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3,3-二氟環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環丁烷甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3-甲基環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-3-氧代環丁烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環戊烷甲醯胺;1-氰基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環戊烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基環戊烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)環己烷甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4-甲基環己烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4,4-二氟環己烷-1-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氮雜環丁烷-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基氮雜環丁烷-3-甲醯胺;1-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氮雜環丁烷-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧雜環丁烷e-3-甲醯胺;3-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧雜環丁烷e-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基吡咯烷-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)四氫呋喃-3-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)呱啶-4-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-1-甲基呱啶-4-甲醯胺;1-乙基-N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)呱啶-4-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)四氫-2H-吡喃-4-甲醯胺;N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)-4-氟四氫-2H-吡喃-4-甲醯胺;2-(7-溴-3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-7-(三氟甲基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-基)乙腈;3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-甲腈;2-(3-(乙基磺醯基)-7-甲氧基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-7-基)環丙烷-1-甲腈;2-(3-(乙基磺醯基)-7-(2,2,2-三氟乙基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(乙基磺醯基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-6-(三氟甲基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-甲腈;2-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-基)乙腈;2-(3-(乙基磺醯基)-7-(1-甲基環丙基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-7-(甲基氨基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)煙腈;2-(5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)乙腈;1-(5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)環丙烷-1-甲腈;2-((5-(乙基磺醯基)-6-(8-氧代-2-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)氧)-2-甲基丙腈;7-(5-(二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(全氟乙基)酞嗪-1(2H)-酮;5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)煙腈;2-(5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)吡啶-3-基)乙腈;1-(5-(乙基磺醯基)-6-(1-氧代-7-(全氟乙基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈;5-(乙基磺醯基)-6-(1-氧代-7-((三氟甲基)磺醯基)酞嗪-2(1H)-基)煙腈;2-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-7-((三氟甲基)磺醯基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-((三氟甲基)磺醯基)酞嗪-1(2H)-酮;1-(5-(乙基磺醯基)-6-(1-氧代-7-((三氟甲基)磺醯基)酞嗪-2(1H)-基)吡啶-3-基)環丙烷-1-甲腈;7-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;7-(3-(乙基磺醯基)-5-(4-(三氟甲氧基)苯基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)乙腈;1-(5-(乙基磺醯基)-6-(8-氧代-3-(三氟甲基)吡啶並[2,3-d]噠嗪-7(8H)-基)吡啶-3-基)環丙烷-1-甲腈;7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-3-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(3-(乙基磺醯基)-5-(乙硫基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((2-(三氟甲基)環丙基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲氧基雜氮環丁烷-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((1-甲基雜氮環丁烷-3-基)氧)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2H-1,2,3-三唑-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-1,2,4-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-(2-羥基-2-甲基丙基)-1H-1,2,3-三唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲基-5-(三氟甲基)-1H-吡唑-1-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,5-雙(三氟甲基)-1H-吡唑-1-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(2,2,2-三氟乙氧基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(4-氟苯基)吡啶-2-基)-7-(2,2,3,3,3-五氟丙氧基)酞嗪-1(2H)-酮;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]嘧啶-7-基)環丙烷-1-甲腈;2-(3-(乙基磺醯基)-6-甲基咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-(乙基磺醯基)-2-(三氟甲基)吡唑並[1,5-a]嘧啶-5-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[2,1-b]噻唑-2-甲腈;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]嘧啶-6-基)環丙烷-1-甲腈;1-(3-(乙基磺醯基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡唑並[1,5-a]吡啶-5-基)環丙烷-1-甲腈;2-(2-(乙基磺醯基)-7-甲基吡唑並[1,5-a]嘧啶-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-1-甲基-6-(三氟甲氧基)-1H-吲哚-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-1H-吡咯並[2,3-b]吡啶-1-基)乙腈;2-(5-(乙基磺醯基)-1-甲基-1H-吡唑並[3,4-b]吡啶-6-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(7-環丙基-2-(乙基磺醯基)咪唑並[1,2-a]嘧啶-3-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)咪唑並[1,2-a]吡嗪-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)咪唑並[1,2-b]噠嗪-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(溴二氟甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(吡啶-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(吡啶-2-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((5-溴吡啶-2-基)氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(嘧啶-2-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((1-甲基-1H-吡唑-3-基)氧)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(3,3-二氟環丁氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,3-二氟丙烷-2-基)氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(新戊基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)甲基)環丙烷-1-甲腈;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丙腈;2-(3-(乙基磺醯基)-5-((1-氟代-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-甲氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2-氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-2-(甲硫基)乙腈;2-(5-((2,2-二氟環丙基)甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;4-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丁腈;2-(5-(環丁基甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟丙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(1-氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-N,N-二甲基-2-(甲硫基)乙醯胺;2-乙基-2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)丁腈;2-(3-(乙基磺醯基)-5-異丁氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2,2,2-三氟乙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2-溴-1,1-二氟乙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((3-環丙基異惡唑-5-基)甲氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲氧基環丁氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基 