TWI744401B - Molecules having certain pesticidal utilities, and intermediates, compositions, and processes related thereto - Google Patents

Molecules having certain pesticidal utilities, and intermediates, compositions, and processes related thereto Download PDF

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TWI744401B
TWI744401B TW106137106A TW106137106A TWI744401B TW I744401 B TWI744401 B TW I744401B TW 106137106 A TW106137106 A TW 106137106A TW 106137106 A TW106137106 A TW 106137106A TW I744401 B TWI744401 B TW I744401B
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alkyl
cycloalkyl
alkenyl
substituted
phenyl
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TW201823239A (en
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娜塔莉 詹派特羅
大衛 A. 德莫特爾
林西 霍爾蒂
蓋瑞 D. 克羅斯
湯瑪斯 C. 史帕克斯
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美商陶氏農業科學公司
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Abstract

This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One” and “Formula Two”).
Figure 106137106-A0202-11-0002-3

Description

具有一定殺蟲效用之分子,及其相關之中間物、組成物暨方法 Molecules with certain insecticidal effects, and related intermediates, compositions and methods 相關申請案之交叉引用Cross-reference of related applications

本申請案主張2016年11月9日提交之美國臨時專利申請案第62/419622號之權益。 This application claims the rights of U.S. Provisional Patent Application No. 62/419622 filed on November 9, 2016.

本發明係關於具有針對線形動物門、節肢動物門及軟體動物門中之害蟲之殺蟲效用之分子的領域、產生此類分子之方法、用於此類方法之中間物、含有此類分子之組成物及使用此類分子抵抗此類害蟲之方法。此等分子可例如用作殺蟎劑、殺昆蟲劑、殺壁蟲劑、殺軟體動物劑及/或殺線蟲劑。 The present invention relates to the field of molecules with insecticidal effects against pests in the phylum Nematodes, arthropods and molluscs, methods for producing such molecules, intermediates for such methods, and containing such molecules Composition and methods of using such molecules to resist such pests. These molecules can be used, for example, as acaricides, insecticides, wall insecticides, molluscicides and/or nematicides.

「許多最危險的人類疾病由蟲媒傳播」(Rivero,A.等人,Insect Control of Vector-Borne Diseases:When is Insect Resistance a Problem? Public Library of Science Pathogens,6(8)(2010))。「歷史上,病媒傳染病(諸如瘧疾、登革熱、黃熱病、瘟疫、虱傳斑疹傷寒等)從十七世紀到二十世紀初造成比所有其他原因組合更多的人類疾病及死亡」(Gubler D.,Resurgent Vector-Borne Diseases as a Global Health Problem,Emerging Infectious Diseases,第4卷,第3期,七-九月(1998))。目前病媒感染疾病造 成約17%的全球寄生性及感染性疾病。據估計,全世界約有2.5億人患有瘧疾,每年約有80萬人死亡-其中85%的死亡發生在五歲以下的兒童。每年另外發生250,000至500,000例出血性登革熱(Matthews,G.,Integrated Vector Management:controlling vectors of malaria and other insect vector borne diseases(2011))。病媒防治在感染性疾病的預防及防治中發揮關鍵作用。然而,殺昆蟲劑抗性(包括多種殺昆蟲劑之抗性)已出現在作為人類疾病主要媒介的所有昆蟲種類中(Rivero等人)。 "Many of the most dangerous human diseases are spread by insect vectors" (Rivero, A. et al., Insect Control of Vector-Borne Diseases: When is Insect Resistance a Problem? Public Library of Science Pathogens, 6(8) (2010)). "Historically, vector-borne diseases (such as malaria, dengue fever, yellow fever, plague, lice-borne typhus, etc.) from the 17th century to the beginning of the 20th century caused more human diseases and deaths than any other combination of causes." Gubler D., Resurgent Vector-Borne Diseases as a Global Health Problem , Emerging Infectious Diseases, Volume 4, Issue 3, July-September (1998)). At present, vector-infected diseases cause about 17% of global parasitic and infectious diseases. It is estimated that about 250 million people worldwide suffer from malaria, and about 800,000 people die every year-85% of these deaths occur in children under the age of five. An additional 250,000 to 500,000 cases of hemorrhagic dengue fever occur every year (Matthews, G., Integrated Vector Management: controlling vectors of malaria and other insect vector borne diseases (2011)). Vector control plays a key role in the prevention and control of infectious diseases. However, insecticide resistance (including resistance to multiple insecticides) has appeared in all insect species that are the main vectors of human diseases (Rivero et al.).

每年,昆蟲、植物病原體及野草破壞潛在食物生產量的超過40%。儘管施用殺蟲劑及使用一系列廣泛的非化學防治劑(諸如輪作及生物防治劑),但此損失仍存在。若僅可保存此食物中的一些,則可用於供養世界上超過三十億營養不良的人類(Pimental,D.,Pest Control in World Agriculture,Agricultural Sciences-第II卷(2009))。 Every year, insects, plant pathogens and weeds destroy more than 40% of potential food production. Despite the application of pesticides and the use of a wide range of non-chemical control agents (such as crop rotation and biological control agents), this loss still exists. If only some of this food can be preserved, it can be used to feed more than 3 billion undernourished humans in the world (Pimental, D., Pest Control in World Agriculture, Agricultural Sciences-Volume II (2009)).

植物寄生線蟲為分佈最廣的害蟲之一,且常常為最隱伏及代價高的害蟲之一。據估計,可歸因於線蟲的損失為發達國家約9%至欠發達國家約15%。然而,在美利堅合眾國,35個州對各種作物的調查指出線蟲衍生之損失高達25%(Nicol,J.等人,Current Nematode Threats to World Agriculture,Genomic and Molecular Genetics of Plant-Nematode Interactions(編者:Jones,J.等人),第2章,(2011))。 Plant parasitic nematodes are one of the most widespread pests, and often one of the most insidious and costly pests. It is estimated that the losses attributable to nematodes range from about 9% in developed countries to about 15% in less developed countries. However, in the United States of America, surveys of various crops in 35 states indicate that nematode-derived losses are as high as 25% (Nicol, J. et al., Current Nematode Threats to World Agriculture , Genomic and Molecular Genetics of Plant-Nematode Interactions (Editor: Jones) , J. et al.), Chapter 2, (2011)).

應注意,腹足動物(蛞蝓及蝸牛)為經濟重要性低於其他節肢動物或線形動物的害蟲,但是在某些區域,腹足動物可能實質上減小產量,嚴重影響收穫產品的品質以及傳播人類、動物及植物疾病。雖然僅數十個種類的腹足動物為嚴重地區性害蟲,但少數種類為世界範圍內的重要害蟲。特定言之,腹足動物影響廣泛多種農業及園藝作物,諸如耕種作物、畜牧作物及纖維作物;蔬菜;灌木水果及喬木水果;草本植物;以及觀賞性植 物(Speiser,B.,Molluscicides,Encyclopedia of Pest Management(2002)。 It should be noted that gastropods (slugs and snails) are pests whose economic importance is lower than that of other arthropods or linear animals. However, in some areas, gastropods may substantially reduce production, which seriously affects the quality and spread of harvested products. Human, animal and plant diseases. Although only dozens of species of gastropods are serious local pests, a few species are important pests worldwide. In particular, gastropods affect a wide range of agricultural and horticultural crops, such as cultivated crops, livestock crops and fiber crops; vegetables; shrub fruits and arbor fruits; herbs; and ornamental plants (Speiser, B., Molluscicides , Encyclopedia of Pest Management (2002).

白蟻對所有類型的私人及公共結構以及農業及林業資源造成損壞。在2003年,據估計白蟻每年在世界範圍造成超過US$200億的損壞(Su,N.Y.,Overview of the global distribution and control of the Formosan subterranean termite,Sociobiology 2003,41,177-192)。 Termites cause damage to all types of private and public structures, as well as agricultural and forestry resources. In 2003, it was estimated that termites caused more than US$20 billion in damage worldwide every year (Su, NY, Overview of the global distribution and control of the Formosan subterranean termite , Sociobiology 2003, 41, 177-192).

因此,出於許多原因(包括上文所提及之原因),存在有新殺蟲劑的需求。 Therefore, for many reasons (including those mentioned above), there is a need for new pesticides.

定義definition

定義中給出之實例一般為非詳盡的且不必理解為限制此文件中所揭示之分子。應理解,一取代基應符合與和其連接之特定分子相關之化學鍵結規則及空間相容性限制。 The examples given in the definition are generally non-exhaustive and need not be construed as limiting the molecules disclosed in this document. It should be understood that a substituent should comply with the chemical bonding rules and steric compatibility restrictions related to the specific molecule to which it is connected.

烯基」意指一由碳及氫組成之非環狀的不飽和的(至少一個碳-碳雙鍵)分支鏈或非分支鏈之取代基,例如乙烯基、丙烯基、丁烯基、戊烯基及己烯基。 " Alkenyl " means an acyclic unsaturated (at least one carbon-carbon double bond) branched or unbranched substituent composed of carbon and hydrogen, such as vinyl, propenyl, butenyl, Pentenyl and hexenyl.

烯氧基」意指一進一步由碳-氧單鍵組成之烯基,例如烯丙氧基、丁烯氧基、戊烯氧基、己烯氧基。 "Alkenyloxy" means an alkenyl group further composed of a carbon-oxygen single bond, such as allyloxy, butenyloxy, pentenyloxy, and hexenyloxy.

烷氧基」意指一進一步由碳-氧單鍵組成之烷基,例如甲氧基、乙氧基、丙氧基、異丙氧基、丁氧基、異丁氧基及第三丁氧基。 "Alkoxy" means a further consisting of carbon - consisting of a single bond, an oxygen, e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, and tertiary butoxy Oxy.

烷基」意指由碳及氫組成之非環狀、飽和、分支鏈或未分支的取代基,例如甲基、乙基、丙基、異丙基、丁基及第三丁基。 " Alkyl " means an acyclic, saturated, branched or unbranched substituent composed of carbon and hydrogen, such as methyl, ethyl, propyl, isopropyl, butyl, and tertiary butyl.

炔基」意指一由碳及氫組成之非環狀的不飽和的(至少一個碳-碳參鍵)分支鏈或非分支鏈之取代基,例如乙炔基、丙炔基、丁炔基及戊炔基。 " Alkynyl " means a non-cyclic unsaturated (at least one carbon-carbon bond) branched or unbranched substituent composed of carbon and hydrogen, such as ethynyl, propynyl, butynyl And pentynyl.

炔氧基」意指一進一步由碳-氧單鍵組成之炔基,例如戊炔氧基、己炔氧基、庚炔氧基及辛炔氧基。 "Alkynyloxy" means an alkynyl group further composed of a carbon-oxygen single bond, such as pentynyloxy, hexynyloxy, heptynyloxy, and octynyloxy.

芳基」意指一由氫及碳組成之環狀的芳族取代基,例如苯基、萘基及聯苯基。 " Aryl " means a cyclic aromatic substituent composed of hydrogen and carbon, such as phenyl, naphthyl, and biphenyl.

環烯基」意指一由碳及氫組成之單環或多環的不飽和(至少一個碳-碳雙鍵)的取代基,例如環丁烯基、環戊烯基、環己烯基、降冰片烯基(norbornenyl)、雙環[2.2.2]辛烯基、四氫萘基、六氫萘基及八氫萘基。 " Cycloalkenyl " means a monocyclic or polycyclic unsaturated (at least one carbon-carbon double bond) substituent composed of carbon and hydrogen, such as cyclobutenyl, cyclopentenyl, and cyclohexenyl , Norbornenyl (norbornenyl), bicyclo[2.2.2] octenyl, tetrahydronaphthyl, hexahydronaphthyl and octahydronaphthyl.

環烯氧基」意指一進一步由碳-氧單鍵組成之環烯基,例如環丁烯氧基、環戊烯氧基、降冰片烯氧基(norbornenyloxy)及雙環[2.2.2]辛烯氧基。 "Cycloalkenyloxy" means a cycloalkenyl group further composed of a carbon-oxygen single bond, such as cyclobutenyloxy, cyclopentenyloxy, norbornenyloxy and bicyclo[2.2.2] Octenoxy.

環烷基」意指由碳及氫組成之單環或多環、飽和取代基,例如環丙基、環丁基、環戊基、降冰片基(norbornyl)、雙環[2.2.2]辛基及十氫萘基。 " Cycloalkyl " means a monocyclic or polycyclic, saturated substituent composed of carbon and hydrogen, such as cyclopropyl, cyclobutyl, cyclopentyl, norbornyl, bicyclo[2.2.2]octyl Base and Decahydronaphthyl.

環烷氧基」意指另外由碳-氧單鍵組成之環烷基,例如環丙氧基、環丁氧基、環戊氧基、降冰片基氧基(norbornyloxy)及雙環[2.2.2]辛氧基。 "Cycloalkoxy" means a cycloalkyl group additionally composed of a carbon-oxygen single bond, such as cyclopropoxy, cyclobutoxy, cyclopentyloxy, norbornyloxy and bicyclo[2.2. 2] Octyloxy.

鹵基」意指氟、氯、溴及碘。 " Halo " means fluorine, chlorine, bromine and iodine.

鹵烷氧基」意指一進一步由一個至最大可能數目之相同或不同的鹵基組成之烷氧基,例如氟甲氧基、三氟甲氧基、2,2-二氟丙氧基、氯甲氧基、三氯甲氧基、1,1,2,2-四氟乙氧基及五氟乙氧基。 "Haloalkoxy" means an alkoxy group further composed of one to the largest possible number of the same or different halo groups, such as fluoromethoxy, trifluoromethoxy, 2,2-difluoropropoxy , Chloromethoxy, trichloromethoxy, 1,1,2,2-tetrafluoroethoxy and pentafluoroethoxy.

鹵烷基」意指一進一步由一個至最大可能數目之相同或不同的鹵基組成之烷基,例如氟甲基、三氟甲基、2,2-二氟丙基、氯甲基、 三氯甲基及1,1,2,2-四氟乙基。 "Haloalkyl" means an alkyl group further composed of one to the largest possible number of the same or different halo groups, such as fluoromethyl, trifluoromethyl, 2,2-difluoropropyl, chloromethyl, Trichloromethyl and 1,1,2,2-tetrafluoroethyl.

雜環基」意指一環狀取代基,其可為完全飽和、部分不飽和或完全不飽和的,其中該環狀結構包含有至少一個碳及至少一個雜原子,其中該雜原子為氮、硫或氧。芳族雜環基取代基之實例包含(但不限於)苯并呋喃基、苯并異噻唑基、苯并異噁唑基、苯并噁唑基、苯并噻吩基、苯并噻唑基、噌啉基(cinnolinyl)、呋喃基、吲唑基、吲哚基、咪唑基、異吲哚基、異喹啉基、異噻唑基、異噁唑基、噁二唑基、噁唑啉基、噁唑基、酞嗪基、吡嗪基、吡唑啉基、吡唑基、噠嗪基、吡啶基、嘧啶基、吡咯基、喹唑啉基、喹啉基、喹喏啉基、四唑基、噻唑啉基、噻唑基、噻吩基、三嗪基及三唑基。完全飽和雜環基取代基之實例包括(但不限於)哌嗪基、哌啶基、嗎啉基、吡咯啶基、四氫呋喃基及四氫哌喃基。部分不飽和雜環基取代基之實例包括(但不限於)1,2,3,4-四氫-喹啉基、4,5-二氫-噁唑基、4,5-二氫-1H-吡唑基、4,5-二氫-異噁唑基及2,3-二氫-[1,3,4]-噁二唑基。 " Heterocyclic group " means a cyclic substituent, which can be fully saturated, partially unsaturated or fully unsaturated, wherein the cyclic structure contains at least one carbon and at least one heteroatom, wherein the heteroatom is nitrogen , Sulfur or oxygen. Examples of aromatic heterocyclyl substituents include, but are not limited to, benzofuranyl, benzisothiazolyl, benzisoxazolyl, benzoxazolyl, benzothienyl, benzothiazolyl, benzothiazolyl Cinnolinyl, furanyl, indazolyl, indolyl, imidazolyl, isoindolyl, isoquinolinyl, isothiazolyl, isoxazolyl, oxadiazolyl, oxazoline, oxazoline Azolyl, phthalazinyl, pyrazinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridyl, pyrimidinyl, pyrrolyl, quinazolinyl, quinolinyl, quinazolinyl, tetrazolyl , Thiazolinyl, thiazolyl, thienyl, triazinyl and triazolyl. Examples of fully saturated heterocyclyl substituents include, but are not limited to, piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, tetrahydrofuranyl, and tetrahydropiperanyl. Examples of partially unsaturated heterocyclyl substituents include (but are not limited to) 1,2,3,4-tetrahydro-quinolinyl, 4,5-dihydro-oxazolyl, 4,5-dihydro-1 H -pyrazolyl, 4,5-dihydro-isoxazolyl and 2,3-dihydro-[1,3,4]-oxadiazolyl.

本文係揭露具有下式(「式1」及/或「式2」)之分子:

Figure 106137106-A0202-12-0005-6
Figure 106137106-A0202-12-0006-7
(A)Ar1係選自(1)呋喃基、苯基、噠嗪基、吡啶基、嘧啶基或噻吩基;或(2)經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基;其中所述經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基係具有一或多個獨立地選自由以下組成之群的取代基:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、 S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(B)Het為5員或6員之飽和或不飽和雜環,其含有獨立地選自氮、硫或氧之一或多個雜原子,且其中Ar1及Ar2係不彼此相鄰(但可相間或相對,諸如,對於5員環其為1,3,而對於6員環其為1,3或1,4),且其中該雜環亦可經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、側氧基、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8) 鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(C)Ar2係選自(1)呋喃基、苯基、噠嗪基、吡啶基、嘧啶基或噻吩基;或(2)經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基;其中所述經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基係具有一或多個獨立地選自由以下組成之群的取代基:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、鹵烷基、環烷基、烷氧基、鹵烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、 OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(D)L為選自以下之連接基團:(1)一飽和或不飽和、經取代或未經取代之直鏈(C1-C4)烴基連接基團;及(2)一飽和或不飽和、經取代或未經取代之環狀(C3-C8)烴基連接基團;其中所述連接基團中之每一者係將Ar2與NY連接,且其中所述經取代之直鏈(C1-C4)烴基連接基團及經取代之環狀(C3-C8)烴基連接基團係具有一或多個獨立地選自R8、R9、R10、R11及R12的取代基,其中R8、R9、R10、R11及R12每一者係選自F、Cl、Br、I、CN、側氧基、(C1-C6)烷基、(C2-C6)烯基、(C2-C6)鹵烯基、(C2-C6)炔基、(C1-C6)鹵烷基、(C3-C6)環烷基、(C3-C6)環烯基、(C3-C6)鹵環烷基、(C1-C6)烷氧基、(C1-C6)鹵烷氧基或苯基;(E)R1係選自由以下組成之群:H、(C1-C8)烷基、(C3-C8)環烷基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-OC(O)-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、(C1-C8)烷基-OC(O)O-(C1-C8)烷基、(C1-C8)烷基-C(O)O-(C1-C8)烷基、C(O)烷基、(C1-C8) 烷基-C(O)-(C1-C8)烷基、(C1-C8)烷基苯基、(C1-C8)烷基-O-苯基;其中烷基、環烷基、烯基及炔基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、側氧基、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(F)Q1係選自由O及S所組成之群;(G)R2係選自由以下所組成之群:(J)、H、(C1-C8)烷基、(C3-C8)環烷基、(C2-C8)烯基、(C2-C8)炔基、C(O)-(C1-C8)烷基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、(C1-C8)烷基苯基、(C1-C8)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1-C8)烷基-(Het-1)、(C1-C8)烷基-OC(O)-(C1-C8)烷基、(C1-C8)烷基-OC(O)O-(C1-C8)烷基、(C1-C8)烷基-OC(O)-NRxRy、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基-(Het-1)、(C1-C8)烷基-C(O)-(Het-1)、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基(NRxRy)-C(O)OH、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基-NRxRy、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基-N(Rx)-C(O)O-(C1-C8)烷基、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基(N(Rx)-C(O)O-(C1-C8)烷基)-C(O)OH、(C1-C8)烷基-C(O)-(Het-1)-C(O)O-(C1-C8)烷基、(C1-C8)烷基-OC(O)O-(C1-C8)烷基、(C1-C8)烷基-OC(O)-(C1-C8)烷基、(C1-C8)烷基-OC(O)-(C3-C8)環烷基、 (C1-C8)烷基-OC(O)-(Het-1)、(C1-C8)烷基-OC(O)-(C1-C8)烷基-N(Rx)-C(O)O-(C1-C8)烷基、(C1-C8)烷基-NRxRy、(C1-C8)烷基-S(O)n-(Het-1)及(C1-C8)烷基-O-(Het-1);其中烷基、環烷基、烯基、炔基、苯基及(Het-1)每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、NRxRy、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)OH、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基)、苯基、苯氧基、Si((C1-C8)烷基)3、S(O)n-NRxRy及(Het-1);(H)R3係選自由以下所組成之群:(C3-C8)環烷基、苯基、(C1-C8)烷基苯基、(C1-C8)烷基-O-苯基、(C2-C8)烯基-O-苯基、(Het-1)、(C1-C8)烷基-(Het-1)及(C1-C8)烷基-O-(Het-1);其中烷基、環烷基、烯基、苯基及(Het-1)每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、NRxRy、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8) 鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C1-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、O-(C1-C8)烷基、S-(C1-C8)烷基、(C1-C8)烷基-O-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基、苯氧基及(Het-1);(I)R4係選自由以下所組成之群:(J)、H、(C1-C8)烷基、(C3-C8)環烷基、(C2-C8)烯基、(C2-C8)炔基、C(O)-(C1-C8)烷基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、(C1-C8)烷基苯基、(C1-C8)烷基-O-苯基、C(O)-(Het-1)、(Het-1)、(C1-C8)烷基-(Het-1)、(C1-C8)烷基-OC(O)-(C1-C8)烷基、(C1-C8)烷基-OC(O)O-(C1-C8)烷基、(C1-C8)烷基-OC(O)-NRxRy、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基-(Het-1)、(C1-C8)烷基-C(O)-(Het-1)、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基(NRxRy)-C(O)OH、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基-NRxRy、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基-N(Rx)-C(O)O-(C1-C8)烷基、(C1-C8)烷基-C(O)-N(Rx)(C1-C8)烷基(N(Rx)-C(O)O-(C1-C8)烷基)-C(O)OH、(C1-C8)烷基-C(O)-(Het-1)-C(O)O-(C1-C8)烷基、(C1-C8)烷基-OC(O)O-(C1-C8)烷基、(C1-C8)烷基-OC(O)-(C1-C8)烷基、(C1-C8)烷基-OC(O)-(C3-C8)環烷基、(C1-C8)烷基-OC(O)-(Het-1)、(C1-C8)烷基-OC(O)-(C1-C8)烷基-N(Rx)-C(O)O-(C1-C8)烷基、(C1-C8)烷基-NRxRy、(C1-C8)烷基-S(O)n-(Het-1)及(C1-C8)烷基-O-(Het-1);其中烷基、環烷基、烯基、炔基、苯基及(Het-1)每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、NRxRy、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷 基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)OH、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基、苯氧基、Si((C1-C8)烷基)3、S(O)n-NRxRy及(Het-1);(J)R2及R4與CX(Q1)(NX)一起形成一個4員或7員之飽和或不飽和雜環,其可進一步含有選自氮、硫及氧之一或多個雜原子,其中各雜環係可選擇性地經一或多個獨立地選自由R5、R6及R7組成之群的取代基取代;其中R5、R6及R7係各獨立地選自由以下組成之群:H、F、Cl、Br、I、CN、OH、NO2、側氧基、硫基、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及(Het-1);(K)Rx及Ry係各獨立地選自由以下組成之群:H、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)H、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、 C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及(C1-C8)烷基苯基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及烷基苯基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及(Het-1);(L)(Het-1)為一個5員或6員之飽和或不飽和雜環,其含有獨立地選自氮、硫或氧之一或多個雜原子;其中該雜環係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、側氧基、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者 係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(M)n係各獨立地為0、1或2;以及N-氧化物、農業上可接受之酸加成鹽、鹽衍生物、溶劑合物、酯衍生物、多晶型物、同位素、溶解的立體異構體及/或互變異構物。 This article discloses molecules with the following formulas (" Formula 1 " and/or " Formula 2 "):
Figure 106137106-A0202-12-0005-6
Figure 106137106-A0202-12-0006-7
(A) Ar 1 is selected from (1) furanyl, phenyl, pyridazinyl, pyridyl, pyrimidinyl or thienyl; or (2) substituted furanyl, substituted phenyl, or substituted da Azinyl, substituted pyridinyl, substituted pyrimidinyl or substituted thienyl; wherein the substituted furyl, substituted phenyl, substituted pyridazinyl, substituted pyridinyl, The substituted pyrimidinyl or substituted thienyl group has one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 ) Alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C (O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O) O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )Alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; wherein alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, phenyl Each of the phenoxy and phenoxy substituents may be optionally substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy Group, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n- (C 1 -C 8 )Haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1 -C 8 )alkane Group -NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 ) Haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 ) Cycloalkane Group, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 ) Alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O) O-(C 1 -C 8 ) alkyl, phenyl and phenoxy; (B) Het is a 5-membered or 6-membered saturated or unsaturated heterocyclic ring, which contains one independently selected from nitrogen, sulfur or oxygen Or multiple heteroatoms, and where Ar 1 and Ar 2 are not adjacent to each other (but may be alternately or opposite to each other, such as 1, 3 for a 5-membered ring, and 1, 3 or 1 for a 6-membered ring, 4), and the heterocyclic ring may also be substituted by one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , pendant oxy, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S (O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O) -(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; of which alkyl, cycloalkyl, alkoxy, alkenyl, alkyne Each of the group, phenyl and phenoxy substituents may be optionally substituted with one or more substituents independently selected from the group consisting of: H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )Haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1- C 8 )alkyl -NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 ) halo Alkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 ) ring Alkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1- C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O ) O-(C 1 -C 8 ) alkyl, phenyl and phenoxy; (C) Ar 2 is selected from (1) furyl, phenyl, pyridazinyl, pyridyl, pyrimidinyl or thienyl; Or (2) substituted furyl, substituted phenyl, substituted pyridazinyl, substituted pyridyl, substituted pyrimidinyl or substituted thienyl; wherein the substituted furyl, The substituted phenyl group, the substituted pyridazinyl group, the substituted pyridinyl group, the substituted pyrimidinyl group or the substituted thienyl group have one or more substituents independently selected from the group consisting of: H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 ) alkyl, (C 3 -C 8 ) cycloalkyl, (C 1 -C 8 ) alkoxy, (C 2 -C 8 ) Alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C( O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n- (C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; Wherein each of the alkyl, haloalkyl, cycloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, phenyl and phenoxy substituents can be optionally substituted by one or more independently Substituent substitution selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkane Oxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl , S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)- NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl , C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O) -(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; (D) L is a linking group selected from: (1) A saturated or unsaturated, substituted or unsubstituted linear (C 1 -C 4 ) hydrocarbyl linking group; and (2) a saturated or unsaturated, substituted or unsubstituted cyclic (C 3- C 8 ) a hydrocarbyl linking group; wherein each of the linking groups connects Ar 2 and N Y , and wherein the substituted linear (C 1 -C 4 ) hydrocarbyl linking group and the The substituted cyclic (C 3 -C 8 ) hydrocarbyl linking group has one or more substituents independently selected from R 8 , R 9 , R 10 , R 11 and R 12 , wherein R 8 , R 9 , Each of R 10 , R 11 and R 12 is selected from F, Cl, Br, I, CN, pendant oxy, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, (C 2 -C 6 )haloalkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )haloalkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkene Group, (C 3 -C 6 )halocycloalkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )haloalkoxy or phenyl; (E) R 1 is selected from the following composition Group: H, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 ) ring Alkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1- C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-C(O)O-( C 1 -C 8 )alkyl, C(O)alkyl, (C 1 -C 8 )alkyl-C(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl Phenyl, (C 1 -C 8 )alkyl-O-phenyl; wherein each of the alkyl, cycloalkyl, alkenyl and alkynyl groups can optionally be independently selected from one or more of the following Substituent substitutions of the group: H, F, Cl, Br, I, CN, NO 2 , pendant oxy, (C 1 -C 8 ) alkyl, (C 1 -C 8 ) haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl , S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2- (C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl , C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C( O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; (F) Q 1 is selected from the group consisting of O and S; (G) R 2 is selected from the group consisting of: (J) , H, (C 1 -C 8 )alkyl, (C 3- C 8 ) Cycloalkyl, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, C(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-O -(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, (C 1 -C 8 )alkylphenyl, ( C 1 -C 8 )alkyl-O-phenyl, C(O)-(Het-1), (Het-1), (C 1 -C 8 )alkyl-(Het-1), (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)-NR x R y , (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl-(Het -1), (C 1 -C 8 )alkyl-C(O)-(Het-1), (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )Alkyl (NR x R y )-C(O)OH, (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl-NR x R y , (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl-N(R x )-C(O)O-(C 1 -C 8 )Alkyl, (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl(N(R x )-C(O)O-(C 1- C 8 )alkyl)-C(O)OH, (C 1 -C 8 )alkyl-C(O)-(Het-1)-C(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 )alkyl , (C 1 -C 8 )alkyl-OC(O)-(C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkyl-OC(O)-(Het-1), (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 )alkyl-N(R x )-C(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 ) Alkyl-NR x R y , (C 1 -C 8 )alkyl-S(O) n -(Het-1) and (C 1 -C 8 )alkyl-O-(Het-1); Wherein each of alkyl, cycloalkyl, alkenyl, alkynyl, phenyl and (Het-1) can be optionally substituted with one or more substituents independently selected from the group consisting of: H , F, Cl, Br, I, CN, NO 2 , NR x R y , (C 1 -C 8 ) alkyl, (C 1 -C 8 ) haloalkyl, (C 3 -C 8 ) cycloalkyl , (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S( O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)H, C( O)OH, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O- (C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 ) alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl), phenyl, phenoxy, Si((C 1- C 8 )alkyl) 3 , S(O) n -NR x R y and (Het-1); (H) R 3 is selected from the group consisting of (C 3 -C 8 ) cycloalkyl, Phenyl, (C 1 -C 8 )alkylphenyl, (C 1 -C 8 )alkyl-O-phenyl, (C 2 -C 8 )alkenyl-O-phenyl, (Het-1) , (C 1 -C 8 )alkyl-(Het-1) and (C 1 -C 8 )alkyl-O-(Het-1); among them alkyl, cycloalkyl, alkenyl, phenyl and ( Each of Het-1) can be optionally substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , NR x R y , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 ) Haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C (O)H, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 ) haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-( C 3 -C 8 )cycloalkyl, C(O)O-(C 1 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, O-(C 1 -C 8 )alkyl, S-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 ) Alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl, phenoxy and (Het-1); (I ) R 4 is selected from the group consisting of (J), H, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 2 -C 8 )alkenyl, ( C 2 -C 8 )alkynyl, C(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1- C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, (C 1 -C 8 )alkylphenyl, (C 1 -C 8 )alkyl-O-phenyl, C (O)-(Het-1), (Het-1), (C 1 -C 8 )alkyl-(Het-1), (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)-NR x R y , (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl-(Het-1), (C 1 -C 8 )alkyl-C (O)-(Het-1), (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl(NR x R y )-C(O) OH, (C 1 -C 8 )alkyl-C(O)-N(R x )(C 1 -C 8 )alkyl-NR x R y , (C 1 -C 8 )alkyl-C(O )-N(R x )(C 1 -C 8 )alkyl-N(R x )-C(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-C (O)-N(R x )(C 1 -C 8 )alkyl(N(R x )-C(O)O-(C 1 -C 8 )alkyl)-C(O)OH、(C 1 -C 8 )Alkyl-C(O)-(Het-1)-C(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-OC(O)-(C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkyl-OC(O)-(Het-1), (C 1 -C 8 )alkyl-OC(O)-(C 1 -C 8 ) Alkyl-N(R x )-C(O)O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-NR x R y , (C 1 -C 8 )alkane -S(O) n -(Het-1) and (C 1 -C 8 )alkyl-O-(Het-1); among them alkyl, cycloalkyl, alkenyl, alkynyl, phenyl and ( Each of Het-1) can be optionally substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , NR x R y , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 ) Alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -( C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)H, C(O)OH, C(O)-NR x R y , (C 1 -C 8 )Alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1- C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3- C 8 )Cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O- (C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl -C(O)O-(C 1 -C 8 )alkyl, phenyl, phenoxy, Si((C 1 -C 8 )alkyl) 3 , S(O) n -NR x R y and ( Het-1); (J) R 2 and R 4 and C X (Q 1 )(N X ) together form a 4-membered or 7-membered saturated or unsaturated heterocyclic ring, which may be further The step contains one or more heteroatoms selected from nitrogen, sulfur and oxygen, wherein each heterocyclic ring system can be optionally substituted with one or more substituents independently selected from the group consisting of R 5 , R 6 and R 7 ; Wherein R 5 , R 6 and R 7 are each independently selected from the group consisting of H, F, Cl, Br, I, CN, OH, NO 2 , pendant oxy, thio, (C 1 -C 8 ) alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )halo Alkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)H, C(O)-(C 1 -C 8 )alkyl , C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C( O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and (Het-1 ); (K) R x and R y are each independently selected from the group consisting of H, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )Alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )Alkyl, C(O)H, C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3- C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 ) Alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 ) Alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and (C 1 -C 8 )alkylphenyl; wherein Alkyl, cycloalkyl, Each of alkoxy, alkenyl, alkynyl, phenyl, and alkylphenyl may be optionally substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br , I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy , (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S (O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)H, C (O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O) O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O) -(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, ( C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1- C 8 ) alkyl, phenyl and (Het-1); (L) (Het-1) is a 5-membered or 6-membered saturated or unsaturated heterocyclic ring, which contains a heterocyclic ring independently selected from nitrogen, sulfur or oxygen One or more heteroatoms; wherein the heterocyclic ring system can be optionally substituted with one or more substituents independently selected from the group consisting of: H, F, Cl, Br, I, CN, NO 2 , side Oxy, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 ) Alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )Alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 ) Cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )Alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkane Base, C(O)- (C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; among them, alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl Each of the, phenyl and phenoxy substituents may be optionally substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 ) Haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1 -C 8 )Alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1- C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3- C 8 )Cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O- (C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl -C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; (M) n is each independently 0, 1 or 2; and N-oxide, agriculturally acceptable Acid addition salts, salt derivatives, solvates, ester derivatives, polymorphs, isotopes, dissolved stereoisomers and/or tautomers.

為避免疑問,NX及NY的代號係指如式1及式2所示之特定位置處的普通氮原子。同樣地,CX的代號係指如式1及式2所示之特定位置處的普通碳原子。 For the avoidance of doubt, the codes of N X and N Y refer to ordinary nitrogen atoms at specific positions as shown in Formula 1 and Formula 2. Similarly, the code designation of C X refers to a common carbon atom at a specific position as shown in Formula 1 and Formula 2.

於一實施例中,Ar1為經取代之苯基。本實施例可與Het、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In one embodiment, Ar 1 is substituted phenyl. This embodiment can be used in combination with Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkage, and/or other embodiments of L.

於另一實施例中,Ar1為一個具有一或多個選自C1-C6鹵烷基及C1-C6鹵烷氧基的取代基之經取代的苯基。本實施例可與Het、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Ar 1 is a substituted phenyl group having one or more substituents selected from C 1 -C 6 haloalkyl and C 1 -C 6 haloalkoxy. This embodiment can be used in combination with Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkage, and/or other embodiments of L.

於另一實施例中,Ar1為一個具有一或多個選自CF3、OCF3及OC2F5的取代基之經取代的苯基。本實施例可與Het、Ar2、R1、R2、R3、 R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Ar 1 is a substituted phenyl group having one or more substituents selected from CF 3 , OCF 3 and OC 2 F 5. This embodiment can be used in combination with Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkage, and/or other embodiments of L.

於另一實施例中,Het係選自苯并呋喃基、苯并異噻唑基、苯并異噁唑基、苯并噁唑基、苯并噻吩基、苯并噻唑基[圖]啉基、呋喃基、吲唑基、吲哚基、咪唑基、異吲哚基、異喹啉基、異噻唑基、異噁唑基、噁二唑基、噁唑啉基、噁唑基、酞嗪基、吡嗪基、吡唑啉基、吡唑基、噠嗪基、吡啶基、嘧啶基、吡咯基、喹唑啉基、喹啉基、喹喏啉基、四唑基、噻唑啉基、噻唑基、噻吩基、三嗪基、三唑基、哌嗪基、哌啶基、嗎啉基、吡咯啶基、四氫呋喃基、四氫哌喃基、1,2,3,4-四氫-喹啉基、4,5-二氫-噁唑基、4,5-二氫-1H-吡唑基、4,5-二氫-異噁唑基及2,3-二氫-[1,3,4]-噁二唑基。 In another embodiment, Het is selected from the group consisting of benzofuranyl, benzisothiazolyl, benzisoxazolyl, benzoxazolyl, benzothienyl, benzothiazolyl [Figure] linyl, Furyl, indazolyl, indolyl, imidazolyl, isoindolyl, isoquinolinyl, isothiazolyl, isoxazolyl, oxadiazolyl, oxazoline, oxazolyl, phthalazinyl , Pyrazinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridinyl, pyrimidinyl, pyrrolyl, quinazolinyl, quinolinyl, quinolinyl, tetrazoline, thiazolinyl, thiazole Group, thienyl, triazinyl, triazolyl, piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydropiperanyl, 1,2,3,4-tetrahydro-quine Linyl, 4,5-dihydro-oxazolyl, 4,5-dihydro-1 H -pyrazolyl, 4,5-dihydro-isoxazolyl and 2,3-dihydro-[1, 3,4]-oxadiazolyl.

於另一實施例中,Het為三唑基。本實施例可與Ar1、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Het is triazolyl. This embodiment can be used in combination with other embodiments of Ar 1 , Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,Het為1,2,4-三唑基。本實施例可與Ar1、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Het is 1,2,4-triazolyl. This embodiment can be used in combination with other embodiments of Ar 1 , Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,Het為噁二唑基。本實施例可與Ar1、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Het is oxadiazolyl. This embodiment can be used in combination with other embodiments of Ar 1 , Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,Het為1,3,4-噁二唑基。本實施例可與Ar1、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Het is 1,3,4-oxadiazolyl. This embodiment can be used in combination with other embodiments of Ar 1 , Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,Het為吡唑基。本實施例可與Ar1、Ar2、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Het is pyrazolyl. This embodiment can be used in combination with other embodiments of Ar 1 , Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,Ar2為苯基。本實施例可與Ar1、Het、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Ar 2 is phenyl. This embodiment can be used in combination with other embodiments of Ar 1 , Het, R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkages, and/or L.

於另一實施例中,Ar2為經取代之苯基。本實施例可與Ar1、 Het、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Ar 2 is substituted phenyl. This embodiment can be used in combination with other embodiments of Ar 1 , Het, R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkages, and/or L.

於另一實施例中,Ar2為一個具有一或多個選自C1-C6烷基的取代基之經取代的苯基。本實施例可與Ar1、Het、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Ar 2 is a substituted phenyl group having one or more substituents selected from C 1 -C 6 alkyl groups. This embodiment can be used in combination with other embodiments of Ar 1 , Het, R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkages, and/or L.

於另一實施例中,Ar2為一個具有一或多個取代基(且其中該取代基為CH3)的經取代之苯基。本實施例可與Ar1、Het、R1、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Ar 2 is a substituted phenyl group with one or more substituents (and wherein the substituent is CH 3 ). This embodiment can be used in combination with other embodiments of Ar 1 , Het, R 1 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl linkages, and/or L.