二氟甲磺酸酯;3-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)環丁烷-1-甲腈;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基氟甲磺酸酯;3-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-3-甲基丁腈;5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基三氟甲磺酸酯;2-(3-(乙基磺醯基)-5-((1-甲氧基-2-甲基丙烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)-N,N,2-三甲基丙醯胺;2-(3-(乙基磺醯基)-5-((3-甲基氧雜環丁烷-3-基)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;(E)-2-(3-(乙基磺醯基)-5-(2-(甲基亞氨基)丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((三甲基silyl)甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2-氧丙氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-((2-甲基-3-氧代丁烷-2-基)氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(烯丙氧基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-丙氧基吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-乙氧基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(甲氧基甲氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-環丁基-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(2,2-二氟環丙基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(2-甲基氧雜環丁烷-2-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(乙基磺醯基)-5-(3-甲基硫雜環丁烷基-3-基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-(1,1-二氧負離子基硫雜環丁烷基-2-基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;6-((5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-3-基)氧)煙腈;2-(3-(乙基磺醯基)-5-(硫雜環丁烷基-3-基氧基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氧負離子基硫雜環丁烷基-3-基)氧)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(5-((1,1-二氧負離子基硫雜環丁烷基-3-基)甲基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;7-(3-(乙基磺醯基)-5-(三氟甲基)吡啶-2-基)-2-(三氟甲基)吡啶並[2,3-d]噠嗪-8(7H)-酮;2-(3-(N-甲基乙基磺醯亞胺基)-5-(3-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(3-(N-甲基乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;N-(乙基((氧代)(2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-3-基)-l6-亞硫烷基)氰胺;2-(3-(N-乙基乙基磺醯亞胺基)-5-(4-(1,1,2,2-四氟乙氧基)苯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(乙基磺醯亞胺基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;2-(6-溴-3-(N-甲基乙基磺醯亞胺基)咪唑並[1,2-a]吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮;1-(3-(乙基磺醯亞胺基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-基)環丙烷-1-甲腈;3-(乙基磺醯亞胺基)-2-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)咪唑並[1,2-a]吡啶-6-甲腈;2-(6-(環丙基氨基)-3-(乙基磺醯基)吡啶-2-基)-7-(三氟甲基)酞嗪-1(2H)-酮和N-(5-(乙基磺醯基)-6-(1-氧代-7-(三氟甲基)酞嗪-2(1H)-基)吡啶-2-基)環丙烷甲醯胺。The compound of formula (I) according to claim 1, wherein the compound of formula (I) is selected from 2-(3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl )Phthalazine-1(2H)-one; 2-(3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5 -Bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-bromo-3-(ethylsulfonyl) )Pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-chloro-3-(ethylsulfonyl)pyridin-2-yl)-6 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl) -6-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylthio)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-6-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-6-( Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(5-methyl-3-(trifluoromethyl)-1H-pyrazole- 1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(3-(trifluoro) (Methyl)-1H-pyrazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) -6-(3-(Trifluoromethyl)-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -Ketone; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(Ethylthio)-6'-fluoro-[3,3'-dipyridine]-6-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(Ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H) -Ketone; 2-(5-(Ethylsulfonyl)-6'-fluoro-[3,3'-dipyridine]-6-yl)-6-(trifluoromethyl)phthalazine-1( 2H)-one; 7-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H )-Ketone; 7-(3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(6-Chloro-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8 (7H)-ketone; 7-(3-(ethylsulfonyl)-5-(3-fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoro Methyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)- 3-(Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy) (Phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl) )-5-(4-Fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H)-one; 7-(3-(ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d ]Pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoro Methyl)pyrido[2,3-d]pyridazine-8(7H)-one; 4-(5-(ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl) )Pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)benzonitrile; 7-(3-(ethylsulfonyl)-6-(4-(tri Fluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethyl) Sulfonyl)-5-phenylpyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(5-(3 ,5-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)- Ketone; 7-(5-(3,5-Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d ]Pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl )-3-(Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-6-(3-(trifluoro (Methyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(6-(3,5- two Chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 3- (3-(Ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)pyridine- 2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylthio)-5-(trifluoromethyl)pyridin-2-yl)- 6-(Trifluoromethyl)quinazolin-4(3H)-one; 7-(3-(ethylsulfonyl)-6-(3-methyl-1H-1,2,4-triazole) -1-yl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl) )-6-(3-Fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8( 7H)-one; 4-(5-(ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H) -Yl)pyridin-2-yl)benzonitrile; 7-(3-(ethylsulfonyl)-6-(4-fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl )-3-(Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 3-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl )-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-6 -(Trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)- 6-(Trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-6- (Trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-phenylpyridin-2-yl)-6-(trifluoromethyl)quine Oxazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-methoxyphenyl)pyridin-2-yl)-6-(trifluoromethyl)quine Oxazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl) Yl)quinazolin-4(3H)-one; 7-(3-(ethylsulfonyl)-6-phenylpyridin-2-yl)-3-(trifluoromethyl)pyrido[2, 3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethoxy)phenyl)pyridine-2 -Yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(5-(2,2-difluorobenzo[d][1 ,3]Dioxol-5-yl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine -8(7H) -Ketone; 7-(6-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3- d]Pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine- 2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 3-(3-(ethylsulfonyl)-5-(3- (Trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 4-(5-(ethylsulfonyl)-6 -(4-oxo-6-(trifluoromethyl)quinazolin-3(4H)-yl)pyridin-3-yl)benzonitrile; 3-(3-(ethylsulfonyl)-5 -(4-(Trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(3,5- Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(4-chloro Phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl) )-5-(3-(Trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethyl) Sulfonyl)-5-(2-fluoro-4-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(3-chloro-4-(trifluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)quinazoline- 4(3H)-one; 3-(3-(ethylsulfonyl)-5-(2-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-6-( Trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(4-fluoro-3-(trifluoromethyl)phenyl)pyridine- 2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(2-fluoro-5-(trifluoro) Methoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(4 -Fluoro-3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonate) Yl)-5-(4-fluoro-3-methoxyphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-( 2,4-Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-( Ethylsulfonyl)-5-(4-fluoro-3-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-( 5-(4-chlorophenyl)-3-(ethyl Sulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-cyclopropyl-3-(ethylsulfonyl)pyridine- 2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(4-fluorophenyl)pyridin-2-yl )-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-pyrazole- 1-yl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6-(4-(trifluoro) Methoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-(4- (1,1,2,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)quinazolin-4(3H)-one; 2-(6-( 4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2-chloro -4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-5-(3,4,5-trifluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-( Ethylsulfonyl)-5-(4-fluoro-2-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-( 6-Chloro-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) -6-(4-Fluoro-2-methylphenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-(2-chloro -4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-6-(3,4,5-trifluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-bromo -3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5-(3,5-dichlorophenyl) -3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5 -(4-Fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-( 4-(Trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 2-(3-(ethylsulfonyl) -5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6- (4-Fluorophenyl)pyridine-2 -Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl) -7-(Trifluoromethyl)phthalazine-1(2H)-one; 3-(5-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl) -7-(Trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridine- 2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 4-(5-(ethylsulfonyl)-6-(4-oxo-7-(trifluoro) Methyl)quinazolin-3(4H)-yl)pyridin-3-yl)benzonitrile; 3-(3-(ethylsulfonyl)-5-(4-methoxyphenyl)pyridine- 2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridine-2- Yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl) -7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone; 2-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 3-(3-(Ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazoline-4( 3H)-one; 3-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7- (Trifluoromethyl)quinazolin-4(3H)-one; 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy) Phenyl)pyridin-2-yl)-6-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(1,1 ,2,2-Tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) )-5-(4-(Trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-6-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5- (4-Bromophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)quinazolin-4(3H)-one; 3-(3-(ethyl) Sulfonyl)-5-(3-fluoro-4-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)quinazoline-4(3H)- Ketone; 3-(3-(Ethylsulfonyl)-5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl ) Quinazolin-4(3H)-one; 3 -(5-Bromo-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one; 3- (5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidine-4(3H) -Ketone; 3-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidine -4(3H)-ketone; 3-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl) -7-(Trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(3-(trifluoromethoxy) (Yl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)pyrido[3,2-d]pyrimidin-4(3H)-one; 2-(3-(ethylsulfonyl) -5-(4-(perfluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5 -Difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5 -Dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) (Phenyl)-5-(4-(perfluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione; 2-(3- (Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-thione; 2-(3-(ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl Yl)phthalazine-1(2H)-one; 4-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl) )Pyridin-3-yl)benzonitrile; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(5-(3,4-difluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(5-cyclopropyl-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone; 1-(4-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine- 3-yl)phenyl)cyclopropane-1-carbonitrile; 2-(5-(4-(difluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7 -(Trifluoro Methyl)phthalazine-1(2H)-one; 2-(5-(ethylsulfonyl)-6'-fluoro-[3,3'-dipyridyl]-6-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-thione; 2-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-4-methyl-7-( Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(methylthio)phenyl)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-4-methyl- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-thione; 2-(5-(3,4-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3-chloro-5-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy) Phenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4 -(Trifluoromethoxy)phenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfon) Aceto)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-thione; 5-(ethylsulfonyl)-6 -(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)nicotinonitrile; 2-(5-(3,5-dichlorophenyl)-3-(ethylsulfon) (Pyridine-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chlorophenyl)-3-(ethyl Sulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3,5-difluorophenyl) -3-(Ethylsulfonyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-chloro- 3-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2-chloro -5-(trifluoromethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 3-chloro -5-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)benzonitrile; 