於另一實施例中,R1為H。本實施例可與Ar1、Het、Ar2、R2、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 1 is H. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 2 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R2(J)、H、(C1-C6)烷基、(C1-C6)烷基-O-C(O)-(C1-C6)烷基、(C1-C6)烷基-O-C(O)-N(RxRy)或(C1-C6烷基)-S-(Het-1)。本實施例可與Ar1、Het、Ar2、R1、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 2 is (J) , H, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-OC(O)-(C 1 -C 6 )alkyl , (C 1 -C 6 )alkyl-OC(O)-N(R x R y ) or (C 1 -C 6 alkyl)-S-(Het-1). This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R2(J)、H、CH3、(C1-C6)烷基、CH2OC(O)CH(CH3)2、CH2OC(O)N(H)(C(O)OCH2Ph)或CH2S(3,4,5-三甲氧基-2-四氫吡喃)。本實施例可與Ar1、Het、Ar2、R1、R3、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 2 is (J) , H, CH 3 , (C 1 -C 6 )alkyl, CH 2 OC(O)CH(CH 3 ) 2 , CH 2 OC(O)N( H) (C(O)OCH 2 Ph) or CH 2 S (3,4,5-trimethoxy-2-tetrahydropyran). This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 3 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R3為經取代之苯基。本實施例可與Ar1、Het、Ar2、R1、R2、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 3 is substituted phenyl. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R3為經取代之苯基且其中所述經取代之苯基具有一或多個選自F、Cl、(C1-C6)烷基、(C3-C6)環烷基、(C1-C6)烷氧基及苯基的取代基。本實施例可與Ar1、Het、Ar2、R1、R2、R4、Q1、R2及 R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 3 is substituted phenyl and wherein said substituted phenyl has one or more selected from F, Cl, (C 1 -C 6 )alkyl, (C 3 -C 6 ) Cycloalkyl, (C 1 -C 6 )alkoxy and phenyl substituents. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R3為經取代之苯基且其中所述經取代之苯基具有一或多個選自F、CH3、2-CH(CH3)2、CH(CH3)(C2H5)、OCH3及苯基的取代基。本實施例可與Ar1、Het、Ar2、R1、R2、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 3 is substituted phenyl and wherein the substituted phenyl has one or more selected from F, CH 3 , 2-CH(CH 3 ) 2 , CH(CH 3 ) (C 2 H 5 ), OCH 3 and phenyl substituents. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R3為經取代之苯基,其中所述經取代之苯基具有一個以上的取代基且所述取代基中的至少一對並不彼此相鄰。本實施例可與Ar1、Het、Ar2、R1、R2、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 3 is a substituted phenyl group, wherein the substituted phenyl group has more than one substituent and at least one pair of the substituents are not adjacent to each other. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R3為(C1-C6)烷基苯基。本實施例可與Ar1、Het、Ar2、R1、R2、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 3 is (C 1 -C 6 )alkylphenyl. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R3為(Het-1)。本實施例可與Ar1、Het、Ar2、R1、R2、R4、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 3 is (Het-1). This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 4 , Q 1 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R4為H。本實施例可與Ar1、Het、Ar2、R1、R2、R3、Q1、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, R 4 is H. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 3 , Q 1 , R 2 and R 4 hydrocarbyl linkages, and/or L.

於另一實施例中,Q1為O。本實施例可與Ar1、Het、Ar2、R1、R2、R3、R4、R2及R4烴基鍵聯、及/或L之其他實施例組合使用。 In another embodiment, Q 1 is O. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , R 2 and R 4 hydrocarbyl bonding, and/or L.

於另一實施例中,R2及R4為烴基鍵聯且所述烴基鍵聯係經側氧基或(C1-C6)烷基取代。本實施例可與Ar1、Het、Ar2、R1、R2、R3、R4、Q1、及/或L之其他實施例組合使用。 In another embodiment, R 2 and R 4 are hydrocarbyl linkages and the hydrocarbyl linkages are substituted with pendant oxy groups or (C 1 -C 6 )alkyl groups. This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , and/or L.

於另一實施例中,R2及R4為烴基鍵聯且所述烴基鍵聯為CH2C(O),C(C(OH)(CH3)2)C(O)、C(環丙基)C(O)、C(CH3)2C(O)、CFHC(O)、CBrHC(O)、CH(CH3)C(O)、CH2CH2,CH2C(OH)(CH3)、CH2CH2CH2, CH2CH2C(O)、CH2CH(CH3)CH2、N(CH3)C(O),N(CH2CH3)C(O)、CH=C(CH3)或CH2CH(CH3)。本實施例可與Ar1、Het、Ar2、R1、R2、R3、R4、Q1、及/或L之其他實施例組合使用 In another embodiment, R 2 and R 4 are hydrocarbyl linkages and the hydrocarbyl linkages are CH 2 C(O), C(C(OH)(CH 3 ) 2 )C(O), C(ring Propyl) C(O), C(CH 3 ) 2 C(O), CFHC(O), CBrHC(O), CH(CH 3 )C(O), CH 2 CH 2 , CH 2 C(OH) (CH 3 ), CH 2 CH 2 CH 2 , CH 2 CH 2 C(O), CH 2 CH(CH 3 )CH 2 , N(CH 3 )C(O), N(CH 2 CH 3 )C( O), CH=C(CH 3 ) or CH 2 CH(CH 3 ). This embodiment can be used in combination with other embodiments of Ar 1 , Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , and/or L

於另一實施例中,L為CH2、CH2CH2,CH2CH(CH3),CH2C(CH3)2、CH2CH(CH2CH3)、CH=CH、CH(CH3)CH2、C(CH3)2CH2、CHBrCH2、CH2C(環丙基)、CH(CH2CH3)CH2、C(CH3)=CH、CH2CH2CH2、CH(CH3)CH(CH3)、CH2CH2CH2CH2、C≡CCH2CH2、環丙基或環己基。本實施例可與Ar1、Het、Ar2、R1、R2、R3、R4、Q1、及/或R2與R4烴基鍵聯之其他實施例組合使用。 In another embodiment, L is CH 2 , CH 2 CH 2 , CH 2 CH(CH 3 ), CH 2 C(CH 3 ) 2 , CH 2 CH(CH 2 CH 3 ), CH=CH, CH( CH 3 )CH 2 , C(CH 3 ) 2 CH 2 , CHBrCH 2 , CH 2 C(cyclopropyl), CH(CH 2 CH 3 ) CH 2 , C(CH 3 )=CH, CH 2 CH 2 CH 2. CH(CH 3 )CH(CH 3 ), CH 2 CH 2 CH 2 CH 2 , C≡CCH 2 CH 2, cyclopropyl or cyclohexyl. This embodiment can be used in combination with other embodiments in which Ar 1 , Het, Ar 2 , R 1 , R 2 , R 3 , R 4 , Q 1 , and/or R 2 and R 4 are bonded to hydrocarbon groups.

許多式1及式2之分子可描述為二或多種互變異構物形式,諸如當R1、R2或R4為H時。任一與所有其他互變異構物皆包含於此式1及此式2之範疇中,且不應推斷為該分子皆存在有其畫出形式之互變異構物。 Many molecules of Formula 1 and Formula 2 can be described as two or more tautomeric forms, such as when R 1 , R 2 or R 4 is H. Any and all other tautomers are included in the categories of this formula 1 and this formula 2, and it should not be inferred that there are tautomers in their drawn forms for the molecule.

製備三芳基-中間物Preparation of triaryl-intermediate

式1及式2分子可藉由產生三芳基中間物Ar1-Het-Ar2來製備,之後將其聯結成適當之中間物,以形成希望之化合物。有多種多樣的三芳基中間物可用於製備式1及式2分子,其中此三芳基中間物之Ar2上含有適當之官能基,其可與希望官能基之其他部分聯結。適當之官能基包括胺基、異氰酸酯、羧基或鹵素(較佳為溴或碘)。這些三芳基中間物可以先前描述於化學文獻中之方法製備,包含Crouse等人,WO2009102736(其全部揭露內容係以引用方式併入本文中)。 Molecules of Formula 1 and Formula 2 can be prepared by generating triaryl intermediates Ar 1 -Het-Ar 2 and then linking them into appropriate intermediates to form the desired compound. There are a variety of triaryl intermediates that can be used to prepare molecules of formula 1 and formula 2, wherein the Ar 2 of the triaryl intermediate contains appropriate functional groups that can be linked to other parts of the desired functional group. Suitable functional groups include amine, isocyanate, carboxyl or halogen (preferably bromine or iodine). These triaryl intermediates can be prepared by methods previously described in the chemical literature, including Crouse et al., WO2009102736 (the entire disclosure of which is incorporated herein by reference).

用於作為製備式1分子之前驅物之三芳基醛,可依據Crouse等人(US 2012/0202688 A1)中描述流程製備。上述某些流程需要使用鹵素-芳基中間物,Ar1-Het-Ph-Br,其為新穎之中間物。這些可依據下面的流程圖 1。3-(4-溴化苯基)-1,2,4-三唑(1-2)係於二步驟中,由4-溴苯甲醯胺(1-1),於先前描述之條件下製備(步驟 a ,Crouse等人,WO2009102736)。之後此三唑可耦合至芳基鹵化物1-3(R=(C1-C6)鹵烷氧基),如4-三氟甲氧基苯基溴化苯,於碳酸銫或碳酸鉀存在下,於極性非質子溶劑如二甲基甲醯胺中進行。此反應經銅鹽類如碘化亞銅(I)與螯合劑如8-羥基喹啉催化,二者之存在量皆為約0.05至約0.25當量,於溫度範圍約80℃至約140℃下進行,形成1-芳基-3-(4-溴化苯基)三唑1-4(步驟 b )。 The triaryl aldehyde used as the precursor of the formula 1 molecule can be prepared according to the process described in Crouse et al. (US 2012/0202688 A1). Some of the above procedures require the use of a halogen-aryl intermediate, Ar 1 -Het-Ph-Br, which is a novel intermediate. These can be based on the following flow chart 1. 3-(4 -Bromophenyl)-1,2,4-triazole (1-2 ) is linked in two steps, from 4-bromobenzamide ( 1- 1 ), prepared under the previously described conditions (step a , Crouse et al., WO2009102736). This triazole can then be coupled to aryl halide 1-3 (R=(C 1 -C 6 )haloalkoxy), such as 4-trifluoromethoxyphenyl benzene bromide, in cesium carbonate or potassium carbonate In the presence, it is carried out in a polar aprotic solvent such as dimethylformamide. This reaction is catalyzed by copper salts such as cuprous (I) iodide and chelating agents such as 8-hydroxyquinoline, both of which are present in an amount of about 0.05 to about 0.25 equivalents, at a temperature range of about 80°C to about 140°C Proceeding to form 1-aryl-3-(4-bromophenyl)triazole 1-4 (step b ).

Figure 106137106-A0202-12-0020-8
Figure 106137106-A0202-12-0020-8

製備1-原子鍵聯之中間物Preparation of 1-atom bonding intermediates

於其中L為一個碳之連接基團的式1及式2分子係可由酸或胺中間物製備,分別如流程圖2與流程圖3所述。未經取代或經R8單-或二-取代之酸前驅物2-5(Ar1-Het-Ar2-L-CO2H)係可依據流程圖2所式而製備。硼酸酯2-2(步驟 a )可使用Miyaura條件,由鹵化苯基酯2-1製備。硼酸酯與溴-雜環之耦合2-3(步驟 b )可使用鈀催化劑與膦配位基,於鹼(諸如碳酸氫鈉、磷酸鉀或氟化銫)的存在下,在適當溶劑系統(諸如二噁烷/水)中,於溫度約50℃至約120℃下進行,以形成三芳基酯中間物2-4。在各種鈀催化劑中,較佳為四(三苯基膦)鈀(0),儘管可使用其他已知之鈀催化劑。 酯類之皂化反應可藉由使用強鹼如氫氧化鈉或氫氧化鋰,於甲醇或乙醇中,其具有或不具四氫呋喃/水,以提供希望之羧酸2-5(步驟 c )。 The molecular systems of Formula 1 and Formula 2 in which L is a carbon linking group can be prepared from acid or amine intermediates, as described in Scheme 2 and Scheme 3, respectively. The unsubstituted or R 8 mono- or di-substituted acid precursor 2-5 (Ar 1 -Het-Ar 2 -L-CO 2 H) can be prepared according to the formula of Flow Diagram 2. Borate 2-2 (step a ) can be prepared from halogenated phenyl ester 2-1 using Miyaura conditions. The coupling of borate and bromine-heterocycle 2-3 (step b ) can use a palladium catalyst and a phosphine ligand in the presence of a base (such as sodium bicarbonate, potassium phosphate or cesium fluoride) in a suitable solvent system (Such as dioxane/water) at a temperature of about 50°C to about 120°C to form the triaryl ester intermediate 2-4 . Among various palladium catalysts, tetrakis(triphenylphosphine)palladium(0) is preferred, although other known palladium catalysts can be used. The saponification reaction of esters can be achieved by using a strong base such as sodium hydroxide or lithium hydroxide in methanol or ethanol, with or without tetrahydrofuran/water, to provide the desired carboxylic acid 2-5 (step c ).

Figure 106137106-A0202-12-0021-9
Figure 106137106-A0202-12-0021-9

未經取代或經R8單-或二-取代之胺類前驅物3-5(Ar1-Het-Ar2-L-NH2)係可依據流程圖3製備。鹵化苯甲胺3-1可經保護,使用芐基氯化甲酸酯,於鹼(諸如三乙基胺)的存在下,於非質子溶劑(諸如二氯甲烷)中,於約-10℃至約10℃下,而得到經N-羧基芐基(Cbz)保護的芐基胺3-2(步驟 a )。或者,可使用其他N-保護基團(諸如第三-丁氧基羰基(BOC)或9-茀基甲基羰基(Fmoc))於步驟 a 中,使用類似於Cbz之條件。經Cbz保護之硼酸酯3-3可使用Miyaura條件製備(步驟 b )。硼酸酯與溴-雜環之耦合2-3可使用鈀催化劑與膦配位基,於鹼(諸如碳酸氫鈉、磷酸鉀或氟化銫)的存在下,在適當溶劑系統(諸如二噁烷/水)中,於溫度約50℃至約120℃下進行,以形成N-經保護胺基烷基苯基中間物3-4(步驟 c )。Cbz 基團的移除係可於酸性條件下,以強酸(諸如溴化氫)達成,隨後以鹼(諸如碳酸氫鈉或氫氧化鈉)進行中和,以提供自由胺基前驅物3-5(Ar1-Het-Ar2-L-NH2,步驟 d )。類似之方法可應用於其中L為大於一個碳之化合物上。 The unsubstituted or R 8 mono- or di-substituted amine precursor 3-5 (Ar 1 -Het-Ar 2 -L-NH 2 ) can be prepared according to Flow Diagram 3. Halogenated benzylamine 3-1 can be protected, using benzyl chloroformate, in the presence of a base (such as triethylamine) in an aprotic solvent (such as dichloromethane) at about -10°C To about 10° C. to obtain benzylamine 3-2 protected by N -carboxybenzyl (Cbz) (step a ). Alternatively, other N -protecting groups (such as tertiary-butoxycarbonyl (BOC) or 9-phosphorylmethylcarbonyl (Fmoc)) can be used in step a , using conditions similar to Cbz. The Cbz-protected boronate 3-3 can be prepared using Miyaura conditions (step b ). The coupling of borate and bromine-heterocycle 2-3 can use a palladium catalyst and a phosphine ligand, in the presence of a base (such as sodium bicarbonate, potassium phosphate or cesium fluoride), in a suitable solvent system (such as dioxin) In alkane/water), it is carried out at a temperature of about 50°C to about 120°C to form the N -protected aminoalkylphenyl intermediate 3-4 (step c ). The removal of Cbz groups can be achieved under acidic conditions with strong acids (such as hydrogen bromide), followed by neutralization with alkalis (such as sodium bicarbonate or sodium hydroxide) to provide free amine precursors 3-5 (Ar 1 -Het-Ar 2 -L-NH 2 , step d ). A similar method can be applied to compounds where L is more than one carbon.

Figure 106137106-A0202-12-0022-10
Figure 106137106-A0202-12-0022-10

製備乙基鍵聯中間物Preparation of ethyl linkage intermediate

其中L為二原子基團之化合物之製備,係描述於流程圖4至流程圖6。醛類4-1(R9=H)(描述於US 2012/0202688 A1)與試劑如二乙基膦乙酸乙酯,或Wittig試劑如乙基2-(三苯基膦烯)丙酸酯),或αα-經取代醋酸酯,如乙基2-氟醋酸酯或乙基2-氰醋酸酯之縮合反應,係於適當鹼如 氫化鈉或n-丁基鋰存在下,於非質子溶劑如四氫呋喃或乙醚中,於溫度約-78℃至約20℃下,製備丙烯酸酯4-2(步驟 a ),其未經取代或經R9及/或R10單取代。所得酯類之皂化反應可使用強鹼如氫氧化鈉進行,於甲醇或乙醇中,其具有或不具四氫呋喃/水,以提供乙烯基羧酸4-3(步驟 b )。在一些案例中,醛類4-1(R9=H)之部分縮合可產生醇類中間物4-4(步驟 c )之分離,尤其是當R10為拉電子基時。此醇類經親核性試劑如Deoxo-Fluor®取代(步驟 d ),之後進行皂化反應,如上所述(步驟 e ),可產生高度經取代之乙基羧酸4-5,其額外地經R11取代,其中R11係定義如R8。較佳為飽和性連結,該丙烯酸酯4-2便可轉換為對應之環丙烷4-6,未經取代或經R12單-或二-取代;具有硫偶極體,如自三甲基碘化鋶原位形成,於無機鹼如氫化鈉存在下,於極性非質子溶劑如二甲基亞碸或四氫呋喃中進行(步驟 f )。同樣地,丙烯酸酯4-2可還原為原始烷類4-8,使用氫氣與鈀催化劑(步驟 h )。環丙烷與烷酯皆可於上述鹼性條件下皂化,以分別產生自由羧酸4-7(步驟 g )與4-9(步驟 i )。 The preparation of compounds in which L is a diatomic group is described in Scheme 4 to Scheme 6. Aldehydes 4-1 (R 9 =H) (described in US 2012/0202688 A1) and reagents such as ethyl diethylphosphinoacetate, or Wittig reagents such as ethyl 2-(triphenylphosphine) propionate) , Or αα-substituted acetate, such as the condensation reaction of ethyl 2-fluoroacetate or ethyl 2-cyanoacetate, in the presence of a suitable base such as sodium hydride or n -butyl lithium, in an aprotic solvent such as In tetrahydrofuran or diethyl ether, at a temperature of about -78°C to about 20°C, acrylate 4-2 is prepared (step a ), which is unsubstituted or monosubstituted by R 9 and/or R 10 . The saponification reaction of the resulting esters can be carried out using a strong base such as sodium hydroxide, in methanol or ethanol, with or without tetrahydrofuran/water, to provide vinyl carboxylic acid 4-3 (step b ). In some cases, partial condensation of aldehydes 4-1 (R 9 =H) can produce separation of alcohol intermediates 4-4 (step c ), especially when R 10 is an electron withdrawing group. This alcohol is substituted with a nucleophilic reagent such as Deoxo-Fluor® (step d ), followed by a saponification reaction, as described above (step e ), to produce highly substituted ethyl carboxylic acid 4-5 , which is additionally R 11 is substituted, where R 11 is defined as R 8 . Preferably, the saturating link is used, and the acrylate 4-2 can be converted to the corresponding cyclopropane 4-6 , unsubstituted or mono- or di-substituted by R 12 ; with a sulfur dipole, such as from trimethyl The alumium iodide is formed in situ in the presence of an inorganic base such as sodium hydride in a polar aprotic solvent such as dimethyl sulfoxide or tetrahydrofuran (step f ). Similarly, the acrylate 4-2 can be reduced to the original alkanes 4-8 using hydrogen and a palladium catalyst (step h ). Both cyclopropane and alkyl esters can be saponified under the above alkaline conditions to produce free carboxylic acids 4-7 (step g ) and 4-9 (step i ), respectively.

以類似方式,酮類4-1(R9=烷基)之縮合(描述於WO 2011017504 A1)與二乙基膦乙酸乙酯,或Wittig試劑如乙基2-(三苯基膦烯)丙酸酯),或α-α經取代醋酸酯,如乙基2-氟醋酸酯或乙基2-氰醋酸酯之縮合反應,在類似上述之條件下,可得到αα-烷基丙烯酸酯4-2或醇類4-4。之後如上述處理4-24-4,其中R9=H可產生對應之不飽和(4-3)或飽和(4-54-74-9)羧酸。 In a similar manner, the condensation of ketones 4-1 (R 9 = alkyl) (described in WO 2011017504 A1) with ethyl diethylphosphinoacetate, or Wittig reagents such as ethyl 2-(triphenylphosphene) propylene Acid ester), or α-α substituted acetate, such as the condensation reaction of ethyl 2-fluoroacetate or ethyl 2-cyanoacetate, under conditions similar to the above, α-alkyl acrylate 4- 2 or alcohols 4-4 . After processing 4-2 or 4-4 as above, where R 9 =H can produce corresponding unsaturated ( 4-3 ) or saturated ( 4-5 , 4-7 , 4-9) carboxylic acid.

Figure 106137106-A0202-12-0024-11
Figure 106137106-A0202-12-0024-11

替代性地,其中L為二原子基團之化合物之製備係描述於流程圖5。首先使用描述於Molander等人,Org.Lett.2007,9,pp 203-206之條件,耦合溴化物5-1(Ar1-Het-Ar2-Br,步驟 a )與(2-((第三-丁氧基羰基)胺基)乙基)三氟硼酸鉀,於鈀催化劑如醋酸鈀(II),以及鹼如碳酸銫存在下,於溫度約80℃至約120℃,形成對應之2-(第三丁氧基羰基)胺基)乙基衍生物5-2。此材料進一步以約1至約5當量之酸如三氟醋酸(TFA)或氯化氫處理,於非質子溶劑如二氯甲烷或二噁烷中,於溫度約0℃至約50℃下,產生第三丁氧基羰基之切割,形成胺類5-3(Ar1-Het-Ar2-L-NH3 +A-,其中A-為CF3CO2 -或Cl-,步驟 b )的鹽。 Alternatively, the preparation of compounds in which L is a diatomic group is described in Scheme 5. First, using the conditions described in Molander et al., Org . Lett. 2007 , 9 , pp 203-206, coupling bromide 5-1 (Ar 1 -Het-Ar 2 -Br, step a ) and (2-((section (Tri-butoxycarbonyl)amino)ethyl)potassium trifluoroborate, in the presence of a palladium catalyst such as palladium(II) acetate, and a base such as cesium carbonate, at a temperature of about 80°C to about 120°C, the corresponding 2 -(Third-butoxycarbonyl)amino)ethyl derivative 5-2 . This material is further treated with about 1 to about 5 equivalents of acid such as trifluoroacetic acid (TFA) or hydrogen chloride in an aprotic solvent such as dichloromethane or dioxane at a temperature of about 0°C to about 50°C to produce cutting of the three-butoxycarbonyl group, forming amines 5-3 (Ar 1 -Het-Ar 2 -L-NH 3 + a -, wherein a - is CF 3 CO 2 - or Cl -, step b) salts.

Figure 106137106-A0202-12-0025-12
Figure 106137106-A0202-12-0025-12

胺基烷基前驅物6-5(Ar1-Het-Ar2-L-NH2),其中L為2-碳原子,經R9單-或二-取代,其中R9如上述定義;並經R10單-或二-取代,其中R10如上述定義,可依據流程圖6製備。未經取代之鹵化苯基甲醇6-1(R9及R10為H),其中X選自Cl、Br或I,為商業上可購得。其R9位置經單-或二取代之甲醇6-1可製備自相對應之鹵化苯基醋酸酯6-I(步驟 a ),以類似於Shin等人,Bioorg.Med.Chem.Lett. 2008,18,pp 4424-4427中所描述之方法,之後以金屬氫化物如鋰鋁氫化物還原,於醚類溶劑如四氫呋喃或乙醚中,於溫度約0℃或以下進行。6-I6-II二者可更進一步經R10單-取代(步驟 b 或步驟 c ),以金屬氫化物如異丁基氫化鋁還原成相對應之醛類,並以格任亞試劑(Grignard reagent)處理,以類似於Brimble等人,Org.Lett. 2012,14,pp 5820-5823中所述之方法。甲醇6-1可以酞亞醯胺處理,於Mitsunobu條件下,產生N-酞亞醯胺基中間物6-2(步驟 d )。鹵化物可於Miyaura條件下轉換為硼酸酯,以形成硼酸酯類6-3(步驟 e )。硼酸酯類與溴-雜環2-3之耦合可使用鈀催化劑如四(三苯基膦)鈀(0),於鹼如碳酸氫鈉之存在下,於適當溶劑系統中如二噁烷/水,於溫度約50℃至約120℃下進行,提供N-酞亞醯胺基中間物6-4(步驟 f )。使用聯胺與甲醇或其他適宜溶劑進行去保護,可得胺類6-5(步驟 g )。 Aminoalkyl precursor 6-5 (Ar 1 -Het-Ar 2 -L-NH 2 ), wherein L is a 2-carbon atom, mono- or di-substituted by R 9 , wherein R 9 is as defined above; and Mono- or di-substituted by R 10 , where R 10 is as defined above, can be prepared according to Scheme 6. Unsubstituted halogenated phenylmethanol 6-1 (R 9 and R 10 are H), where X is selected from Cl, Br or I, is commercially available. Methanol 6-1 whose R 9 position is mono- or di-substituted can be prepared from the corresponding halogenated phenyl acetate 6-I (step a ), similar to Shin et al., Bioorg.Med.Chem.Lett. 2008 , 18 , pp 4424-4427, followed by reduction with a metal hydride such as lithium aluminum hydride, in an ether solvent such as tetrahydrofuran or diethyl ether, at a temperature of about 0°C or below. Both 6-I and 6-II through 10 can be further mono R - substituted (step b or step C), to a metal hydride such as diisobutyl aluminum hydride to the corresponding aldehydes and Grignard in Grignard reagent was processed in a manner similar to that described in Brimble et al., Org. Lett. 2012 , 14 , pp 5820-5823. Methanol 6-1 can be treated with phthalimide to produce N -phthalimide intermediate 6-2 under Mitsunobu conditions (step d ). Halides can be converted to borate esters under Miyaura conditions to form borate esters 6-3 (step e ). The coupling of borate and bromine-heterocycle 2-3 can use palladium catalyst such as tetrakis(triphenylphosphine)palladium(0) in the presence of a base such as sodium bicarbonate in a suitable solvent system such as dioxane/ Water, carried out at a temperature of about 50°C to about 120°C, provides N -phthalimide intermediate 6-4 (step f ). Use hydrazine and methanol or other suitable solvents for deprotection to obtain amines 6-5 (step g ).

Figure 106137106-A0202-12-0026-13
Figure 106137106-A0202-12-0026-13

替代性地,其中L為2-原子連接基團之化合物亦可依據流程圖6a製備。醛類4-1(R9=H,步驟 a )之烯烴化可以伸甲基苯基膦達成,其可製備自甲基三苯基碘化鏻,於鹼如氫化鈉或1,8-二氮雜雙環十一-7-烯存在下,於非質子溶劑如四氫呋喃或二氯甲烷中,於溫度約-78℃至約40℃下進行。6-2a進一步以硼氫化試劑(諸如9-硼二環(3.3.1)壬烷)(9-BBN)在一非質子溶劑(諸如四氫呋喃)中進行硼氫化反應,之後以氧化劑如過氧化氫進行氧化作用,產生乙醇6-3a(步驟 b )。甲醇6-3a可以酞亞醯胺處理,於Mitsunobu條件下,以產生N-酞亞醯胺基中間物6-5a,其中R10=H(步驟 c )。使用聯胺與甲醇或其他適當溶劑進行去保護,可得胺類6-6a(步驟 f )。此外,6-3a可更進一步以R10進行單-取代,其中R10係如上述定義(步驟 d ),藉由將對應之醛類進行氧化,於Swern條件下,之後如上述加入格任亞試劑(Grignard reagent)(流程圖6)而達成。甲醇6-4a可進一步以酞亞醯胺處理, 於Mitsunobu條件下,以產生N-酞亞醯胺基中間物6-5a(步驟 e )。使用聯胺與甲醇或其他適當溶劑進行去保護,可得胺類6-6a(步驟 f )。 Alternatively, compounds in which L is a 2-atom linking group can also be prepared according to Scheme 6a. The olefination of aldehydes 4-1 (R 9 =H, step a ) can be achieved by methylphenyl phosphine, which can be prepared from methyl triphenyl phosphonium iodide and used in bases such as sodium hydride or 1,8-di It is carried out in the presence of azabicycloundec-7-ene in an aprotic solvent such as tetrahydrofuran or dichloromethane at a temperature of about -78°C to about 40°C. 6-2a is further subjected to the borohydride reaction with a borohydride reagent (such as 9-borobicyclo(3.3.1) nonane) (9-BBN) in an aprotic solvent (such as tetrahydrofuran), followed by an oxidizing agent such as hydrogen peroxide Oxidation is performed to produce ethanol 6-3a (step b ). Methanol 6-3a can be treated with phthalimide under Mitsunobu conditions to produce N -phthalimide-based intermediate 6-5a , where R 10 =H (step c ). Deprotection with hydrazine and methanol or other suitable solvents can obtain amines 6-6a (step f ). Further, 6-3a to R 10 may further be mono - substituted, wherein R 10 is as defined line (step d) above, the corresponding aldehydes by oxidizing, in Swern conditions, such as after any of the above-described alkylene Jia Ruge Reagent (Grignard reagent) (flow chart 6). Methanol 6-4a can be further treated with phthalimide under Mitsunobu conditions to produce N -phthalimide-based intermediate 6-5a (step e ). Deprotection with hydrazine and methanol or other suitable solvents can obtain amines 6-6a (step f ).

Figure 106137106-A0202-12-0027-14
Figure 106137106-A0202-12-0027-14

流程圖6b列出建構其中連接基團L為二原子連接基團之類似物之另一路徑。2,4-戊烷-2,4-二酮與5-1之銅催化芳基化反應(J.Am.Chem.Soc. 2010,132,8273),可提供經取代之丙酮中間物6-1b(步驟 a )。使用本領域技術人員熟悉的各種條件中的任何一種之還原性胺化反應(步驟 b )係可產生胺類6-2b。當連接基團含有不對稱中心時,如中間物6-2b,這些中間物可分離出其純異構物形式,使用不對稱管柱,或使用由不對稱酸如(+)與(-)酒石酸製備之鹽類之分液結晶法。 Scheme 6b lists another way to construct analogs where the linking group L is a diatomic linking group. Copper-catalyzed arylation reaction of 2,4-pentane-2,4-dione and 5-1 (J.Am.Chem.Soc. 2010 , 132 , 8273), can provide substituted acetone intermediate 6 1b (Step a ). A reductive amination reaction (step b ) using any of various conditions familiar to those skilled in the art can produce amines 6-2b . When the linking group contains an asymmetric center, such as intermediates 6-2b , these intermediates can be separated into their pure isomeric forms, using asymmetric columns, or using asymmetric acids such as (+) and (-) Liquid separation crystallization method of salts prepared by tartaric acid.

Figure 106137106-A0202-12-0028-15
Figure 106137106-A0202-12-0028-15

建構其中乙基連接基團為6-員環之一部分之類似物,可起始自溴化物5-15-1以2-環己-1-烯基-4,4,5,5-四甲基-1,3,2-二噁硼烷耦合(流程圖6b,步驟 c ),於標準Suzuki耦合條件下,可產生烯類6-3b。以標準試劑如間-氯過氧苯甲酸進行氧化(步驟 d ),之後進行酸催化重排,使用三氯化銦(J.Org.Chem. 1998,63,8212)可產生酮類6-5b。還原性胺化與轉換為目標分子,可使用上述條件達成。 The construction of analogs in which the ethyl linking group is part of a 6-membered ring can start from bromide 5-1 . 5-1 Coupled with 2-cyclohex-1-enyl-4,4,5,5-tetramethyl-1,3,2-dioxborane (flow diagram 6b, step c ), coupled with standard Suzuki Under conditions, olefins 6-3b can be produced. In standard reagents such as m - chloroperoxybenzoic acid oxidation (step d), followed by acid-catalyzed rearrangement, using indium trichloride may produce ketones 6-5b (J.Org.Chem 1998, 63,8212.) . Reductive amination and conversion into target molecules can be achieved using the above conditions.

製備丙基鍵聯中間物Preparation of propyl linkage intermediate

製備其中L為三原子基團之化合物,係如流程圖7與8所示。胺基烷基前驅物7-5(Ar1-Het-Ar2-L-NH2),其中L為3-碳原子,經R9單-或二-取代,其中R9如上述定義;以及未經取代或經R10單-取代,其中R10如上述定義;可如流程圖7製備。鹵化苯基甲醇7-1,其中X為Br,且R9與R10為H,為商業上可購得。R9經單-或二-取代之甲醇7-1,可製備自相對應之鹵化苯基醋酸酯7-I(步驟 a ),以類似於Shin等人,Bioorg.Med. Chem.Lett. 2008,18,pp 4424-4427所描述之方法,之後以金屬氫化物如鋰鋁氫化物還原,於醚類溶劑如四氫呋喃,於溫度約0℃或更低下進行。7-I7-II二者可進一步經R10單取代(步驟 b 或步驟 c ),經由將對應之醛類以金屬氫化物如二異丁基氫化鋁還原,並以格任亞試劑(Grignard reagent)如甲基溴化鎂處理,以類似於Brimble等人,Org.Lett.2012,14,pp 5820-5823所描述之方法。甲醇7-1可以酞亞醯胺處理,於Mitsunobu條件下,以產生N-酞亞醯胺基中間物7-2(步驟 d )。 The preparation of compounds in which L is a triatomic group is shown in Schemes 7 and 8. Aminoalkyl precursor 7-5 (Ar 1 -Het-Ar 2 -L-NH 2 ), where L is a 3-carbon atom, mono- or di-substituted by R 9 , where R 9 is as defined above; and Unsubstituted or mono-substituted by R 10 , where R 10 is as defined above; it can be prepared as in Scheme 7. Halogenated benzyl alcohol 7-1 , where X is Br, and R 9 and R 10 are H, is commercially available. Mono- or di-substituted methanol 7-1 with R 9 can be prepared from the corresponding halogenated phenyl acetate 7-I (step a ), similar to Shin et al., Bioorg. Med. Chem. Lett. 2008 , 18 , pp 4424-4427, followed by reduction with a metal hydride such as lithium aluminum hydride, in an ether solvent such as tetrahydrofuran, at a temperature of about 0°C or lower. Both 7-I and 7-II can be further monosubstituted by R 10 (step b or step c ), by reducing the corresponding aldehydes with metal hydrides such as diisobutylaluminum hydride, and using Grignard reagent ( Grignard reagent) is treated as methylmagnesium bromide in a manner similar to that described in Brimble et al., Org . Lett. 2012 , 14 , pp 5820-5823. Methanol 7-1 can be treated with phthalimid under Mitsunobu conditions to produce N -phthalimid intermediate 7-2 (step d ).

Figure 106137106-A0202-12-0029-16
Figure 106137106-A0202-12-0029-16

該鹵化物可於Miyaura條件下轉換,以形成硼酸酯類7-3(步驟 e )。硼酸酯類與溴-雜環2-3之耦合可使用鈀催化劑如四(三苯基膦)鈀(0),於鹼如碳酸氫鈉之存在下,在適當溶劑系統如二噁烷/水中,於溫度約50℃至約120℃下進行,提供N-酞亞醯胺基中間物7-4(步驟 f )。使用聯胺與甲 醇或其他適宜溶劑進行去保護,可得胺類7-5(步驟 g )。 The halide can be converted under Miyaura conditions to form borate esters 7-3 (step e ). The coupling of borate and bromine-heterocycle 2-3 can use palladium catalyst such as tetrakis(triphenylphosphine)palladium(0) in the presence of a base such as sodium bicarbonate in a suitable solvent system such as dioxane/water , Carried out at a temperature of about 50°C to about 120°C, to provide N -phthalimide intermediate 7-4 (step f ). Using hydrazine and methanol or other suitable solvents for deprotection, amines 7-5 can be obtained (step g ).

替代性地,其中L為3-原子連接基團之化合物亦可如流程圖8製備。溴化物5-1(Ar1-Het-Ar2-Br)可與適當之炔基醇8-1耦合,其未經取代或經R10單-取代,其中R10如上述定義,於鈀催化劑如雙三苯基膦二氯化鈀(II)、碘化銅(I),以及鹼如三乙胺的存在下,於溫度約50℃至約120℃,產生相對應之炔基醇衍生物8-2(步驟 a )。所得之甲醇8-2可以酞亞醯胺處理,於Mitsunobu條件下,以產生N-酞亞醯胺基中間物8-3(步驟 b ),其可使用聯胺與甲醇或其他適宜溶劑轉換為胺類(8-7,步驟 e )。甲醇8-2可使用過渡金屬如鈀催化劑還原,於氫氣環境下,以提供烯基或完全飽和之烷基甲醇8-4,其R10未經取代。此外,甲醇8-2可以金屬氫化物如鋰鋁氫化物處理,以提供(E)-烯基甲醇8-4。同樣地,甲醇8-2可經保護基如第三丁基二苯基矽烷(TBDPS)保護,並以氫金屬化試劑如Schwartz試劑處理,之後以親電試劑如元素碘或N-溴琥珀酸醯亞胺(NBS)進行淬滅。替代性地,甲醇8-2可以金屬轉移化試劑如二硼酸頻那醇酯處理,以進一步用於過渡金屬催化耦合反應中,如Suzuki或Negishi耦合,以製備經R9單-或二-取代之甲醇8-4,其中R9如上述定義(步驟 c )。去保護之後,所得之甲醇8-4可以酞亞醯胺處理,於Mitsunobu條件下,產生可被轉換之N-酞亞醯胺基中間物8-5(步驟 d )。 Alternatively, compounds in which L is a 3-atom linking group can also be prepared as shown in Scheme 8. Bromide 5-1 (Ar 1 -Het-Ar 2 -Br) can be coupled with an appropriate alkynyl alcohol 8-1 , which is unsubstituted or mono-substituted by R 10 , where R 10 is as defined above, on a palladium catalyst For example, in the presence of bistriphenylphosphine palladium(II) dichloride, copper(I) iodide, and a base such as triethylamine, the corresponding alkynyl alcohol derivative is produced at a temperature of about 50°C to about 120°C 8-2 (Step a ). The resulting methanol 8-2 can be treated with phthalimide under Mitsunobu conditions to produce N -phthalimide intermediate 8-3 (step b ), which can be converted into using hydrazine and methanol or other suitable solvents Amines ( 8-7 , step e ). Methanol 8-2 can be reduced with a transition metal such as palladium catalyst under hydrogen atmosphere to provide alkenyl or fully saturated alkyl methanol 8-4 , R 10 of which is unsubstituted. In addition, methanol 8-2 can be treated with a metal hydride such as lithium aluminum hydride to provide ( E )-alkenyl methanol 8-4 . Similarly, methanol 8-2 can be protected with a protecting group such as tertiary butyldiphenyl silane (TBDPS), and treated with a hydrogen metallation reagent such as Schwartz reagent, followed by electrophilic reagent such as elemental iodine or N -bromosuccinic acid NBS is quenched. Alternatively, methanol 8-2 can be treated with a metal transfer reagent such as pinacol diborate for further use in transition metal catalyzed coupling reactions, such as Suzuki or Negishi coupling, to prepare R 9 mono- or di-substituted The methanol 8-4 , where R 9 is as defined above (step c ). After deprotection, the resulting methanol 8-4 can be treated with phthalimide, under Mitsunobu conditions, to produce an N -phthalimide intermediate 8-5 that can be converted (step d ).

Figure 106137106-A0202-12-0031-17
Figure 106137106-A0202-12-0031-17

製備丁基鍵聯之中間物Preparation of butyl linkage intermediate

其中L為4-原子連接基團之化合物可如流程圖9製備。溴化物5-1(Ar1-Het-Ar2-Br)可與適當之炔基醇耦合9-1(步驟 a ),其未經取代或經R10單取代,其中R10如上述定義;經R9單-或二-取代,其中R9如上述定義;於鈀催化劑如雙三苯基膦二氯鈀(II)、碘化銅(I),以及鹼如三乙胺的存在下,於溫度約50℃至約120℃下,以產生相對應之炔基醇衍生物9-2。所得甲醇9-2可以酞亞醯胺處理,於Mitsunobu條件下(步驟b),產生N-酞亞醯胺基中間物9-3,其可使用聯胺與甲醇或其他適宜溶劑轉換為胺類9-7(步驟e)。甲醇9-2可使用過渡金屬催化劑如鈀還原,於氫氣環境下,得烯基或完全飽和之烷基甲醇9-4(步驟c),其R13未經取代。此外,甲醇9-2可 以金屬氫化物如鋰鋁氫化物處理,得(E)-烯基甲醇9-4(步驟c)。同樣地,甲醇9-2可以保護基如第三-丁基二苯基矽烷(TBDPS)保護,並以氫金屬化試劑如Schwartz試劑處理,之後以親電試劑如元素碘或(NBS)進行淬滅。此外,甲醇9-2可以金屬轉移化試劑如二硼酸頻那醇酯(pinacol diboron)處理,以進一步用於過渡金屬催化耦合反應,如Suzuki或Negishi耦合,以製備甲醇9-4,其經R13單-或二-取代,其中R13如上述R8所定義(步驟 c )。 Compounds in which L is a 4-atom linking group can be prepared as shown in Scheme 9. Bromide 5-1 (Ar 1 -Het-Ar 2 -Br) can be coupled with an appropriate alkynyl alcohol 9-1 (step a ), which is unsubstituted or monosubstituted by R 10 , wherein R 10 is as defined above; Mono- or di-substituted by R 9 , where R 9 is as defined above; in the presence of a palladium catalyst such as bistriphenylphosphine dichloropalladium(II), copper(I) iodide, and a base such as triethylamine, At a temperature of about 50°C to about 120°C, the corresponding alkynyl alcohol derivative 9-2 is produced. The obtained methanol 9-2 can be treated with phthalimide, under Mitsunobu conditions (step b), to produce N-phthalimide intermediate 9-3, which can be converted into amines using hydrazine and methanol or other suitable solvents 9-7 (Step e ). Methanol 9-2 can be reduced with a transition metal catalyst such as palladium, and under hydrogen atmosphere, an alkenyl or fully saturated alkyl methanol 9-4 is obtained (step c), and R 13 is unsubstituted. In addition, methanol 9-2 can be treated with a metal hydride such as lithium aluminum hydride to obtain (E) -alkenyl methanol 9-4 (step c). Similarly, methanol 9-2 can be protected with a protecting group such as tertiary butyl diphenyl silane (TBDPS) and treated with a hydrogen metallation reagent such as Schwartz reagent, and then quenched with an electrophilic reagent such as elemental iodine or (NBS). Extinct. In addition, methanol 9-2 can be treated with a metal transfer reagent such as pinacol diboron for further use in transition metal catalyzed coupling reactions, such as Suzuki or Negishi coupling, to prepare methanol 9-4 . 13 mono- or di-substituted, wherein R 13 is as defined for R 8 above (step c ).

Figure 106137106-A0202-12-0032-18
Figure 106137106-A0202-12-0032-18

在去保護之後,所得甲醇9-4可以酞亞醯胺處理,於Mitsunobu條件下(步驟 d ),以產生N-酞亞醯胺基中間物9-5,其可使用聯胺與甲醇或其他適宜溶劑轉換為胺類9-6(步驟 e )。 After deprotection, the obtained methanol 9-4 can be treated with phthalimide under Mitsunobu conditions (step d ) to produce N -phthalimide intermediate 9-5 , which can use hydrazine and methanol or other The suitable solvent is converted to amines 9-6 (step e ).

製備N-芳基噻唑啉酮硫脲Preparation of N-arylthiazolinone thiourea

可藉由將噻唑啉酮亞胺(例如10-3)與三芳基異硫氰酸酯(例如10-2)反應而製備N-芳基噻唑啉酮硫脲(thiazolidinone thioureas)(例 如10-4)。如流程圖10所示,三芳基異硫氰酸酯係可由已知的氟胺中間物(出於US 9,029,560 B2,例如10-1)所製備。 N-aryl thiazolinone thioureas (thiazolidinone thioureas) (such as 10-4 ) can be prepared by reacting thiazolinone imines (e.g. 10-3 ) with triaryl isothiocyanates (e.g. 10-2) ). As shown in Flow Diagram 10, triaryl isothiocyanates can be prepared from known fluoroamine intermediates (from US 9,029,560 B2, for example 10-1 ).

Figure 106137106-A0202-12-0033-19
Figure 106137106-A0202-12-0033-19

可在三乙胺及甲苯磺醯氯THF溶液存在下,使用二硫化碳由三芳基乙胺鹽化合物11-2製備所述三芳基乙基異硫氰酸酯化合物11-3。如流程圖11所示,胺鹽11-1係在一個具BOC保護的乙胺鉀氟硼酸鹽之Suzuki耦合以及在二氯甲烷中以TFA去保護之後,產自該三芳基溴化物。 The triarylethyl isothiocyanate compound 11-3 can be prepared from the triarylethylamine salt compound 11-2 in the presence of triethylamine and toluenesulfonyl chloride THF solution using carbon disulfide. As shown in Flow Diagram 11, the amine salt 11-1 is produced from the triaryl bromide after Suzuki coupling of a BOC-protected potassium ethylamine fluoroborate and deprotection with TFA in dichloromethane.

Figure 106137106-A0202-12-0034-20
Figure 106137106-A0202-12-0034-20

實例Instance

此等實例用於說明目的且不應理解為將揭示內容侷限於僅此等實例中所揭示之實施例。 These examples are for illustrative purposes and should not be construed as limiting the disclosure to only the embodiments disclosed in these examples.

自市售來源獲得之起始物質、試劑及溶劑未經進一步純化即使用。無水溶劑以Sure/SealTM購買自Aldrich且按原樣使用。熔點在Thomas Hoover Unimelt毛細管熔點設備或來自Stanford Research Systems之OptiMelt自動化熔點系統上獲得且未校正。使用「室溫」之實例在溫度介於約20℃至約24℃範圍之氣候控制實驗室中進行。分子給定其根據Symyx Draw、ChemDraw或ACD Name Pro內之命名程式命名的已知名稱。若此類程式不能命名分子,則該分子使用常規命名法則命名。除非另外陳述,否則1H NMR光譜資料呈ppm(δ)形式且在300、400或600MHz下記錄;13C NMR光譜資料呈ppm(δ)形式且在75、100或150MHz下記錄。 The starting materials, reagents and solvents obtained from commercially available sources were used without further purification. The anhydrous solvent was purchased from Aldrich as Sure/Seal™ and used as is. The melting point was obtained on Thomas Hoover Unimelt capillary melting point equipment or OptiMelt automated melting point system from Stanford Research Systems and was not corrected. The example of using "room temperature" is performed in a climate control laboratory with a temperature ranging from about 20°C to about 24°C. The molecule is given its known name according to the naming program in Symyx Draw, ChemDraw or ACD Name Pro. If this type of program cannot name the molecule, the molecule is named using conventional nomenclature. Unless otherwise stated, 1 H NMR spectral data is in ppm (δ) format and recorded at 300, 400, or 600 MHz; 13 C NMR spectral data is in ppm (δ) format and recorded at 75, 100, or 150 MHz.

實例1:3-(4-bromophenyl)-1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑之製備Example 1: Preparation of 3-(4-bromophenyl)-1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazole

Figure 106137106-A0202-12-0035-21
Figure 106137106-A0202-12-0035-21

將二甲基亞碸(DMSO;100毫升(mL))及1-碘-4-(三氟甲氧基)苯(16.63g,57.7mmol)添加至在圓底燒瓶中的3-(4-溴苯基)-1H-1,2,4-三唑(14.52克(g)、64.8毫莫耳(mmol))、碘化銅(I)(CuI;3.55g,18.6mmol)及碳酸銫(39.0g,120mmol)。使反應混合物脫氣5分鐘(min)並接著在100℃下加熱過夜。將反應混合物冷卻至室溫,以乙酸乙酯(EtOAc)稀釋並經由Celite®過濾。用EtOAc沖洗Celite®濾餅。將飽和(satd)氯化銨(NH4Cl)溶液添加至濾液中,並攪拌混合物1小時。分離各層且用EtOAc(3x)萃取水層。合併之有機萃取物經無水硫酸鎂(MgSO4)乾燥且濃縮於Celite®上。通過急速層析法(0-40% EtOAc/己烷)純化,得到呈白色固體狀之標題化合物(12.8g,55%):1H NMR(400MHz,CDCl3)δ 8.55(s,1H),8.08-8.03(m,2H),7.80-7.75(m,2H),7.63-7.57(m,2H),7.41-7.35(m,2H).ESIMS m/z 384,386([M]+)。 Dimethyl sulfenite (DMSO; 100 milliliters (mL)) and 1-iodo-4-(trifluoromethoxy)benzene (16.63g, 57.7mmol) were added to the 3-(4- Bromophenyl)-1 H -1,2,4-triazole (14.52 g (g), 64.8 millimoles (mmol)), copper(I) iodide (CuI; 3.55g, 18.6mmol) and cesium carbonate (39.0g, 120mmol). The reaction mixture was degassed for 5 minutes (min) and then heated at 100°C overnight. The reaction mixture was cooled to room temperature, diluted with ethyl acetate (EtOAc) and filtered through Celite ®. Celite ® filter cake was rinsed with EtOAc. A saturated (satd) ammonium chloride (NH 4 Cl) solution was added to the filtrate, and the mixture was stirred for 1 hour. The layers were separated and the aqueous layer was extracted with EtOAc (3x). The combined organic extracts were dried over anhydrous magnesium sulfate (MgSO 4) and concentrated dried over Celite ®. Purified by flash chromatography (0-40% EtOAc/hexane) to obtain the title compound (12.8g, 55%) as a white solid: 1 H NMR (400MHz, CDCl 3 )δ 8.55(s, 1H), 8.08-8.03 (m, 2H), 7.80-7.75 (m, 2H), 7.63-7.57 (m, 2H), 7.41-7.35 (m, 2H). ESIMS m/z 384, 386 ([M] + ).

實例2:(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯乙基)胺基甲酸第三丁酯之製備Example 2: (4-(1-(4-(Trifluoromethoxy)phenyl)-1H-1,2,4-triazol-3-yl)phenethyl)carbamic acid tert-butyl ester preparation

Figure 106137106-A0202-12-0035-22
Figure 106137106-A0202-12-0035-22

將3-(4-溴苯基)-1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑(5.15g,13.4mmol)、(2-((第三丁氧基羰基)胺基)乙基)三氟硼酸鉀(3.37g,13.4mmol)、二環己基(2',6'-二異丙氧基-[1,1'-聯苯基]-2-基)膦(634毫克(mg),1.36mmol)、乙酸鈀(II)(249mg,1.1mmol)及碳酸銫(13.52g,41.5mmol)之甲苯/ 水(4:1;125mL)混合液加熱至95℃經過周末。將反應混合物冷卻至室溫,經由Celite®過濾並以EtOAc清洗。分離各層且用EtOAc萃取水層。合併之有機層係經無水MgSO4乾燥、過濾且濃縮。通過急速管柱層析法(0-50% EtOAc/己烷)純化,得到呈灰白色固體狀之所要化合物(5.23g,83%):mp 149-153℃;1H NMR(400MHz,CDCl3)δ 8.55(s,1H),8.13(d,J=8.3Hz,2H),7.83-7.76(m,2H),7.41-7.36(m,2H),7.31(d,J=8.2Hz,2H),4.56(s,1H),3.42(d,J=6.3Hz,2H),2.86(t,J=6.9Hz,2H),1.44(s,9H);ESIMS m/z 449([M+H]+)。 Combine 3-(4-bromophenyl)-1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazole (5.15g, 13.4mmol), (2-( (Third-butoxycarbonyl)amino)ethyl)potassium trifluoroborate (3.37g, 13.4mmol), dicyclohexyl(2',6'-diisopropoxy-(1,1'-biphenyl) Yl]-2-yl)phosphine (634 mg (mg), 1.36 mmol), palladium(II) acetate (249 mg, 1.1 mmol) and cesium carbonate (13.52g, 41.5 mmol) in toluene/water (4:1; 125mL) ) The mixture was heated to 95°C over the weekend. The reaction mixture was cooled to room temperature, filtered through Celite ® and washed with EtOAc. The layers were separated and the aqueous layer was extracted with EtOAc. The combined organic layers were dried over anhydrous-based MgSO 4, filtered and concentrated. Purified by flash column chromatography (0-50% EtOAc/hexane), the desired compound (5.23g, 83%) was obtained as an off-white solid: mp 149-153°C; 1 H NMR (400MHz, CDCl 3 ) δ 8.55(s,1H),8.13(d, J =8.3Hz,2H),7.83-7.76(m,2H),7.41-7.36(m,2H),7.31(d, J =8.2Hz,2H), 4.56(s,1H),3.42(d, J =6.3Hz,2H),2.86(t, J =6.9Hz,2H),1.44(s,9H); ESIMS m/z 449([M+H] + ).

實例3:2-(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯基)乙-1-胺鎓鹽2,2,2-三氟乙酸鹽之製備Example 3: 2-(4-(1-(4-(Trifluoromethoxy)phenyl)-1 H -1,2,4-triazol-3-yl)phenyl)eth-1-amine Preparation of salt 2,2,2-trifluoroacetate

Figure 106137106-A0202-12-0036-23
Figure 106137106-A0202-12-0036-23

將三氟乙酸(TFA;0.25mL,3.2mmol)添加至4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯乙基胺基甲酸第三丁酯(0.48g,1.07mmol)之二氯甲烷溶液(5.4mL),並於室溫下攪拌該混合物過夜。液相層析質譜儀(LC-MS)的分析顯示出一個起始材料-產物為2:1的混合物,故添加額外的TFA(0.25mL,3.2mmol)。於室溫下攪拌該混合物過夜。該反應混合物係於真空烘箱中濃縮及乾燥,以得到呈黃色固體狀之所要化合物(803mg,100%):1H NMR(400MHz,DMSO-d 6)δ 9.41(s,1H),8.17-7.99(m,4H),7.88(s,3H),7.66-7.60(m,2H),7.43(dd,J=8.5,2.3Hz,2H),3.11(dt,J=8.7,5.9Hz,2H),2.94(dd,J=9.3,6.4Hz,2H);19F NMR(376MHz,DMSO-d 6)δ -57.00,-74.71,-74.85;13C NMR(101MHz,DMSO-d 6)δ 161.90,147.12,143.81,138.89,135.65,129.22,128.78,126.36,122.57,121.10,32.87,24.91;ESIMS m/z 349([M+H]+)。 Trifluoroacetic acid (TFA; 0.25mL, 3.2mmol) was added to 4-(1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazol-3-yl) A dichloromethane solution (5.4 mL) of tert-butyl phenethylcarbamate (0.48 g, 1.07 mmol), and the mixture was stirred at room temperature overnight. Liquid chromatography mass spectrometer (LC-MS) analysis showed a starting material-product mixture of 2:1, so additional TFA (0.25 mL, 3.2 mmol) was added. The mixture was stirred overnight at room temperature. The reaction mixture was concentrated and dried in a vacuum oven to obtain the desired compound (803 mg, 100%) as a yellow solid: 1 H NMR (400MHz, DMSO- d 6 ) δ 9.41(s, 1H), 8.17-7.99 (m,4H),7.88(s,3H),7.66-7.60(m,2H),7.43(dd, J =8.5,2.3Hz,2H),3.11(dt, J =8.7,5.9Hz,2H), 2.94 (dd, J =9.3, 6.4 Hz, 2H); 19 F NMR (376MHz, DMSO- d 6 ) δ -57.00, -74.71, -74.85; 13 C NMR (101MHz, DMSO- d 6 ) δ 161.90, 147.12 ,143.81,138.89,135.65,129.22,128.78,126.36,122.57,121.10,32.87,24.91; ESIMS m/z 349 ([M+H] + ).

實例4:3-(4-(2-異硫氰基乙基)苯基)-1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑之製備Example 4: 3-(4-(2-isothiocyanoethyl)phenyl)-1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazole preparation

Figure 106137106-A0202-12-0037-24
Figure 106137106-A0202-12-0037-24

於室溫下在氮氣(N2)環境中將2-(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯基)乙-1-胺鎓鹽2,2,2-三氟乙酸鹽(325mg,0.70mmol)溶解在四氫呋喃(THF;12mL)中,並添加三乙胺(0.32mL,2.296mmol)。在26分鐘內通過注射器分批加入二硫化碳(43微升(μL),0.713mmol)。於室溫下攪拌該反應物過夜。將該反應混合物冷卻至0℃並加入甲苯磺醯氯(156mg,0.82mmol)。在1小時內將反應混合物加溫至室溫而形成一厚沉澱物。用1當量(N)的鹽酸(HCl)淬滅該反應混合物。用乙醚(3x)萃取該反應混合物,並以水(3x)及新鮮配製的飽和碳酸氫鈉(NaHCO3)溶液洗滌該有機層,經無水MgSO4乾燥該反應混合物,並濃縮該反應混合物以得到黃色油狀物。通過急速層析法(0-40% EtOAc/己烷)純化,得到呈白色固體狀之所要化合物(228mg,71%):1H NMR(400MHz,CDCl3)δ 8.58(s,1H),8.19-8.14(m,2H),7.81(dd,J=8.9,1.5Hz,2H),7.39(d,J=8.9Hz,2H),7.34(d,J=8.2Hz,2H),3.78(td,J=6.9,1.5Hz,2H),3.06(t,J=6.9Hz,2H);ESIMS m/z 391([M+H]+)。 In a nitrogen (N 2 ) environment at room temperature, 2-(4-(1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazol-3-yl )Phenyl)ethan-1-ammonium salt 2,2,2-trifluoroacetate (325 mg, 0.70 mmol) was dissolved in tetrahydrofuran (THF; 12 mL), and triethylamine (0.32 mL, 2.296 mmol) was added. Carbon disulfide (43 microliters (μL), 0.713 mmol) was added in batches via a syringe within 26 minutes. The reaction was stirred overnight at room temperature. The reaction mixture was cooled to 0°C and tosyl chloride (156 mg, 0.82 mmol) was added. The reaction mixture was warmed to room temperature within 1 hour to form a thick precipitate. The reaction mixture was quenched with 1 equivalent (N) of hydrochloric acid (HCl). The reaction mixture was extracted with ether (3x), and the organic layer was washed with water (3x) and a freshly prepared saturated sodium bicarbonate (NaHCO 3 ) solution. The reaction mixture was dried over anhydrous MgSO 4 and the reaction mixture was concentrated to obtain Yellow oil. Purification by flash chromatography (0-40% EtOAc/hexane) gave the desired compound (228 mg, 71%) as a white solid: 1 H NMR (400MHz, CDCl 3 ) δ 8.58 (s, 1H), 8.19 -8.14(m,2H),7.81(dd, J =8.9,1.5Hz,2H),7.39(d, J =8.9Hz,2H),7.34(d, J =8.2Hz,2H),3.78(td, J = 6.9, 1.5 Hz, 2H), 3.06 (t, J = 6.9 Hz, 2H); ESIMS m/z 391 ([M+H] + ).

實例5:(Z)-1-(3-(2-異丙基-5-甲基苯基)-4-氧噻唑亞烷-2-基)-3-(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯乙基)硫脲之製備Example 5: (Z)-1-(3-(2-isopropyl-5-methylphenyl)-4-oxiazolidin-2-yl)-3-(4-(1-(4- (Trifluoromethoxy) phenyl) -1 H -1,2,4-triazol-3-yl) phenethyl) thiourea

Figure 106137106-A0202-12-0038-25
Figure 106137106-A0202-12-0038-25

將3-(4-(2-異硫氰基乙基)苯基)-1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑(55mg,0.14mmol)及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮(50mg,0.20mmol)之N,N-二甲基甲醯胺(DMF;0.47mL)溶液加熱至130℃歷時4小時。LC-MS的分析顯示出已轉變為所要的產物。以水稀釋該反應混合物並以二氯甲烷萃取。有機層係經過一相分離器過濾、濃縮、並裝填於Celite®濾筒上。通過急速層析法(0-40,40-60,60-100% EtOAc/B,其中B=1:1二氯甲烷/己烷)純化,得到了不純的產物。藉逆相急速層析法(0-100%乙腈/H2O)進一步純化,而得到呈黃色油質固體之所要化合物(44mg,47%):1H NMR(400MHz,CDCl3)δ 8.55(d,J=3.6Hz,1H),8.13-7.98(m,2H),7.80(dd,J=9.0,3.4Hz,2H),7.43-7.35(m,2H),7.32-7.19(m,4H),6.92(dt,J=5.7,2.8Hz,1H),6.86-6.76(m,1H),3.95-3.85(m,3H),3.75(dq,J=13.6,6.9Hz,1H),3.04-2.87(m,2H),2.72-2.47(m,1H),2.32(d,J=3.4Hz,3H),1.22-1.05(m,6H);19F NMR(376MHz,CDCl3)δ -58.02;ESIMS m/z 639([M+H]+)。 Add 3-(4-(2-isothiocyanoethyl)phenyl)-1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazole (55mg, 0.14mmol) and 2-imino-3-(2-isopropyl-5-methylphenyl)thiazolidine-4-one (50mg, 0.20mmol) of N,N -dimethylformamide ( DMF; 0.47 mL) The solution was heated to 130°C for 4 hours. LC-MS analysis showed that it had been converted to the desired product. The reaction mixture was diluted with water and extracted with dichloromethane. The organic layer is filtered through a phase separator, concentrated, and packed on the Celite ® filter cartridge. Purified by flash chromatography (0-40, 40-60, 60-100% EtOAc/B, where B=1:1 dichloromethane/hexane), an impure product was obtained. Reverse phase flash chromatography (0-100% acetonitrile/H 2 O) was further purified to obtain the desired compound (44 mg, 47%) as a yellow oily solid: 1 H NMR (400MHz, CDCl 3 )δ 8.55( d, J =3.6Hz,1H),8.13-7.98(m,2H),7.80(dd, J =9.0,3.4Hz,2H),7.43-7.35(m,2H),7.32-7.19(m,4H) ,6.92(dt, J =5.7,2.8Hz,1H),6.86-6.76(m,1H),3.95-3.85(m,3H),3.75(dq, J =13.6,6.9Hz,1H),3.04-2.87 (m,2H), 2.72-2.47(m,1H), 2.32(d, J =3.4Hz,3H), 1.22-1.05(m,6H); 19 F NMR(376MHz, CDCl 3 )δ -58.02; ESIMS m/z 639 ([M+H] + ).

亦根據實例5中的程序進行(Z)-1-(3-(2-異丙基苯基)-4-氧噻唑亞烷-2-基)-3-(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯乙基)硫脲之製備(Z)-1-(3-(2-isopropylphenyl)-4-oxiazolidin-2-yl)-3-(4-(1-(4- (Trifluoromethoxy) phenyl) -1 H -1,2,4-triazol-3-yl) phenethyl) thiourea

Figure 106137106-A0202-12-0039-26
Figure 106137106-A0202-12-0039-26

分離得到呈黃色油狀之標題化合物(76mg,79%):1H NMR(400MHz,CDCl3)δ 8.56(d,J=2.2Hz,1H),8.11-8.03(m,2H),7.81(dd,J=9.2,2.6Hz,2H),7.53-7.31(m,4H),7.30-7.27(m,1H),7.25(s,1H),7.05-6.86(m,2H),3.97-3.70(m,4H),3.06-2.90(m,2H),2.73-2.59(m,1H),1.30-1.05(m,6H);19F NMR(376MHz,CDCl3)δ -58.03;ESIMS m/z 625([M+H]+)。 The title compound (76 mg, 79%) was isolated as a yellow oil: 1 H NMR (400MHz, CDCl 3 ) δ 8.56 (d, J = 2.2 Hz, 1H), 8.11-8.03 (m, 2H), 7.81 (dd , J =9.2,2.6Hz,2H),7.53-7.31(m,4H),7.30-7.27(m,1H),7.25(s,1H),7.05-6.86(m,2H),3.97-3.70(m ,4H),3.06-2.90(m,2H),2.73-2.59(m,1H),1.30-1.05(m,6H); 19 F NMR(376MHz,CDCl 3 )δ -58.03; ESIMS m/z 625( [M+H] + ).

實例6:3-(4-(1-氟-2-異硫氰酸基乙基)苯基)-1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑之製備Example 6: 3-(4-(1-fluoro-2-isothiocyanatoethyl)phenyl)-1-(4-(trifluoromethoxy)phenyl)-1 H -1,2, Preparation of 4-triazole

Figure 106137106-A0202-12-0039-27
Figure 106137106-A0202-12-0039-27

於室溫下在N2環境中將2-氟-2-(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯基)乙-1-胺鎓鹽酸鹽(500mg,1.24mmol)溶解於THF(3.10mL)中,並加入三乙胺(0.190mL,1.366mmol)。通過注射器分批加入二硫化碳(0.075mL,1.24mmol),並使該反應混合物在室溫下攪拌3小時。將反應瓶置於冰浴中並冷卻到0℃。將甲苯磺醯氯(0.97g,5.09mmol)一次加入,攪拌該反應混合物並使其加溫至室溫過夜。用1N HCl淬滅該反應混合物並以乙醚(3x)萃取。合併之有機層係經水及飽和NaHCO3溶液洗滌,在無水MgSO4上乾燥,並真空濃縮以產出(200mg,38%),且其係未經進一 步純化而使用:1H NMR(400MHz,CDCl3)δ 8.58(s,1H),8.33-8.19(m,2H),7.86-7.75(m,2H),7.53-7.44(m,2H),7.40(dq,J=8.9,1.0Hz,2H),5.70(ddd,J=46.8,6.7,3.9Hz,1H),4.08-3.75(m,2H);19F NMR(376MHz,CDCl3)δ -58.02,-182.46;HRMS-ESI(m/z)[M+H]+ C18H13F4N4OS之計算值,409.0668;實驗值,409.0703。 The 2 -fluoro-2-(4-(1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazole-3- (Yl)phenyl)ethan-1-aminium hydrochloride (500 mg, 1.24 mmol) was dissolved in THF (3.10 mL), and triethylamine (0.190 mL, 1.366 mmol) was added. Carbon disulfide (0.075 mL, 1.24 mmol) was added in batches via a syringe, and the reaction mixture was allowed to stir at room temperature for 3 hours. The reaction flask was placed in an ice bath and cooled to 0°C. Toluenesulfonyl chloride (0.97 g, 5.09 mmol) was added all at once, and the reaction mixture was stirred and allowed to warm to room temperature overnight. The reaction mixture was quenched with 1N HCl and extracted with ether (3x). The combined organic layer was washed with water and saturated NaHCO 3 solution, dried over anhydrous MgSO 4 and concentrated in vacuo to yield (200 mg, 38%), which was used without further purification: 1 H NMR (400MHz, CDCl 3 )δ 8.58(s,1H),8.33-8.19(m,2H),7.86-7.75(m,2H),7.53-7.44(m,2H),7.40(dq, J =8.9,1.0Hz,2H ), 5.70 (ddd, J = 46.8, 6.7, 3.9 Hz, 1H), 4.08-3.75 (m, 2H); 19 F NMR (376MHz, CDCl 3 )δ -58.02, -182.46; HRMS-ESI ( m/z ) [M+H] + C 18 H 13 F 4 N 4 OS calculated value, 409.0668; experimental value, 409.0703.

實例7:(Z)-1-(2-氟-2-(4-(1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑-3-基)苯基)乙基)-3-(3-(2-異丙基-5-甲基苯基)-4-氧噻唑亞烷-2-基)硫脲Example 7: (Z)-1-(2-fluoro-2-(4-(1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-triazole-3- (Yl)phenyl)ethyl)-3-(3-(2-isopropyl-5-methylphenyl)-4-oxthiazolidin-2-yl)thiourea

Figure 106137106-A0202-12-0040-28
Figure 106137106-A0202-12-0040-28

將3-(4-(1-氟-2-異硫氰基乙基)苯基)-1-(4-(三氟甲氧基)苯基)-1H-1,2,4-三唑(85mg,0.208mmol)及2-亞胺基-3-(2-異丙基-5-甲基苯基)噻唑烷-4-酮(51.7mg,0.208mmol)之DMF(0.47mL)混合液在室溫下攪拌2小時,並在110℃下使用Vigreux管柱直至注意到起始材料耗盡。接著將該反應混合物冷卻至室溫並裝填於Celite®濾筒上。通過急速層析法純化而產出呈黃色泡沫狀之標題化合物(62mg,43%):1H NMR(400MHz,CDCl3)δ 8.57(s,1H),8.21(dd,J=8.1,2.4Hz,2H),7.82-7.75(m,2H),7.51-7.44(m,2H),7.40(dd,J=8.7,6.6Hz,3H),6.91-6.83(m,1H),5.85(td,J=9.4,2.7Hz,1H),4.46-4.17(m,1H),3.97-3.83(m,3H),3.80-3.56(m,1H),2.66(dq,J=13.2,6.6Hz,2H),2.36(d,J=5.7Hz,3H),1.21-1.13(m,6H);19F NMR(376 MHz,CDCl3)δ -58.02,-184.83;13C NMR(126MHz,CDCl3)δ 189.81,172.39,169.87,162.90,148.47,143.09,141.62,138.41,136.86,135.49,132.67,131.13,128.46,126.84,125.68,122.43,121.26,33.64,28.37,23.68,20.83;HRMS-ESI(m/z)([M+H]+)C31H29F4N6O2S2之計算值,657.1651;實驗值,657.1719。 Add 3-(4-(1-fluoro-2-isothiocyanoethyl)phenyl)-1-(4-(trifluoromethoxy)phenyl)-1 H -1,2,4-tri Azole (85mg, 0.208mmol) and 2-imino-3-(2-isopropyl-5-methylphenyl)thiazolidine-4-one (51.7mg, 0.208mmol) in DMF (0.47mL) The solution was stirred at room temperature for 2 hours, and a Vigreux column was used at 110°C until the consumption of the starting material was noticed. The reaction mixture was then cooled to room temperature and loaded on Celite ® cartridge. Purified by flash chromatography, the title compound (62 mg, 43%) was produced as a yellow foam: 1 H NMR (400MHz, CDCl 3 ) δ 8.57 (s, 1H), 8.21 (dd, J = 8.1, 2.4 Hz) ,2H),7.82-7.75(m,2H),7.51-7.44(m,2H),7.40(dd, J =8.7,6.6Hz,3H),6.91-6.83(m,1H),5.85(td, J =9.4,2.7Hz,1H),4.46-4.17(m,1H),3.97-3.83(m,3H),3.80-3.56(m,1H),2.66(dq, J =13.2,6.6Hz,2H), 2.36(d, J =5.7Hz,3H),1.21-1.13(m,6H); 19 F NMR(376 MHz,CDCl 3 )δ -58.02,-184.83; 13 C NMR(126MHz,CDCl 3 )δ 189.81, 172.39,169.87,162.90,148.47,143.09,141.62,138.41,136.86,135.49,132.67,131.13,128.46,126.84,125.68,122.43,121.26,33.64,28.37,23.68,20.83; HRMS-ESI( m/z )([ M+H] + )C 31 H 29 F 4 N 6 O 2 S 2 calculated value, 657.1651; experimental value, 657.1719.

使用本文所揭露之程序時下列分子清單係可做為實例(表1)。 The following list of molecules can be used as an example when using the procedures disclosed in this article (Table 1).

Figure 106137106-A0202-12-0041-29
Figure 106137106-A0202-12-0041-29
Figure 106137106-A0202-12-0042-30
Figure 106137106-A0202-12-0042-30
Figure 106137106-A0202-12-0043-31
Figure 106137106-A0202-12-0043-31
Figure 106137106-A0202-12-0044-32
Figure 106137106-A0202-12-0044-32
Figure 106137106-A0202-12-0045-33
Figure 106137106-A0202-12-0045-33
Figure 106137106-A0202-12-0046-34
Figure 106137106-A0202-12-0046-34
Figure 106137106-A0202-12-0047-35
Figure 106137106-A0202-12-0047-35
Figure 106137106-A0202-12-0048-36
Figure 106137106-A0202-12-0048-36
Figure 106137106-A0202-12-0049-37
Figure 106137106-A0202-12-0049-37
Figure 106137106-A0202-12-0050-38
Figure 106137106-A0202-12-0050-38
Figure 106137106-A0202-12-0051-39
Figure 106137106-A0202-12-0051-39
Figure 106137106-A0202-12-0052-40
Figure 106137106-A0202-12-0052-40
Figure 106137106-A0202-12-0053-41
Figure 106137106-A0202-12-0053-41
Figure 106137106-A0202-12-0054-42
Figure 106137106-A0202-12-0054-42
Figure 106137106-A0202-12-0055-43
Figure 106137106-A0202-12-0055-43
Figure 106137106-A0202-12-0056-44
Figure 106137106-A0202-12-0056-44
Figure 106137106-A0202-12-0057-45
Figure 106137106-A0202-12-0057-45
Figure 106137106-A0202-12-0058-46
Figure 106137106-A0202-12-0058-46
Figure 106137106-A0202-12-0059-47
Figure 106137106-A0202-12-0059-47
Figure 106137106-A0202-12-0060-48
Figure 106137106-A0202-12-0060-48
Figure 106137106-A0202-12-0061-49
Figure 106137106-A0202-12-0061-49
Figure 106137106-A0202-12-0062-50
Figure 106137106-A0202-12-0062-50
Figure 106137106-A0202-12-0063-51
Figure 106137106-A0202-12-0063-51
Figure 106137106-A0202-12-0064-52
Figure 106137106-A0202-12-0064-52
Figure 106137106-A0202-12-0065-53
Figure 106137106-A0202-12-0065-53
Figure 106137106-A0202-12-0066-54
Figure 106137106-A0202-12-0066-54
Figure 106137106-A0202-12-0067-55
Figure 106137106-A0202-12-0067-55
Figure 106137106-A0202-12-0068-56
Figure 106137106-A0202-12-0068-56
Figure 106137106-A0202-12-0069-57
Figure 106137106-A0202-12-0069-57
Figure 106137106-A0202-12-0070-58
Figure 106137106-A0202-12-0070-58
Figure 106137106-A0202-12-0071-59
Figure 106137106-A0202-12-0071-59

使用本文所揭露之程序時下列分子清單亦可做為實例(表2)。 The following list of molecules can also be used as examples when using the procedures disclosed in this article (Table 2).

Figure 106137106-A0202-12-0071-60
Figure 106137106-A0202-12-0071-60
Figure 106137106-A0202-12-0072-61
Figure 106137106-A0202-12-0072-61
Figure 106137106-A0202-12-0073-62
Figure 106137106-A0202-12-0073-62
Figure 106137106-A0202-12-0074-63
Figure 106137106-A0202-12-0074-63

實例A:對於甜菜夜蛾(Spodoptera exigua)(“BAW”)及粉紋夜蛾(Trichoplusia ni)(“CL”)之生物分析Example A: Biological analysis of Spodoptera exigua ("BAW") and Trichoplusia ni ("CL")

甜菜夜蛾具有極少有效寄生蟲、疾病或捕食者以降低其種 群。BAW侵染許多野草、樹、草、豆科植物及農作物。在不同地點,蘆筍、棉花、玉米、大豆、菸草、苜蓿、糖用甜菜、胡椒、蕃茄、馬鈴薯、洋蔥、豌豆、向日葵及柑橘在其他植物當中具有重要經濟意義。粉紋夜蛾為夜蛾科之一員。其被發現遍及整個世界。粉紋夜蛾會侵襲甘藍菜、花椰菜、椰菜、抱子甘藍(Brussel sprout)、蕃茄、黃瓜、馬鈴薯、芥藍、蕪箐、芥菜、胡椒、茄子、西瓜、甜瓜、西葫蘆、哈密瓜、豌豆、豆、羽衣甘藍、萵苣、菠菜、芹菜、香芹、甜菜、豌豆、苜蓿、大豆及棉花。此物種由於其貪婪的食用葉子而對植物極具破壞性。然而,就甘藍菜而言,其不僅以外包葉為食,而且可鑽入生長的頭部。幼蟲每日食用其三倍重量之植物體。攝食部位因大量堆積黏性、濕潤的排泄物而顯著。 Beet armyworm has very few effective parasites, diseases or predators to reduce its population. BAW infects many weeds, trees, grasses, legumes and crops. In different locations, asparagus, cotton, corn, soybeans, tobacco, alfalfa, sugar beets, peppers, tomatoes, potatoes, onions, peas, sunflowers and citrus have important economic significance among other plants. Pyrus noctuidae is a member of the Noctuidae. It was found all over the world. The pink moth can invade cabbage, cauliflower, broccoli, Brussels sprout, tomato, cucumber, potato, kale, turnip, mustard, pepper, eggplant, watermelon, melon, zucchini, cantaloupe, peas, Beans, kale, lettuce, spinach, celery, parsley, beets, peas, alfalfa, soybeans and cotton. This species is extremely destructive to plants due to its voracious eating of leaves. However, in the case of cabbage, it not only feeds on outer leaves, but also penetrates into the growing head. The larvae eat three times their weight of the plant body daily. The feeding site is marked by a large accumulation of viscous, moist excrement.

因此,由於以上因素,防治此等害蟲為重要的。此外,防治此等稱為咀嚼害蟲之害蟲(BAW及CL)的分子適用於防治在植物上咀嚼之其他害蟲。 Therefore, due to the above factors, it is important to control these pests. In addition, molecules that control these pests called chewing pests (BAW and CL) are suitable for controlling other pests that chew on plants.

使用以下實例中所述之程序針對BAW及CL測試此文件中所揭示之某些分子。在報導結果時,使用「BAW & CL評級表」(參見表格部分)。 Some of the molecules disclosed in this document were tested against BAW and CL using the procedures described in the following examples. When reporting the results, use the " BAW & CL Rating Form" (see the table section).

對於BAW之生物分析Bioanalysis for BAW

使用128孔飼料盤分析進行對於BAW之生物分析。將一至五個第二齡期BAW幼蟲置於先前已填充有1mL人工飼料之飼料盤的各孔(3mL)中,該飼料盤已施用(八個孔中之每一者)50μg/cm2測試化合物(溶解於50μL的90:10丙酮-水混合物中)且隨後使其乾燥。飼料盤用透明的自黏罩覆蓋且保持在25℃、14:10光-暗環境下五至七天。記錄各孔幼蟲之死亡率百分比;接著平均八個孔之活性。結果係於標題為「表格ABC:生物結果」之表格中標出(參見表格部分)。 A 128-well feed pan analysis was used for the biological analysis of BAW. Place one to five second-instar BAW larvae in each hole (3mL) of a feed tray previously filled with 1 mL of artificial feed. The feed tray has been applied (each of the eight holes) 50μg/cm 2 for testing The compound (dissolved in 50 μL of a 90:10 acetone-water mixture) and then allowed to dry. The feed pan is covered with a transparent self-adhesive cover and kept at 25°C and 14:10 light-dark environment for five to seven days. Record the mortality percentage of larvae in each hole; then average the activity of eight holes. The results are indicated in the table titled "Form ABC: Biological Results" (see the table section).

對於CL之生物分析Bioanalysis for CL

使用128孔飼料盤分析進行對於CL之生物分析。將一至五個第二齡期CL幼蟲置於先前已填充有1mL人工飼料之飼料盤的各孔(3mL)中,該飼料盤已施用(八個孔中之每一者)50μg/cm2測試化合物(溶解於50μL的90:10丙酮-水混合物中)且隨後使其乾燥。飼料盤用透明的自黏罩覆蓋且保持在25℃、14:10光-暗環境下五至七天。記錄各孔幼蟲之死亡率百分比;接著平均八個孔之活性。結果係於標題為「表格ABC:生物結果」之表格中標出(參見表格部分)。 The biological analysis of CL was performed using 128-well feed pan analysis. Place one to five second-instar CL larvae in each hole (3mL) of a feed tray previously filled with 1 mL of artificial feed. The feed tray has been applied (each of the eight holes) 50μg/cm 2 for testing The compound (dissolved in 50 μL of a 90:10 acetone-water mixture) and then allowed to dry. The feed pan is covered with a transparent self-adhesive cover and kept at 25°C and 14:10 light-dark environment for five to seven days. Record the mortality percentage of larvae in each hole; then average the activity of eight holes. The results are indicated in the table titled "Form ABC: Biological Results" (see the table section).

實例B:對於桃蚜(“GPA”)(Myzus persicae)之生物分析。Example B: Biological analysis of green peach aphid ("GPA") ( Myzus persicae).

GPA為最顯著的桃樹蚜蟲,導致生長減慢、葉子枯萎及多個組織死亡。其亦為有危害的,因為其充當病媒,將植物病毒諸如馬鈴薯Y病毒及馬鈴薯卷葉病毒傳播至茄科(Solanaceae)成員及將多種花葉病毒傳播至許多其他糧食作物。在其他植物當中,GPA侵襲以下植物,諸如椰菜、牛蒡、甘藍菜、胡蘿蔔、花椰菜、蘿蔔、茄子、綠豆、萵苣、澳洲胡桃、番木瓜、胡椒、甘薯、蕃茄、豆瓣菜及筍瓜。GPA亦侵襲許多觀賞作物,諸如康乃馨、菊花、開花白球甘藍、一品紅及玫瑰。GPA已產生對許多殺蟲劑之抗性。因此,由於以上因素,防治此害蟲為重要的。此外,防治此稱為刺吸害蟲之害蟲(GPA)的分子適用於防治在植物上刺吸之其他害蟲。 GPA is the most significant species of peach aphids, causing slower growth, leaf wilting, and the death of multiple tissues. It is also harmful because it acts as a vector, spreading plant viruses such as potato Y virus and potato leaf roll virus to members of the Solanaceae family (Solanaceae ) and various mosaic viruses to many other food crops. Among other plants, GPA attacks the following plants, such as broccoli, burdock, cabbage, carrot, cauliflower, radish, eggplant, mung bean, lettuce, macadamia, papaya, pepper, sweet potato, tomato, watercress and winter squash. GPA also affects many ornamental crops, such as carnations, chrysanthemums, flowering white cabbage, poinsettia and roses. GPA has developed resistance to many insecticides. Therefore, due to the above factors, it is important to control this pest. In addition, the molecules known as piercing-sucking pests (GPA) are suitable for controlling other pests that pierce and suck on plants.