2-(3-(Ethylsulfonyl)-5 -(2-Fluoro-5-(trifluoromethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-( 4-chloro-2-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2-(5- (4-Bromophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethyl Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2-methylpropionate; 2-(4-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenoxy Yl)-2,2-difluoro-N,N-dimethylacetamide; 2-(3-(ethylsulfonyl)-5-(3,3,3-trifluoropropyl-1- En-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-( 2,2,3,3,3-Pentafluoropropoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-( 2,2-Difluorobenzo[d][1,3]dioxol-5-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl Yl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)- Yl)pyridin-3-yl)oxy)acetonitrile; 2-(3-(ethylsulfonyl)-5-(1,1,2,3,3,3-hexafluoropropoxy)pyridine-2- Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-hydroxyphenyl)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-hydroxypyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(5-(2-chloro-4-fluorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridine-2- Group)-7-(trifluoromethyl)phthalazine-1(2H)-one; 5'-(ethylsulfonyl)-6'-(1-oxo-7-(trifluoromethyl)phthalein Azin-2(1H)-yl)-[2,3'-dipyridine]-5-carbonitrile; 2-(5-(ethylsulfonyl)-6-(1-oxo-7-(three Fluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)pyrimidine-5-carbonitrile; 2-(3-(ethylsulfonyl)-5-(2,2,2-tri Fluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2,2, 3,3,3-pentafluoropropoxy) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-fluorophenyl)pyridine-2 -Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-3-(trifluoromethyl) )-1H-pyrazol-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5 -(Pyrimidine-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-methyl Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((methylthio)methoxy) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(cyclopropylmethoxy)-3-(ethylsulfonyl)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5-bromo-3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl) Yl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(5-bromo-3-(ethylsulfonyl)pyridin-2-yl)-6-( Trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(5-((dimethyl((oxo)-l6-sulfinyl)) Amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)- 5-((Methylsulfonyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(4-(ethylsulfonyl) )-6-(3-(trifluoromethyl)phenyl)pyridazin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-5-(oxetan-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2-((5 -(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2-methylpropionyl Amine; 2-(3-(Ethylsulfonyl)-6-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(5-((diethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5'-(ethylsulfonyl)-4-(trifluoromethyl)-[2,3 '-Dipyridine]-6'-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5'-(ethylsulfonyl)-5-(trifluoromethyl) Yl)-[2,3'-dipyridyl]-6'-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3-(benzyloxy) Cyclobutoxy)-3-( Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(3-chloro-4-fluorophenyl)-3- (Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-(4- Fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(3-(ethylsulfon) Amino)-5-(2-methoxypyrimidin-5-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2-(5-(ethyl Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)acetonitrile; 2-(5-bromo-3-( Ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-(4-(trifluoro) Methoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(3-( Ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d] [1,2,3]Triazine-4(3H)-one; 3-(3-(ethylthio)-5-(4-fluorophenyl)pyridin-2-yl)-6-(trifluoromethyl Yl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(5-(4-chlorophenyl)-3-(ethylthio)pyridin-2-yl) -6-(Trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(5-(2-bromo-1,1,2,2-tetra Fluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylthio) -5-(4-(Trifluoromethoxy)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H) -Ketone; 3-(5-(4-chlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2, 3] Triazine-4(3H)-one; 3-(5-(3,5-dichlorophenyl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl Yl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(5-(3,5-difluorophenyl)-3-(ethylsulfonyl)pyridine -2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(5-(3-chloro-5-fluorobenzene) Yl)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3 -(3-(Ethylsulfonyl)-5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2 ,3] Triazine-4(3H)-one; 2 -(5-((4,4-Difluorobut-3-en-1-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(3-(ethylthio)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-1H-pyrazol-5-yl)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-1H-pyrazole-4) -Yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-fluoro-5 -(Trifluoromethyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 1-(5-(ethylsulfonyl)-6- (1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropane-1-carbonitrile; 2-(3-(ethylsulfonyl) -5-(4-(Methylsulfonyl)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylthio) )-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; (5-(ethylsulfonyl)-6-( 1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl) ethyl phosphonate; 2-(5-(dimethylphosphoryl)- 3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonylimino)-5 -(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-( 3-(Ethylsulfonyl)-5-((S-methylsulfonylimino)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -Ketone; 2-(3-(ethylsulfonylimino)-5-(4-fluorophenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-5-(1,1,2,2-tetrafluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine- 1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridine-2- Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(3-(ethylsulfonyl)-5-hydroxypyridin-2-yl)-6-(trifluoromethyl) Yl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(3-(ethylthio)pyridin-2-yl)-6-(trifluoromethyl)benzene And [d][1,2,3]triazine-4(3H)-one; 3-(3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo [d][1,2 ,3] Triazine-4(3H)-one; 3-(5-((diethyl((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridine- 2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-(3-(ethylsulfonyl)-5- (Ethylthio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-fluorophenyl)-3-(N-methyl) Ethylsulfonylimino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; (5-(ethylsulfonylimino)-6-(1-oxygen) Tert-butyl -7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)carbamate; 2-(5-((ethyl(methyl)((oxo) -l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3-(5- ((Ethyl(isopropyl)((oxo)-l6-sulfinyl)amino)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzene And [d][1,2,3]triazine-4(3H)-one; 5-(ethylsulfonyl)-6-(4-oxo-6-(trifluoromethyl)benzo[ d][1,2,3]triazine-3(4H)-yl)pyridin-3-yl dimethylsulfamate; 2-((5-(ethylsulfonyl)-6-(4- Oxo-6-(trifluoromethyl)benzo[d][1,2,3]triazine-3(4H)-yl)pyridin-3-yl)oxy)acetonitrile; 3-(3-(ethyl) Sulfonyl)-5-(2,2,2-trifluoroethoxy)pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine -4(3H)-one; 3-(5-(cyclopropylmethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-6-(trifluoromethyl)benzo[d ][1,2,3]triazine-4(3H)-one; 3-(3-(ethylsulfonyl)-5-(methoxymethoxy)pyridin-2-yl)-6- (Trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 3-(5-(difluoromethoxy)-3-(ethylsulfonyl) Pyridin-2-yl)-6-(trifluoromethyl)benzo[d][1,2,3]triazine-4(3H)-one; 2-((5-(ethylsulfonyl) -6-(4-oxo-6-(trifluoromethyl)benzo[d][1,2,3]triazine-3(4H)-yl)pyridin-3-yl)oxy)-2- Methylpropionamide; 2-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl )-2-Methylpropionitrile; 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl Dimethyl sulfamate; 2-(5-amino-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2- (5- Chloro-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-6 -(1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-5-((4-oxoanion-1,4l6-xanthene-4-yl subunit) amino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-one; 2-(6-bromo-3-(ethylthio)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H )-Ketone; 2-(5-(difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one ; 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl ) Cyclopropane-1-carboxamide; 2-(3-(ethylsulfonyl)-6-(5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)pyridine -2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((2,2,2-trifluoroethane) (Yl)thio)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3,5-bis(ethylsulfonyl)pyridin-2-yl) )-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-((1,1-difluoroethyl)thio)-3-(ethylsulfonyl)pyridine -2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(ethylsulfonylimino)-3-(ethylsulfonyl)pyridine- 2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-((1,1-difluoroethyl)sulfonyl)-3-(ethylsulfon (Dimethyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(4-(dimethylphosphoryl)phenyl)-3- (Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; N-(5-(ethylsulfonyl)-6-(1- Oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopropanecarboxamide; 2-((5-(ethylsulfonyl)-6-( 1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-2-methylpropionitrile; 2-(3-(ethylsulfonyl) )-5-isopropoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(( 1,1,1-Trifluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-( 3-(Ethylsulfonyl)-5-(trifluoromethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-( Ethyl sulfonate Aceto)-5-(1-oxyanion-4,5-dihydro-3H-1l6-isothiazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1 (2H)-ketone; 2-(3-(ethylsulfonyl)-5-((3-hydroxy-1-oxytetrahydro-1l6-thiophen-1-yl subunit) amino)pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((4-oxoanion-1,4l6-xanthene -4-yl subunit)amino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 4-(5-(ethylsulfonyl)-6-( 1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)benzenesulfonyl fluoride; 2-(5-(4-(dimethylphosphoryl) Phenyl)-3-(ethylsulfonylimino)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 5'-(ethylsulfonylimino) -6'-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)-[3,3'-dipyridine]-6-sulfonyl fluoride; 5-(ethyl Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3-sulfonyl fluoride; 2-(5-(4-(1, 1-Difluoroethyl)phenyl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3- (Ethylsulfonyl)-5-(1-(trifluoromethyl)cyclopropyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2- (3-(Ethylsulfonyl)-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoro Methyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-methyl-3-(trifluoromethyl)-1H-pyrazole-5- Yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-isobutyl-1H -Pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3 -Methoxy-1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(1'- (Difluoromethyl)-5-(ethylsulfonyl)-6'-oxo-1',6'-dihydro-[3,3'-dipyridine]-6-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-isopropylpyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-one; 2-(5-(3,5-dimethylisoxazol-4-yl)-3-(ethylsulfonyl)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-(1,1,2,2-tetrafluoroethoxy) )Phenyl)pyridin-2-yl)-4-methyl-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonylimino)-5 -(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 4-( 5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)phenylsulfur fluoride; 2- (3-(Ethylsulfonylimino)-5-((1,1,1-trifluoro-2-methylpropan-2-yl)oxy)pyridin-2-yl)-7-(tri Fluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonylimino)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2 (1H)-yl)pyridin-3-yl)oxy)-2-methylpropionitrile; 2-(3-(ethylsulfonyl)-5-((methylsulfinyl)methoxy) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2,2,3,3-tetra Fluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1,1, 2-Trifluoro-2-(trifluoromethoxy)ethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-5-(2,2,3,4,4,4-hexafluorobutoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-5-(2,2,3,3,3-pentafluoropropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(5-(2,2-difluoro-2-(trifluoromethoxy)ethoxy)-3-(ethylsulfonyl)pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalein) (Azin-2(1H)-yl)pyridin-3-yl)-2,2-difluorocyclopropane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxygen) Substitution-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-2,2-dimethylcyclopropane-1-carboxamide; N-(5-(ethyl Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-fluorocyclopropane-1-carboxamide ; N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methyl Cyclopropane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine -3-yl)-N-methyl ring Butanecarboxamide; 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl) Pyridin-3-yl) cyclopropane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H )-Yl)pyridin-3-yl)-3,3-dimethylcyclobutane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7 -(Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3,3-difluorocyclobutane-1-carboxamide; N-(5-(ethylsulfonamide) Yl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclobutanecarboxamide; N-(5-(ethyl) Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylcyclobutane-1-methyl