使用以下實例中所述之程序針對GPA測試此文件中所揭示之某些分子。在報導結果時,使用「GPA評級表」(參見表格部分)。 The procedures described in the following examples were used to test certain molecules disclosed in this document against GPA. When reporting the results, use the "GPA Rating Form" (see the table section).

使用在3吋盆中生長、具有2-3個小(3-5cm)真葉的甘藍菜苗作為測試基質。幼苗在化學施用之前一天經20-50個GPA(無翅成蟲及若蟲期)侵染。每一處理使用四盆單獨幼苗。將測試化合物(2mg)溶解於2mL丙酮/甲醇(1:1)溶劑中,形成1000ppm測試化合物之儲備溶液。儲備溶液用 0.025% Tween 20水溶液稀釋5倍以獲得200ppm測試化合物溶液。手持式抽氣型噴霧器用於將溶液噴霧至甘藍菜葉子兩側直至流走為止。參考植物(溶劑檢查)用僅含有20體積%丙酮/甲醇(1:1)溶劑之稀釋劑噴霧。經處理之植物在分級之前在大致25℃及環境相對濕度(RH)下之保存室中保存三天。藉由在顯微鏡下計數每一植物之活蚜蟲的數目進行評估。使用如下阿爾伯特校正公式(Abbott's correction formula)(W.S.Abbott,“A Method of Computing the Effectiveness of an Insecticide”J.Econ.Entomol.18(1925),pp.265-267)量測防治百分比。 A cabbage seedling grown in a 3-inch pot with 2-3 small (3-5 cm) true leaves was used as the test substrate. The seedlings were infested with 20-50 GPA (wingless adult and nymph stage) a day before chemical application. Four pots of individual seedlings were used for each treatment. The test compound (2 mg) was dissolved in 2 mL of acetone/methanol (1:1) solvent to form a 1000 ppm test compound stock solution. The stock solution was diluted 5 times with a 0.025% Tween 20 aqueous solution to obtain a 200 ppm test compound solution. The hand-held suction sprayer is used to spray the solution on both sides of the cabbage leaves until it runs away. The reference plant (solvent check) is sprayed with a thinner containing only 20% by volume of acetone/methanol (1:1) solvent. The treated plants were stored in a storage room at approximately 25°C and ambient relative humidity (RH) for three days before being classified. It is evaluated by counting the number of live aphids per plant under a microscope. The following Abbott's correction formula (W.S. Abbott, "A Method of Computing the Effectiveness of an Insecticide" J. Econ. Entomol. 18 (1925), pp. 265-267) was used to measure the control percentage.

經校正之防治%=100 *(X-Y)/XCorrected control %=100 *(X-Y)/X

其中X=溶劑檢查植物上活蚜蟲的數目及Y=經處理之植物上活蚜蟲的數目結果係於標題為「表格ABC:生物結果」之表格中標出(參見表格部分)。 Where X = the number of live aphids on the solvent-checked plant and Y = the number of live aphids on the treated plant. The results are indicated in the table titled "Form ABC: Biological Results" (see the table section).

實例C:對於黃熱病蚊“YFM”(埃及斑蚊(Aedes aegypti))。Example C: For yellow fever mosquito "YFM" ( Aedes aegypti ).

YFM更喜歡在日間以人類血液為食且在人類住所或靠近人類住所最常見。YFM為傳播數種疾病之病媒。其為可散佈登革熱及黃熱病病毒的蚊子。黃熱病為瘧疾之後第二危險的蚊媒疾病。黃熱病為急性病毒出血性疾病且高達50%之嚴重患病人員在未治療的情況下將死於黃熱病。據估計,全世界每年有200,000例黃熱病,導致30,000例死亡。登革熱為兇險的病毒疾病;其由於可產生劇烈疼痛而有時稱為「斷骨熱」或「碎心熱」。登革熱每年殺死約20,000人。因此,由於以上因素,防治此害蟲為重要的。此外,防治此稱為刺吸害蟲之害蟲(YFM)的分子適用於防治造成人類及動物患病之其他害蟲。 YFM prefers to feed on human blood during the day and is most common in human dwellings or close to human dwellings. YFM is a vector that spreads several diseases. It is a mosquito that can spread dengue and yellow fever viruses. Yellow fever is the second most dangerous mosquito-borne disease after malaria. Yellow fever is an acute viral hemorrhagic disease and up to 50% of severely ill people will die of yellow fever without treatment. It is estimated that there are 200,000 cases of yellow fever worldwide each year, resulting in 30,000 deaths. Dengue fever is a dangerous viral disease; it is sometimes called "Bone Broken Fever" or "Broken Heart Fever" because it can cause severe pain. Dengue fever kills about 20,000 people every year. Therefore, due to the above factors, it is important to control this pest. In addition, the molecules known as piercing insect pests (YFM) are suitable for controlling other pests that cause diseases in humans and animals.

使用以下段落中所述之程序針對YFM測試此文件中所揭示之某些分子。在報導結果時,使用「YFM評級表」(參見表格部分)。 Use the procedure described in the following paragraphs to test certain molecules disclosed in this document against YFM. When reporting the results, use the "YFM Rating Form " (see the table section).

使用含有溶解於100μL二甲亞碸(DMSO)中之400μg分子(相當於4000ppm溶液)之母盤。母盤每孔含有15μL組合分子。向此板之各孔中添加135μL的90:10水:丙酮混合物。機器人(Biomek® NXP實驗室自動化工作站)經程式化以自母盤抽吸15μL施配至空96孔淺板(「子」板)中。每一母盤形成6個代表(「子」盤)。所形成之子盤緊接著用YFM幼蟲侵染。 Use a master disc containing 400 μg molecules (equivalent to 4000 ppm solution) dissolved in 100 μL dimethylsulfoxide (DMSO). Each well of the master disc contains 15 μL of combined molecules. Add 135 μL of 90:10 water:acetone mixture to each well of this plate. The robot (Biomek® NXP laboratory automation workstation) is programmed to aspirate 15 μL from the master disk and dispense into an empty 96-well shallow plate ("daughter" plate). Each master disk forms 6 representatives ("daughter" disks). The resulting daughter disc is then infested with YFM larvae.

在欲處理板之前一天,將蚊子卵置於含有肝臟粉末之Millipore水中以開始孵化(4g於400mL中)。在使用機器人形成子盤後,將子盤用220μL肝臟粉末/蚊子幼蟲(約1日齡幼蟲)混合物侵染。在板用蚊子幼蟲侵染後,使用非蒸發蓋覆蓋板以減弱乾燥。在分級之前,將板保存在室溫下3天。3天後,觀察各孔且基於死亡率評分。 One day before the plate was to be treated, the mosquito eggs were placed in Millipore water containing liver powder to start hatching (4 g in 400 mL). After forming the sub-disc using a robot, the sub-disc was infested with 220 μL of liver powder/mosquito larvae (approximately 1 day old larvae) mixture. After the plate is infested with mosquito larvae, cover the plate with a non-evaporative cover to reduce drying. Before grading, the plates were stored at room temperature for 3 days. After 3 days, each well was observed and scored based on mortality.

農業上可接受之酸加成鹽、鹽衍生物、溶劑合物、酯衍生物、多晶型物、同位素及放射性核素Agriculturally acceptable acid addition salts, salt derivatives, solvates, ester derivatives, polymorphs, isotopes and radionuclides

式1及/或式2之分子可調配成農業上可接受之酸加成鹽。藉助於非限制性實例,胺官能基可與鹽酸、氫溴酸、硫酸、磷酸、乙酸、苯甲酸、檸檬酸、丙二酸、柳酸、蘋果酸、反丁烯二酸、乙二酸、丁二酸、酒石酸、乳酸、葡萄糖酸、抗壞血酸、順丁烯二酸、天冬胺酸、苯磺酸、甲磺酸、乙磺酸、羥基-甲磺酸及羥基乙磺酸形成鹽。此外,藉助於非限制性實例,酸官能基可形成鹽,包括由鹼金屬或鹼土金屬衍生之鹽及由氨及胺衍生之鹽。較佳陽離子之實例包括鈉、鉀及鎂。 The molecules of Formula 1 and/or Formula 2 can be formulated into agriculturally acceptable acid addition salts. By way of non-limiting examples, amine functional groups can be combined with hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, acetic acid, benzoic acid, citric acid, malonic acid, salicylic acid, malic acid, fumaric acid, oxalic acid, Succinic acid, tartaric acid, lactic acid, gluconic acid, ascorbic acid, maleic acid, aspartic acid, benzenesulfonic acid, methanesulfonic acid, ethanesulfonic acid, hydroxy-methanesulfonic acid and isethionic acid form salts. In addition, by way of non-limiting examples, acid functional groups can form salts, including salts derived from alkali metals or alkaline earth metals and salts derived from ammonia and amines. Examples of preferred cations include sodium, potassium and magnesium.

式1及/或式2之分子可調配成鹽衍生物。藉助於非限制性實例,鹽衍生物可藉由使游離鹼與足以產生鹽之量的所需酸接觸來製備。 游離鹼可藉由用適合之稀鹼水溶液(諸如稀氫氧化鈉、碳酸鉀、氨及碳酸氫鈉水溶液)處理鹽來再生。作為一個實例,在許多情況下,殺蟲劑(諸如2,4-D)藉由將其轉化成其二甲胺鹽而更可溶於水。 The molecules of Formula 1 and/or Formula 2 can be formulated into salt derivatives. By way of non-limiting example, salt derivatives can be prepared by contacting the free base with the desired acid in an amount sufficient to produce the salt. The free base can be regenerated by treating the salt with a suitable dilute aqueous alkali solution, such as dilute sodium hydroxide, potassium carbonate, ammonia, and sodium bicarbonate aqueous solutions. As an example, in many cases, pesticides (such as 2,4-D) are more soluble in water by converting them into their dimethylamine salt.

式1及/或式2之分子可與溶劑一起調配成穩定複合物,使得複合物在非複合溶劑去除之後保持完整。此等複合物常常稱為「溶劑合物」。然而,使用水作為溶劑形成穩定水合物尤其合乎需要。 The molecules of Formula 1 and/or Formula 2 can be formulated with a solvent to form a stable complex, so that the complex remains intact after the non-complex solvent is removed. These complexes are often referred to as "solvates." However, it is especially desirable to use water as a solvent to form stable hydrates.

式1及/或式2之分子可製成酯衍生物。此等酯衍生物可接著以與施用此文件中所揭示之分子相同的方式施用。 The molecules of Formula 1 and/or Formula 2 can be made into ester derivatives. These ester derivatives can then be administered in the same manner as the molecules disclosed in this document.

式1及/或式2之分子可製成為多種晶體多晶型物。多晶型現象在農用化學品開發中為重要的,因為相同分子之不同晶體多晶型物或結構可具有大大不同的物理特性及生物效能。 The molecules of Formula 1 and/or Formula 2 can be made into a variety of crystal polymorphs. Polymorphism is important in the development of agrochemicals because different crystal polymorphs or structures of the same molecule can have greatly different physical properties and biological effects.

式1及/或式2之分子可用不同同位素製成。具有2H(亦稱為氘)代替1H之分子具有特別重要性。 The molecules of Formula 1 and/or Formula 2 can be made of different isotopes. Molecules with 2 H (also called deuterium) instead of 1 H are of particular importance.

式1及/或式2之分子可用不同放射性核素製成。具有14C之分子具有特別重要性。 The molecules of Formula 1 and/or Formula 2 can be made of different radionuclides. Molecules with 14 C are of special importance.

立體異構物Stereoisomers

式1及/或式2之分子可能存在一或多種立體異構物。因此,特定的分子可以外消旋混合物形式產生。熟習此項技術者應瞭解,一種立體異構體可比其他立體異構體更具活性。個別立體異構體可藉由已知選擇性合成程序、藉由習知合成程序使用解析之起始物質、或藉由習知解析程序來獲得。本文中所揭示之特定分子可以兩種或兩種以上異構體形式存在。所述之各種異構物包含幾何異構物、非鏡像異構物及鏡像異構物。因此,本文中所揭示之分子包括幾何異構體、外消旋混合物、個別立體異構體及光學活性混合物。熟習此項技術者應瞭解,一種異構體可比其他異構體更 具活性。本發明中所揭示之結構出於明晰之目的僅以一種幾何形式繪製,但意欲表示該分子之所有幾何形式。 The molecules of Formula 1 and/or Formula 2 may have one or more stereoisomers. Therefore, specific molecules can be produced as a racemic mixture. Those familiar with this technique should understand that one stereoisomer can be more active than other stereoisomers. Individual stereoisomers can be obtained by known selective synthesis procedures, by conventional synthesis procedures using analytical starting materials, or by conventional analytical procedures. The specific molecules disclosed herein can exist in two or more isomer forms. The various isomers include geometric isomers, diastereomers and enantiomers. Therefore, the molecules disclosed herein include geometric isomers, racemic mixtures, individual stereoisomers and optically active mixtures. Those familiar with this technique should understand that one isomer can be more active than the other isomers. The structure disclosed in the present invention is drawn in only one geometric form for the purpose of clarity, but it is intended to represent all geometric forms of the molecule.

組合combination

於另一實施例中,式1及/或式2之分子可與一或多種各具有與式1及/或式2之分子的作用模式(「MoA」)相同、類似或不同的作用模式的化合物組合使用(諸如以組分混合物形式、或同時或依序施用)。作用模式包括例如以下:乙醯膽鹼酯酶(AChE)抑制劑;GABA閘控氯離子通道拮抗劑;鈉通道調節劑;菸鹼性乙醯膽鹼(nAChR)促效劑;菸鹼性乙醯膽鹼受體(nAChR)異位活化劑;氯離子通道活化劑;保幼激素模擬物;雜項非特異性(多位點)抑制劑;選擇性同翅目攝食阻斷劑;蟎生長抑制劑;昆蟲中腸膜之微生物瓦解劑;粒線體ATP合成酶之抑制劑;經由破壞質子梯度之氧化磷酸化的去偶合劑;菸鹼性乙醯膽鹼受體(nAChR)通道阻斷劑;0型幾丁質生物合成之抑制劑;1型幾丁質生物合成之抑制劑;雙翅目蛻皮干擾劑;蛻皮激素受體促效劑;章魚胺受體促效劑;粒線體複合物III電子傳輸抑制劑;粒線體複合物I電子傳輸抑制劑;電壓依賴性鈉通道阻斷劑;乙醯CoA羧化酶之抑制劑;粒線體複合物IV電子傳輸抑制劑;粒線體複合物II電子傳輸抑制劑;以及蘭尼鹼(Ryanodine)受體調節劑。 In another embodiment, the molecule of Formula 1 and/or Formula 2 can be combined with one or more of the same, similar or different mode of action ("MoA") of the molecule of Formula 1 and/or Formula 2 The compounds are used in combination (such as in the form of a mixture of components, or simultaneous or sequential application). Modes of action include, for example, the following: acetylcholinesterase (AChE) inhibitors; GABA gated chloride channel antagonists; sodium channel modulators; nicotinic acetylcholine (nAChR) agonists; nicotinic beta Ectopic activator of cholinergic receptor (nAChR); chloride channel activator; juvenile hormone mimics; miscellaneous non-specific (multi-site) inhibitors; selective homopteran feeding blockers; mite growth inhibition Agent; Microbial disintegrant of insect midgut membrane; Inhibitor of mitochondrial ATP synthase; Decoupler via oxidative phosphorylation that disrupts proton gradient; Nicotine acetylcholine receptor (nAChR) channel blocker ; Inhibitor of type 0 chitin biosynthesis; Inhibitor of type 1 chitin biosynthesis; Diptera ecdysis interfering agent; Ecdysone receptor agonist; Octopamine receptor agonist; Mitochondrial complex Compound III electron transport inhibitor; Mitochondrial complex I electron transport inhibitor; Voltage-dependent sodium channel blocker; Inhibitor of acetyl CoA carboxylase; Mitochondrial complex IV electron transport inhibitor; Mitochondria Complex II electron transport inhibitor; and Ryanodine receptor modulator.

於另一實施例中,式1及/或式2之分子可與一或多種具有殺蟎、殺藻、殺鳥、殺細菌、殺真菌、除草、殺昆蟲、殺軟體動物、殺線蟲、殺鼠及/或殺病毒特性之化合物組合使用(諸如以組分混合物形式、或同時或依序施用)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be combined with one or more of acaricides, algaecides, birds, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, and Compounds with murine and/or virucidal properties are used in combination (such as in the form of a mixture of components, or simultaneously or sequentially).

式1及/或式2之分子可一或多種化合物組合使用(諸如以組分混合物形式、或同時或依序施用),該等化合物為拒食劑、避鳥劑、化學不育劑、除草劑安全劑、昆蟲引誘劑、防蟲劑、哺乳動物驅避劑、交配 干擾劑、植物活化劑、植物生長調節劑及/或增效劑。 The molecules of Formula 1 and/or Formula 2 can be used in combination with one or more compounds (such as in the form of a mixture of components, or applied simultaneously or sequentially), and these compounds are antifeedants, bird avoidants, chemical sterilization agents, and herbicides Safeners, insect attractants, insect repellents, mammalian repellents, mating interfering agents, plant activators, plant growth regulators and/or synergists.

於另一實施例中,式1及/或式2之分子可與以下化合物中之一或多者組合使用(諸如以組分混合物形式、或同時或依序施用):(3-乙氧基丙基)溴化汞、1,2-二氯丙烷、1,3-二氯丙烯、1-甲基環丙稀、1-萘酚、2-(辛基硫基)乙醇、2,3,5-三-碘苯甲酸、2,3,6-TBA、2,3,6-TBA-二甲基銨、2,3,6-TBA-鋰、2,3,6-TBA-鉀、2,3,6-TBA-鈉、2,4,5-T、2,4,5-T-2-丁氧基丙酯、2,4,5-T-2-乙基己酯、2,4,5-T-3-丁氧基丙酯、2,4,5-TB、2,4,5-T-丁氧甲酯、2,4,5-T-丁氧乙酯、2,4,5-T-丁酯、2,4,5-T-異丁酯、2,4,5-T-異辛酯、2,4,5-T-異丙酯、2,4,5-T-甲酯、2,4,5-T-戊酯、2,4,5-T-鈉、2,4,5-T-三乙銨、2,4,5-T-三乙醇胺、2,4-D、2,4-D-2-丁氧基丙酯、2,4-D-2-乙基己酯、2,4-D-3-丁氧基丙酯、2,4-D-銨、2,4-DB、2,4-DB-丁酯、2,4-DB-二甲基銨、2,4-DB-異辛酯、2,4-DB-鉀、2,4-DB-鈉、2,4-D-丁氧乙酯、2,4-D-丁酯、2,4-D-二乙基銨、2,4-D-二甲基銨、2,4-D-二乙醇胺、2,4-D-十二烷基銨、2,4-DEB、2,4-DEP、2,4-D-乙酯、2,4-D-庚基銨、2,4-D-異丁酯、2,4-D-異辛酯、2,4-D-異丙酯、2,4-D-異丙基銨、2,4-D-鋰、2,4-D-甲基庚酯、2,4-D-甲酯、2,4-D-辛酯、2,4-D-戊酯、2,4-D-鉀、2,4-D-丙酯、2,4-D-鈉、2,4-D-四氫糠基酯、2,4-D-十四烷基銨、2,4-D-三乙銨、2,4-D-參(2-羥基丙基)銨、2,4-D-三乙醇胺、2iP、2-甲氧基乙基氯化汞、2-苯基苯酚、3,4-DA、3,4-DB、3,4-DP、4-胺基吡啶、4-CPA、4-CPA-二乙醇胺、4-CPA-鉀、4-CPA-鈉、4-CPB、4-CPP、4-羥基苯乙醇、8-羥基喹啉硫酸酯、8-苯基汞氧基喹啉、阿巴汀(abamectin)、脫落酸(abscisic acid)、ACC、歐殺松(acephate)、亞醌蟎(acequinocyl)、啶蟲脒(acetamiprid)、家蠅磷(acethion)、乙草胺(acetochlor)、乙酯磷(acetophos)、乙醯蟲腈(acetoprole)、阿拉酸式苯(acibenzolar)、阿拉酸式苯-S-甲酯、三氟羧草醚(acifluorfen)、三氟羧草醚-甲酯、三氟羧草醚-鈉、苯草醚(aclonifen)、 阿萊普(acrep)、阿納寧(acrinathrin)、丙烯醛(acrolein)、丙烯腈(acrylonitrile)、阿普泰克(acypetacs)、阿普泰克-銅、阿普泰克-鋅、阿非度吡平(afidopyropen)、甲草胺(alachlor)、棉靈威(alanycarb)、阿苯達唑(albendazole)、得滅克(aldicarb)、阿迪嗎啉(aldimorph)、涕滅碸威(aldoxycarb)、艾氏劑(aldrin)、丙烯除蟲菊酯(allethrin)、蒜素(allicin)、草毒死(allidochlor)、阿洛氨菌素(allosamidin)、禾草滅(alloxydim)、禾草滅-鈉、烯丙醇、除害威(allyxycarb)、五氯戊酮酸(alorac)、α-賽滅寧(alpha-cypermethrin)、α-安殺番(alpha-endosulfan)、辛唑嘧菌胺(ametoctradin)、特津酮(ametridione)、莠滅淨(ametryn)、胺嗪草酮(amibuzin)、胺唑草酮(amicarbazone)、拌種靈(amicarthiazol)、賽果(amidithion)、安米氟美(amidoflumet)、醯嘧磺隆(amidosulfuron)、滅害威(aminocarb)、環丙嘧啶酸(aminocyclopyrachlor)、環丙嘧啶酸-甲酯、環丙嘧啶酸-鉀、氯胺吡啶酸(aminopyralid)、氯胺吡啶酸-鉀、氯胺吡啶酸-參(2-羥基丙基)銨、胺草磷-甲酯(amiprofos-methyl)、胺草磷(amiprophos)、安美速(amisulbrom)、胺吸磷(amiton)、胺吸磷乙二酸酯、三亞蟎(amitraz)、殺草強(amitrole)、胺基磺酸銨、α-萘乙酸銨、代森銨(amobam)、氨丙膦酸(ampropylfos)、毒藜鹼(anabasine)、毒藜鹼硫酸酯、嘧啶醇(ancymidol)、敵菌靈(anilazine)、莎稗磷(anilofos)、疏草隆(anisuron)、蒽醌、安妥(antu)、唑磷嗪(apholate)、殺蟎特(aramite)、三氧化二砷、福美胂(asomate)、阿司匹林(aspirin)、黃草靈(asulam)、黃草靈-鉀、黃草靈-鈉、乙基殺撲磷(athidathion)、阿特拉通(atraton)、莠去津(atrazine)、金色制酶素(aureofungin)、艾維激素(aviglycine)、艾維激素鹽酸鹽、氧環唑(azaconazole)、印楝素(azadirachtin)、草芬定(azafenidin)、亞滅松(azamethiphos)、四唑嘧磺隆(azimsulfuron)、穀速松-乙酯(azinphos-ethyl)、穀速松-甲酯、疊氮淨(aziprotryne)、氧化福美雙(azithiram)、偶氮苯、三唑錫(azocyclotin)、偶氮磷(azothoate)、亞托敏(azoxystrobin)、菊乙胺酯 (bachmedesh)、燕麥靈(barban)、六氟矽酸鋇、聚硫化鋇、熏菊酯(barthrin)、BCPC、氟丁醯草胺(beflubutamid)、本達樂(benalaxyl)、本達樂-M、草除靈(benazolin)、草除靈-二甲基銨、草除靈-乙酯、草除靈-鉀、苯卡巴腙(bencarbazone)、苯氯噻(benclothiaz)、惡蟲威(bendiocarb)、氟草胺(benfluralin)、免扶克(benfuracarb)、呋草磺(benfuresate)、麥鏽靈(benodanil)、免賴得(benomyl)、解草酮(benoxacor)、苯噁磷(benoxafos)、敵菌腙(benquinox)、苄嘧磺隆(bensulfuron)、苄嘧磺隆-甲酯、地散磷(bensulide)、殺蟲磺(bensultap)、苯它隆(bentaluron)、滅草松(bentazone)、滅草松-鈉、苯噻菌胺(benthiavalicarb)、苯噻菌胺-異丙酯、苯噻菌清(benthiazole)、苯草滅(bentranil)、胺酸殺(benzadox)、胺酸殺-銨、苯紮氯銨(benzalkonium chloride)、苄烯酸(benzamacril)、苄烯酸-異丁酯、抑菌啉(benzamorf)、雙苯嘧草酮(benzfendizone)、芐草胺(benzipram)、苯并雙環酮(benzobicyclon)、吡草酮(benzofenap)、氟磺胺草(benzofluor)、苯基異羥肟酸(benzohydroxamic acid)、苯丙烯氟菌唑(benzovindiflupyr)、苯蟎特(benzoximate)、新燕靈(benzoylprop)、新燕靈-乙酯、苯噻隆(benzthiazuron)、苯甲酸苯甲酯、苄基腺嘌呤、小蘖鹼(berberine)、氯化小檗鹼、β-賽扶寧(beta-cyfluthrin)、β-賽滅寧(beta-cypermethrin)、苯噻嗪(bethoxazin)、雙環吡喃酮(bicyclopyrone)、畢芬載(bifenazate)、必芬諾(bifenox)、畢芬寧(bifenthrin)、吡氟菌酯(bifujunzhi)、畢拉草(bilanafos)、畢拉草-鈉、百蟎克(binapacryl)、病氰硝(bingqingxiao)、生物丙烯菊酯(bioallethrin)、戊環苄呋菊酯(bioethanomethrin)、生物氯菊酯(biopermethrin)、苄呋菊酯(bioresmethrin)、聯苯、吡殺茲(bisazir)、噻枯唑(bismerthiazol)、雙草醚(bispyribac)、雙草醚-鈉、雙三氟蟲脲(bistrifluron)、比多農(bitertanol)、硫雙二氯酚(bithionol)、必殺吩(bixafen)、殺稻瘟菌素-S(blasticidin-S)、硼砂(borax)、波爾多混合劑(Bordeaux mixture)、硼酸、白 可列(boscalid)、油菜素內酯(brassinolide)、油菜素內酯-乙酯、小蠹性信息素(brevicomin)、溴鼠靈(brodifacoum)、溴滅菊酯(brofenvalerate)、溴氟醯胺(broflanilide)、溴氟菊酯(brofluthrinate)、除草定(bromacil)、除草定-鋰、除草定-鈉、溴敵隆(bromadiolone)、溴鼠胺(bromethalin)、溴苄呋菊酯(bromethrin)、溴苯烯磷(bromfenvinfos)、溴乙醯胺、糠草腈(bromobonil)、溴丁醯草胺(bromobutide)、溴烯殺(bromocyclen)、溴-DDT、殺草全(bromofenoxim)、溴硫磷(bromophos)、溴硫磷-乙酯、溴蟎酯(bromopropylate)、溴菌腈(bromothalonil)、溴苯腈(bromoxynil)、溴苯腈丁酸酯、溴苯腈庚酸酯、溴苯腈辛酸酯、溴苯腈-鉀、溴莠敏(brompyrazon)、糠菌唑(bromuconazole)、溴硝醇(bronopol)、增效特(bucarpolate)、合殺威(bufencarb)、特克草(buminafos)、布瑞莫(bupirimate)、布芬淨(buprofezin)、伯更狄混合液(Burgundy mixture)、白消安(busulfan)、畜蟲威(butacarb)、丁草胺(butachlor)、氟丙嘧草酯(butafenacil)、抑草磷(butamifos)、特嘧硫磷(butathiofos)、丁烯草胺(butenachlor)、苄烯菊酯(butethrin)、特咪唑草(buthidazole)、丁硫啶(buthiobate)、丁噻隆(buthiuron)、丁酮威(butocarboxim)、丁酯磷(butonate)、避蚊酮(butopyronoxyl)、丁酮碸威(butoxycarboxim)、地樂胺(butralin)、丁苯草酮(butroxydim)、炔草隆(buturon)、丁胺、丁草敵(butylate)、二甲次胂酸(cacodylic acid)、硫線磷(cadusafos)、唑草胺(cafenstrole)、砷酸鈣、氯酸鈣、氰胺化鈣、聚硫化鈣、敵敵鈣(calvinphos)、克草胺酯(cambendichlor)、毒殺芬(camphechlor)、樟腦(camphor)、四氯丹(captafol)、蓋普丹(captan)、嗎菌威(carbamorph)、氯滅殺威(carbanolate)、加保利(carbaryl)、卡巴草靈(carbasulam)、貝芬替(carbendazim)、貝芬替苯磺酸酯、貝芬替亞硫酸酯、長殺草(carbetamide)、加保扶(carbofuran)、二硫化碳、四氯化碳、三硫磷(carbophenothion)、丁基加保扶(carbosulfan)、甲草威(carboxazole)、環二混 劑(carboxide)、萎鏽靈(carboxin)、唑草酮(carfentrazone)、唑草酮-乙酯、加普胺(carpropamid)、培丹(cartap)、培丹鹽酸鹽、香芹酚(carvacrol)、香芹酮(carvone)、CDEA、葉枯炔(cellocidin)、CEPC、賽拉羅(ceralure)、切欣特混合液(Cheshunt mixture)、蟎離丹(chinomethionat)、聚葡萄胺糖(chitosan)、滅瘟唑(chlobenthiazone)、甲氧除草醚(chlomethoxyfen)、氯醛糖(chloralose)、克爛本(chloramben)、克爛本-銨、克爛本-二乙醇胺、克爛本-甲酯、克爛本-甲基銨、克爛本-鈉、氯胺磷(chloramine phosphorus)、氯黴素(chloramphenicol)、雙胺靈(chloraniformethan)、四氯醌(chloranil)、丁醯草胺(chloranocryl)、氯蟲苯甲醯胺(chlorantraniliprole)、炔禾靈(chlorazifop)、炔禾靈-炔丙酯、可樂津(chlorazine)、氯殺蟎(chlorbenside)、滅幼脲(chlorbenzuron)、冰片丹(chlorbicyclen)、氯溴隆(chlorbromuron)、氯炔靈(chlorbufam)、氯丹(chlordane)、十氯酮(chlordecone)、殺蟲脒(chlordimeform)、殺蟲脒鹽酸鹽、氯烯炔菊酯(chlorempenthrin)、氯氧磷(chlorethoxyfos)、乙氧苯隆(chloreturon)、伐草克(chlorfenac)、伐草克-銨、伐草克-鈉、克凡派(chlorfenapyr)、苯咪唑菌(chlorfenazole)、殺蟎醇(chlorfenethol)、燕麥酯(chlorfenprop)、殺蟎酯(chlorfenson)、敵蟎特(chlorfensulphide)、克芬松(chlorfenvinphos)、克福隆(chlorfluazuron)、氟啼殺(chlorflurazole)、氯甲丹(chlorfluren)、氯甲丹-甲酯、氯茀素(chlorflurenol)、氯茀素-甲酯、氯草敏(chloridazon)、氯嘧磺隆(chlorimuron)、氯嘧磺隆-乙酯、氯甲磷(chlormephos)、克美素(chlormequat)、氯化克美素(chlormequat chloride)、氯乙靈(chlornidine)、草枯醚(chlornitrofen)、乙酯殺蟎醇(chlorobenzilate)、氯二硝萘(chlorodinitronaphthalene)、氯仿、滅蟎眯(chloromebuform)、滅蟲脲(chloromethiuron)、地茂散(chloroneb)、氯敵鼠(chlorophacinone)、氯敵鼠-鈉、氯化苦(chloropicrin)、三氯丙酸(chloropon)、氯丙炔菊酯(chloroprallethrin)、丙酯殺蟎醇(chloropropylate)、四氯異苯腈 (chlorothalonil)、綠麥隆(chlorotoluron)、枯草隆(chloroxuron)、羥敵草腈(chloroxynil)、三丁氯苄膦(chlorphonium)、氯化三丁氯苄膦(chlorphonium chloride)、氯腈肟磷(chlorphoxim)、氯吡唑磷(chlorprazophos)、草敗死(chlorprocarb)、氯苯胺靈(chlorpropham)、陶斯松(chlorpyrifos)、陶斯松-甲酯、四氯喹噁啉(chlorquinox)、氯磺隆(chlorsulfuron)、敵草索(chlorthal)、敵草索-二甲酯、敵草索-單甲酯、草克樂(chlorthiamid)、蟲蟎磷(chlorthiophos)、克氯得(chlozolinate)、氯化膽鹼、環蟲醯肼(chromafenozide)、瓜菊酯I(cinerin I)、瓜菊酯II、瓜菊酯、吲哚酮草酯(cinidon-ethyl)、環庚草醚(cinmethylin)、醚磺隆(cinosulfuron)、氰苯醯胺(ciobutide)、咯草隆(cisanilide)、順式苄呋菊酯(cismethrin)、氯醯草膦(clacyfos)、克草同(clethodim)、甘寶素(climbazole)、碘氯啶酯(cliodinate)、炔草酸(clodinafop)、炔草酸-炔丙酯、地蟲威(cloethocarb)、苯噠嗪酸(clofencet)、苯噠嗪酸-鉀、克芬蟎(clofentezine)、降固醇酸(clofibric acid)、草氯丙酸(clofop)、草氯丙酸-異丁酯、可滅蹤(clomazone)、稗草胺(clomeprop)、坐果安(cloprop)、氯丙氧定(cloproxydim)、畢克草(clopyralid)、畢克草-甲酯、畢克草-乙醇胺、畢克草-鉀、畢克草-參(2-羥基丙基)銨、解毒喹(cloquintocet)、解毒喹-庚酯、氯酯磺草胺(cloransulam)、氯酯磺草胺-甲酯、氯氰碘柳胺(closantel)、噻蟲胺(clothianidin)、克黴唑(clotrimazole)、坐果酸(cloxyfonac)、坐果酸-鈉、CMA、科得引誘劑(codlelure)、噻唑硫磷(colophonate)、乙酸銅、乙醯亞砷酸銅、砷酸銅、鹼式碳酸銅、氫氧化銅、環烷酸銅、油酸銅、鹼性氯氧化銅、矽酸銅、硫酸銅、鉻酸銅鋅、氯殺鼠靈(coumachlor)、克鼠靈(coumafuryl)、蠅毒磷(coumaphos)、殺鼠迷(coumatetralyl)、畜蟲磷(coumithoate)、丁香菌酯(coumoxystrobin)、CPMC、CPMF、CPPC、醚草敏(credazine)、甲酚、鼠立死(crimidine)、克羅米通(crotamiton)、巴毒磷(crotoxyphos)、育畜磷(crufomate)、冰晶石(cryolite)、 誘蠅酮(cue-lure)、硫雜靈(cufraneb)、苄草隆(cumyluron)、福美銅氯(cuprobam)、氧化亞銅、莪術醇(curcumenol)、氰胺、氰草淨(cyanatryn)、氰草津(cyanazine)、苯腈磷(cyanofenphos)、殺螟腈(cyanophos)、果蟲磷(cyanthoate)、氰蟲醯胺(cyantraniliprole)、賽座滅(cyazofamid)、灑布淨(cybutryne)、環菌胺(cyclafuramid)、環丙酸醯胺(cyclanilide)、環胺普羅(cyclaniliprole)、環蟲菊酯(cyclethrin)、環草敵(cycloate)、環己醯亞胺(cycloheximide)、環蟎酯(cycloprate)、乙氰菊脂(cycloprothrin)、環噠草特(cyclopyrimorate)、環磺隆(cyclosulfamuron)、環殺草(cycloxydim)、環莠隆(cycluron)、腈吡蟎酯(cyenopyrafen)、環氟菌胺(cyflufenamid)、丁氟蟎酯(cyflumetofen)、賽扶寧(cyfluthrin)、氯氟氰蟲醯胺(cyhalodiamide)、賽扶草(cyhalofop)、賽扶草-丁酯、賽洛寧(cyhalothrin)、錫蟎丹(cyhexatin)、蟎蜱胺(cymiazole)、蟎蜱胺鹽酸鹽、克絕(cymoxanil)、解草胺腈(cyometrinil)、氰菌靈(cypendazole)、賽滅寧(cypermethrin)、牧草快(cyperquat)、氯化牧草快、賽酚寧(cyphenothrin)、環草津(cyprazine)、三環塞草胺(cyprazole)、環克座(cyproconazole)、嘧菌環胺(cyprodinil)、酯菌胺(cyprofuram)、環丙草胺(cypromid)、可普磺醯胺(cyprosulfamide)、賽滅淨(cyromazine)、畜蜱磷(cythioate)、殺草隆(daimuron)、茅草枯(dalapon)、茅草枯-鈣、茅草枯-鎂、茅草枯-鈉、丁醯肼(daminozide)、噠幼酮(dayoutong)、邁隆(dazomet)、邁隆-鈉、DBCP、d-樟腦、DCIP、DCPTA、DDT、咪菌威(debacarb)、癸磷錫(decafentin)、一甲呋喃丹(decarbofuran)、去氫乙酸、敵草樂(delachlor)、第滅寧(deltamethrin)、田樂磷(demephion)、田樂磷-O、田樂磷-S、內吸磷(demeton)、內吸磷-甲酯、內吸磷-O、內吸磷-O-甲酯、內吸磷-S、內吸磷-S-甲酯、碸吸磷(demeton-S-methylsulphon)、甜菜安(desmedipham)、敵草淨(desmetryn)、d-反式氯炔丙菊酯(d-fanshiluquebingjuzhi)、汰芬諾克(diafenthiuron)、氯亞胺硫磷(dialifos)、燕 麥敵(di-allate)、二胺磷(diamidafos)、矽藻土、大利松(diazinon)、鄰苯二甲酸二丁酯、丁二酸二丁酯、麥草畏(dicamba)、麥草畏-二甘醇胺、麥草畏-二甲基銨、麥草畏-二乙醇胺、麥草畏-異丙基銨、麥草畏-甲酯、麥草畏-乙醇胺、麥草畏-鉀、麥草畏-鈉、麥草畏-三乙醇胺、異氯硫磷(dicapthon)、敵草腈(dichlobenil)、dichlobentiazox、除線磷(dichlofenthion)、益發靈(dichlofluanid)、二氯萘醌(dichlone)、氯全隆(dichloralurea)、滅幼脲(dichlorbenzuron)、二氯茀醇(dichlorflurenol)、二氯茀醇-甲酯、苄胺靈(dichlormate)、二氯丙烯胺(dichlormid)、二氯酚(dichlorophen)、滴丙酸(dichlorprop)、滴丙酸-2-乙基己酯、滴丙酸-丁氧乙酯、滴丙酸-二甲基銨、滴丙酸-乙基銨、滴丙酸-異辛酯、滴丙酸-甲酯、滴丙酸-P、滴丙酸-P-2-乙基己酯、滴丙酸-P-二甲基銨、滴丙酸-鉀、滴丙酸-P-鉀、滴丙酸-P-鈉、滴丙酸-鈉、二氯松(dichlorvos)、菌核利(dichlozoline)、苄氯三唑醇(diclobutrazol)、二氯西莫(diclocymet)、禾草靈(diclofop)、禾草靈-甲酯、達滅淨(diclomezine)、達滅淨-鈉、氯硝胺(dicloran)、二氯滅嗪(dicloromezotiaz)、雙氯磺草胺(diclosulam)、開樂散(dicofol)、雙殺鼠靈(dicoumarol)、敵來死(dicresyl)、雙特松(dicrotophos)、地昔尼爾(dicyclanil)、迪賽隆(dicyclonon)、狄氏劑(dieldrin)、除蟎靈(dienochlor)、二乙除草雙(diethamquat)、二乙除草雙二氯化物、安塔(diethatyl)、安塔-乙酯、乙黴威(diethofencarb)、增效磷(dietholate)、焦碳酸二乙酯、避蚊胺(diethyltoluamide)、鼠得克(difenacoum)、待克利(difenoconazole)、氟苯戊烯酸(difenopenten)、氟苯戊烯酸-乙酯、枯莠隆(difenoxuron)、苯敵快(difenzoquat)、苯敵快甲硫酸鹽(difenzoquat metilsulfate)、噻鼠靈(difethialone)、氟蟎嗪(diflovidazin)、二福隆(diflubenzuron)、吡氟草胺(diflufenican)、二氟吡隆(diflufenzopyr)、二氟吡隆-鈉、二氟林(diflumetorim)、敵草克(dikegulac)、敵草克-鈉、雙羥丙茶鹼(dilor)、敵瑪替夫(dimatif)、四 氟甲醚菊酯(dimefluthrin)、甲氟磷(dimefox)、噁唑隆(dimefuron)、哌草丹(dimepiperate)、菌核淨(dimetachlone)、地麥威(dimetan)、混滅威(dimethacarb)、二甲草胺(dimethachlor)、異戊乙淨(dimethametryn)、二甲噻草胺(dimethenamid)、二甲噻草胺-P、噻節因(dimethipin)、二甲嘧酚(dimethirimol)、大滅松(dimethoate)、達滅芬(dimethomorph)、苄菌酯(dimethrin)、驅蚊靈(dimethyl carbate)、鄰苯二甲酸二甲酯、甲基毒蟲畏(dimethylvinphos)、敵蠅威(dimetilan)、草滅散(dimexano)、dimidazon、地莫菌胺(dimoxystrobin)、消蟎酚(dinex)、消蟎酚-diclexine、啶菌噁唑(dingjunezuo)、達克利(diniconazole)、達克利-M、敵樂胺(dinitramine)、大脫蟎(dinobuton)、白粉克(dinocap)、白粉克-4、白粉克-6、鄰敵蟎消(dinocton)、迪樂芬諾(dinofenate)、硝戊酯(dinopenton)、丙硝酚(dinoprop)、戊硝酚(dinosam)、地樂酚(dinoseb)、地樂酚乙酸酯、地樂酚-銨、地樂酚-二乙醇胺、地樂酚-鈉、地樂酚-三乙醇胺、硝辛酯(dinosulfon)、呋蟲胺(dinotefuran)、特樂酚(dinoterb)、特樂酚乙酸酯、硝丁酯(dinoterbon)、苯蟲醚(diofenolan)、蔬果磷(dioxabenzofos)、二氧威(dioxacarb)、敵殺磷(dioxathion)、敵鼠(diphacinone)、敵鼠-鈉、草乃敵(diphenamid)、二苯碸、二苯胺、地樂靈(dipropalin)、異丙淨(dipropetryn)、dipymetitrone、雙硫氧吡啶(dipyrithione)、敵草快(diquat)、敵草快二溴化物、雌舞毒蛾引誘劑(disparlure)、賽松(disul)、二硫龍(disulfiram)、二硫松(disulfoton)、賽松-鈉、滅菌磷(ditalimfos)、腈硫醌(dithianon)、噻喃磷(dithicrofos)、蟎速克(dithioether)、氟硫草定(dithiopyr)、達有龍(diuron)、d-檸檬烯、DMPA、DNOC、DNOC-銨、DNOC-鉀、DNOC-鈉、嗎菌靈(dodemorph)、嗎菌靈乙酸酯、嗎菌靈苯甲酸酯、多地辛(dodicin)、多地辛鹽酸鹽、多地辛-鈉、多寧(dodine)、苯氧炔蟎(dofenapyn)、穀蠢引誘劑(dominicalure)、多拉克汀(doramectin)、敵菌酮(drazoxolon)、DSMA、毒氟磷(dufulin)、EBEP、 EBP、蛻皮甾酮(ecdysterone)、護粒松(edifenphos)、甘草津(eglinazine)、甘草津-乙酯、因滅汀(emamectin)、因滅汀苯甲酸酯、EMPC、烯炔菊酯(empenthrin)、安殺番(endosulfan)、草多索(endothal)、草多索-二銨、草多索-二鉀、草多索-二鈉、因毒磷(endothion)、安特靈(endrin)、烯肟菌酯(enestroburin)、enoxastrobin、EPN、丙醯芸苔素內酯(epocholeone)、保幼醚(epofenonane)、依普座(epoxiconazole)、依立諾克丁(eprinomectin)、磺唑草(epronaz)、ε-甲氧苄氟菊酯(epsilon-metofluthrin)、ε-momfluorothrin、EPTC、抑草蓬(erbon)、麥角鈣化醇(ergocalciferol)、二氯己醯草胺(erlujixiancaoan)、生物烯丙菊酯(esdépalléthrine)、益化利(esfenvalerate)、戊草丹(esprocarb)、乙烯矽(etacelasil)、乙環唑(etaconazole)、依他伏殺(etaphos)、代森硫(etem)、噻唑菌胺(ethaboxam)、克草胺(ethachlor)、乙丁烯氟靈(ethalfluralin)、胺苯磺隆(ethametsulfuron)、胺苯磺隆-甲酯、殺草胺(ethaprochlor)、益收生長素(ethephon)、噻二唑隆(ethidimuron)、殺蟲丹(ethiofencarb)、抑草威(ethiolate)、愛殺松(ethion)、乙嗪草酮(ethiozin)、乙蟲清(ethiprole)、依瑞莫(ethirimol)、益果-甲酯(ethoate-methyl)、乙呋草黃(ethofumesate)、驅蚊醇(ethohexadiol)、普伏松(ethoprophos)、氯氟草醚(ethoxyfen)、氯氟草醚-乙酯、促長啉(ethoxyquin)、乙氧嘧磺隆(ethoxysulfuron)、吲熟酯(ethychlozate)、甲酸乙酯、α-萘乙酸乙酯、乙基-DDD、乙烯、二溴化乙烯、二氯化乙烯、氧化乙烯、乙蒜素(ethylicin)、2,3-二羥基丙基硫醇乙基汞、乙酸乙基汞、溴化乙基汞、氯化乙基汞、磷酸乙基汞、硝草酚(etinofen)、乙胺草醚(etnipromid)、乙氧苯草胺(etobenzanid)、依芬寧(etofenprox)、依殺蟎(etoxazole)、依得利(etridiazole)、乙嘧硫磷(etrimfos)、丁香酚(eugenol)、EXD、凡殺同(famoxadone)、氨磺磷(famphur)、咪唑菌酮(fenamidone)、敵克松(fenaminosulf)、烯肟菌胺(fenaminstrobin)、芬滅松(fenamiphos)、咪菌腈(fenapanil)、芬瑞莫(fenarimol)、 氟苯吡草(fenasulam)、抗蟎唑(fenazaflor)、芬殺蟎(fenazaquin)、芬克座(fenbuconazole)、芬布錫(fenbutatin oxide)、解草唑(fenchlorazole)、解草唑-乙酯、皮蠅硫磷(fenchlorphos)、解草啶(fenclorim)、乙苯威(fenethacarb)、五氟苯菊酯(fenfluthrin)、甲呋醯胺(fenfuram)、環醯菌胺(fenhexamid)、種衣酯(fenitropan)、撲滅松(fenitrothion)、酚菌酮(fenjuntong)、仲丁威(fenobucarb)、涕丙酸(fenoprop)、涕丙酸-3-丁氧基丙酯、涕丙酸-丁氧甲酯、涕丙酸-丁氧乙酯、涕丙酸-丁酯、涕丙酸-異辛酯、涕丙酸-甲酯、涕丙酸-鉀、苯硫威(fenothiocarb)、非諾克林(fenoxacrim)、氰菌胺(fenoxanil)、精噁唑禾草靈(fenoxaprop)、精噁唑禾草靈-乙酯、精噁唑禾草靈-P、精噁唑禾草靈-P-乙酯、異噁苯碸(fenoxasulfone)、芬諾克(fenoxycarb)、拌種咯(fenpiclonil)、fenpicoxamid、吡氯氰菊酯(fenpirithrin)、芬普寧(fenpropathrin)、苯鏽啶(fenpropidin)、芬普福(fenpropimorph)、胺苯吡菌酮(fenpyrazamine)、芬普蟎(fenpyroximate)、fenquinotrione、噠嗪抑雄素(fenridazon)、噠嗪抑雄素-鉀、噠嗪抑雄素-丙酯、除蟎酯(fenson)、豐索磷(fensulfothion)、氯苯氧乙醇(fenteracol)、噻唑禾草靈(fenthiaprop)、噻唑禾草靈-乙酯、芬殺松(fenthion)、芬殺松-乙酯、三苯錫(fentin)、乙酸三苯錫、氯化三苯錫、氫氧化三苯錫、四唑醯草胺(fentrazamide)、芳氟胺(fentrifanil)、非草隆(fenuron)、非草隆TCA、芬化利(fenvalerate)、福美鐵(ferbam)、富米綜(ferimzone)、硫酸亞鐵、費普尼(fipronil)、氟燕靈(flamprop)、氟燕靈-異丙酯、氟燕靈-M、氟燕靈-甲酯、氟燕靈-M-異丙酯、氟燕靈-M-甲酯、嘧啶磺隆(flazasulfuron)、氟鼠靈(flocoumafen)、flometoquin、氟啶蟲醯胺(flonicamid)、雙氟磺草胺(florasulam)、氯氟吡啶酯(florpyrauxifen)、嘧蟎酯(fluacrypyrim)、fluazaindolizine、伏寄普(fluazifop)、伏寄普-丁酯、伏寄普-甲酯、伏寄普-P、伏寄普-P-丁酯、扶吉胺(fluazinam)、異丙吡草酯(fluazolate)、啶蜱脲(fluazuron)、氟蟲雙醯胺 (flubendiamide)、氟蟎噻(flubenzimine)、氟酮磺隆(flucarbazone)、氟酮磺隆-鈉、氟吡磺隆(flucetosulfuron)、氟消草(fluchloralin)、伏康脲(flucofuron)、氟環脲(flucycloxuron)、護賽寧(flucythrinate)、護汰寧(fludioxonil)、聯氟蟎(fluenetil)、氟噻蟲碸(fluensulfone)、氟噻草胺(flufenacet)、氟芬內林(flufenerim)、吡氟草胺(flufenican)、氟芬隆(flufenoxuron)、氟菌蟎酯(flufenoxystrobin)、三氟醚(flufenprox)、氟噠嗪草酮(flufenpyr)、氟噠嗪草酮-乙酯、丁烯氟蟲腈(flufiprole)、fluhexafon、氟氯苯菊酯(flumethrin)、氟醯菌胺(flumetover)、氟節胺(flumetralin)、唑嘧磺草胺(flumetsulam)、氟默嗪(flumezin)、氟烯草酸(flumiclorac)、氟烯草酸-戊酯、丙炔氟草胺(flumioxazin)、氟米丙平(flumipropyn)、氟嗎啉(flumorph)、伏草隆(fluometuron)、氟吡菌胺(fluopicolide)、氟吡菌醯胺(fluopyram)、氟殺蟎(fluorbenside)、增糖胺(fluoridamid)、氟乙醯胺(fluoroacetamide)、消草醚(fluorodifen)、乙羧氟草醚(fluoroglycofen)、乙羧氟草醚-乙酯、唑呋草(fluoroimide)、唑唆草(fluoromidine)、氟除草醚(fluoronitrofen)、氟硫隆(fluothiuron)、三氟苯唑(fluotrimazole)、氟嘧菌酯(fluoxastrobin)、氟胺草唑(flupoxam)、flupropacil、氟鼠啶(flupropadine)、四氟丙酸(flupropanate)、四氟丙酸-鈉、flupyradifurone、氟啶嘧磺隆(flupyrsulfuron)、氟啶嘧磺隆-甲酯、氟啶嘧磺隆-甲酯-鈉、氟喹唑(fluquinconazole)、解草安(flurazole)、抑草丁(flurenol)、抑草丁-丁酯、抑草丁-甲酯、氟啶草酮(fluridone)、氟咯草酮(flurochloridone)、氟草定(fluroxypyr)、氟草定-丁氧甲酯、氟草定-甲基庚酯、調嘧醇(flurprimidol)、氟磺醯胺(flursulamid)、呋草酮(flurtamone)、護矽得(flusilazole)、氟硫滅(flusulfamide)、嗪草酸(fluthiacet)、嗪草酸-甲酯、氟替尼(flutianil)、福多寧(flutolanil)、護汰芬(flutriafol)、福化利(fluvalinate)、氟殺甲醯(fluxametamide)、氟唑菌醯胺(fluxapyroxad)、肟草安(fluxofenim)、福爾培(folpet)、氟磺胺草 醚(fomesafen)、氟磺胺草醚-鈉、地蟲磷(fonofos)、甲醯嘧磺隆(foramsulfuron)、氯吡脲(forchlorfenuron)、甲醛、複滅蟎(formetanate)、複滅蟎鹽酸鹽、安果(formothion)、胺甲威(formparanate)、胺甲威鹽酸鹽、殺木膦(fosamine)、殺木膦-銨、福賽得(fosetyl)、福賽得-鋁、丁苯硫磷(fosmethilan)、福司吡酯(fospirate)、噻唑磷(fosthiazate)、丁硫環磷(fosthietan)、弗羅塔林(frontalin)、麥穗靈(fuberidazole)、氟草淨(fucaojing)、氟草醚(fucaomi)、氟萘禾草靈(funaihecaoling)、呋苯硫脲(fuphenthiourea)、乙二醇縮糖醛(furalane)、呋霜靈(furalaxyl)、炔呋菊酯(furamethrin)、福拉比(furametpyr)、呋線威(furathiocarb)、二甲呋醯胺(furcarbanil)、氟康唑(furconazole)、順式氟康唑、抗蟲菊(furethrin)、糠醛(furfural)、呋喃解草唑(furilazole)、拌種胺(furmecyclox)、呋菌隆(furophanate)、呋氧草醚(furyloxyfen)、γ-賽洛寧(gamma-cyhalothrin)、γ-HCH、格蟎酯(genit)、赤黴酸(gibberellic acid)、赤黴素(gibberellins)、鼠甘伏(gliftor)、草銨膦(glufosinate)、草銨膦-銨、草銨膦-P、草銨膦-P-銨、草銨膦-P-鈉、果綠定(glyodin)、乙二肟(glyoxime)、草甘膦(glyphosate)、草甘膦-二銨、草甘膦-二甲基銨、草甘膦-異丙基銨、草甘膦-單銨、草甘膦-鉀、草甘膦-倍半鈉、草甘膦-三甲基硫、草甘二膦(glyphosine)、棉紅鈴蟲性誘劑(gossyplure)、誘殺烯混劑(grandlure)、灰黃黴素(griseofulvin)、雙胍辛(guazatine)、雙胍辛乙酸鹽、丙烯酸喹啉酯(halacrinate)、halauxifen、氟氯吡啶酯(halauxifen-methyl)、苄蟎醚(halfenprox)、合芬隆(halofenozide)、氟硝磺醯胺(halosafen)、氯吡嘧磺隆(halosulfuron)、氯吡嘧磺隆-甲酯、氟啶草(haloxydine)、精吡氟氯禾靈(haloxyfop)、精吡氟氯禾靈-乙氧乙酯、精吡氟氯禾靈-甲酯、精吡氟氯禾靈-P、精吡氟氯禾靈-P-乙氧乙酯、精吡氟氯禾靈-P-甲酯、精吡氟氯禾靈-鈉、HCH、六甲蜜胺(hemel)、六甲磷(hempa)、HEOD、飛布達(heptachlor)、heptafluthrin、庚烯磷(heptenophos)、增產肟 (heptopargil)、除莠黴素(herbimycin)、速殺硫磷(heterophos)、六氯丙酮、六氯苯、六氯丁二烯、六氯酚、菲克利(hexaconazole)、六伏隆(hexaflumuron)、六氟砷酸鉀(hexaflurate)、己誘劑(hexalure)、己醯胺(hexamide)、六嗪同(hexazinone)、hexylthiofos、合賽多(hexythiazox)、HHDN、holosulf、huancaiwo、磺草靈(huangcaoling)、環菌唑(huanjunzuo)、愛美松(hydramethylnon)、汞加芬(hydrargaphen)、熟石灰、氰化氫、烯蟲乙酯(hydroprene)、惡黴靈(hymexazol)、奮淋威(hyquincarb)、IAA、IBA、埃卡瑞丁(icaridin)、依滅列(imazalil)、依滅列硝酸鹽、依滅列硫酸鹽、咪草酸(imazamethabenz)、咪草酸-甲酯、甲氧咪草菸(imazamox)、甲氧咪草菸-銨、甲基咪草菸(imazapic)、甲基咪草菸-銨、依滅草(imazapyr)、依滅草-異丙基銨、滅草喹(imazaquin)、滅草喹-銨、滅草喹-甲酯、滅草喹-鈉、咪草菸(imazethapyr)、咪草菸-銨、唑吡嘧磺隆(imazosulfuron)、亞胺唑(imibenconazole)、新菸磷(imicyafos)、吡蟲啉(imidacloprid)、氯噻啉(imidaclothiz)、克熱淨(iminoctadine)、克熱淨三乙酸鹽、克熱淨三烷基苯磺酸鹽、依普寧(imiprothrin)、依納素(inabenfide)、茚草酮(indanofan)、茚嗪氟草胺(indaziflam)、因得克(indoxacarb)、枯瘟淨(inezin)、碘草腈(iodobonil)、iodocarb、碘甲烷、碘甲磺隆(iodosulfuron)、碘甲磺隆-甲酯、碘甲磺隆-甲酯-鈉、iofensulfuron、iofensulfuron-sodium、碘苯腈(ioxynil)、碘苯腈辛酸鹽、碘苯腈-鋰、碘苯腈-鈉、抑草津(ipazine)、種菌唑(ipconazole)、艾分卡巴腙(ipfencarbazone)、依普芬三氟康納唑(ipfentrifluconazole)、丙基喜樂松(iprobenfos)、依普同(iprodione)、纈黴威(iprovalicarb)、丙草定(iprymidam)、齒小蠹二烯醇(ipsdienol)、小蠹烯醇(ipsenol)、IPSP、isamidofos、依殺松(isazofos)、碳氯靈(isobenzan)、丁咪胺(isocarbamid)、水胺硫磷(isocarbophos)、異草定(isocil)、異艾氏劑(isodrin)、異柳磷(isofenphos)、異柳磷-甲酯、艾索非他米(isofetamid)、異索威(isolan)、 丁嗪草酮(isomethiozin)、異草完隆(isonoruron)、isopolinate、葉蟬散(isoprocarb)、異丙樂靈(isopropalin)、稻瘟靈(isoprothiolane)、異丙隆(isoproturon)、吡唑萘菌胺(isopyrazam)、isopyrimol、異拌磷(isothioate)、異噻菌胺(isotianil)、異惡隆(isouron)、異醯菌酮(isovaledione)、異噁草胺(isoxaben)、異噁氯草酮(isoxachlortole)、雙苯噁唑酸(isoxadifen)、雙苯噁唑酸-乙酯、異噁唑草酮(isoxaflutole)、異噁草醚(isoxapyrifop)、加福松(isoxathion)、伊維菌素(ivermectin)、浸種磷(izopamfos)、japonilure、喃烯菊酯(japothrins)、茉莉菊酯I(jasmolin I)、茉莉菊酯II、茉莉酸(jasmonic acid)、甲磺蟲腙(jiahuangchongzong)、甲基增效磷(jiajizengxiaolin)、甲香菌酯(jiaxiangjunzhi)、解草烷(jiecaowan)、解草烯(jiecaoxi)、碘硫磷(jodfenphos)、保幼激素I、保幼激素II、保幼激素III、噻嗯菊酯(kadethrin)、κ-畢芬寧(kappa-bifenthrin)、κ-七氟菊酯(kappa-tefluthrin)、卡草靈(karbutilate)、karetazan、karetazan-potassium、春日黴素(kasugamycin)、春日黴素鹽酸鹽、克菌靈(kejunlin)、氯戊環(kelevan)、ketospiradox、ketospiradox-potassium、活動素(kinetin)、烯蟲炔酯(kinoprene)、克收欣-甲酯(kresoxim-methyl)、喹草烯(kuicaoxi)、乳氟禾草靈(lactofen)、λ-賽洛寧(lambda-cyhalothrin)、蘭可三酮(lancotrione)、latilure、砷酸鉛、環草定(lenacil)、雷皮菌素(lepimectin)、溴苯磷(leptophos)、靈丹(lindane)、三甲基二氧三環壬烷(lineatin)、利穀隆(linuron)、啶蟲磷(lirimfos)、夜蛾性誘劑(litlure)、粉紋夜蛾性誘劑(looplure)、祿芬隆(lufenuron)、氯啶菌酯(lvdingjunzhi)、氯醯草膦(lvxiancaolin)、噻唑磷(lythidathion)、MAA、馬拉硫磷(malathion)、順丁烯二醯肼、丙蟎氰(malonoben)、麥芽糊精(maltodextrin)、MAMA、代森錳銅(mancopper)、代森錳鋅(mancozeb)、滿得賓(mandestrobin)、雙炔醯菌胺(mandipropamid)、錳乃浦(maneb)、苦參鹼(matrine)、疊氮磷(mazidox)、MCPA、MCPA-2-乙基己 酯、MCPA-丁氧乙酯、MCPA-丁酯、MCPA-二甲基銨、MCPA-二乙醇胺、MCPA-乙酯、MCPA-異丁酯、MCPA-異辛酯、MCPA-異丙酯、MCPA-甲酯、MCPA-乙醇胺、MCPA-鉀、MCPA-鈉、MCPA-硫基乙酯、MCPA-三乙醇胺、MCPB、MCPB-乙酯、MCPB-甲酯、MCPB-鈉、滅鏽胺(mebenil)、滅蚜磷(mecarbam)、mecarbinzid、甲基減蚜磷(mecarphon)、2-甲-4-氯丙酸(mecoprop)、2-甲-4-氯丙酸-2-乙基己酯、2-甲-4-氯丙酸-二甲基銨、2-甲-4-氯丙酸-二乙醇胺、2-甲-4-氯丙酸-乙二酯、2-甲-4-氯丙酸-異辛酯、2-甲-4-氯丙酸-甲酯、2-甲-4-氯丙酸-P、2-甲-4-氯丙酸-P-2-乙基己酯、2-甲-4-氯丙酸-P-二甲基銨、2-甲-4-氯丙酸-P-異丁酯、2-甲-4-氯丙酸-鉀、2-甲-4-氯丙酸-P-鉀、2-甲-4-氯丙酸-鈉、2-甲-4-氯丙酸-三乙醇胺、殺蟎脒(medimeform)、地樂施(medinoterb)、地樂施乙酸酯、誘殺酯(medlure)、苯噻醯草胺(mefenacet)、吡唑解草酸(mefenpyr)、吡唑解草酸-二乙酯、美芬三康唑(mefentrifluconazole)、氟磺醯草胺(mefluidide)、氟磺醯草胺-二乙醇胺、氟磺醯草胺-鉀、十四碳二烯酸(megatomoic acid)、滅蚜松(menazon)、嘧菌胺(mepanipyrim)、氯氟醚菊酯(meperfluthrin)、mephenate、地安磷(mephosfolan)、壯棉素(mepiquat)、氯化壯棉素、五硼酸壯棉素、滅普寧(mepronil)、敵蟎普(meptyldinocap)、氯化汞、氧化汞、氯化亞汞、脫葉亞磷(merphos)、滅莠津(mesoprazine)、甲基二磺隆(mesosulfuron)、甲基二磺隆-甲酯、甲基磺草酮(mesotrione)、甲硫芬(mesulfen)、甲亞碸磷(mesulfenfos)、氰氟蟲胺(metaflumizone)、滅達樂(metalaxyl)、滅達樂-M、蝸牛敵(metaldehyde)、威百畝(metam)、威百畝-銨、噁唑醯草胺(metamifop)、苯嗪草酮(metamitron)、威百畝-鉀、威百畝-鈉、吡草胺(metazachlor)、雙醚氯吡嘧磺隆(metazosulfuron)、間氯敵菌酮(metazoxolon)、滅特座(metconazole)、甲基涕巴(metepa)、二甲達草伏(metflurazon)、甲基苯噻隆(methabenzthiazuron)、蟲 蟎畏(methacrifos)、美索丙鉑林(methalpropalin)、達馬松(methamidophos)、滅速克(methasulfocarb)、滅草唑(methazole)、呋菌胺(methfuroxam)、滅大松(methidathion)、甲硫苯威(methiobencarb)、滅賜克(methiocarb)、甲硫嘧磺隆(methiopyrisulfuron)、甲硫涕巴(methiotepa)、methiozolin、滅草恆(methiuron)、殺蟲乙烯磷(methocrotophos)、醚草通(methometon)、納乃得(methomyl)、美賜平(methoprene)、蓋草津(methoprotryne)、奎納克林-丁酯(methoquin-butyl)、甲醚菊酯(methothrin)、甲氧滴滴涕(methoxychlor)、滅芬諾(methoxyfenozide)、去草酮(methoxyphenone)、甲基不育特(methyl apholate)、溴化甲烷、甲基丁香酚(methyl eugenol)、碘化甲烷、異硫氰酸甲酯、甲基乙酯磷(methylacetophos)、甲基氯仿、甲基殺草隆(methyldymron)、二氯甲烷、苯甲酸甲基汞、氰胍甲汞(methylmercury dicyandiamide)、五氯苯酚甲基汞(methylmercury pentachlorophenoxide)、甲基新癸醯胺、免得爛(metiram)、吡喃隆(metobenzuron)、溴穀隆(metobromuron)、甲氧苄氟菊酯(metofluthrin)、異丙甲草胺(metolachlor)、速滅威(metolcarb)、苯氧菌胺(metominostrobin)、磺草唑胺(metosulam)、惡蟲酮(metoxadiazone)、甲氧隆(metoxuron)、滅芬農(metrafenone)、賽克津(metribuzin)、噻菌胺(metsulfovax)、甲磺隆(metsulfuron)、甲磺隆-甲酯、美文松(mevinphos)、茲克威(mexacarbate)、滅鼠安(mieshuan)、密滅汀(milbemectin)、米爾貝肟(milbemycin oxime)、代森環(milneb)、丙胺氟(mipafox)、滅蟻靈(mirex)、MNAF、蘑菇醇(moguchun)、草達滅(molinate)、殺蟲單(molosultap)、momfluorothrin、庚醯草胺(monalide)、特噁唑隆(monisouron)、單氯乙酸、亞素靈(monocrotophos)、綠穀隆(monolinuron)、單嘧磺隆(monosulfuron)、單嘧磺隆-酯、滅草隆(monuron)、滅草隆TCA、伐草快(morfamquat)、伐草快二氯化物、嗎啉脒胍(moroxydine)、嗎啉脒胍鹽酸鹽、茂果(morphothion)、morzid、莫昔克丁(moxidectin)、MSMA、家蠅 引誘劑(muscalure)、邁克尼(myclobutanil)、米克啉(myclozolin)、N-(乙基汞)-對甲苯磺醯苯胺、鈉乃浦(nabam)、萘肽磷(naftalofos)、二溴磷(naled)、萘、萘乙醯胺、萘二甲酸酐、萘氧基乙酸、萘丙胺(naproanilide)、敵草胺(napropamide)、敵草胺-M、萘草胺(naptalam)、萘草胺-鈉、遊黴素(natamycin)、草不隆(neburon)、氯硝柳胺(niclosamide)、氯硝柳胺-乙醇胺、菸嘧磺隆(nicosulfuron)、菸鹼、氟蟻靈(nifluridide)、氟氯草胺(nipyraclofen)、烯啶蟲胺(nitenpyram)、硝乙脲噻唑(nithiazine)、磺樂靈(nitralin)、氯啶(nitrapyrin)、戊氰威(nitrilacarb)、除草醚(nitrofen)、三氟甲草醚(nitrofluorfen)、硝基苯乙烯、異丙消(nitrothal-isopropyl)、鼠特靈(norbormide)、達草滅(norflurazon)、降菸鹼(nornicotine)、草完隆(noruron)、諾伐隆(novaluron)、多氟脲(noviflumuron)、尼瑞莫(nuarimol)、OCH、八氯二丙醚、辛噻酮(octhilinone)、呋醯胺(ofurace)、氧樂果(omethoate)、坪草丹(orbencarb)、歐弗拉洛(orfralure)、鄰二氯苯、嘧苯胺磺隆(orthosulfamuron)、oryctalure、肟醚菌胺(orysastrobin)、氨磺樂靈(oryzalin)、蛇床子素(osthol)、ostramone、解草腈(oxabetrinil)、丙炔噁草酮(oxadiargyl)、噁草酮(oxadiazon)、歐殺斯(oxadixyl)、草胺酸鹽(oxamate)、歐殺滅(oxamyl)、草噠松(oxapyrazon)、草噠松-二甲醇胺、草噠松-鈉、環氧嘧磺隆(oxasulfuron)、奧賽普林(oxathiapiprolin)、噁嗪草酮(oxaziclomefone)、喹啉銅(oxine-copper)、歐索林酸(oxolinic acid)、噁咪唑(oxpoconazole)、噁咪唑反丁烯二酸鹽、嘉保信(oxycarboxin)、滅多松-甲酯(oxydemeton-methyl)、異亞碸磷(oxydeprofos)、碸拌磷(oxydisulfoton)、乙氧氟草醚(oxyfluorfen)、氧化苦參鹼(oxymatrine)、土黴素(oxytetracycline)、土黴素鹽酸鹽、巴克素(paclobutrazol)、哌蟲啶(paichongding)、對二氯苯、對氟隆(parafluron)、巴拉刈(paraquat)、巴拉刈二氯化物、巴拉刈二甲基硫酸鹽、巴拉松(parathion)、巴拉松-甲酯、苯吡醇(parinol)、克草猛(pebulate)、 披扶座(pefurazoate)、天竺葵酸(pelargonic acid)、平克座(penconazole)、賓克隆(pencycuron)、二甲戊樂靈(pendimethalin)、噴福芬(penflufen)、氟幼脲(penfluron)、平速爛(penoxsulam)、五氯苯酚、月桂酸五氯苯酯、戊醯苯草胺(pentanochlor)、吡噻菌胺(penthiopyrad)、戊烯氰氯菊酯(pentmethrin)、環戊噁草酮(pentoxazone)、氟草磺胺(perfluidone)、百滅寧(permethrin)、烯草胺(pethoxamid)、氰烯菌酯(phenamacril)、葉枯淨(phenazine oxide)、棉胺寧(phenisopham)、芬硫磷(phenkapton)、甜菜寧(phenmedipham)、甜菜寧-乙酯、稀草隆(phenobenzuron)、苯醚菊酯(phenothrin)、苯蟎醚(phenproxide)、賽達松(phenthoate)、苯基汞脲(phenylmercuriurea)、乙酸苯基汞、氯化苯基汞、鄰苯二酚之苯基汞衍生物、硝酸苯基汞、水楊酸苯基汞、福瑞松(phorate)、毒鼠磷(phosacetim)、裕必松(phosalone)、氯瘟磷(phosdiphen)、硫環磷(phosfolan)、硫環磷-甲酯、甘胺硫磷(phosglycin)、益滅松(phosmet)、對氯硫磷(phosnichlor)、福賜米松(phosphamidon)、膦、磷蟲威(phosphocarb)、磷、三磷錫(phostin)、巴賽松(phoxim)、巴賽松-甲酯、稻瘟酞(phthalide)、皮卡布西(picarbutrazox)、胺氯吡啶酸(picloram)、胺氯吡啶酸-2-乙基己酯、胺氯吡啶酸-異辛酯、胺氯吡啶酸-甲酯、胺氯吡啶酸-乙醇胺、胺氯吡啶酸-鉀、胺氯吡啶酸-三乙銨、胺氯吡啶酸-參(2-羥基丙基)銨、氟吡草胺(picolinafen)、啶氧菌酯(picoxystrobin)、殺鼠酮(pindone)、殺鼠酮-鈉、唑啉草酯(pinoxadcn)、粉病靈(piperalin)、胡椒基丁醚(piperonyl butoxide)、胡椒基環己烯酮(piperonyl cyclonene)、哌草磷(piperophos)、哌壯素(piproctanyl)、溴化哌壯素、增效醛(piprotal)、甲胺啼磷(pirimetaphos)、比加普(pirimicarb)、嘧啶氧磷(pirimioxyphos)、亞特松-乙酯(pirimiphos-ethyl)、亞特松-甲酯、三氯殺蟲酯(plifenate)、聚胺基甲酸酯、多氧菌素(polyoxins)、保粒黴素(polyoxorim)、保粒黴素-鋅、多噻烷(polythialan)、亞砷酸鉀、疊氮化鉀、氰酸鉀、赤黴酸 鉀(potassium gibberellate)、環烷酸鉀、聚硫化鉀、硫氰化鉀、α-萘乙酸鉀、pp'-DDT、普亞列寧(prallethrin)、早熟素I(precocene I)、早熟素II、早熟素III、丙草胺(pretilachlor)、乙醯嘧啶磷(primidophos)、氟嘧磺隆(primisulfuron)、氟嘧磺隆-甲酯、撲殺熱(probenazole)、咪醯胺(prochloraz)、咪醯胺-錳、丙氯醇(proclonol)、環丙腈津(procyazine)、撲滅寧(procymidone)、胺基丙氟靈(prodiamine)、布飛松(profenofos)、氟唑草胺(profluazol)、環丙氟靈(profluralin)、丙氟菊酯(profluthrin)、環苯草酮(profoxydim)、甘撲津(proglinazine)、甘撲津-乙酯、調環酸(prohexadione)、調環酸-鈣、茉莉酮(prohydrojasmon)、蜱虱威(promacyl)、猛殺威(promecarb)、撲滅通(prometon)、撲草淨(prometryn)、捕滅鼠(promurit)、撲草胺(propachlor)、普羅帕脒(propamidine)、普羅帕脒二鹽酸鹽、霜黴威(propamocarb)、霜黴威鹽酸鹽、敵稗(propanil)、丙蟲磷(propaphos)、喔草酯(propaquizafop)、毆蟎多(propargite)、撲蟲菊(proparthrin)、撲滅津(propazine)、巴胺磷(propetamphos)、苯胺靈(propham)、普克利(propiconazole)、甲基鋅乃浦(propineb)、異丙草胺(propisochlor)、安丹(propoxur)、丙苯磺隆(propoxycarbazone)、丙苯磺隆-鈉、增效酯(propyl isome)、丙嘧磺隆(propyrisulfuron)、戊炔草胺(propyzamide)、丙氧喹啉(proquinazid)、補骨內酯(prosuler)、甲硫磺樂靈(prosulfalin)、苄草丹(prosulfocarb)、氟磺隆(prosulfuron)、乙噻唑磷(prothidathion)、硫菌威(prothiocarb)、硫菌威鹽酸鹽、丙硫菌唑(prothioconazole)、普硫松(prothiofos)、發硫磷(prothoate)、丙苯烴菊酯(protrifenbute)、撲滅生(proxan)、撲滅生-鈉、廣草胺(prynachlor)、比達農(pydanon)、pydiflumetofen、pyflubumide、派滅淨(pymetrozine)、比鏽靈(pyracarbolid)、吡唑硫磷(pyraclofos)、雙唑草腈(pyraclonil)、百克敏(pyraclostrobin)、吡草醚(pyraflufen)、吡草醚-乙酯、氟蟲腈(pyrafluprole)、嘧啶威(pyramat)、唑胺菌酯(pyrametostrobin)、唑菌酯 (pyraoxystrobin)、磺醯草吡唑(pyrasulfotole)、pyraziflumid、吡唑特(pyrazolynate)、白粉松(pyrazophos)、吡嘧磺隆(pyrazosulfuron)、吡嘧磺隆-乙酯、硫吡唑磷(pyrazothion)、苄草唑(pyrazoxyfen)、pyresmethrin、必列寧I(pyrethrin I)、必列寧II、除蟲菊精(pyrethrins)、異丙酯草醚(pyribambenz-isopropyl)、丙酯草醚(pyribambenz-propyl)、吡菌苯威(pyribencarb)、嘧啶肟草醚(pyribenzoxim)、稗草丹(pyributicarb)、氯草定(pyriclor)、比達本(pyridaben)、吡啶達醇(pyridafol)、啶蟲丙醚(pyridalyl)、噠嗪硫磷(pyridaphenthion)、噠草特(pyridate)、啶菌腈(pyridinitril)、比芬諾(pyrifenox)、哌氟喹腙(pyrifluquinazon)、環酯草醚(pyriftalid)、嘧黴胺(pyrimethanil)、嘧蟎醚(pyrimidifen)、嘧草醚(pyriminobac)、嘧草醚-甲酯(pyriminobac-methyl)、嘧蟎胺(pyriminostrobin)、嘧啶硫蕃(pyrimisulfan)、嘧硫磷(pyrimitate)、滅鼠優(pyrinuron)、pyriofenone、派瑞樂(pyriprole)、吡啶醇(pyripropanol)、百利普芬(pyriproxyfen)、啶菌噁唑(pyrisoxazole)、嘧硫草醚(pyrithiobac)、嘧硫草醚-鈉、吡唑威(pyrolan)、百快隆(pyroquilon)、嘧氧碸(pyroxasulfone)、甲氧磺草胺(pyroxsulam)、吡氯靈(pyroxychlor)、吡氧呋(pyroxyfur)、苦木素(quassia)、羥基喹啉基乙酮(quinacetol)、羥基喹啉基乙酮硫酸鹽、喹硫磷(quinalphos)、喹硫磷-甲酯、醌菌腙(quinazamid)、二氯喹啉酸(quinclorac)、quinconazole、喹草酸(quinmerac)、滅藻醌(quinoclamine)、quinofumelin、氯藻胺(quinonamid)、畜寧磷(quinothion)、快諾芬(quinoxyfen)、喹硫磷(quintiofos)、五氯硝基苯(quintozene)、快伏草(quizalofop)、快伏草-乙酯、快伏草-P、快伏草-P-乙酯、喹禾糠酯(quizalofop-P-tefuryl)、驅蚊酯(quwenzhi)、驅蠅定(quyingding)、吡咪唑(rabenzazole)、碘醚柳胺(rafoxanide)、rebemide、rescalure、列滅寧(resmethrin)、硫氰苯乙胺(rhodethanil)、鬧羊花毒素III(rhodojaponin-III)、病毒唑(ribavirin)、碸嘧磺隆(rimsulfuron)、魚藤 酮(rotenone)、魚尼丁(ryania)、苯嘧磺草胺(saflufenacil)、噻菌茂(saijunmao)、噻森銅(saisentong)、水楊醯苯胺、血根鹼(sanguinarine)、散道寧(santonin)、八甲磷(schradan)、海蔥糖苷(scilliroside)、另丁津(sebuthylazine)、密草通(secbumeton)、氟唑環菌胺(sedaxane)、司拉克丁(selamectin)、單甲脒(semiamitraz)、單甲脒鹽酸鹽(semiamitraz chloride)、增效菊(sesamex)、芝麻林素(sesamolin)、西殺草(sethoxydim)、雙甲胺草磷(shuangjiaancaolin)、環草隆(siduron)、誘蟲環(siglure)、矽護芬(silafluofen)、毒鼠矽(silatrane)、矽膠、矽硫芬(silthiofam)、西瑪津(simazine)、矽氟唑(simeconazole)、西瑪通(simeton)、西草淨(simetryn)、殺雄啉(sintofen)、SMA、高效異丙甲草胺(S-metolachlor)、亞砷酸鈉、疊氮化鈉、氯酸鈉、氟化鈉、氟乙酸鈉、六氟矽酸鈉、環烷酸鈉、鄰苯基苯酚鈉、五氯苯酚鈉、聚硫化鈉、硫氰酸鈉、α-萘乙酸鈉、蘇硫磷(sophamide)、斯平托蘭(spinetoram)、賜諾殺(spinosad)、賜派芬(spirodiclofen)、螺甲蟎酯(spiromesifen)、螺蟲乙酯(spirotetramat)、螺環菌胺(spiroxamine)、鏈黴素(streptomycin)、鏈黴素倍半硫酸鹽、番木鼈鹼(strychnine)、食菌甲誘醇(sulcatol)、磺苯醚隆(sulcofuron)、磺苯醚隆-鈉、磺草酮(sulcotrione)、草克死(sulfallate)、甲磺草胺(sulfentrazone)、舒非侖(sulfiram)、氟蟲胺(sulfluramid)、甲嘧磺隆(sulfometuron)、甲嘧磺隆-甲酯、磺醯磺隆(sulfosulfuron)、治螟磷(sulfotep)、氟啶蟲胺腈(sulfoxaflor)、亞碸、硫肟醚(sulfoxime)、硫、硫酸、硫醯氟、sulglycapin、硫丙磷(sulprofos)、戊苯碸(sultropen)、滅草靈(swep)、τ-福化利(tau-fluvalinate)、稗草烯(tavron)、噻蟎威(tazimcarb)、TCA、TCA-銨、TCA-鈣、TCA-乙二酯、TCA-鎂、TCA-鈉、TDE、得克利(tebuconazole)、得芬諾(tebufenozide)、得芬瑞(tebufenpyrad)、特普弗洛奎(tebufloquin)、丁基嘧啶磷(tebupirimfos)、牧草胺(tebutam)、得匍隆(tebuthiuron)、克枯爛(tecloftalam)、四氯硝基苯(tecnazene)、福美雙聯 (tecoram)、得福隆(teflubenzuron)、七氟菊酯(tefluthrin)、特呋喃隆(tefuryltrione)、環磺酮(tembotrione)、雙硫磷(temephos)、涕巴(tepa)、TEPP、吡喃草酮(tepraloxydim)、環戊烯丙菊酯(terallethrin)、特草定(terbacil)、特草靈(terbucarb)、猛殺草(terbuchlor)、託福松(terbufos)、甲氧去草淨(terbumeton)、特丁津(terbuthylazine)、去草淨(terbutryn)、特效烯(tetcyclacis)、四氯乙烷、樂本松(tetrachlorvinphos)、四克利(tetraconazole)、四氯殺蟎碸(tetradifon)、四氟隆(tetrafluron)、治滅寧(tetramethrin)、四氟醚菊酯(tetramethylfluthrin)、四胺、殺蟎素(tetranactin)、氟氰蟲醯胺(tetraniliprole)、殺蟎好(tetrasul)、硫酸鉈、甲氧噻草胺(thenylchlor)、θ-賽滅寧(theta-cypermethrin)、腐絕(thiabendazole)、噻蟲啉(thiacloprid)、噻二氟(thiadifluor)、噻蟲嗪(thiamethoxam)、噻丙腈(thiapronil)、噻氟隆(thiazafluron)、噻草定(thiazopyr)、苯噻硫磷(thicrofos)、噻菌腈(thicyofen)、噻二唑胺(thidiazimin)、噻苯隆(thidiazuron)、噻酮磺隆(thiencarbazone)、噻酮磺隆-甲酯、噻吩磺隆(thifensulfuron)、噻吩磺隆-甲酯、賽氟滅(thifluzamide)、禾草丹(thiobencarb)、抗蟲威(thiocarboxime)、硫氯苯亞胺(thiochlorfenphim)、硫賜安(thiocyclam)、硫賜安鹽酸鹽、硫賜安乙二酸鹽、噻菌銅(thiodiazole-copper)、硫敵克(thiodicarb)、久效威(thiofanox)、硫氟肟醚(thiofluoximate)、硫代六甲磷(thiohempa)、硫柳汞(thiomersal)、甲基乙拌磷(thiometon)、硫磷嗪(thionazin)、多保淨(thiophanate)、甲基多保淨、克殺蟎(thioquinox)、胺基硫脲(thiosemicarbazide)、殺蟲雙(thiosultap)、殺蟲雙-二銨、殺蟲雙-二鈉、殺蟲雙-單鈉、噻替派(thiotepa)、得恩地(thiram)、蘇雲金素(thuringiensin)、汰敵寧(tiadinil)、tiafenacil、調節安(tiaojiean)、仲草丹(tiocarbazil)、tioclorim、tioxazafen、硫氰苯甲醯胺(tioxymid)、威線肟(tirpate)、脫克松(tolclofos-methyl)、脫芬瑞(tolfenpyrad)、托普洛卡(tolprocarb)、tolpyralate、 甲基益發靈(tolylfluanid)、乙酸甲苯汞、苯吡唑草酮(topramezone)、肟草酮(tralkoxydim)、溴氯氰菊酯(tralocythrin)、泰滅寧(tralomethrin)、特拉瑞(tralopyril)、拜富寧(transfluthrin)、反氯菊酯(transpermethrin)、不孕津(tretamine)、三十烷醇(triacontanol)、三泰芬(triadimefon)、三泰隆(triadimenol)、triafamone、野麥畏(tri-allate)、威菌磷(triamiphos)、抑芽唑(triapenthenol)、苯蟎噻(triarathene)、嘧菌醇(triarimol)、醚苯磺隆(triasulfuron)、唑蚜威(triazamate)、葉鏽特(triazbutil)、三嗪氟草胺(triaziflam)、三落松(triazophos)、咪唑嗪(triazoxide)、苯磺隆(tribenuron)、苯磺隆-甲酯、脫葉磷(tribufos)、氧化三丁基錫、殺草畏(tricamba)、水楊菌胺(trichlamide)、三氯松(trichlorfon)、異皮蠅磷-3(trichlormetaphos-3)、毒壤膦(trichloronat)、綠草定(triclopyr)、綠草定-丁氧乙酯、綠草定-乙酯、三環吡菌威(triclopyricarb)、綠草定-三乙銨、三環唑(tricyclazole)、三得芬(tridemorph)、滅草環(tridiphane)、草達津(trietazine)、蝸螺淨(trifenmorph)、三氯丙氧磷(trifenofos)、三氟敏(trifloxystrobin)、三氟啶磺隆(trifloxysulfuron)、三氟啶磺隆-鈉、trifludimoxazin、triflumezopyrim、賽福座(triflumizole)、三福隆(triflumuron)、氟樂靈(trifluralin)、氟胺磺隆(triflusulfuron)、氟胺磺隆-甲酯、trifop、trifop-methyl、三氟禾草肟(trifopsime)、賽福寧(triforine)、三羥基三嗪、誘蠅羧酯(trimedlure)、混滅威(trimethacarb)、三甲隆(trimeturon)、抗倒酸(trinexapac)、抗倒酯(trinexapac-ethyl)、烯蟲硫酯(triprene)、弗草酮(tripropindan)、雷公藤內酯(triptolide)、草達克(tritac)、滅菌唑(triticonazole)、三氟甲磺隆(tritosulfuron)、trunc-call、烯效唑(uniconazole)、烯效唑-P、福美甲胂(urbacide)、烏瑞替派(uredepa)、戊酸酯、維利微素(validamycin)、霜黴滅(valifenalate)、異殺鼠酮(valone)、蚜滅多(vamidothion)、抑黴胺(vangard)、凡尼普羅(vaniliprole)、滅草猛(vernolate)、免克寧(vinclozolin)、華法林 (warfarin)、華法林-鉀、華法林-鈉、硝蟲硫磷(xiaochongliulin)、辛菌胺(xinjunan)、烯肟菌胺(xiwojunan)、XMC、二甲苯草胺(xylachlor)、二甲苯酚(xylenols)、滅殺威(xylylcarb)、yishijing、氰菌胺(zarilamid)、玉米素(zeatin)、增效胺(zengxiaoan)、ξ-賽滅寧(zeta-cypermethrin)、環烷酸鋅、磷化鋅、噻唑鋅、鋅乃浦(zineb)、益穗(ziram)、左拉普磷(zolaprofos)、座賽胺(zoxamide)、唑嘧磺隆(zuomihuanglong)、α-氯乙醇、α-蛻皮激素、α-multistriatin及α-萘乙酸。更多的資訊可查詢位於http://www.alanwood.net/pesticides/index.html之「COMPENDIUM OF PESTICIDE COMMON NAMES」。亦可查詢「THE PESTICIDE MANUAL」第15版,C D S Tomlin編,British Crop Production Council版權所有(2009),或其先前或最新的版本。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used in combination with one or more of the following compounds (such as in the form of a mixture of components, or simultaneously or sequentially): (3-ethoxy Propyl)mercury bromide, 1,2-dichloropropane, 1,3-dichloropropene, 1-methylcyclopropene, 1-naphthol, 2-(octylthio)ethanol, 2,3, 5-tri-iodobenzoic acid, 2,3,6-TBA, 2,3,6-TBA-dimethylammonium, 2,3,6-TBA-lithium, 2,3,6-TBA-potassium, 2 ,3,6-TBA-sodium, 2,4,5-T, 2,4,5-T-2-butoxypropyl, 2,4,5-T-2-ethylhexyl, 2, 4,5-T-3-butoxypropyl ester, 2,4,5-TB, 2,4,5-T-butoxymethyl ester, 2,4,5-T-butoxyethyl ester, 2,4,5-TB 4,5-T-butyl ester, 2,4,5-T-isobutyl ester, 2,4,5-T-isooctyl ester, 2,4,5-T-isopropyl ester, 2,4,5 -T-methyl ester, 2,4,5-T-pentyl ester, 2,4,5-T-sodium, 2,4,5-T-triethylammonium, 2,4,5-T-triethanolamine, 2,4-D, 2,4-D-2-butoxypropyl, 2,4-D-2-ethylhexyl, 2,4-D-3-butoxypropyl, 2,4 -D-ammonium, 2,4-DB, 2,4-DB-butyl ester, 2,4-DB-dimethylammonium, 2,4-DB-isooctyl ester, 2,4-DB-potassium, 2 ,4-DB-sodium, 2,4-D-butoxyethyl, 2,4-D-butyl ester, 2,4-D-diethylammonium, 2,4-D-dimethylammonium, 2 ,4-D-diethanolamine, 2,4-D-dodecylammonium, 2,4-DEB, 2,4-DEP, 2,4-D-ethyl, 2,4-D-heptylammonium , 2,4-D-isobutyl ester, 2,4-D-isooctyl ester, 2,4-D-isopropyl ester, 2,4-D-isopropylammonium, 2,4-D-lithium, 2,4-D-methylheptyl ester, 2,4-D-methyl ester, 2,4-D-octyl ester, 2,4-D-pentyl ester, 2,4-D-potassium, 2,4- D-propyl ester, 2,4-D-sodium, 2,4-D-tetrahydrofurfuryl ester, 2,4-D-tetradecylammonium, 2,4-D-triethylammonium, 2,4 -D-(2-hydroxypropyl)ammonium, 2,4-D-triethanolamine, 2iP, 2-methoxyethylmercury chloride, 2-phenylphenol, 3,4-DA, 3,4 -DB, 3,4-DP, 4-aminopyridine, 4-CPA, 4-CPA-diethanolamine, 4-CPA-potassium, 4-CPA-sodium, 4-CPB, 4-CPP, 4-hydroxybenzene Ethanol, 8-hydroxyquinoline sulfate, 8-phenylmercury oxyquinoline, abamectin, abscisic acid, ACC, acephate, acequinocyl, Acetamiprid (acetamiprid), housefly phosphorus (acethion), acetochlor (acetoc hlor), acetophos, acetoprole, acibenzolar, acibenzolar, acifluorfen, acifluorfen, acifluorfen -Methyl ester, acifluorfen-sodium, aclonifen, acrep, acrinathrin, acrolein, acrylonitrile, acypetacs , Alputac-copper, Alputac-zinc, afidopyropen, alachlor, alanycarb, albendazole, aldicarb , Aldimorph, aldoxycarb, aldrin, allethrin, allicin, allidochlor, allicin (allosamidin), alloxydim, alloxydim, allyl alcohol, allyxycarb, alorac, alpha- cypermethrin, alpha-cypermethrin Alpha- endosulfan, ametoctradin, ametridone, ametryn, amibuzin, amicarbazone, seed dressing Amicarthiazol, amidithion, amidoflumet, amidosulfuron, aminocarb, aminocyclopyrachlor, cyprodinil-methyl, Cyclopyrimidic acid-potassium, aminopyralid, chlorpyralid, chlorpyralid-potassium, chlorpyralid-ginseng (2-hydroxypropyl) ammonium, amiprofos-methyl, amine Amiprophos, amisulbrom, amiton, amidoxalate, amitraz, amitrole, ammonium sulfamate, α-naphthoacetic acid Ammonium, amobam, amprodronic acid (ampropylfos), anabasine, quinoasine sulfate, ancymidol, anilazine, anilofos, Anisuron, anthracene Quinone, antu, azophosazine (apholate), aramite, arsenic trioxide, asomate, aspirin, aspirin, asulam, oxaline-potassium, oxaline-sodium, ethyl acetonide Athidathion, atraton, atrazine, aureofungin, aviglycine, avidone hydrochloride, azaconazole, Azadirachtin, azafenidin, azamethiphos, azimsulfuron, azinphos-ethyl, azinphos-methyl, azamethiphos Aziprotryne, azithiram, azobenzene, azocyclotin, azothoate, azoxystrobin, bachmedesh, barban ), barium hexafluorosilicate, polybarium sulfide, barthrin, BCPC, beflubutamid, beflubutamid, benalaxyl, benalaxyl, benazolin, Meclofen-Dimethylammonium, Meclofen-ethyl, Meclofen-Potassium, Bencarbazone, Benclothiaz, Bendiocarb, Benfluralin, Benfuracarb, benfuresate, benodanil, benomyl, benomyl, benoxacor, benoxafos, benquinox, benzyl Bensulfuron (bensulfuron), bensulfuron-methyl-methyl, bensulide, bensultap, bentaluron, bentazone, bensulfuron-sodium, benzene Benthiavalicarb, benzalkonium isopropyl, benthiazole, bentranil, benzadox, benzalkonium, benzalkonium chloride chloride), benzenoic acid (benzamacril), benzenoic acid-isobutyl ester, benzamoorf, benzfendizone, benzipram, benzobicycloketone (benzobi cyclon), benzofenap, benzofluor, benzohydroxamic acid, benzovindiflupyr, benzoximate, benzoylprop , Xinyanling-ethyl ester, benzthiazuron, benzthiazuron, benzyl adenine, berberine, berberine chloride, beta-cyfluthrin, Beta-cypermethrin, bethoxazin, bicyclopyrone, bifenazate, bifenox, bifenthrin, pyrflunomide bifujunzhi), bilanafos, bilanafos-sodium, binapacryl, bingqingxiao, bioallethrin, bioethanomethrin, biochlorine Bipermethrin, bioresmethrin, biphenyl, bisazir, bismerthiazol, bispyribac, bispyribac-sodium, bistriflufenazone ( bistrifluron, bitertanol, bithionol, bixafen, blasticidin-S, borax, Bordeaux mixture , Boric acid, boscalid, brassinolide, brassinolide-ethyl ester, brevicomin, brodifacoum, brofenvalerate, Broflanilide, brofluthrinate, bromacil, bromacil, bromacil, bromadiolone, bromadiolone, bromethalin, bromacil Bromethrin, bromfenvinfos, bromoacetamide, bromobonil, bromobutide, bromocyclen, bromo-DDT, bromofenoxim ), bromophos, bromophos -Ethyl acetate, bromopropylate, bromothalonil, bromoxynil, bromoxynil butyrate, bromoxynil heptanoate, bromoxynil octanoate, bromoxynil- Potassium, brompyrazon, bromuconazole, bronopol, bucarpolate, bufencarb, buminafos, bupirimate , Buprofezin, Burgundy mixture, busulfan, butacarb, butachlor, butafenacil, butafenacil Phosphorus (butamifos), butathiofos, butenachlor, butethrin, buthidazole, butthiobate, buthiuron, butanone Butocarboxim, butonate, butopyronoxyl, butoxycarboxim, butralin, butroxydim, buturon, butyl Amine, butylate, cacodylic acid, cadusafos, cafenstrole, calcium arsenate, calcium chlorate, calcium cyanamide, calcium polysulfide, Calvinphos, cambendichlor, camphechlor, camphor, captafol, captan, carbamorph, chlorpheniramine Carbanolate, carbaryl, carbasulam, carbendazim, befentyl benzene sulfonate, befenty sulfite, carbetamide, carbetamide (carbofuran), carbon disulfide, carbon tetrachloride, carbophenothion, carbosulfan, carboxazole, carboxide, carboxin, azole Carfentrazone, carfentrazone-ethyl ester, carpropamid, cartap, perdan hydrochloride Salt, carvacrol, carvone, CDEA, cellocidin, CEPC, ceralure, Cheshunt mixture, chinomethionat , Chitosan, chlobenthiazone, chlomethoxyfen, chloralose, chloramben, chloramben, chloramben, chlobenthiazone , Chloramine-methyl, chloranben-methylammonium, chloramine-sodium, chloramine phosphorus, chloramphenicol, chloraniformethan, chloranil , Chloranocryl (chloranocryl), chlorantraniliprole, chlorazifop, propargyl propargyl, chlorazine, chlorbenside, chlorfenuron (chlorbenzuron), chlorbicyclen, chlorbromuron, chlorbufam, chlordane, chlordecone, chlordimeform, chlordimeform, hydrochloride , Chlorempenthrin (chlorempenthrin), chlorethoxyfos (chlorethoxyfos), chloreturon (chloreturon), chlorfenac (chlorfenac), valtrox-ammonium, valvax-sodium, chlorfenapyr , Chlorfenazole, chlorfenethol, chlorfenprop, chlorfenson, chlorfensulphide, chlorfenvinphos, chlorfluazuron, fluorine Chlorflurazole, chlorfluren, chlorflurenol, chlorflurenol, chlorflurazole, chloridazon, chlorimuron, chlorine Sumosulfuron ethyl ester, chlormephos, chlormequat, chlormequat chloride, chlornidine, Chlornitrofen, chlorobenzilate, chlorodinitronaphthalene, chloroform, chloromebuform, chloromethiuron, chloroneb, chlorhexidine (chlorophacinone), chlorhexidine sodium, chloropicrin, trichloropon, chloroprallethrin, chloropropylate, chlorothalonil ), chlorotoluron, chloroxuron, chloroxynil, chlorphonium, chlorphonium chloride, chlorphoxim ), chlorprazophos, chlorprocarb, chlorpropham, chlorpyrifos, talussone-methyl ester, chlorquinox, chlorsulfuron, chlorsulfuron Chlorthal, Dioxyl-dimethyl, Dioxyl-monomethyl ester, Chlorthiamid, Chlorthiophos, Chlozolinate, Choline Chloride, Ringworm Chromafenozide, cinerin I, cinerrin II, cinerrin, cinidon-ethyl, cinmethylin, cinosulfuron, Ciobutide, cisanilide, cismethrin, clacyfos, clacyfos, clacyfos, clacyfos, clacyfos, climbazole, clacyfos cliodinate), clodinafop, clodinafop, cloethocarb, clofencet, pyridazine-potassium, clofentezine, norsterol acid clofibric acid), clofop, isobutyl chloropropionate, clomazone, clomeprop, cloprop, cloproxydim ), Clopyralid, Clopyralid, Cloquintocet, Cloquintocet, Cloquintocet -Heptylester, cloransulam, cloransulam-methyl, closantel, clothianidin, clotrimazole, cloxyfonac , Citrus acid-sodium, CMA, codlelure, colophonate, copper acetate, copper acetyl arsenite, copper arsenate, basic copper carbonate, copper hydroxide, copper naphthenate , Copper oleate, alkaline copper oxychloride, copper silicate, copper sulfate, copper zinc chromate, coumachlor, coumafuryl, coumaphos, coumatetralyl ), coumithoate, coumoxystrobin, CPMC, CPMF, CPPC, credazine, cresol, crimidine, crotamiton, palatophos (crotoxyphos), crufomate, cryolite, cue-lure, cufraneb, cumyluron, cuprobam, cuprous oxide , Curcumenol, cyanamide, cyanatryn, cyanazine, cyanofenphos, cyanophos, cyanthoate, cyantraniliprole ), cyazofamid, cybutryne, cyclafuramid, cyclanilide, cyclaniliprole, cyclethrin, cyclafuramid (cycloate), cycloheximide, cycloprate, cycloprothrin, cyclopyrimorate, cyclosulfamuron, cycloxydim, Cycluron, cyenopyrafen, cyflufenamid, cyflumetofen, cyfluthrin, Cyhalodiamide, Cyhalofop, Cyhalofop, Cyhalothrin, Cyhexatin, Cymiazole, Cyhalofop Hydrochloride Salt, cymoxanil, cyometrinil, cypendazole, cypermethrin, cyperquat, chlorinated forage, cyphenothrin, cyclamate (cyprazine), cyprazole, cyproconazole, cyprodinil, cyprofuram, cypromid, cyprosulfamide ), cyromazine, cythioate, daimuron, dalapon, dalapon-calcium, dalapon-magnesium, dalapon-sodium, daminozide , Dayoutong, myron (dazomet), myron-sodium, DBCP, d-camphor, DCIP, DCPTA, DDT, debacarb, decafentin, carbofuran ( decarbofuran), dehydroacetic acid, delachlor, deltamethrin, demephion, decarbofuran-O, demephion-S, demeton, demeton -Methyl ester, systemic phosphorus-O, systemic phosphorus-O-methyl, systemic phosphorus-S, systemic phosphorus-S-methyl, demeton-S-methylsulphon, desmedipham , Desmetryn, d-trans chlorpropargyl (d-fanshiluquebingjuzhi), diafenthiuron, dialifos, di-allate, diamine Phosphorus (diamidafos), diatomaceous earth, diazinon, dibutyl phthalate, dibutyl succinate, dicamba, dicamba-diglycolamine, dicamba-dimethyl Ammonium, dicamba-diethanolamine, dicamba-isopropylammonium, dicamba-methyl ester, dicamba-ethanolamine, dicamba-potassium, dicamba-sodium, dicamba-triethanolamine, dicapthon , Dichlobenil, dichlobentiazox, dichlofenthion, dichlofen luanid), dichlone, dichloralurea, dichlorbenzuron, dichlorflurenol, dichloroquinol-methyl, dichlormate, dichloralurea Allylamine (dichlormid), dichlorophen (dichlorophen), dichlorprop, 2-ethylhexyl dipropionate, dipropionic acid-butoxyethyl, dichlorophen Propionic acid-ethylammonium, drip propionic acid-isooctyl ester, drip propionic acid-methyl ester, drip propionic acid-P, drip propionic acid-P-2-ethylhexyl, drip propionic acid-P-dimethyl Ammonium, tripropionate-potassium, tripropionate-P-potassium, tripropionate-P-sodium, tripropionate-sodium, dichlorvos, dichlozoline, benzylchlorotriazole ( diclobutrazol), diclocymet, diclofop, diclofop-methyl, diclomezine, diclomezine-sodium, dicloran, diclofop ( dicloromezotiaz), diclosulam (diclosulam), dicofol, dicoumarol, diclotophos, dicyclanil, diclotophos Dicyclonon, dieldrin, dienochlor, diethamquat, diethyl herbicide dichloride, diethatyl, dieldrin, dienochlor Diethofencarb, dietholate, diethyl pyrocarbonate, diethyltoluamide, difenacoum, difenoconazole, difenopenten, flufenopenten Ethyl enoate, difenoxuron, difenzoquat, difenzoquat metilsulfate, difethialone, diflovidazin, diflubenzuron ), diflufenican (diflufenican), diflufenzopyr, diflufenican-sodium, diflumetorim, dikegulac, diflufenican-sodium, dihyprophylline (dilor), dimatif, dimefluthrin , Dimefox, dimefuron, dimepiperate, dimetachlone, dimetan, dimethacarb, dimethachlor , Dimethametryn, Dimethenamid, Dimethenamid-P, Dimethipin, Dimethirimol, Dimethoate, Dimethenamid Dimethomorph, dimethrin, dimethyl carbate, dimethyl phthalate, dimethylvinphos, dimetilan, dimexano , Dimidazon, dimoxystrobin, dinex, diclexine, dingjunezuo, diniconazole, darkeli-M, dinitramine, Dinobuton, dinocap, dinocap-4, dinocap-6, dinocton, dinofenate, dinopenton, propionol dinoprop), dinoprop, dinosam, dinosab, dinosyl acetate, dinosult-ammonium, dinoss-diethanolamine, dinosal-sodium, disspros-triethanolamine, Dinosulfon (dinosulfon), dinotefuran (dinotefuran), telofol (dinoterb), telofol acetate, dinoterbon, diofenolan, dioxabenzofos, dioxy Dioxacarb, dioxathion, diphacinone, diphenamid, diphenamid, dipropalin, dipropetryn , Dipymetitrone, dipyrithione, diquat, diquat dibromide, female gypsy moth attractant (disparlure), disul, disulfiram, disulfiram (disulfoton), thiasone-sodium, ditalimfos, dithianon, dithicrofos, dithicrofos oether), dithiopyr, diuron, d-limonene, DMPA, DNOC, DNOC-ammonium, DNOC-potassium, DNOC-sodium, dodemorph, dodemorph acetic acid Ester, mobendazim benzoate, dodicin, dodecin hydrochloride, dodecine-sodium, dodine, dofenapyn, dominicalure ), doramectin, drazoxolon, DSMA, dufulin, EBEP, EBP, ecdysterone, edifenphos, eglinazine, glycyrrhizin Kusatsu-ethyl ester, emmentin (emamectin), imametine benzoate, EMPC, empenthrin, endosulfan, endothal, oxodoxol-diammonium , Hordoxol-dipotassium, hordoxol-disodium, endothion, endrin, enestroburin, enoxastrobin, EPN, epocholeone ), epofenonane, epoxiconazole, eprinomectin, sulfentrazone (epronaz), ε-metofluthrin (epsilon-metofluthrin), ε-momfluorothrin, EPTC, erbon, ergocalciferol, erlujixiancaoan, esdépalléthrine, esfenvalerate, esprocarb, Ethyl silicon (etacelasil), etaconazole (etaconazole), etaphos (etaphos), sulphur (etem), ethaboxam (ethaboxam), ethalamine (ethachlor), ethalfluralin (ethalfluralin) , Ethametsulfuron, ethametsulfuron-methyl, ethaprochlor, ethephon, ethidimuron, ethiofencarb, imidacarb (ethiolate), ethion, ethiozin, ethiprole, ethirimol, ethion hoate-methyl), ethofumesate, ethohexadiol, ethoprophos, ethoxyfen, chloroflufen-ethyl, ethoxyquin, Ethoxysulfuron, ethychlozate, ethyl formate, ethyl α-naphthalene, ethyl-DDD, ethylene, ethylene dibromide, ethylene dichloride, ethylene oxide, and allicin (ethylicin), 2,3-dihydroxypropyl mercaptan ethyl mercury, ethyl mercury acetate, ethyl mercury bromide, ethyl mercury chloride, ethyl mercury phosphate, etinofen (etinofen), acetochlor Etnipromid, etobenzanid, etofenprox, etoxazole, etridiazole, etrimfos, eugenol, EXD , Famoxadone, famphur, fenamidone, fenaminosulf, fenaminstrobin, fenamiphos, fenapanil , Fenarimol, fenasulam, fenazaflor, fenazaquin, fenbuconazole, fenbutatin oxide, fenchlorazole ), fenfluthrin-ethyl ester, fenchlorphos, fenclorim, fenethacarb, fenfluthrin, fenfuram, cyclamate Fenhexamid, fenitropan, fenitrothion, fenjuntong, fenobucarb, fenoprop, fenoprop, and 3-butoxypropionate Ester, Alproic acid-Butoxymethyl, Alproic acid-Butoxyethyl, Alproic acid-Butyl, Alproic acid-isooctyl, Alproic acid-methyl, Alproic acid-potassium, Phenyl sulfide Fenothiocarb, fenoxacrim, fenoxanil, fenoxaprop, fenoxaprop-ethyl, fenoxaprop-P, fenoxaprop Fenoxaprop-P-ethyl ester, fenoxasulfone, fenoxycarb, seed dressing (f enpiclonil), fenpicoxamid, fenpirithrin, fenpropathrin, fenpropidin, fenpropimorph, fenpyrazamine, fenpyroximate, fenquinotrione, fenquinotrione Fenridazon, pyridazinon androgen-potassium, pyridazinonin androgen-propyl ester, fenson, fensulfothion, fenteracol, thiazolin Fenthiaprop, thiazoxyprop-ethyl, fenthion, fenthion-ethyl, fentin, triphenyltin acetate, triphenyltin chloride, triphenyltin hydroxide , Fentrazamide, fentrifanil, fenuron, fenuron TCA, fenvalerate, ferbam, ferimzone, sulfuric acid Ferrous, fipronil, flamprop, flamyl-isopropyl, flamyl-M, flamyl-methyl, flamyl-M-isopropyl, flamprop Lin-M-methyl, pyrimsulfuron (flazasulfuron), flocoumafen (flocoumafen), flometoquin, flonicamid (flonicamid), diflufentrazone (florasulam), florpyrauxifen (florpyrauxifen), pyrimidine Fluacrypyrim (fluacrypyrim), fluazaindolizine, fluazifop (fluazifop), voyophore-butyl ester, voyophore-methyl ester, voyophore-P, voyophore-P-butyl ester, fluazinam (fluazinam) , Fluazolate, fluazuron, flubendiamide, flubenzimine, flucarbazone, flucarbazone-sodium, fluazuron Flucetosulfuron, fluchloralin, flucofuron, flucycloxuron, flucythrinate, fludioxonil, fluenetil, fluthiocarbazone Fluensulfone, flufenacet, flufenerim, flufenican, flufenox uron), flufenoxystrobin (flufenoxystrobin), trifluoroether (flufenprox), flufenpyr (flufenpyr), flupyridazine-ethyl, butene fipronil (flufiprole), fluhexafon, fluorochlorobenzene Pyrethrin, flumetover, flumetralin, flumetsulam, flumezin, flumiclorac, flumetralin , Flumioxazin, flumipropyn, flumorph, fluometuron, fluopicolide, fluopyram, fluopyram Fluorbenside, fluoridamid, fluoroacetamide, fluorodifen, fluoroglycofen, fluoroglycofen, fluoroglycofen-ethyl, carfentrazone fluoroimide, fluoromidine, fluoronitrofen, fluothiuron, fluotrimazole, fluoxastrobin, flupoxam, flupropacil, Flupropadine, flupropanate, tetrafluoropropionate-sodium, flupyradifurone, flupyrsulfuron, flupyrsulfuron-methyl, flupyrsulfuron-methyl -Sodium, fluquinconazole, flurazole, flurenol, imambutazone-butyl, imambutazone-methyl, fluridone, flurazole (flurochloridone), fluroxypyr, fluroxypyr, fluroxypyr, fluroxypyr-methylheptyl, flurprimidol, flursulamid, flurtamone , Flusilazole, flusulfamide, fluthiacet, fluthiacet, flutianil, flutolanil, flutriafol, fluthiacet Fluvalinate, fluxametamide, fluvalinate (fl uxapyroxad), fluxofenim, folpet, fomesafen, fomesafen-sodium, fonofos, foramsulfuron, clopyr Urea (forchlorfenuron), formaldehyde, formetanate, forchlorfenuron hydrochloride, formothion, formparanate, fosamine hydrochloride, fosamine, wood Phosphine-ammonium, fosetyl, fosmethilan, fosmethilan, fospirate, fosthiazate, fosthietan, frotalin frontalin, fuberidazole, fucaojing, fucaomi, funaihecaoling, fuphenthiourea, furalane , Furalaxyl, furamethrin, furametpyr, furathiocarb, furcarbanil, furconazole, fluconazole Azole, furethrin, furfural, furilazole, furmecyclox, furophanate, furyloxyfen, γ-xeronin gamma-cyhalothrin), γ-HCH, genit, gibberellic acid, gibberellins, gliftor, glufosinate, glufosinate-ammonium , Glufosinate-P, glufosinate-P-ammonium, glufosinate-P-sodium, glyodin, glyoxime, glyphosate, glyphosate-diammonium , Glyphosate-dimethylammonium, glyphosate-isopropylammonium, glyphosate-monoammonium, glyphosate-potassium, glyphosate-sesquisodium, glyphosate-trimethylsulfur, grass Glyphosine, gossyplure, grandlure, griseofulvin, guazatine, biguanoctyl acetate, quinolinyl acrylate ( halacrinate), halauxifen, fluclopyridine (halauxi fen-methyl), halfenprox, halofenozide, halosafen, halosulfuron, chlorpyrisulfuron-methyl, halofenozide haloxydine), haloxyfop, haloxyfop, haloxyfop-ethoxyethyl, haloxyfop-methyl, haloxyfop-P, haloxyfop -P-ethoxyethyl, haloxyfop-P-methyl, haloxyfop-P-methyl, haloxyfop-sodium, HCH, hexamethylmelamine (hemel), hexamethylphos (hempa), HEOD, Febuda ( heptachlor), heptafluthrin, heptenophos, heptopargil, herbimycin, heterophos, hexachloroacetone, hexachlorobenzene, hexachlorobutadiene, hexachloro Phenol, hexaconazole, hexaflumuron, potassium hexaflurate, hexalure, hexamide, hexazinone, hexylthiofos, hexylthiofos (hexythiazox), HHDN, holosulf, huancaiwo, huangcaoling, huanjunzuo, hydramethylnon, hydrargaphen, slaked lime, hydrogen cyanide, hydroprene , Hymexazol, hyquincarb, IAA, IBA, icaridin, imazalil, imazalil nitrate, imazalil sulfate, imazamethabenz ), imazamox-methyl, imazamox (imazamox), imazamox-ammonium, imazapic (imazapic), imazamox-ammonium, imazapyr, imi Imazaquin, imazaquin, imazaquin-ammonium, imazaquin-methyl, imazaquin-sodium, imazethapyr, imazaquin-ammonium, zolpyrazine Imazosulfuron, imibenconazole, imicyafos, imidacloprid, imidaclothiz, iminoctadine, iminoctadine triacetate, imidacloprid Alkylbenzene sulfonate, imipothrin, inabenfide, indano fan), indaziflam, indoxacarb, inezin, iodobonil, iodocarb, methyl iodide, iodosulfuron, iodosulfuron -Methyl, iodosulfuron-methyl-sodium, iofensulfuron, iofensulfuron-sodium, ioxynil, ioxynil, octanoate, iodobenzonitrile-lithium, iodobenzonitrile-sodium, ipazine , Ipconazole, ipfencarbazone, ipfentrifluconazole, iprobenfos, iprodione, iprovalicarb, c Iprymidam, ipsdienol, ipsenol, IPSP, isamidofos, isazofos, isobenzan, isocarbamid, water Isocarbophos, isocil, isodrin, isofenphos, isofenphos-methyl, isofetamid, isolan ), isomethiozin, isonoruron, isopolinate, isoprocarb, isopropalin, isoprothiolane, isoproturon, pyridine Pyraclostrobin (isopyrazam), isopyrimol, isothioate, isotianil, isouron, isovaledione, isooxaben, isooxaben Isoxachlortole, isoxadifen, isoxadifen, isoxaflutole, isoxaflutole, isoxapyrifop, isoxathion, ivi Ivermectin, soaking phosphorus (izopamfos), japonilure, japothrins, jasmolin I, jasmolin II, jasmonic acid, jiahuangchongzong , Methyl synergist (jiajizengxia olin), jiaxiangjunzhi, jiecaowan, jiecaoxi, jodfenphos, juvenile hormone I, juvenile hormone II, juvenile hormone III, thien chrysanthemum Esters (kadethrin), κ-bifenthrin (kappa-bifenthrin), κ-tefluthrin (kappa-tefluthrin), karbutilate, karetazan, karetazan-potassium, kasugamycin, kasugamycin salt Acid salt, kejunlin, kelevan, ketospiradox, ketospiradox-potassium, kinetin, kinoprene, kresoxim-methyl, quinine Kuicaoxi, lactofen, lambda-cyhalothrin, lancotrione, latilure, lead arsenate, lenacil, Lepidium Lepimectin, leptophos, lindane, lineatin, linuron, lirimfos, sex attractant (litlure), looplure, lufenuron, lvdingjunzhi, lvxiancaolin, lythidathion, MAA, malathion (malathion), maleic hydrazine, malonoben, maltodextrin, MAMA, mancopper, mancozeb, mandestrobin , Mandipropamid, maneb, matrine, mazidox, MCPA, MCPA-2-ethylhexyl ester, MCPA-butoxyethyl, MCPA -Butyl ester, MCPA-dimethylammonium, MCPA-diethanolamine, MCPA-ethyl, MCPA-isobutyl, MCPA-isooctyl, MCPA-isopropyl, MCPA-methyl, MCPA-ethanolamine, MCPA- Potassium, MCPA-sodium, MCPA-thioethyl, MCPA-triethanolamine, MCPB, MCPB-ethyl, MCPB-methyl, MCPB-sodium, mebenil, mebenil (mecarbam), mecarbinzid, mecarphon, 2-methyl-4-chloropropionic acid (mecoprop), 2-methyl-4-chloropropionic acid-2-ethylhexyl ester, 2-methyl-4 -Chloropropionic acid-dimethylammonium, 2-methyl-4-chloropropionic acid-diethanolamine, 2-methyl-4-chloropropionic acid-ethylene diester, 2-methyl-4-chloropropionic acid-isooctyl ester , 2-methyl-4-chloropropionic acid-methyl ester, 2-methyl-4-chloropropionic acid-P, 2-methyl-4-chloropropionic acid-P-2-ethylhexyl ester, 2-methyl-4 -Chloropropionic acid-P-dimethylammonium, 2-methyl-4-chloropropionic acid-P-isobutyl ester, 2-methyl-4-chloropropionic acid-potassium, 2-methyl-4-chloropropionic acid- P-potassium, 2-methyl-4-chloropropionic acid-sodium, 2-methyl-4-chloropropionic acid-triethanolamine, medimeform, medinoterb, dioxin acetate, Medlure, mefenacet, mefenpyr, mefentrifluconazole, mefentrifluconazole, mefluidide, Fomesafen-diethanolamine, fomesafen-potassium, megatomoic acid, menazon, mepanipyrim, meperfluthrin , Mephenate, mephosfolan, mepiquat, mepiquat, mepiquat, mepronil, meptyldinocap, mercuric chloride, mercuric oxide, chlorine Mercurous, merphos, mesoprazine, mesosulfuron, mesosulfuron-methyl, mesotrione, mesulfen , Mesulfenfos, metaflumizone, metalaxyl, metaldehyde-M, metaldehyde, metam, metaflumizone, metaldehyde Metamifop, metamitron, metazac-potassium, metazac-sodium, metazachlor, metazosulfuron (metazosulfuron), metachlordichlor Ketones (metazoxolon), metconazole, metepa, metflurazon, methabenzthiazuron, methacrifos, methoproplatin (methalpropal in), methamidophos, methasulfocarb, methazole, methfuroxam, methidathion, methobencarb, methocarb ), methiopyrisulfuron (methiopyrisulfuron), methiotepa (methiotepa), metiozolin, methiuron, methocrotophos, methometon, methomyl, Methoprene, methoprotryne, methoquin-butyl, methotthrin, methoxychlor, methoxyfenozide, weed Methoxyphenone, methyl apholate, methyl bromide, methyl eugenol, methyl iodide, methyl isothiocyanate, methylacetophos, methyl Chloroform, methyldymron (methyldymron), dichloromethane, methylmercury benzoate, methylmercury dicyandiamide, methylmercury pentachlorophenoxide, methyl neodecylamide, avoid bad (metiram), metobenzuron, metobromuron, metofluthrin, metolachlor, metolcarb, metominostrobin ), metosulam, metoxadiazone, metoxuron, metrafenone, metribuzin, metsulfovax, metsulfuron ), metsulfuron-methyl, mevinphos, mexacarbate, mieshuan, milbemectin, milbemycin oxime, milneb , Propylamine fluoride (mipafox), mirex, MNAF, moguchun, molinate , Molosultap, momfluorothrin, monalide, monisouron, monochloroacetic acid, monocrotophos, monolinuron, monosulfuron ), monosulfuron-ester, monuron, monuron TCA, morfamquat, morfamquat dichloride, moroxydine, morpholinamidoguanidine hydrochloride , Morphothion, morzid, moxidectin, MSMA, housefly attractant (muscalure), myclobutanil, myclozolin, N-(ethylmercury)-p-toluene Sulfanilide, nabam, naftalofos, naled, naphthalene, naphthylacetamide, naphthalenedicarboxylic anhydride, naphthoxyacetic acid, naproanilide, diquat Napropamide, napropamide-M, naphtochlor (naptalam), naphthachlor sodium, natamycin, neburon, niclosamide, niclosamide -Ethanolamine, nicosulfuron, nicotine, nifluridide, nipyraclofen, nitenpyram, nithiazine, nitralin ), nitrapyrin, nitrilacarb, nitrofen, nitrofluorfen, nitrostyrene, nitrothal-isopropyl, norbormide , Norflurazon, nornicotine, noruron, novaluron, noviflumuron, nuarimol, OCH, octachlorodipropyl ether , Octhilinone, ofurace, omethoate, orbencarb, orfralure, o-dichlorobenzene, orthosulfamuron, oryctalure, orysastrobin, oryzalin, osthol, ostramone, oxabetrinil, c Oxadiargyl, oxadiazon, oxadixyl, oxamate, oxamyl, oxapyrazon, oxadiazon, oxadiazon Amine, oxasulfuron-sodium, oxasulfuron, oxathiapiprolin, oxaziclomefone, oxine-copper, oxolinic acid, Oxpoconazole, oxpoconazole fumarate, oxycarboxin, oxydemeton-methyl, oxydeprofos, oxydisulfoton, oxyfluoride Oxyfluorfen, oxymatrine, oxytetracycline, oxytetracycline hydrochloride, paclobutrazol, paichongding, p-dichlorobenzene, p-fluron ( parafluron), paraquat, paraquat dichloride, parafluron dimethyl sulfate, parathion, parafluron-methyl, parinol, parinol (pebulate), pefurazoate, pelargonic acid, penconazole, pencycuron, pendimethalin, penflufen, hexaflumuron (penfluron), penoxsulam, pentachlorophenol, pentachlorophenyl laurate, pentanochlor, penthiopyrad, pentmethrin, cyclic Penoxazone, perfluidone, permethrin, pethoxamid, phenamacril, phenazine oxide, phenisopham ), phenkapton, phenmedipham, betainin-ethyl ester, phenobenzuron, phenothrin, phenproxide, phenthoate, Phenylmercuriurea (phenylmercuriurea), phenylmercuric acetate, phenylmercury chloride, o-benzene Phenylmercury derivatives of diphenols, phenylmercury nitrate, phenylmercury salicylate, phorate, phosacetim, phosalone, phosdiphen, sulfur ring Phosfolan, phosphos-methyl, phosglycin, phosmet, phosnichlor, phosphamidon, phosphine, phosphocarb , Phosphorus, phostin, phoxim, phoxim, phthalide, picarbutrazox, picloram, clopyral -2-ethylhexyl ester, clopyralic acid-isooctyl ester, clopyralic acid-methyl ester, clopyralic acid-ethanolamine, clopyralic acid-potassium, clopyralic acid-triethylammonium, amine chloride Pyridine acid-ginseng (2-hydroxypropyl) ammonium, picolinafen (picolinafen), picoxystrobin (picoxystrobin), rodentone (pindone), rodentone-sodium, pinoxadcn, Piperalin, piperonyl butoxide, piperonyl cyclonene, piperophos, piproctanyl, piperonyl bromide, synergistic aldehyde (piprotal), pirimetaphos, pirimicarb, pirimioxyphos, pirimiphos-ethyl, pirimiphos-ethyl, triclosan-methyl, triclosan (plifenate), polyurethane, polyoxins, polyoxorim, polyoxorim, zinc, polythialan, potassium arsenite, potassium azide , Potassium cyanate, potassium gibberellate (potassium gibberellate), potassium naphthenate, potassium polysulfide, potassium thiocyanate, potassium α-naphthalene acetate, pp'-DDT, prallethrin, precociousin I ( precocene I), precocin II, precocin III, pretilachlor, primidophos, primisulfuron, flumesulfuron-methyl, probenazole, imidazole Prochloraz, imidamide-manganese, proclonol, procyazine, procymidone, profluramine (pr odiamine), profenofos, profluazol, profluralin, profluthrin, profoxydim, proglinazine, profluazol Ethyl-ethyl, prohexadione, prohexadione, prohydrojasmon, promacyl, promecarb, prometon, prometryn , Promurit, propachlor, propamidine, propamidine dihydrochloride, propamocarb, propamocarb hydrochloride, propanil, Propaphos, propaquizafop, propargite, proparthrin, propazine, propetamphos, propham, propargite propiconazole, propineb, propisochlor, propoxur, propoxycarbazone, propoxycarbazone-sodium, propyl isome, propyl Propyrisulfuron, propyzamide, proquinazid, prosuler, prosulfalin, prosulfocarb, flusulfuron prosulfuron), prothidathion, prothiocarb, prothioconazole hydrochloride, prothioconazole, prothiofos, prothoate, pyrethrum Protrifenbute, proxan, protrifenbute-sodium, prynachlor, pydanon, pydiflumetofen, pyflubumide, pymetrozine, pyracarbolid, pyrazole Pyraclofos, pyraclonil, pyraclostrobin, pyraflufen, pyraflufen-ethyl, fipronil (pyrafluprole), pyrafluprole (py Ramat, pyrametostrobin, pyraoxystrobin, pyrasulfotole, pyraziflumid, pyrazolynate, pyrazophos, pyrazosulfuron, Pyrimsulfuron-ethyl, pyrazothion, pyrazoxyfen, pyresmethrin, pyrethrin I, pyrethrin II, pyrethrins, isoprofen (pyribambenz-isopropyl), pyribambenz-propyl, pyribencarb, pyribenzoxim, pyributicarb, pyriclor, bidaben ( pyridaben, pyridafol, pyridalyl, pyridaphenthion, pyridate, pyridinitril, pyrifenox, pipefloquine Hydrazone (pyrifluquinazon), pyriftalid, pyrimethanil, pyrimidifen, pyriminobac, pyriminobac-methyl, pyriminobac-methyl, pyriminobac-methyl pyriminostrobin, pyrimisulfan, pyrimitate, pyrinuron, pyriofenone, pyriprole, pyripropanol, pyriproxyfen, pyriprofen Pyrisoxazole, pyrithiobac, pyrithiobac-sodium, pyrolan, pyroquilon, pyroxasulfone, pyroxsulam, Pyroxychlor, pyroxyfur, quassia, quinacetol, quinacetol, quinalphos, quinalphos, quinalphos -Methyl esters, quinazamid, quinclorac, quinconazole, quinmerac, quinazamid Quinoclamine, quinofumelin, quinonamid, quinothion, quinoxyfen, quintiofos, quintozene, quizalofop , Quizalofop-ethyl, quizalofop-P-ethyl, quizalofop-P-tefuryl, quwenzhi, quyingding, pyridine Rabenzazole, rafoxanide, rebemide, rescalure, resmethrin, rhodethanil, rhodojaponin-III, ribavirin, Rimsulfuron, rotenone, ryania, saflufenacil, saijunmao, saisentong, salicylaniline, blood root Alkali (sanguinarine), Santonin (santonin), Octamethphos (schradan), Squill glucoside (scilliroside), Sebuthylazine, Sebuthylazine, secbumeton, sedaxane, sedaxane Selamectin, semiformamidine (semiamitraz), monoformamidine hydrochloride (semiamitraz chloride), sesamex, sesamolin, sethoxydim, methamidophos (shuangjiaancaolin), siduron, siglure, silafluofen, silatrane, silicone, silthiofam, simazine, silicofluoride Simeconazole, simeton, simetryn, sintofen, SMA, S-metolachlor, sodium arsenite, sodium azide, Sodium chlorate, sodium fluoride, sodium fluoroacetate, sodium hexafluorosilicate, sodium naphthenate, sodium o-phenylphenol, sodium pentachlorophenol, sodium polysulfide, sodium thiocyanate, sodium α-naphthaleneacetate, threon Sophamide, spinetoram, spinosad, spirodiclofen, spiromesifen (sp iromesifen, spirotetramat, spiroxamine, streptomycin, streptomycin sesquisulfate, strychnine, sulcatol , Sulcofuron, sulcofuron-sodium, sulcotrione, sulfallate, sulfentrazone, sulfiram, sulfluramid ), sulfometuron, metsulfuron-methyl, sulfosulfuron, sulfotep, sulfoxaflor, sulfoxime, sulfoxime ), sulfur, sulfuric acid, thiofluoride, sulglycapin, sulprofos, sultropen, swep, tau-fluvalinate, tavron , Tazimcarb, TCA, TCA-ammonium, TCA-calcium, TCA-ethylene glycol, TCA-magnesium, TCA-sodium, TDE, tebuconazole, tebufenozide, tebufenozide (tebufenpyrad), tebufloquin, tebupirimfos, tebutam, tebuthiuron, tecloftalam, tecnazene, Tecoram, teflubenzuron, tefluthrin, tefuryltrione, tembotrione, temephos, tepa, TEPP , Tepraloxydim, terallethrin, terbacil, terbucarb, terbuchlor, terbufos, terallethrin Terbumeton, terbuthylazine, terbutryn, tetcyclacis, tetrachloroethane, tetrachlorvinphos, tetraconazole, tetradifon ), tetrafluron, tetram ethrin), tetrafluthrin (tetramethylfluthrin), tetraamine, miticidin (tetranactin), tetraniliprole, tetrasul, thallium sulphate, thenylchlor, Theta-cypermethrin, thiabendazole, thiacloprid, thiadifluor, thiamethoxam, thiapronil, thiazafluron ), thiazopyr, thicrofos, thicyofen, thidiazimin, thidiazuron, thiencarbazone, thiencarbazone Methyl methyl, thifensulfuron (thifensulfuron), thifensulfuron-methyl, thifluzamide, thiobencarb, thiocarboxime, thiochlorfenphim, sulfur Thiocyclam, thiocyanate hydrochloride, thiodiazole oxalate, thiodiazole-copper, thiodicarb, thiofanox, thiofluoximate ), thiohempa, thiomersal, thiometon, thionazin, thiophanate, thioquinox , Thiosemicarbazide (thiosemicarbazide), thiosultap, bis-diammonium, bis-di-sodium, bis-mono-sodium, thiotepa, thiram, Thuringiensin, tiadinil, tiafenacil, tiaojiean, tiocarbazil, tioclorim, tioxazafen, tioxymid, tirpate, deoxy Tolclofos-methyl, tolfenpyrad, tolprocarb, tolpyralate, tolylfluanid, tolylfluanid, toluene mercury acetate, topramezone , Tralkoxydim (tralkoxydim), deltacythrin (tralocythrin), tymening (tralomethrin), tralopyril (tralopyril), transfluthrin (transfluthrin), transpermethrin (transpermethrin), infertility (tretamine), Triacontanol, triadimefon, triadimenol, triafamone, tri-allate, triamiphos, triapenthenol, benzalkonium triarathene, triarimol, triasulfuron, triazamate, triazbutil, triaziflam, triazophos, imidazosin (triazoxide), tribenuron, tribenuron-methyl, tribufos, tributyltin oxide, tricamba, trichlamide, trichlorfon , Trichlormetaphos-3, trichloronat, triclopyr, triclopyr-butoxyethyl, triclopyr-ethyl, triclopyricarb ), triclopyr-triethylammonium, tricyclazole, triidemorph, tridiphane, trietazine, trifenmorph, trichloroproxen (trifenofos), trifloxystrobin, trifloxysulfuron, trifloxysulfuron-sodium, trifludimoxazin, triflumezopyrim, triflumizole, triflumuron, trifluralin ( trifluralin, triflusulfuron, triflusulfuron-methyl, trifop, trifop-methyl, trifopsime, triforine, trihydroxytriazine, flytrap (trimedlure), trimethacarb, trimeturon, trinexapac, trinexapac-ethyl, trimethacarb (trip rene), tripropindan, triptolide, tritac, triticonazole, tritosulfuron, trunc-call, uniconazole , Uniconazole-P, urbacide, uredepa, valerate, validamycin, valifenalate, valone, aphid Vamidothion, vangard, vaniliprole, vernolate, vinclozolin, warfarin, warfarin-potassium, warfarin- Sodium, xiaochongliulin, xinjunan, xiwojunan, XMC, xylachlor, xylenols, xylylcarb, yishijing , Zarilamid, zeatin, zengxiaoan, ξ-cypermethrin, zinc naphthenate, zinc phosphide, zinc thiazole, zineb , Ziram, zolaprofos, zoxamide, zuomihuanglong, α-chloroethanol, α-ecdysone, α-multistriatin and α-naphthoacetic acid. For more information, please refer to "COMPENDIUM OF PESTICIDE COMMON NAMES " at http://www.alanwood.net/pesticides/index.html. You can also check the 15th edition of "THE PESTICIDE MANUAL ", edited by CDS Tomlin, copyrighted by the British Crop Production Council (2009), or its previous or latest version.