Amine; N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-3- Methylcyclobutane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl) )Pyridin-3-yl)-3-oxocyclobutane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl) )Phthalazine-2(1H)-yl)pyridin-3-yl)cyclopentanecarboxamide; 1-cyano-N-(5-(ethylsulfonyl)-6-(1-oxo- 7-(Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclopentane-1-carboxamide; N-(5-(ethylsulfonyl)-6-( 1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylcyclopentane-1-carboxamide; N-(5-( Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)cyclohexanecarboxamide; N-(5 -(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4-methylcyclohexane- 1-Formamide; N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl )-4,4-Difluorocyclohexane-1-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine- 2(1H)-yl)pyridin-3-yl)azetidine-3-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(three Fluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1-methylazetidine-3-carboxamide; 1-ethyl-N-(5-(ethyl) Sulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)azetidine-3-methanamide; N -(5-(Ethylsulfonyl)-6-(1- Oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxetane e-3-formamide; 3-ethyl-N-(5- (Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxetane e-3-methyl Amide; N-(5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-1 -Methylpyrrolidine-3-methanamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl) )Pyridin-3-yl)tetrahydrofuran-3-carboxamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H )-Yl)pyridin-3-yl)piperidine-4-methamide; N-(5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine -2(1H)-yl)pyridin-3-yl)-1-methylpiperidine-4-carboxamide; 1-ethyl-N-(5-(ethylsulfonyl)-6-(1 -Oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)piperidine-4-methamide; N-(5-(ethylsulfonyl)- 6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)tetrahydro-2H-pyran-4-carboxamide; N-(5 -(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)-4-fluorotetrahydro-2H- Pyran-4-carboxamide; 2-(7-bromo-3-(ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(3-(ethylsulfonyl)-7-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl) Fluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H) -Yl)imidazo[1,2-a]pyridin-7-yl)acetonitrile; 3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2 (1H)-yl)imidazo[1,2-a]pyridine-7-carbonitrile; 2-(3-(ethylsulfonyl)-7-methoxyimidazo[1,2-a]pyridine -2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; 1-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalein Azin-2(1H)-yl)imidazo[1,2-a]pyridin-7-yl)cyclopropane-1-carbonitrile; 2-(3-(ethylsulfonyl)-7-(2, 2,2-Trifluoroethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-bromo- 3-(Ethylsulfonyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl) Sulfonyl)-6-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 3- (Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-6-carbonitrile; 2-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine- 6-yl)acetonitrile; 2-(3-(ethylsulfonyl)-7-(1-methylcyclopropyl)imidazo[1,2-a]pyridin-2-yl)-7-(tris Fluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-7-(methylamino)imidazo[1,2-a]pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 7-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy) )Phenyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl) -5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine -8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl)-2-(trifluoromethyl )Pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-2 -(Trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 5-(ethylsulfonyl)-6-(8-oxo-2-(trifluoromethyl) Yl)pyrido[2,3-d]pyridazine-7(8H)-yl)nicotinonitrile; 2-(5-(ethylsulfonyl)-6-(8-oxo-2-(trifluoro Methyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)acetonitrile; 1-(5-(ethylsulfonyl)-6-(8-oxo) -2-(Trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)cyclopropane-1-carbonitrile; 2-((5-(ethyl Sulfonyl)-6-(8-oxo-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridin-3-yl)oxy)- 2-methylpropionitrile; 7-(5-(difluoromethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3 -d]Pyridazine-8(7H)-one; 2-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-(perfluoroethyl)phthalein Azin-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(perfluoroethyl)phthalazine- 1(2H)-ketone; 2-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)- 7-(perfluoroethyl)phthalazine-1(2H)-one; 5-(ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H) )-Yl)nicotinonitrile; 2-(5-(ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)pyridine-3- Yl)acetonitrile; 1-(5-(ethylsulfonyl)-6-(1-oxo-7-(perfluoroethyl)phthalazine-2(1H)-yl)pyridin-3-yl) ring Propane-1-carbonitrile; 5-(ethylsulfonyl)-6-(1-oxo-7-((trifluoromethyl)sulfonyl)phthalazine-2(1H)-yl)nicotinonitrile ; 2-(3-(Ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-7-((trifluoromethyl)sulfonyl)phthalazine-1(2H)- Ketone; 2-(3-(Ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-((trifluoromethyl)sulfonyl)phthalazine-1(2H )-Ketone; 1-(5-(ethylsulfonyl)-6-(1-oxo-7-((trifluoromethyl)sulfonyl)phthalazine-2(1H)-yl)pyridine- 3-yl)cyclopropane-1-carbonitrile; 7-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-3-(trifluoromethyl)pyridine And [2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl)-5-(4-(1,1,2,2-tetrafluoroethoxy) )Phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 7-(3-(ethylsulfonyl) -5-(4-(Trifluoromethoxy)phenyl)pyridin-2-yl)-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 2-(5-(Ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H)-yl)pyridine- 3-yl)acetonitrile; 1-(5-(ethylsulfonyl)-6-(8-oxo-3-(trifluoromethyl)pyrido[2,3-d]pyridazine-7(8H )-Yl)pyridin-3-yl)cyclopropane-1-carbonitrile; 7-(3-(ethylsulfonyl)-5-(trifluoromethyl)pyridin-2-yl)-3-(tris Fluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 2-(3-(ethylsulfonyl)-5-(ethylthio)pyridin-2-yl)- 7-(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((2-(trifluoromethyl)cyclopropyl)methoxy )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-methoxy azacyclo Butane-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-((1 -Methyl azacyclic ring Butane-3-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-( 1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) Yl)-5-(2H-1,2,3-triazol-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 2-(3 -(Ethylsulfonyl)-5-(3-(trifluoromethyl)-1H-1,2,4-triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl) )Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-(2-hydroxy-2-methylpropyl)-1H-1,2,3- Triazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3- (Trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfon) Amino)-5-(3-methyl-5-(trifluoromethyl)-1H-pyrazol-1-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-one; 2-(5-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)-7-(2 ,2,2-Trifluoroethoxy)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(4-fluorophenyl)pyridin-2-yl)- 7-(2,2,3,3,3-pentafluoropropoxy)phthalazine-1(2H)-one; 1-(3-(ethylsulfonyl)-2-(1-oxo- 7-(Trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyrimidin-7-yl)cyclopropane-1-carbonitrile; 2-(3-(ethylsulfon) (Acidyl)-6-methylimidazo[1,2-a]pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(6-(ethyl) Sulfonyl)-2-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-5-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 5- (Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[2,1-b]thiazole-2-carbonitrile; 1-(3-(Ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyrimidine- 6-yl)cyclopropane-1-carbonitrile; 1-(3-(ethylsulfonyl)-2-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl )Pyrazolo[1,5-a]pyridin-5-yl)cyclopropane-1-carbonitrile; 2-(2-(ethylsulfonyl)-7-methylpyrazolo[1,5- a] pyridine Pyridin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-1-methyl-6-(trifluoromethoxy) Yl)-1H-indol-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(ethylsulfonyl)-6-(1-oxygen) Substituted-7-(trifluoromethyl)phthalazine-2(1H)-yl)-1H-pyrrolo[2,3-b]pyridin-1-yl)acetonitrile; 2-(5-(ethylsulfonyl) Yl)-1-methyl-1H-pyrazolo[3,4-b]pyridin-6-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(7- Cyclopropyl-2-(ethylsulfonyl)imidazo[1,2-a]pyrimidin-3-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-( 3-(Ethylsulfonyl)imidazo[1,2-a]pyrazin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-( Ethylsulfonyl)imidazo[1,2-b]pyridazin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(bromodifluoro) Methoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) )-5-(pyridin-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) -5-(pyridin-2-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-((5-bromopyridine-2) -Yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) Aceto)-5-(pyrimidin-2-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) Yl)-5-((1-methyl-1H-pyrazol-3-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2- (5-(3,3-Difluorocyclobutoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,2-Difluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one ; 2-(5-((1,3-Difluoropropan-2-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine -1(2H)-one; 2-(3-(ethylsulfonyl)-5-(neopentyloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-one; 1-(((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3- Oxy)methyl)cyclopropane-1-carbonitrile; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2( 1H) -Yl)pyridin-3-yl)oxy)propionitrile; 2-(3-(ethylsulfonyl)-5-((1-fluoro-2-methylpropan-2-yl)oxy)pyridine -2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-methoxypyridin-2-yl)-7 -(Trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2-fluoroethoxy)pyridin-2-yl)-7-( Trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2( 1H)-yl)pyridin-3-yl)oxy)-2-(methylthio)acetonitrile; 2-(5-((2,2-difluorocyclopropyl)methoxy)-3-(ethyl Sulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 4-((5-(ethylsulfonyl)-6-(1-oxo) -7-(Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)butyronitrile; 2-(5-(cyclobutylmethoxy)-3-(ethylsulfonyl) )Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,2-difluoropropoxy)-3-(ethylsulfonyl) Yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(1-fluoroethoxy) Pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-( Trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-N,N-dimethyl-2-(methylthio)acetamide; 2-ethyl-2- ((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)butyronitrile; 2 -(3-(Ethylsulfonyl)-5-isobutoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethyl Sulfonyl)-5-(2,2,2-trifluoroethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5 -(2-Bromo-1,1-difluoroethoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one ; 2-(5-((3-cyclopropylisoxazol-5-yl)methoxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl) Phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(3-methoxycyclobutoxy)pyridin-2-yl)-7-(trifluoromethyl )Phthalazine-1(2H)-one; 5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3 -Difluoromethanesulfonate; 3-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine -3-yl)oxy) ring Butane-1-carbonitrile; 5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl fluoride Methanesulfonate; 3-((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl )Oxy)-3-methylbutyronitrile; 5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridine-3 -Yl trifluoromethanesulfonate; 2-(3-(ethylsulfonyl)-5-((1-methoxy-2-methylpropan-2-yl)oxy)pyridin-2-yl )-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-((5-(ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl) Phthalazine-2(1H)-yl)pyridin-3-yl)oxy)-N,N,2-trimethylpropionamide; 2-(3-(ethylsulfonyl)-5-((3 -Methyloxetan-3-yl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; (E)-2-(3 -(Ethylsulfonyl)-5-(2-(methylimino)propoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2 -(3-(Ethylsulfonyl)-5-((trimethylsilyl)methoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(Ethylsulfonyl)-5-(2-oxypropoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2- (3-(Ethylsulfonyl)-5-((2-methyl-3-oxobutan-2-yl)oxy)pyridin-2-yl)-7-(trifluoromethyl)phthalein Azin-1(2H)-one; 2-(5-(allyloxy)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1( 2H)-one; 2-(3-(ethylsulfonyl)-5-propoxypyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2- (5-Ethoxy-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) (Phenyl)-5-(methoxymethoxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-cyclobutyl-3- (Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-(2,2-difluorocyclopropyl)-3 -(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl)-5-(2 -Methyloxetan-2-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(3-(ethylsulfonyl) -5-(3-Methylthietane-3-yl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 2-(5-( 1,1-Dioxon Subgroup thietane-2-yl)-3-(ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazin-1(2H)-one; 6 ((5-(Ethylsulfonyl)-6-(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-3-yl)oxy)nicotinonitrile; 2 -(3-(Ethylsulfonyl)-5-(thietanyl-3-yloxy)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H) -Ketone; 2-(5-((1,1-dioxanylthietane-3-yl)oxy)-3-(ethylsulfonyl)pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(5-((1,1-dioxanion thietane-3-yl)methyl)-3-(ethyl Sulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 7-(3-(ethylsulfonyl)-5-(trifluoromethyl) )Pyridin-2-yl)-2-(trifluoromethyl)pyrido[2,3-d]pyridazine-8(7H)-one; 2-(3-(N-methylethylsulfonamide) Amino)-5-(3-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)- Ketone; 2-(3-(N-methylethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl) -7-(Trifluoromethyl)phthalazine-1(2H)-one; N-(ethyl((oxo)(2-(1-oxo-7-(trifluoromethyl)phthalazine-2) (1H)-yl)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-3-yl)-16-sulfinyl)cyanamide; 2-( 3-(N-Ethylethylsulfonylimino)-5-(4-(1,1,2,2-tetrafluoroethoxy)phenyl)pyridin-2-yl)-7-(three Fluoromethyl)phthalazine-1(2H)-one; 2-(6-bromo-3-(ethylsulfonylimino)imidazo[1,2-a]pyridin-2-yl)-7- (Trifluoromethyl)phthalazine-1(2H)-one; 2-(6-bromo-3-(N-methylethylsulfonylimino)imidazo[1,2-a]pyridine-2 -Yl)-7-(trifluoromethyl)phthalazine-1(2H)-one; 1-(3-(ethylsulfonylimino)-2-(1-oxo-7-(trifluoro (Methyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridin-6-yl)cyclopropane-1-carbonitrile; 3-(ethylsulfonylimino)-2- (1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)imidazo[1,2-a]pyridine-6-carbonitrile; 2-(6-(cyclopropylamino )-3-(Ethylsulfonyl)pyridin-2-yl)-7-(trifluoromethyl)phthalazine-1(2H)-one and N-(5-(ethylsulfonyl)-6 -(1-oxo-7-(trifluoromethyl)phthalazine-2(1H)-yl)pyridin-2-yl)cyclopropanecarboxamide. 一種控制或預防昆蟲和/或蟎蟲害的組合物,其包含生物有效量的式(I)化合物或其農學上可接受的鹽、異構體/結構異構體、立體異構體、非對映異構體、對映異構體、互變異構體、多晶型物、金屬絡合物或N-氧化物以及至少另外一種選自表面活性劑和助劑的成分。A composition for controlling or preventing insects and/or mite pests, which comprises a biologically effective amount of a compound of formula (I) or an agronomically acceptable salt, isomer/structural isomer, stereoisomer, non-pair Enantiomers, enantiomers, tautomers, polymorphs, metal complexes or N-oxides and at least one other ingredient selected from surfactants and adjuvants. 如請求項6所述的組合物,其中所述組合物還包含至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、生物農藥、除草劑、植物生長調節劑、抗生素、肥料或營養素的一種生物活性相容化合物。The composition according to claim 6, wherein the composition further comprises at least one selected suicide fungicide, insecticide, nematicide, acaricide, biological pesticide, herbicide, plant growth regulator, antibiotic, fertilizer Or a biologically active compatible compound of nutrients. 如請求項6所述的組合物,其中所述的式(I)化合物的生物學有效量的範圍為組合物總重量的0.1%-99%,優選組合物總重量的5%-50%。The composition according to claim 6, wherein the biologically effective amount of the compound of formula (I) ranges from 0.1% to 99% of the total weight of the composition, preferably from 5% to 50% of the total weight of the composition. 一種組合,其包含生物有效量的如請求項1所述的化合物和至少一種選自殺真菌劑、殺蟲劑、殺線蟲劑、殺蟎劑、殺生物劑、除草劑、植物生長調節劑、抗生素、肥料和營養素的生物活性相容化合物。A combination comprising a biologically effective amount of the compound according to claim 1 and at least one selected suicide fungicide, insecticide, nematicide, acaricide, biocide, herbicide, plant growth regulator, antibiotic , Fertilizer and nutrient bioactive compatible compound. 一種對抗昆蟲和蟎類害蟲的方法,其包括用生物有效量的如請求項1或6或9所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸昆蟲和蟎蟲、其棲息地、繁殖地、食物、植物、種子、土壤、無脊椎動物害蟲生長或可能生長的區域,或希望免受蟲害或侵擾的材料、植物、種子、土壤、表面或空間使其免受害蟲侵擾或侵染。A method for combating insects and mites, which comprises using a biologically effective amount of the compound of formula (I) or its salt, metal complex, N-oxide, isomer as described in claim 1 or 6 or 9 , Polymorphs, compositions or combinations that come into contact with insects and mites, their habitats, breeding grounds, food, plants, seeds, soil, areas where invertebrate pests grow or may grow, or materials that wish to be protected from pests or infestations , Plants, seeds, soil, surfaces or spaces to protect them from pests or infestation. 一種保護農作物免受昆蟲和蟎蟲侵襲或侵擾的方法,其包括用生物有效量的如請求項1或6或9所述的化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸農作物。A method for protecting crops from insects and mites infestation or infestation, which comprises using a biologically effective amount of the compound or its salt, metal complex, N-oxide, isomer as described in claim 1 or 6 or 9 , Polymorphs, compositions or combinations contact crops. 如請求項10或11所述的方法,其中所述方法包括在農業或園藝作物中施用有效劑量的式(I)化合物,其量為1g至5000g/公頃。The method according to claim 10 or 11, wherein the method comprises applying an effective dose of the compound of formula (I) to agricultural or horticultural crops in an amount of 1 g to 5000 g/ha. 一種保護種子、植物和植物部分免受土壤昆蟲,以及保護幼苗根和芽免受土壤和葉面昆蟲侵擾的方法,其包括在播種前和/或在催芽後用如請求項1或6或9所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸種子。A method for protecting seeds, plants and plant parts from soil insects, and protecting seedling roots and shoots from soil and foliar insects, which includes applying such methods as claim 1 or 6 or 9 before sowing and/or after germination The compound of formula (I) or its salt, metal complex, N-oxide, isomer, polymorph, composition or combination contact seed. 一種保護種子、植物和植物部分免受土壤昆蟲,以及保護幼苗根和芽免受土壤和葉面昆蟲侵擾的方法,其包括在播種前和/或在催芽後用如請求項1或6或9所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸種子。A method for protecting seeds, plants and plant parts from soil insects, and protecting seedling roots and shoots from soil and foliar insects, which includes applying such methods as claim 1 or 6 or 9 before sowing and/or after germination The compound of formula (I) or its salt, metal complex, N-oxide, isomer, polymorph, composition or combination contact seed. 一種保護種子、植物和植物部分免受土壤昆蟲,以及保護幼苗根和芽免受土壤和葉面昆蟲侵擾的方法,其包括在播種前和/或在催芽後用如請求項1或6或9所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸種子。A method for protecting seeds, plants and plant parts from soil insects, and protecting seedling roots and shoots from soil and foliar insects, which includes applying such methods as claim 1 or 6 or 9 before sowing and/or after germination The compound of formula (I) or its salt, metal complex, N-oxide, isomer, polymorph, composition or combination contact seed. 一種保護種子、植物和植物部分免受土壤昆蟲,以及保護幼苗根和芽免受土壤和葉面昆蟲侵擾的方法,其包括在播種前和/或在催芽後用如請求項1或6或9所述的式(I)化合物或其鹽、金屬絡合物、N-氧化物、異構體、多晶型物、組合物或組合接觸種子。A method for protecting seeds, plants and plant parts from soil insects, and protecting seedling roots and shoots from soil and foliar insects, which includes applying such methods as claim 1 or 6 or 9 before sowing and/or after germination The compound of formula (I) or its salt, metal complex, N-oxide, isomer, polymorph, composition or combination contact seed.
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