於另一實施例中,式1及/或式2之分子亦可與一或多種生物殺蟲劑組合使用(諸如以組分混合物形式、或同時或依序施用)。術語「生物殺蟲劑」一詞用於以與化學殺蟲劑相似的方式施用的微生物害蟲防治劑。其通常為細菌,但亦存在真菌防治劑之實例,包括木黴菌屬(Trichoderma spp.)及白粉寄生孢(Ampelomyces quisqualis)(葡萄白粉病之防治劑)。枯草桿菌係被用來防治植物病原體。野草及嚙齒動物已亦使用微生物劑防治。一種熟知的殺昆蟲劑實例為蘇力菌(Bacillus thuringiensis),亦即鱗翅目(Lepidoptera)、鞘翅目(Coleoptera)及雙翅目(Diptera)之細菌疾病。因為其對其他生物體幾乎無影響,所以其視為比合成殺蟲劑更環保。生物殺昆蟲劑包括基於以下之產品:昆蟲病原真菌(例如綠僵菌(Metarhizium anisopliae));昆蟲病原線蟲(例如夜蛾斯氏線蟲(Steinernema feltiae);及昆蟲病原病毒(例如蘋果蠹蛾顆粒體病毒(Cydia pomonella granulovirus))。 In another embodiment, the molecules of Formula 1 and/or Formula 2 may also be used in combination with one or more biological insecticides (such as in the form of a mixture of components, or applied simultaneously or sequentially). The term "biological insecticide" is used for microbial pest control agents that are applied in a manner similar to chemical insecticides. It is usually a bacterium, but there are also examples of fungal control agents, including Trichoderma spp. and Ampelomyces quisqualis (a control agent for grape powdery mildew). The Bacillus subtilis strain is used to control plant pathogens. Weeds and rodents have also been controlled with microbial agents. An example of a well-known insecticide is Bacillus thuringiensis , namely Lepidoptera, Coleoptera, and Diptera bacterial diseases. Because it has almost no effect on other organisms, it is considered to be more environmentally friendly than synthetic pesticides. Bioinsecticides include products based on: insect pathogenic fungi (such as Metarhizium anisopliae ); entomopathogenic nematodes (such as Steinernema feltiae ); and insect pathogenic viruses (such as codling moth granules) Virus ( Cydia pomonella granulovirus )).

昆蟲病原生物體之其他實例包括(但不限於)桿狀病毒、細菌及其他原核生物體、真菌、原蟲及微孢子蟲(Microsproridia)。生物學衍生之 殺昆蟲劑包括(但不限於)魚藤精(rotenone)、藜蘆定鹼(veratridine)以及微生物毒素;昆蟲耐受性或抗性植物品種;及藉由重組DNA技術修飾之生物體以產生殺昆蟲劑或將抗昆蟲特性傳輸至經遺傳修飾生物體。於一實施例中,式1及/或式2之分子可與種子處理及土壤改良領域中之一或多種生物殺蟲劑一起使用。The Manual of Biocontrol Agents給出可用生物殺昆蟲劑(及其他基於生物學之防治)產品之綜述。Copping L.G.(編)(2004).The Manual of Biocontrol Agents(原名Biopesticide Manual)第3版.British Crop Production Council(BCPC),Farnham,Surrey UK。 Other examples of entomopathogenic organisms include, but are not limited to, baculovirus, bacteria and other prokaryotic organisms, fungi, protozoa, and Microsproridia. Biologically derived insecticides include (but are not limited to) rotenone, veratridine and microbial toxins; insect-tolerant or resistant plant species; and organisms modified by recombinant DNA technology To produce insecticides or transmit insect-resistant properties to genetically modified organisms. In one embodiment, the molecules of Formula 1 and/or Formula 2 can be used with one or more biological pesticides in the field of seed treatment and soil improvement. The Manual of Biocontrol Agents gives an overview of available bioinsecticides (and other biologically based control) products. Copping LG (ed.) (2004). The Manual of Biocontrol Agents (formerly known as Biopesticide Manual ) 3rd edition. British Crop Production Council (BCPC), Farnham, Surrey UK.

於另一實施例中,以上可能的組合可以廣泛多種重量比使用。例而言,一種兩組分混合物,式1及/或式2之分子與另一化合物之重量比可為約100:1至約1:100;在另一個實例中,該重量比可為約50:1至約1:50;在另一個實例中,該重量比可為約20:1至約1:20;在另一個實例中,該重量比可為約10:1至約1:10;在另一個實例中,該重量比可為約5:1至1:5;在另一個實例中,該重量比可為約3:1至約1:3;在另一個實例中,該重量比可為約2:1至約1:2;及在最後一個實例中,該重量比可為約1:1。然而,較佳地,小於約10:1至約1:10之重量比為較佳的。有時使用包含一或多種式1及/或式2之分子及一或多種來自以上可能組合之其他化合物的三或四組分混合物亦為較佳的。 In another embodiment, the above possible combinations can be used in a wide variety of weight ratios. For example, for a two-component mixture, the weight ratio of the molecules of formula 1 and/or formula 2 to the other compound may be about 100:1 to about 1:100; in another example, the weight ratio may be about 50:1 to about 1:50; in another example, the weight ratio may be about 20:1 to about 1:20; in another example, the weight ratio may be about 10:1 to about 1:10 In another example, the weight ratio may be about 5:1 to 1:5; in another example, the weight ratio may be about 3:1 to about 1:3; in another example, the weight The ratio may be about 2:1 to about 1:2; and in the last example, the weight ratio may be about 1:1. However, preferably, a weight ratio of less than about 10:1 to about 1:10 is preferred. Sometimes it is also preferable to use a three- or four-component mixture containing one or more molecules of Formula 1 and/or Formula 2 and one or more other compounds from the above possible combinations.

調配物Formulation

殺蟲劑鮮少適合以其純的形式施用。其通常需要添加其他物質,藉此該殺蟲劑能以促成方便施用、處理、輸送、儲存及最大殺蟲劑活性之所需濃度及適宜形式使用。因此,殺蟲劑係配製成例如餌劑、濃縮乳劑、粉劑、可乳化性濃縮液、燻蒸劑、膠劑、粒劑、微膠囊、種子處理劑、懸浮濃縮物、濃懸乳劑、片劑、水溶性液劑、水分散性粒劑或乾懸浮 劑、可濕性粉劑及超低容量液劑。有關調配物類型的進一步資訊,請參見國際作物生命協會(CropLife International)所出版之「殺蟲劑調配物類型總表及國際編號系統(Catalogue of Pesticide Formulation Types and International Coding System)」第二號技術專論(Technical Monograph)第五版(2002年)。 Insecticides are rarely suitable for application in their pure form. It usually requires the addition of other substances so that the insecticide can be used in a desired concentration and suitable form that facilitates convenient application, handling, transportation, storage, and maximum insecticide activity. Therefore, insecticides are formulated into, for example, baits, concentrated emulsions, powders, emulsifiable concentrates, fumigants, gums, granules, microcapsules, seed treatment agents, suspension concentrates, concentrated suspension emulsions, tablets , Water-soluble liquids, water-dispersible granules or dry suspensions, wettable powders and ultra-low volume liquids. For further information on the types of formulations, please refer to the "Catalogue of Pesticide Formulation Types and International Coding System" No. 2 technology published by CropLife International Monograph (Technical Monograph) fifth edition (2002).

殺蟲劑最常以自該等殺蟲劑的濃縮調配物製備之水懸劑或乳劑形式施用。該等水溶性、水懸浮性或可乳化性調配物係通常稱作可濕性粉劑或水分散性粒劑之固製劑,或為通常稱作可乳化性濃縮液或水懸劑之液態製劑。可壓製成水分散性粒劑之可濕性粉劑係包括該殺蟲劑、一種載劑及表面活性劑之一種密切混合物。該殺蟲劑的濃度係通常自約10重量%至約90重量%。該載劑通常選自鎂鋁海泡石黏土、蒙脫石黏土、矽藻土或純化矽酸鹽。包括約0.5%至約10%的可濕性粉劑之有效表面活性劑,係磺酸化木質素、縮合萘磺酸酯、萘磺酸酯、烷基苯磺酸酯、烷基硫酸酯及非離子性表面活性劑諸如烷基苯酚的環氧乙烷加成物。 Insecticides are most commonly applied in the form of aqueous suspensions or emulsions prepared from concentrated formulations of such insecticides. These water-soluble, water-suspendable or emulsifiable formulations are generally referred to as solid formulations of wettable powders or water-dispersible granules, or liquid formulations generally referred to as emulsifiable concentrates or aqueous suspensions. The wettable powder that can be compressed into water-dispersible granules includes an intimate mixture of the insecticide, a carrier and a surfactant. The concentration of the pesticide is usually from about 10% by weight to about 90% by weight. The carrier is usually selected from magnesia-aluminum sepiolite clay, montmorillonite clay, diatomaceous earth or purified silicate. Effective surfactants including about 0.5% to about 10% of wettable powder, such as sulfonated lignin, condensed naphthalene sulfonate, naphthalene sulfonate, alkylbenzene sulfonate, alkyl sulfate, and non-ionic Surfactants such as ethylene oxide adducts of alkylphenols.

殺蟲劑的可乳化性濃縮液包括溶於一載劑中之一適宜濃度諸如每公升液體自約50至約500克的殺蟲劑,該載劑係一種水混溶性溶劑或非水混溶性有機溶劑與乳化劑之混合物。適用的有機溶劑包含芳族類,特別是二甲苯類與石油分餾物,尤其是石油的高沸點萘與烯烴的部分,諸如重芳族石油腦。亦可使用其他有機溶劑,諸如包含松香衍生物在內之萜烯溶劑、脂族酮類諸如環己酮及複合醇類諸如2-乙氧基乙醇。用於可乳化性濃縮液之適宜乳化劑係選自習用的陰離子性與非離子性表面活性劑。 The emulsifiable concentrate of insecticide comprises an insecticide dissolved in a carrier at a suitable concentration, such as from about 50 to about 500 grams per liter of liquid, which is a water-miscible solvent or non-water-miscible A mixture of organic solvents and emulsifiers. Suitable organic solvents include aromatics, especially xylenes and petroleum fractions, especially the high-boiling naphthalene and olefin parts of petroleum, such as heavy aromatic naphtha. Other organic solvents may also be used, such as terpene solvents including rosin derivatives, aliphatic ketones such as cyclohexanone, and complex alcohols such as 2-ethoxyethanol. Suitable emulsifiers for emulsifiable concentrates are selected from conventional anionic and nonionic surfactants.

水懸劑係包括以約5重量%至約50重量%的濃度範圍分散於一種含水載劑中之非水溶性殺蟲劑的懸浮液。藉由將該殺蟲劑細磨及強力地混入由水與表面活性劑所組成之一載劑中,以製備懸浮液。亦可添加諸如無機鹽類與合成或天然膠類之成分,以增加該含水載劑的密度與黏度。 通常最有效者係藉由在一器具諸如混砂機、球磨機或活塞型均質機中製備含水混合物及加以均質化,而同時研磨與混合該殺蟲劑。 Aqueous suspensions include suspensions of water-insoluble pesticides dispersed in an aqueous carrier in a concentration range of about 5% to about 50% by weight. The insecticide is finely ground and strongly mixed into a carrier composed of water and surfactant to prepare a suspension. Ingredients such as inorganic salts and synthetic or natural gums can also be added to increase the density and viscosity of the aqueous carrier. Generally, the most effective method is to prepare and homogenize the aqueous mixture in an appliance such as a sand mixer, a ball mill or a piston-type homogenizer, while grinding and mixing the insecticide at the same time.

殺蟲劑亦可藉由特別適用於土壤之粒狀組合物形式施用。粒狀組合物通常含有約0.5重量%至約10重量%的殺蟲劑,該殺蟲劑係分散於包括黏土或一種類似物質之一載劑中。通常藉由將殺蟲劑溶解在一種適宜溶劑中,及施用至已預先形成介於約0.5至3毫米範圍的適當顆粒尺寸之一種粒狀載劑,而製備該等組合物。可藉由產生載劑與化合物之糰狀物或糊狀物,及經壓碎與乾燥而得所欲的粒狀顆粒尺寸,而配製該等組合物。 Insecticides can also be applied in the form of granular compositions that are particularly suitable for soil. Granular compositions usually contain about 0.5% to about 10% by weight of an insecticide dispersed in a carrier including clay or a similar substance. These compositions are usually prepared by dissolving the insecticide in a suitable solvent and applying it to a granular carrier that has been preformed with a suitable particle size in the range of about 0.5 to 3 mm. These compositions can be formulated by producing a mass or paste of the carrier and the compound, and crushing and drying to obtain the desired granular particle size.

藉由密切地混合粉末形式的該殺蟲劑與一種適宜的粉狀農業載劑諸如高嶺土、磨碎的火山岩之類,而製備含有殺蟲劑的粉劑。粉劑可適宜地含有自約1%至約10%的該殺蟲劑。粉劑可施用作為種子敷料,或藉由粉劑吹送機作為葉片施藥。 The insecticide-containing powder is prepared by intimately mixing the insecticide in powder form with a suitable powdered agricultural carrier such as kaolin, ground volcanic rock, and the like. The powder may suitably contain from about 1% to about 10% of the insecticide. The powder can be applied as a seed dressing, or by a powder blowing machine as a leaf application.

以通常位於廣泛用於農業化學中之諸如撒佈油的石油油料之一種適當有機溶劑中的液劑形式施用殺蟲劑,亦同樣地實用。 It is also practical to apply the insecticide in the form of a liquid usually in an appropriate organic solvent such as petroleum oils widely used in agricultural chemistry, such as spreading oil.

亦可藉由噴霧劑組合物的形式施用殺蟲劑。在該等組合物中,該殺蟲劑係溶解或分散於一種產生壓力性推進劑混合物之一載劑中。噴霧劑組合物係封裝於一容器中,而混合物係經由該容器的一個霧化閥而噴散。 The insecticide can also be applied in the form of a spray composition. In these compositions, the insecticide is dissolved or dispersed in a carrier of a pressure-generating propellant mixture. The spray composition is packaged in a container, and the mixture is sprayed through an atomizing valve of the container.

當該殺蟲劑與食物或引誘劑或二者混合時,則形成殺蟲劑餌劑。當有該等害蟲吃該食餌劑時,其等亦攝入該殺蟲劑。餌劑的形式可為粒劑、膠劑、水懸粉劑、液態製劑或固態製劑。其等可用於害蟲的躲藏處。 When the insecticide is mixed with food or attractant or both, it forms an insecticide bait. When the pests eat the bait, they also ingest the pesticide. The bait can be in the form of granules, gels, water suspension powders, liquid preparations or solid preparations. It can be used as a hiding place for pests.

燻蒸劑係具有相對高的蒸氣壓力之殺蟲劑,及因而能以濃度足以殺滅土壤或密閉空間中的害蟲之氣體形式存在。該燻蒸劑的毒性係 與其濃度與暴露時間成正比。其等的特徵在於擴散能力良好,及藉由侵入該害蟲的呼吸系統或經由該害蟲的表皮層吸收而發揮作用。燻蒸劑係用於控制防氣板下、在氣密式房或建築物中或在特殊室中所儲存產物之害蟲。 The fumigant is an insecticide with a relatively high vapor pressure, and therefore can exist in the form of a gas with a concentration sufficient to kill pests in the soil or confined spaces. The toxicity of the fumigant is proportional to its concentration and exposure time. They are characterized by good spreading ability and function by invading the pest's respiratory system or being absorbed through the pest's epidermis. Fumigants are used to control pests in products stored under gas-proof panels, in airtight rooms or buildings, or in special rooms.

可藉由將該殺蟲劑顆粒或微滴懸浮於各種類型的塑性聚合物中,而將殺蟲劑微膠囊化。藉由改變聚合物的化學或藉由改變加工處理因子,可形成具有各種尺寸、溶解度、壁厚度及滲透程度的微膠囊。該等因子掌控其內的有效成分之釋出速度,進而影響該產品的殘餘功效、作用速度及氣味。 The insecticide can be microencapsulated by suspending the insecticide particles or droplets in various types of plastic polymers. By changing the chemistry of the polymer or by changing the processing factors, microcapsules with various sizes, solubility, wall thickness and degree of penetration can be formed. These factors control the release rate of the active ingredients in it, which in turn affects the residual efficacy, speed of action and smell of the product.

藉由將殺蟲劑溶於一溶劑,及該一溶劑係將該殺蟲劑留置於溶液中,而製備油劑。相較於其他調配物,殺蟲劑的油劑通常較快速地擊昏與殺滅害蟲,因溶劑本身具有殺蟲作用,及對於外皮的蠟質覆蓋物之溶解作用增加殺蟲劑的吸收速度。油劑的其他優點包含較佳的儲存安定性、較佳的裂隙滲透作用及對於油脂表面的附著作用較佳。 The oil agent is prepared by dissolving the insecticide in a solvent and leaving the insecticide in the solution in the solvent. Compared with other formulations, insecticide oils usually stun and kill pests faster, because the solvent itself has an insecticidal effect, and the dissolution of the waxy covering on the skin increases the absorption rate of the insecticide. . Other advantages of oils include better storage stability, better fissure penetration, and better side effects on the surface of grease.

另一實施例係一種油水型乳劑,其中該乳劑包括各具有一層狀液晶塗層及分散於一水相中之油滴,其中各油滴包含在農業上具活性之至少一種化合物及個別經包含下列各者之一個單層狀或多層狀層塗覆:(1)至少一種非離子性親脂性表面活性劑、(2)至少一種非離子性親水性表面活性劑及(3)至少一種離子性表面活性劑,其中該油滴具有一小於800奈米之平均粒徑。有關該實施例的進一步資訊係揭露於2007年2月1日公開及專利申請案序號為11/495,228之第20070027034號美國專利公開案。為方便使用,該實施例將稱作「OIWE」。 Another embodiment is an oil-water emulsion, wherein the emulsion includes oil droplets each having a layer-like liquid crystal coating and dispersed in an aqueous phase, wherein each oil droplet contains at least one compound and individual chemical compounds that are active in agriculture. A single-layer or multi-layer coating comprising: (1) at least one nonionic lipophilic surfactant, (2) at least one nonionic hydrophilic surfactant, and (3) at least one An ionic surfactant, wherein the oil droplets have an average particle size of less than 800 nanometers. Further information about this embodiment is disclosed in the US Patent Publication No. 20070027034 published on February 1, 2007 and with the patent application serial number 11/495,228. For ease of use, this embodiment will be referred to as "OIWE".

進一步的資訊請參見由D.Dent所著及版權為CAB國際公司所有之「昆蟲有害生物管理(Insect Pest Management)」乙書第二版(2000年)。此外,更詳細的資訊請參見由Arnold Mallis所著及2004年版權為GIE 媒體有限公司所有之「害蟲防治手冊-住家害蟲之行為、生活史及防治(Handbook of Pest Control-The Behavior,Life History,and Control of Household Pests)」乙書第九版。 For further information, please refer to "Insect Pest Management" second edition (2000) written by D. Dent and copyrighted by CAB International. In addition, for more detailed information, please refer to the "Handbook of Pest Control-The Behavior, Life History," written by Arnold Mallis and copyrighted by GIE Media Co., Ltd. in 2004. and Control of Household Pests)" Book B, Ninth Edition.

其他調配物成分Other formulation ingredients

一般而言,當化學式1中所揭露的分子用於一調配物中時,該調配物亦可含有其他組分。該等組分包含但不限於(此係一個非詳盡無遺及非互相排除的清單)濕潤劑、撒布劑、黏著劑、滲透劑、緩衝劑、螯合劑、減偏流劑、相容劑、消泡劑、清潔劑及乳化劑。現即說明一些組分。 Generally speaking, when the molecule disclosed in Chemical Formula 1 is used in a formulation, the formulation may also contain other components. These components include but are not limited to (this is a non-exhaustive and non-mutually exclusive list) wetting agents, spreading agents, adhesives, penetrants, buffers, chelating agents, flow-reducing agents, compatibilizers, defoamers Agents, cleaners and emulsifiers. Some components are now explained.

濕潤劑係當添加至一液態製劑時藉由降低該液態製劑與其撒布表面之間的界面張力而增加該液態製劑的撒布或滲透力之一物質。濕潤劑係因二項主要功能而用於農用化學調配物中:在加工處理與生產期間增加粉末在水中之濕潤率,以產生可溶性液態製劑的濃縮物或懸浮濃縮物;及在噴灑槽中混合一產物與水之期間,減少該可濕性粉劑的濕潤時間及增進水進入水分散性粒劑中的滲透作用。用於可濕性粉劑、懸浮濃縮物及水分散性粒劑調配物中之濕潤劑實例為:月桂基硫酸鈉;二辛基磺基丁二酸鈉;烷基酚乙氧基化物;及脂族醇乙氧基化物。 The humectant is a substance that increases the spreading or penetration power of the liquid preparation by reducing the interfacial tension between the liquid preparation and its spreading surface when added to a liquid preparation. Wetting agents are used in agrochemical formulations for two main functions: increasing the wetting rate of powders in water during processing and production to produce concentrates or suspension concentrates of soluble liquid formulations; and mixing in spray tanks During the period between the product and water, the wetting time of the wettable powder is reduced and the penetration of water into the water-dispersible granules is improved. Examples of wetting agents used in formulations of wettable powders, suspension concentrates and water-dispersible granules are: sodium lauryl sulfate; sodium dioctyl sulfosuccinate; alkylphenol ethoxylates; and lipids Group alcohol ethoxylates.

分散劑係吸附至顆粒表面上及有助於保存顆粒的分散狀態及阻止其等再聚集之一物質。在農用調配物中添加分散劑,以在生產製造期間促進分散與懸浮作用,及確保該等顆粒在噴灑槽中再分散於水中。其等廣泛地用於可濕性粉劑、懸浮濃縮物及水分散性粒劑中。作為分散劑之表面活性劑具有強力吸附至一顆粒表面的能力,及提供一個帶電荷或空間的障壁而阻止顆粒再聚集。最常使用的表面活性劑為陰離子性、非離子性或該二類型的混合物。就可濕性粉劑調配物而言,最常見的分散劑為木質素磺酸鈉。就懸浮濃縮物而言,使用聚電解質諸如萘磺酸鈉甲醛縮合物, 可獲致非常良好的吸附作用與安定作用。亦使用三苯乙烯基苯酚乙氧基磷酸酯。非離子性表面活性劑諸如烷基芳基環氧乙烷縮合物及EO-PO嵌段共聚物,有時係與陰離子性表面活性劑組合作為用於懸浮濃縮物之分散劑。最近幾年,已研發出作為分散劑之非常高分子量的新類型聚合性表面活性劑。其等具有非常長的疏水性「主鏈」及眾多的環氧乙烷鏈,而形成「梳型」表面活性劑之「梳齒」。因為疏水性主鏈在顆粒表面上具有眾多的固著點,該等高分子量聚合物可賦予懸浮濃縮物非常良好的長期安定性。用於農用調配物中的分散劑實例為:木質素磺酸鈉、萘磺酸鈉甲醛縮合物、三苯乙烯基苯酚乙氧基磷酸酯、脂族醇乙氧基化物、烷基乙氧基化物、EO-PO嵌段共聚物及接枝共聚物。 The dispersant is a substance that is adsorbed on the surface of the particles and helps to preserve the dispersed state of the particles and prevent them from re-aggregating. A dispersant is added to the agricultural formulation to promote dispersion and suspension during production and to ensure that the particles are redispersed in the water in the spray tank. They are widely used in wettable powders, suspension concentrates and water-dispersible granules. As a dispersant, the surfactant has the ability to strongly adsorb to the surface of a particle, and provides a barrier of charge or space to prevent the particles from re-aggregating. The most commonly used surfactants are anionic, nonionic or a mixture of the two types. For wettable powder formulations, the most common dispersant is sodium lignosulfonate. For suspension concentrates, the use of polyelectrolytes such as sodium naphthalenesulfonate formaldehyde condensate can achieve very good adsorption and stability. Tristyrylphenol ethoxy phosphate is also used. Nonionic surfactants such as alkylaryl ethylene oxide condensates and EO-PO block copolymers are sometimes combined with anionic surfactants as dispersants for suspension concentrates. In recent years, new types of very high molecular weight polymeric surfactants have been developed as dispersants. They have a very long hydrophobic "main chain" and numerous ethylene oxide chains, which form the "comb teeth" of the "comb" surfactant. Because the hydrophobic backbone has many fixation points on the particle surface, these high molecular weight polymers can give suspension concentrates very good long-term stability. Examples of dispersants used in agricultural formulations are: sodium lignin sulfonate, sodium naphthalene sulfonate formaldehyde condensate, tristyryl phenol ethoxy phosphate, aliphatic alcohol ethoxylate, alkyl ethoxylate Compounds, EO-PO block copolymers and graft copolymers.

乳化劑係使得一液相的微滴懸浮液在另一液相中安定之一物質。若無乳化劑,該二液體將分離成為二個不互溶的液相。最常使用的乳化劑摻合物係含有具12或更多個環氧乙烷單元的烷基酚或脂族醇及十二基苯磺酸的油溶性鈣鹽。自8至18的親水性-親油性均衡值(「HLB」)範圍一般將提供良好的安定乳劑。藉由添加小量的EO-PO嵌段共聚物表面活性劑,有時可增進乳劑的安定性。 Emulsifier is a substance that makes a suspension of droplets in one liquid phase stabilize in another liquid phase. If there is no emulsifier, the two liquids will separate into two immiscible liquid phases. The most commonly used emulsifier blends contain alkylphenols or aliphatic alcohols with 12 or more ethylene oxide units and an oil-soluble calcium salt of dodecylbenzenesulfonic acid. A range of hydrophilic-lipophilic balance ("HLB") from 8 to 18 will generally provide a good stable emulsion. By adding a small amount of EO-PO block copolymer surfactant, sometimes the stability of the emulsion can be improved.

增溶劑係在臨界微胞濃度以上將在水中形成微胞之一種表面活性劑。該等微胞然後可在微胞的疏水性部分之內,將非水溶性物質溶解或增溶。通常用於增溶作用的表面活性劑類型為非離子性、山梨糖醇酐單油酸酯、山梨糖醇酐單油酸酯乙氧基化物及甲基油酸酯。 The solubilizer is a surfactant that will form micelles in water above the critical micelle concentration. These micelles can then dissolve or solubilize water-insoluble substances within the hydrophobic portion of the micelles. The types of surfactants commonly used for solubilization are nonionic, sorbitan monooleate, sorbitan monooleate ethoxylate and methyl oleate.

表面活性劑有時單獨使用,或與其他添加劑諸如作為噴灑槽混合物佐劑之礦物油或植物油一起使用,以增進殺蟲劑對於標的之生物性能。用於生物強化作用之表面活性劑類型一般依該殺蟲劑的性質與作用模式而定。然而,其等通常為非離子性,諸如:烷基乙氧基化物;直鏈脂 族醇乙氧基化物;脂族胺乙氧基化物。 Surfactants are sometimes used alone or together with other additives such as mineral oil or vegetable oil as adjuvants for spray tank mixtures to enhance the biological properties of the insecticide against the target. The type of surfactant used for bioenhancement generally depends on the nature and mode of action of the pesticide. However, they are usually nonionic, such as: alkyl ethoxylates; linear aliphatic alcohol ethoxylates; aliphatic amine ethoxylates.

農用調配物中之一載劑或稀釋劑,係添加至該殺蟲劑以賦予產物所需強度之一物質。載劑通常為具有高吸收能力之物質,而稀釋劑通常為具有低吸收能力之物質。載劑與稀釋劑係用於粉劑、可濕性粉劑、粒劑及水分散性粒劑之調配物。 A carrier or diluent in the agricultural formulation is a substance added to the pesticide to give the product the desired strength. The carrier is usually a substance with high absorption capacity, and the diluent is usually a substance with low absorption capacity. The carrier and diluent are used in the formulation of powders, wettable powders, granules and water-dispersible granules.

有機溶劑主要用於配製可乳化性濃縮液、油水型乳劑、濃懸乳劑及超低容量調配物,及較小程度粒狀調配物。有時使用溶劑的混合物。溶劑的第一個主要群組為脂族石蠟油,諸如煤油或精製石蠟。第二個主要群組(及最常見者)包括芳族溶劑,諸如二甲苯及C9與C10芳族溶劑的較高分子量分餾物。氯化烴類係適用作為共溶劑,以在該調配物於水中乳化時阻止殺蟲劑的結晶作用。有時使用醇類作為共溶劑,以增加溶劑能力。其他溶劑可包含植物油、籽油及植物油與籽油的酯類。 Organic solvents are mainly used to prepare emulsifiable concentrates, oil-water emulsions, concentrated suspension emulsions and ultra-low volume formulations, and to a lesser extent granular formulations. Sometimes a mixture of solvents is used. The first major group of solvents are aliphatic paraffin oils, such as kerosene or refined paraffin. The second major group (and the most common) includes aromatic solvents, such as xylene and higher molecular weight fractions of C9 and C10 aromatic solvents. Chlorinated hydrocarbons are suitable as co-solvents to prevent the crystallization of pesticides when the formulation is emulsified in water. Sometimes alcohols are used as co-solvents to increase solvent capacity. Other solvents may include vegetable oil, seed oil, and esters of vegetable oil and seed oil.

增稠劑或膠凝劑主要用於懸浮濃縮物、乳劑及濃懸乳劑之調配物,以改變該液體的流變或流動性質及阻止分散型顆粒或微滴的分離作用與沉降作用。增稠劑、膠凝劑及抗沉降劑一般分成二類,即非水溶性顆粒及水溶性聚合物。可能使用黏土與矽石來製造懸浮濃縮物調配物。該等物質類型的實例包含但不限於蒙脫石、膨潤土、矽酸鋁鎂及鎂鋁海泡石。多年來已使用水溶性多醣類作為增稠-膠凝劑。最常用的多醣類的類型係種子與海草的天然萃取物,或為合成的纖維素衍生物。該等物質類型之實例包含但不限於瓜爾膠、刺槐豆膠、角叉菜膠、藻朊酸鹽、甲基纖維素、羧甲基纖維素鈉(SCMC)、羥乙基纖維素(HEC)。其他的抗沉降劑類型係以改質澱粉、聚丙烯酸酯、聚乙烯醇及聚環氧乙烷為基礎。另一種良好的抗沉降劑為三仙膠。 Thickeners or gelling agents are mainly used in the formulation of suspension concentrates, emulsions and suspension emulsions to change the rheology or flow properties of the liquid and prevent the separation and sedimentation of dispersed particles or droplets. Thickeners, gelling agents and anti-settling agents are generally divided into two categories, namely, water-insoluble particles and water-soluble polymers. It is possible to use clay and silica to make suspension concentrate formulations. Examples of these substance types include, but are not limited to, montmorillonite, bentonite, aluminum magnesium silicate, and magnesia aluminum sepiolite. Water-soluble polysaccharides have been used as thickening-gelling agents for many years. The most commonly used types of polysaccharides are natural extracts of seeds and seaweed, or synthetic cellulose derivatives. Examples of these substance types include, but are not limited to, guar gum, locust bean gum, carrageenan, alginate, methylcellulose, sodium carboxymethylcellulose (SCMC), hydroxyethylcellulose (HEC ). Other types of anti-settling agents are based on modified starch, polyacrylate, polyvinyl alcohol and polyethylene oxide. Another good anti-settling agent is Sanxian Gum.

微生物可造成所配製產物之腐敗。因此使用防腐劑來消弭 或降低其等的效應。防腐劑的實例包含但不限於:丙酸及其鈉鹽;山梨酸及其鈉或鉀鹽;苯甲酸及其鈉鹽;-羥基苯甲酸鈉鹽;-羥基苯甲酸甲基酯;及1,2-苯並異噻唑啉-3-酮(BIT)。 Microorganisms can cause spoilage of the formulated product. Therefore, preservatives are used to eliminate or reduce their effects. Examples of preservatives include, but are not limited to: propionic acid and its sodium salt; sorbic acid and its sodium or potassium salt; benzoic acid and its sodium salt; p -hydroxybenzoic acid sodium salt; p -hydroxybenzoic acid methyl ester; and 1 ,2-Benzisothiazolin-3-one (BIT).

表面活性劑之存在,通常造成水基調配物在生產與經由噴灑槽施用的混合操作期間形成泡沫。為降低形成泡沫的傾向,通常在生產階段或在裝瓶之前添加消泡劑。一般而言,消泡劑分為二種類型,即矽氧樹脂類與非矽氧樹脂類。矽氧樹脂類通常為二甲基聚矽氧烷的含水乳劑,而該非矽氧樹脂消泡劑為非水溶性油類諸如辛醇與壬醇或為矽石。在該二種情況下,消泡劑的功能係從空氣-水界面置換表面活性劑。 The presence of surfactants usually causes water-based formulations to form foam during the mixing operation of production and application via spray tanks. To reduce the tendency to form foam, defoamers are usually added during the production stage or before bottling. Generally speaking, defoamers are divided into two types, namely silicone resins and non-silicone resins. Silicone resins are usually aqueous emulsions of dimethylpolysiloxane, and the non-silicone defoamers are water-insoluble oils such as octanol and nonanol or silica. In these two cases, the function of the defoamer is to replace the surfactant from the air-water interface.

「綠色」劑(佐劑、表面活性劑、溶劑)可減少作物保護性調配物的整體環境足跡。綠色劑係生物可降解性,及一般衍生自天然及/或永續來源,植物與動物來源。具體的實例為:植物油、籽油及其酯類,以及烷氧基化烷基聚葡萄糖苷。 "Green" agents ( such as adjuvants, surfactants, solvents) can reduce the overall environmental footprint of crop protection formulations. Green agents are biodegradable, and are generally derived from natural and/or sustainable sources, such as plant and animal sources. Specific examples are: vegetable oils, seed oils and their esters, and alkoxylated alkyl polyglucosides.

關於進一步資訊,參見D.A.Knowles所編之「Chemistry and Technology of Agrochemical Formulations」,Kluwer Academic Publishers版權所有(1998)。亦可參見「Insecticides in Agriculture and Environment-Retrospects and Prospects」,A.S.Perry,I.Yamamoto,I.Ishaaya及R.Perry,Springer-Verlag版權所有(1998)。 For further information, see "Chemistry and Technology of Agrochemical Formulations" edited by D.A. Knowles, Copyright Kluwer Academic Publishers (1998). See also "Insecticides in Agriculture and Environment-Retrospects and Prospects", A.S. Perry, I. Yamamoto, I. Ishaaya and R. Perry, Springer-Verlag Copyright (1998).

害蟲Pests

一般而言,式1及/或式2之分子可用於防治害蟲,例如螞蟻、蚜蟲、甲蟲、蠹蟲、蜚蠊、蟋蟀、蠼螋、跳蚤、蒼蠅、蚱蜢、葉蟬、虱、蝗蟲、蟎、蛾、線蟲、蚧、綜合綱害蟲、白蟻、薊馬、扁虱、黃蜂及粉虱。 Generally speaking, the molecules of Formula 1 and/or Formula 2 can be used to control pests, such as ants, aphids, beetles, silverfish, cockroaches, crickets, earwigs, fleas, flies, grasshoppers, leafhoppers, lice, locusts, mites, Moths, nematodes, scales, complex pests, termites, thrips, ticks, wasps and whiteflies.

於另一實施例中,式1及/或式2之分子可用於防治線形動 物門及/或節肢動物門之害蟲。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the phylum Linear and/or Arthropod.

於另一實施例中,式1及/或式2之分子可用於防治螯肢動物亞門(Chelicerata)、多足亞門(Myriapoda)及/或六足亞門(Hexapoda)之害蟲。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of Chelicerata, Myriapoda and/or Hexapoda.

於另一實施例中,式1及/或式2之分子可用於防治蛛形綱(Arachnida)、綜合綱(Symphyla)及/或昆蟲綱(Insecta)之害蟲。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the Arachnida, Symphyla, and/or Insecta.

於另一實施例中,式1及/或式2之分子可用於防治虱目(Anoplura)之害蟲。特定屬之非詳盡清單包括(但不限於)血虱屬(Haematopinus spp.)、甲脅虱屬(Hoplopleura spp.)、長顎虱屬(Linognathus spp.)、虱蝨屬(Pediculus spp.)及鱗虱屬(Polyplax spp.)。特定物種之非詳盡清單包括(但不限於)驢血虱(Haematopinus asini)、豬血虱(Haematopinus suis)、棘顎虱(Linognathus setosus)、綿羊顎虱(Linognathus ovillus)、頭蝨(Pediculus humanus capitis)、體虱(Pediculus humanus humanus)及陰虱(Pthirus pubis)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the Order Anoplura. A non-exhaustive list of specific genera includes (but is not limited to) Haematopinus spp., Hoplopleura spp., Linognathus spp., Pediculus spp., and Polyplax spp. (Polyplax spp.). A non-exhaustive list of specific species includes (but is not limited to) donkey blood louse ( Haematopinus asini ), pig blood louse ( Haematopinus suis ), spiny jaw louse ( Linognathus setosus ), sheep jaw louse ( Linognathus ovillus ), head louse ( Pediculus humanus capitis) ), body lice ( Pediculus humanus humanus ) and pubic lice ( Pthirus pubis ).

於另一實施例中,式1及/或式2之分子可用於防治鞘翅目(Coleoptera)之害蟲。特定屬之非詳盡清單包括(但不限於)三齒豆象屬(Acanthoscelides spp.)、叩頭蟲屬(Agriotes spp.)、花象屬(Anthonomus spp.)、長喙小象屬(Apion spp.)、甘蔗金龜屬(Apogonia spp.)、守瓜屬(Aulacophora spp.)、豆象屬(Bruchus spp.)、天牛屬(Cerosterna spp.)、豆葉甲屬(Cerotoma spp.)、龜象屬(Ceutorhynchus spp.)、凹脛跳甲屬(Chaetocnema spp.)、葉甲屬(Colaspis spp.)、叩甲屬(Ctenicera spp.)、象蟲屬(Curculio spp.)、方頭甲屬(Cyclocephala spp.)、根葉甲屬(Diabrotica spp.)、葉象屬(Hypera spp.)、齒小蠹屬(Ips spp.)、粉蠹屬(Lyctus spp.)、Megascelis spp.、菜花露尾甲屬(Meligethes spp.)、耳象屬(Otiorhynchus spp.)、短喙象屬(Pantomorus spp.)、鰓角金龜屬(Phyllophaga spp.)、條跳甲屬(Phyllotreta spp.)、切根鰓金龜屬 (Rhizotrogus spp.)、虎象屬(Rhynchites spp.)、隱喙象屬(Rhynchophorus spp.)、小蠹屬(Scolytus spp.)、尖隱喙象屬(Sphenophorus spp.)、象蟲屬(Sitophilus spp.)及擬穀盜屬(Tribolium spp.)。特定物種之非詳盡清單包括(但不限於)大豆象(Acanthoscelides obtectus)、白蠟窄吉丁(Agrilus planipennis)、光肩星天牛(Anoplophora glabripennis)、棉鈴象甲(Anthonomus grandis)、黑絨金龜(Ataenius spretulus)、甜菜隱食甲(Atomaria linearis)、甜菜象甲(Bothynoderes punctiventris)、豌豆象(Bruchus pisorum)、四紋豆象(Callosobruchus maculatus)、醬曲露尾甲(Carpophilus hemipterus)、甜菜龜甲(Cassida vittata)、豆葉甲(Cerotoma trifurcata)、白菜籽龜象(Ceutorhynchus assimilis)、Ceutorhynchus napiConoderus scalarisConoderus stigmosus、李象鼻蟲(Conotrachelus nenuphar)、綠花金龜(Cotinis nitida)、天冬負泥甲(Crioceris asparagi)、鏽赤扁穀盜(Cryptolestes ferrugineus)、長角扁穀盜(Cryptolestes pusillus)、土耳其扁穀盜(Cryptolestes turcicus)、密點細枝象(Cylindrocopturus adspersus)、切葉象甲(Deporaus marginatus)、火腿皮蠹(Dermestes lardarius)、白腹皮蠹(Dermestes maculatus)、墨西哥豆瓢蟲(Epilachna varivestis)、蛀莖象甲(Faustinus cubae)、蒼白樹皮象(Hylobius pales)、苜蓿葉象甲(Hypera postica)、咖啡果小蠹(Hypothenemus hampei)、菸草甲(Lasioderma serricorne)、馬鈴薯甲蟲(Leptinotarsa decemlineata)、白蠐螬(Liogenys fuscus)、Liogenys suturalis、稻象甲(Lissorhoptrus oryzophilus)、Maecolaspis joliveti、玉米叩甲(Melanotus communis)、油菜露尾甲(Meligethes aeneus)、西方五月鰓金龜(Melolontha melolontha)、梯頂天牛(Oberea brevis)、線狀天牛(Oberea linearis)、椰子犀角金龜(Oryctes rhinoceros)、大眼鋸穀盜(Oryzaephilus mercator)、鋸胸粉扁蟲(Oryzaephilus surinamensis)、黑角負泥蟲(Oulema melanopus)、稻負泥蟲(Oulema oryzae)、金龜子(Phyllophaga cuyabana)、日本麗金龜(Popillia japonica)、大穀蠹(Prostephanus truncatus)、穀蠹(Rhyzopertha dominica)、豌豆葉象甲(Sitona lineatus)、穀象(Sitophilus granarius)、米象(Sitophilus oryzae)、玉米象(Sitophilus zeamais)、藥材甲蟲(Stegobium paniceum)、赤擬穀盜(Tribolium castaneum)、雜擬穀盜(Tribolium confusum)、花斑皮蠹(Trogoderma variabile)及玉米距步甲蟲(Zabrus tenebrioides)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Coleoptera pests. A non-exhaustive list of specific genera includes (but is not limited to) Acanthoscelides spp., Agriotes spp., Anthonomus spp., Apion spp. ), Apogonia spp., Aulacophora spp., Bruchus spp., Cerosterna spp., Cerotoma spp., Tortoise Genus ( Ceutorhynchus spp.), Chaetocnema spp., Colaspis spp., Ctenicera spp., Curculio spp., Chaetocnema spp. Cyclocephala spp.), Diabrotica spp., Hypera spp., Ips spp., Lyctus spp., Megascelis spp., Cauliflower Dewtail Meligethes spp., Otiorhynchus spp., Pantomorus spp., Phyllophaga spp., Phyllotreta spp., cut root gills Rhizotrogus spp., Rhynchites spp., Rhynchophorus spp., Scolytus spp., Sphenophorus spp., Weevil ( Sitophilus spp.) and Tribolium spp. A non-exhaustive list of specific species includes (but is not limited to) Acanthoscelides obtectus , Agrilus planipennis , Anoplophora glabripennis , Anthonomus grandis , Ataenius spretulus , Atomaria linearis , Bothynoderes punctiventris, Bruchus pisorum , Callosobruchus maculatus , Carpophilus hemipterus , Cassida vittata , Bean leaf beetle ( Cerotoma trifurcata ), cabbage seed turtle elephant ( Ceutorhynchus assimilis ), Ceutorhynchus napi , Conoderus scalaris , Conoderus stigmosus , plum weevil ( Conotrachelus nenuphar ), green beetle (Cotinis nitida ), asparagus Crioceris asparagi , Cryptolestes ferrugineus , Cryptolestes pusillus , Cryptolestes turcicus , Cylindrocopturus adspersus , Deporaus marginatus , Ham skin beetle ( Dermestes lardarius ), white- bellied skin beetle (Dermestes maculatus ), Mexican bean lady beetle ( Epilachna varivestis ), stem- boring weevil (Faustinus cubae), pale bark weevil ( Hylobius pales ), alfalfa leaf weevil ( Hypera postica ), Coffee berry beetle ( Hypothenemus hampei ), tobacco beetle ( Lasioderma serricorne ), potato beetle ( Leptinotarsa decemlineata ), white grub ( Liogenys fuscus ), Liogenys suturalis , Rice weevil ( Lissorhoptrus oryzophilus ), Maecolaspis joliveti , corn beetle ( Melanotus communis ), rape beetle ( Meligethes aeneus ), Western Maygill beetle (Melolontha melolontha ), stepped beetle ( Oberea brevis ), linear Oberea linearis , Oryctes rhinoceros , Oryzaephilus mercator , Oryzaephilus surinamensis , Oulema melanopus , Oulema melanopus, Oryzaephilus mercator Oulema oryzae , Phyllophaga cuyabana , Popillia japonica , Prostephanus truncatus , Rhyzopertha dominica , Sitona lineatus , Sitophilus granarius Sitophilus oryzae , Sitophilus zeamais , Stegobium paniceum, Tribolium castaneum , Tribolium confusum , Trogoderma variabile , and Corn beetle Zabrus tenebrioides ).

於另一實施例中,式1及/或式2之分子可用於防治革翅目(Dermaptera)之害蟲。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the Order Dermaptera.

於另一實施例中,式1及/或式2之分子可用於防治蜚蠊目(Blattaria)之害蟲。特定物種之非詳盡清單包括(但不限於)德國小蠊(Blattella germanica)、東方非蠊(Blatta orientalis)、賓夕法尼亞木蠊(Parcoblatta pennsylvanica)、美洲大蠊(Periplaneta americana)、澳洲大蠊(Periplaneta australasiae)、褐色大蠊(Periplaneta brunnea)、黑胸大蠊(Periplaneta fuliginosa)、蔗蠊(Pycnoscelus surinamensis)及長鬚蜚蠊(Supella longipalpa)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the order Blattaria. A non-exhaustive list of specific species includes (but is not limited to) Blattella germanica , Blatta orientalis , Parcoblatta pennsylvanica , Periplaneta americana , Periplaneta australasiae ), brown cockroach ( Periplaneta brunnea ), black-breasted cockroach ( Periplaneta fuliginosa ), saccharine cockroach (Pycnoscelus surinamensis ) and long- bearded cockroach (Supella longipalpa ).

於另一實施例中,式1及/或式2之分子可用於防治雙翅目(Diptera)之害蟲。特定屬之非詳盡清單包括(但不限於)伊蚊屬(Aedes spp.)、潛蠅屬(Agromyza spp.)、按實蠅屬(Anastrepha spp.)、瘧蚊屬(Anopheles spp.)、果實蠅屬(Bactrocera spp.)、蠟實蠅屬(Ceratitis spp.)、斑虻屬(Chrysops spp.)、錐蠅屬(Cochliomyia spp.)、癭蚊屬(Contarinia spp.)、庫蚊屬(Culex spp.)、葉癭蚊屬(Dasineura spp.)、地種蠅屬(Delia spp.)、果蠅屬(Drosophila spp.)、廁蠅屬(Fannia spp.)、種蠅屬(Hylemyia spp.)、斑潛蠅屬(Liriomyza spp.)、家蠅屬(Musca spp.)、草種蠅屬(Phorbia spp.)、虻屬(Tabanus spp.)及大蚊屬(Tipula spp.)。特定物種之非詳盡清單包括(但不限於)苜蓿斑潛蠅(Agromyza frontella)、加勒比按實蠅(Anastrepha suspensa)、墨西哥按實蠅(Anastrepha ludens)、西印度按實蠅(Anastrepha obliqa)、瓜實蠅(Bactrocera cucurbitae)、東方果實蠅(Bactrocera dorsalis)、入侵實蠅(Bactrocera invadens)、桃果實蠅(Bactrocera zonata)、地中海果實蠅(Ceratitis capitata)、芸苔莢癭蚊(Dasineura brassicae)、灰地種蠅(Delia platura)、夏廁蠅(Fannia canicularis)、瘤脛廁蠅(Fannia scalaris)、大馬胃蠅(Gasterophilus intestinalis)、Gracillia perseae、騷擾角蠅(Haematobia irritans)、紋皮蠅(Hypoderma lineatum)、菜斑潛蠅(Liriomyza brassicae)、綿羊虱蠅(Melophagus ovinus)、秋家蠅(Musca autumnalis)、家蠅(Musca domestica)、羊鼻蠅(Oestrus ovis)、瑞典麥稈蠅(Oscinella frit)、甜菜蠅(Pegomya betae)、胡蘿蔔蠅(Psila rosae)、櫻桃實蠅(Rhagoletis cerasi)、蘋果實蠅(Rhagoletis pomonella)、藍橘繞實蠅(Rhagoletis mendax)、麥紅吸漿蟲(Sitodiplosis mosellana)及廄螫蠅(Stomorys calcitrans)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Diptera pests. A non-exhaustive list of specific genera includes (but is not limited to) Aedes spp., Agromyza spp., Anastrepha spp., Anopheles spp., Fruit Musca (Bactrocera spp.), it is a wax fruit fly (Ceratitis spp.), is a spot fly (Chrysops spp.), worm fly genus (Cochliomyia spp.), midge genus (Contarinia spp.), Culex (Culex spp.), Dasineura spp., Delia spp., Drosophila spp., Fannia spp., Hylemyia spp. , Liriomyza genus (Liriomyza spp.), is a housefly (Musca spp.), is a grass flies (Phorbia spp.), it is a horsefly (Tabanus spp.) and large mosquito genera (Tipula spp.). A non-exhaustive list of specific species includes (but is not limited to) Agromyza frontella , Anastrepha suspensa , Anastrepha ludens , Anastrepha obliqa , Anastrepha obliqa, Anastrepha Bactrocera cucurbitae , Bactrocera dorsalis , Bactrocera invadens , Bactrocera zonata , Ceratitis capitata , Dasineura brassicae , Grey Delia platura , Fannia canicularis , Fannia scalaris , Gasterophilus intestinalis , Gracillia perseae , Haematobia irritans , Hypoderma lineatum ), Liriomyza brassicae , sheep louse ( Melophagus ovinus ), autumn housefly ( Musca autumnalis ), house fly ( Musca domestica ), sheep nose fly ( Oestrus ovis ), Swedish wheat stalk fly (Oscinella frit) ), beet fly ( Pegomya betae ), carrot fly ( Psila rosae ), cherry fruit fly ( Rhagoletis cerasi ), apple fruit fly ( Rhagoletis pomonella ), blue orange fruit fly ( Rhagoletis mendax ), wheat red midge ( Sitodiplosis mosellana ) and Stomorys calcitrans (Stomorys calcitrans ).

於另一實施例中,式1及/或式2之分子可用於防治半翅目(Hemiptera)之害蟲。特定屬之非詳盡清單包括(但不限於)球蚜屬(Adelges spp.)、白輪盾蚧屬(Aulacaspis spp.)、沫蟬屬(Aphrophora spp.)、蚜屬(Aphis spp.)、小粉虱屬(Bemisia spp.)、蠟蚧屬(Ceroplastes spp.)、雪盾蚧屬(Chionaspis spp.)、褐圓盾蚧屬(Chrysomphalus spp.)、Coccus spp.、小綠葉蟬屬(Empoasca spp.)、牡蠣蚧屬(Lepidosaphes spp.)、蝽屬(Lagynotomus spp.)、草盲蝽屬(Lygus spp.)、長管蚜屬(Macrosiphum spp.)、黑尾葉蟬屬(Nephotettix spp.)、稻綠蝽屬(Nezara spp.)、長沫蟬屬(Philaenus spp.)、植盲蝽屬(Phytocoris spp.)、璧蝽屬(Piezodorus spp.)、臀紋粉蚧屬(Planococcus spp.)、粉蚧屬(Pseudococcus spp.)、縊管蚜屬(Rhopalosiphum spp.)、黑盔蚧屬(Saissetia spp.)、彩斑蚜屬(Therioaphis spp.)、Toumeyella spp.、桔蚜屬 (Toxoptera spp.)、粉虱屬(Trialeurodes spp.)、錐蝽屬(Triatoma spp)及矢尖蚧屬(Unaspis spp.)。特定物種之非詳盡清單包括(但不限於)喜綠蝽(Acrosternum hilare)、豌豆蚜(Acyrthosiphon pisum)、歐洲甘藍粉虱(Aleyrodes proletella)、螺旋粉虱(Aleurodicus dispersus)、軟毛粉虱(Aleurothrixus floccosus)、二點小綠葉蟬(Amrasca biguttula biguttula)、紅園蚧(Aonidiella aurantii)、棉蚜(Aphis gossypii)、大豆蚜(Aphis glycines)、蘋果蚜(Aphis pomi)、馬鈴薯長鬚蚜(Aulacorthum solani)、銀葉粉虱(Bemisia argentifolii)、菸粉虱(Bemisia tabaci)、多毛長蝽(Blissus leucopterus)、天門冬小管蚜(Brachycorynella asparagi)、水稻粉紅粉介殼蟲(Brevennia rehi)、甘藍蚜(Brevicoryne brassicae)、Calocoris norvegicus、紅蠟蚧(Ceroplastes rubens)、熱帶臭蟲(Cimex hemipterus)、溫帶臭蟲(Cimex lectularius)、Dagbertus fasciatus、Dichelops furcatus、麥雙尾蚜(Diuraphis noxia)、柑橘木虱(Diaphorina citri)、車前圓尾蚜(Dysaphis plantaginea)、Dysdercus suturellus、Edessa meditabunda、蘋果綿蚜(Eriosoma lanigerum)、Eurygaster maura、Euschistus heros、褐臭蝽(Euschistus servus)、腰果刺盲蝽(Helopeltis antonii)、茶角盲蝽(Helopeltis theivora)、吹綿蚧(Icerya purchasi)、檬果褐葉蟬(Idioscopus nitidulus)、灰飛虱(Laodelphax striatellus)、大稻緣蝽(Leptocorisa oratorius)、異稻緣蝽(Leptocorisa varicornis)、豆莢草盲蝽(Lygus hesperus)、木槿曼粉蚧(Maconellicoccus hirsutus)、大戟長管蚜(Macrosiphum euphorbiae)、麥長管蚜(Macrosiphum granarium)、薔薇長管蚜(Macrosiphum rosae)、紫菀葉蟬(Macrosteles quadrilineatus)、Mahanarva frimbiolata、麥無網長管蚜(Metopolophium dirhodum)、Mictis longicornis、桃蚜(Myzus persicae)、Nephotettix cinctipes、Neurocolpus longirostris、稻綠蝽(Nezara viridula)、 褐稻虱(Nilaparvata lugens)、糠片盾蚧(Parlatoria pergandii)、黑片盾蚧(Parlatoria ziziphi)、玉米蠟蟬(Peregrinus maidis)、根瘤蚜(Phylloxera vitifoliae)、Physokermes piceae、Phytocoris californicus、Phytocoris relativus、Piezodorus guildinii、四線盲蝽(Poecilocapsus lineatus)、Psallus vaccinicola、Pseudacysta perseae、菠蘿粉蚧(Pseudococcus brevipes)、梨圓盾蚧(Quadraspidiotus perniciosus)、玉米蚜(Rhopalosiphum maidis)、禾穀縊管蚜(Rhopalosiphum padi)、橄欖黑盔蚧(Saissetia oleae)、Scaptocoris castanea、麥二叉蚜(Schizaphis graminum)、麥長管蚜(Sitobion avenae)、白背飛虱(Sogatella furcifera)、溫室白粉虱(Trialeurodes vaporariorum)、青麻白粉虱(Trialeurodes abutiloneus)、矢尖蚧(Unaspis yanonensis)及Zulia entrerriana。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Hemiptera pests. A non-exhaustive list of specific genera includes (but is not limited to) Adelges spp., Aulacaspis spp., Aphrophora spp., Aphis spp., Aphis spp. Bemisia spp., Ceroplastes spp., Chionaspis spp., Chrysomphalus spp., Coccus spp., Empoasca spp. .), Lepidosaphes spp., Lagynotomus spp., Lygus spp., Macrosiphum spp., Nephotettix spp. , Nezara spp., Philaenus spp., Phytocoris spp., Piezodorus spp., Planococcus spp. , Pseudococcus spp., Rhopalosiphum spp., Saissetia spp., Therioaphis spp., Toumeyella spp., Toxoptera spp. .), Trialeurodes spp., Triatoma spp and Unaspis spp. A non-exhaustive list of specific species includes (but is not limited to) Acrosternum hilare , Acyrthosiphon pisum , Aleyrodes proletella , Aleurodicus dispersus , Aleurothrixus floccosus ), Amrasca biguttula biguttula , Aonidiella aurantii, Aphis gossypii, Aphis glycines, Apple aphid (Aphis pomi), Potato aphid (Aulacorthum solani) , Bemisia argentifolii, Bemisia tabaci, Blissus leucopterus, Brachycorynella asparagi, Brevennia rehi, Brevicoryne brassicae ), Calocoris norvegicus, Ceroplastes rubens, Tropical bug (Cimex hemipterus), Temperate bug (Cimex lectularius), Dabertus fasciatus, Dichelops furcatus, Diuraphis noxia (Diuraphis noxia), Citrus psyllid (Diaphorina trixia) Dysaphis plantaginea (Dysaphis plantaginea), Dysdercus suturellus, Edessa meditabunda, Apple cotton aphid (Eriosoma lanigerum), Eurygaster maura, Euschistus heros, Euschistus servus, Helope Antonii (Helopeltis theivora), Icerya purchasi, Idioscopus nitidulus, Laodelphax striatellus, Leptocorisa oratorius, Leptocorisa varicornis, Pea pod Lygus (Lygus hesperus) , Maconellicoccus hirsutus, Macrosiphum euphorbiae, Macrosiphum granarium, Macrosiphum rosae, Macrosteles quadrilineatus, Mahanarva frimbiolata, wheat Metopolophium dirhodum, Mictis longicornis, Myzus persicae, Nephotettix cinctipes, Neurocolpus longirostris, Nezara viridula, Nilaparvata lugens, Paria pergandii , Parlatoria ziziphi, Peregrinus maidis, Phylloxera vitifoliae, Physokermes piceae, Phytocoris californicus, Phytocoris relativus, Piezodorus guildinii, Piezodorus guildinii, Phytocoris linea perseae, Pseudococcus brevipes, Quadraspidiotus perniciosus, Rhopalosiphum maidis, Rhopalosiphum padi, Saissetia oleae, Scaptocoris castanea, Scaptocoris castanea Schizaphis graminum, Sitobion avenae, Sogatella furcifera, Trialeurodes vaporariorum, Trialeurodes abutiloneus, Unaspis yanonensis and Zulia entrerriana.

於另一實施例中,式1及/或式2之分子可用於防治膜翅目(Hymenoptera)之害蟲。特定屬之非詳盡清單包括(但不限於)頂切葉蟻屬(Acromyrmex spp.)、切葉蟻屬(Atta spp.)、弓背蟻屬(Camponotus spp.)、松葉蜂屬(Diprion spp.)、蟻屬(Formica spp.)、小家蟻屬(Monomorium spp.)、新松葉蜂屬(Neodiprion spp.)、收穫蟻屬(Pogonomyrmex spp.)、馬蜂屬(Polistes spp.)、火蟻屬(Solenopsis spp.)、黃胡蜂屬(Vespula spp.)及木蜂屬(Xylocopa spp.)。特定物種之非詳盡清單包括(但不限於)新疆菜葉蜂(Athalia rosae)、德州切葉蟻(Atta texana)、阿根廷虹臭蟻(Iridomyrmex humilis)、小黑蟻(Monomorium minimum)、小黃家蟻(Monomorium pharaonis)、紅火蟻(Solenopsis invicta)、熱帶火蟻(Solenopsis geminata)、Solenopsis molesta、Solenopsis richtery、南方火蟻(Solenopsis xyloni)及酸臭蟻(Tapinoma sessile)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the Order Hymenoptera. A non-exhaustive list of specific genera includes (but is not limited to) Acromyrmex spp., Atta spp., Camponotus spp., Diprion spp. ), Formica spp., Monomorium spp., Neodiprion spp., Pogonomyrmex spp., Polistes spp., Fire Ant (Solenopsis spp.), Vespula spp. and Xylocopa spp. A non-exhaustive list of specific species includes (but is not limited to) Athalia rosae, Atta texana, Iridomyrmex humilis, Monomorium minimum, Xiaohuangjia Ants (Monomorium pharaonis), red fire ants (Solenopsis invicta), tropical fire ants (Solenopsis geminata), Solenopsis molesta, Solenopsis richtery, southern fire ants (Solenopsis xyloni) and tapinoma sessile.

於另一實施例中,式1及/或式2之分子可用於防治等翅目 (Isoptera)之害蟲。特定屬之非詳盡清單包括(但不限於)乳白蟻屬(Coptotermes spp.)、角象白蟻屬(Cornitermes spp.)、堆砂白蟻屬(Cryptotermes spp.)、異白蟻屬(Heterotermes spp.)、木白蟻屬(Kalotermes spp.)、楹白蟻屬(Incisitermes spp.)、大白蟻屬(Macrotermes spp.)、邊白蟻屬(Marginitermes spp.)、鋸白蟻屬(Microcerotermes spp.)、Procarnitermes spp.、散白蟻屬(Reticulitermes spp.)、長鼻白蟻屬(Schedorhinotermes spp.)及古白蟻屬(Zootermopsis spp.)。特定物種之非詳盡清單包括(但不限於)大家白蟻(Coptotermes curvignathus)、大唇乳白蟻(Coptotermes frenchi)、臺灣乳白蟻(Coptotermes formosanus)、Heterotermes aureus、甘蔗白蟻(Microtermes obesi)、Reticulitermes banyulensis、Reticulitermes grassei、黃胸散白蟻(Reticulitermes flavipes)、Reticulitermes hageni、Reticulitermes hesperus、Reticulitermes santonensis、棲北散白蟻(Reticulitermes speratus)、Reticulitermes tibialis及南方散白蟻(Reticulitermes virginicus)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the Order Isoptera. A non-exhaustive list of specific genera includes (but is not limited to) Coptotermes spp., Cornitermes spp., Cryptotermes spp., Heterotermes spp., Kalotermes spp., Incisitermes spp., Macrotermes spp., Marginitermes spp., Microcerotermes spp., Procarnitermes spp., Scatter Termites (Reticulitermes spp.), Proboscis (Schedorhinotermes spp.) and Paleotermites (Zootermopsis spp.). The non-exhaustive list of specific species includes (but is not limited to) Coptotermes curvignathus, Coptotermes frenchi, Coptotermes formosanus, Heterotermes aureus, Microtermes obesi, Reticulitermes banyulensis, Reticuli grassei, Reticulitermes flavipes, Reticulitermes hageni, Reticulitermes hesperus, Reticulitermes santonensis, Reticulitermes speratus, Reticulitermes tibialis, and Reticulitermes virginicus.

於另一實施例中,式1及/或式2之分子可用於防治鱗翅目(Lepidoptera)之害蟲。特定屬之非詳盡清單包括(但不限於)褐帶卷蛾屬(Adoxophyes spp.)、地虎屬(Agrotis spp.)、帶卷蛾屬(Argyrotaenia spp.)、卷葉蛾屬(Cacoecia spp.)、麗細蛾屬(Caloptilia spp.)、禾草螟屬(Chilo spp.)、錁紋夜蛾屬(Chrysodeixis spp.)、豆粉蝶屬(Colias spp.)、草螟屬(Crambus spp.)、絹螟屬(Diaphania spp.)、桿草螟屬(Diatraea spp.)、鑽夜蛾屬(Earias spp.)、粉斑螟屬(Ephestia spp.)、Epimecis spp.、髒切葉蛾屬(Feltia spp.)、角劍夜蛾屬(Gortyna spp.)、鈴夜蛾屬(Helicoverpa spp.)、實夜蛾屬(Heliothis spp.)、Indarbela spp.、潛葉細蛾屬(Lithocolletis spp.)、Loxagrotis spp.、天幕毛蟲屬(Malacosoma spp.)、疆夜蛾屬(Peridroma spp.)、小潛細蛾屬(Phyllonorycter spp.)、黏蟲屬(Pseudaletia spp.)、蛀莖夜蛾屬(Sesamia spp.)、 夜蛾屬(Spodoptera spp.)、透翅蛾屬(Synanthedon spp.)及巢蛾屬(Yponomeuta spp.)。特定物種之非詳盡清單包括(但不限於)飛揚阿夜蛾(Achaea janata)、棉褐帶卷蛾(Adoxophyes orana)、小地老虎(Agrotis ipsilon)、棉葉波紋葉蛾(Alabama argillacea)、Amorbia cuneana、臍橙螟蛾(Amyelois transitella)、Anacamptodes defectaria、桃條麥蛾(Anarsia lineatella)、黃麻橋夜蛾(Anomis sabulifera)、黎豆夜蛾(Anticarsia gemmatalis)、果樹黃卷蛾(Archips argyrospila)、玫瑰黃卷蛾(Archips rosana)、桔帶卷蛾(Argyrotaenia citrana)、丫紋夜蛾(Autographa gamma)、Bonagota cranaodes、禾弄蝶(Borbo cinnara)、棉潛蛾(Bucculatrix thurberiella)、菸捲蛾(Capua reticulana)、桃小食心蟲(Carposina niponensis)、橫線尾夜蛾(Chlumetia transversa)、薔薇斜條卷葉蛾(Choristoneura rosaceana)、稻縱卷葉螟(Cnaphalocrocis medinalis)、可可細蛾(Conopomorpha cramerella)、芳香木蠹蛾(Cossus cossus)、Cydia caryana、李小食心蟲(Cydia funebrana)、梨小食心蟲(Cydia molesta)、豌豆小卷蛾(Cydia nigricana)、蘋果蠹蛾(Cydia pomonella)、Darna diducta、小蔗桿草螟(Diatraea saccharalis)、西南玉米螟(Diatraea grandiosella)、埃及金剛鑽(Earias insulana)、翠紋鑽夜蛾(Earias vittella)、Ecdytolopha aurantianum、南美玉米苗斑螟(Elasmopalpus lignosellus)、粉斑螟(Ephestia cautella)、菸草粉斑螟(Ephestia elutella)、地中海斑螟(Ephestia kuehniella)、Epinotia aporema、蘋淡褐卷蛾(Epiphyas postvittana)、Erionota thrax、葡萄螟蛾(Eupoecilia ambiguella)、原切根蟲(Euxoa auxiliaris)、東方果實蛾(Grapholita molesta)、三紋螟蛾(Hedylepta indicata)、棉鈴蟲(Helicoverpa armigera)、穀實夜蛾(Helicoverpa zea)、美洲菸葉蛾(Heliothis virescens)、菜螟(Hellula undalis)、番茄蠹蛾(Keiferia lycopersicella)、茄黃斑螟(Leucinodes orbonalis)、咖啡 點潛蛾(Lencoptera coffeella)、旋紋潛蛾(Leucoptera malifoliella)、葡萄漿果小卷蛾(Lobesia botrana)、Loxagrotis albicosta、舞毒蛾(Lymantria dispar)、窄翅潛葉蛾(Lyonetia clerkella)、Mahasena corbetti、甘藍夜蛾(Mamestra brassicae)、豆莢野螟(Maruca testulalis)、Metisa plana、Mythimna unipuncta、Neoleucinodes elegantalis、稻三點螟(Nymphula depunctalis)、冬尺蠖蛾(Operophtera brumata)、歐洲玉米螟(Ostrinia nubilalis)、Oxydia vesulia、葡萄褐卷蛾(Pandemis cerasana)、蘋褐卷蛾(Pandemis heparana)、非洲達摩鳳蝶(Papilio demodocus)、紅鈴蟲(Pectinophora gossypiella)、豆雜角夜蛾(Peridroma saucia)、咖啡潛葉蛾(Perileucoptera coffeella)、馬鈴薯塊莖蛾(Phthorimaea operculella)、橘細潛蛾(Phyllocnistis citrella)、菜粉蝶(Pieris rapae)、苜蓿綠夜蛾(Plathypena scabra)、印度穀螟(Plodia interpunctella)、小菜蛾(Plutella xylostella)、Polychrosis viteana、Prays endocarpa、油橄欖巢蛾(Prays oleae)、一星黏蟲(Pseudaletia unipuncta)、大豆夜蛾(Pseudoplusia includens)、Rcchiplusia nu、三化螟(Scirpophaga incertulas)、大螟(Sesamia inferens)、莖螟(Sesamia nonagrioides)、蕁麻毛蟲(Setora nitens)、麥蛾(Sitotroga cerealella)、葡萄長鬚卷葉蛾(Sparganothis pilleriana)、甜菜夜蛾(Spodoptera exigua)、草地黏蟲(Spodoptera frugiperda)、亞熱帶黏蟲(Spodoptera eridania)、鳳梨鑽心蟲(Thecla basilides)、衣蛾(Tineola bisselliella)、粉紋夜蛾(Trichoplusia ni)、番茄斑潛蠅(Tuta absoluta)、咖啡木蠹蛾(Zeuzera coffeae)及梨豹蠹蛾(Zeuzera pyrina)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Lepidoptera pests. A non-exhaustive list of specific genera includes (but is not limited to) Adoxophyes spp., Agrotis spp., Argyrotaenia spp., Cacoecia spp. ), Caloptilia spp., Chilo spp., Chrysodeixis spp., Colias spp., Crambus spp. , Diaphania spp., Diatraea spp., Earias spp., Ephestia spp., Epimecis spp., Diatraea spp. Feltia spp., Gortyna spp., Helicoverpa spp., Heliothis spp., Indarbela spp., Lithocolletis spp. , Loxagrotis spp., Malacosoma spp., Peridroma spp., Phyllonorycter spp., Pseudaletia spp., Pseudaletia spp. Sesamia spp.), Spodoptera spp., Synanthedon spp. and Yponomeuta spp. A non-exhaustive list of specific species includes (but is not limited to) Achaea janata, Adoxophyes orana, Agrotis ipsilon, Alabama argillacea, Amorbia cuneana, navel orange borer (Amyelois transitella), Anacamptodes defectaria, peach-striped wheat moth (Anarsia lineatella), Huang Maqiao nocturnal moth (Anomis sabulifera), Anticarsia gemmatalis (Anticarsia gemmatalis), fruit tree yellow roll moth (Archips argyrospila), Archips rosana, Argyrotaenia citrana, Autographa gamma, Bonagota cranaodes, Borbo cinnara, Bucculatrix thurberiella, Capua reticulana, Carposina niponensis, Chlumetia transversa, Choristoneura rosaceana, Cnaphalocrocis medinalis, Conopomorpha cramerella, Cossus cossus, Cydia caryana, Cydia funebrana, Cydia molesta, Cydia nigricana, Cydia pomonella, Darna diducta, Small cane Diatraea saccharalis, Southwest Corn Borer (Diatraea grandiosella), Egyptian Diamond (Earias insulana), Earias vittella, Ecdytolopha aurantianum, South American Corn Borer (Elasmopalpus lignosellus), Ephestia cautella), tobacco powder moth (Ephestia elutella), Mediterranean moth (Ephestia kuehniella), Epinotia aporema, apple hazel moth (Epiphy as postvittana), Erionota thrax, grape borer (Eupoecilia ambiguella), original rootworm (Euxoa auxiliaris), oriental fruit moth (Grapholita molesta), three-striped moth (Hedylepta indicata), cotton bollworm (Helicoverpa armigera), grain Night moth (Helicoverpa zea), American tobacco leaf moth (Heliothis virescens), cabbage moth (Hellula undalis), tomato codling moth (Keiferia lycopersicella), eggplant yellow spot moth (Leucinodes orbonalis), coffee spotted leaf lobster (Lencoptera coffeella), spiral lili (Leucoptera malifoliella), grape berry small roll moth (Lobesia botrana), Loxagrotis albicosta, gypsy moth (Lymantria dispar), narrow-winged leaf miner (Lyonetia clerkella), Mahasena corbetti, Mamestra brassicae, pod wild borer ( Maruca testulalis), Metisa plana, Mythimna unipuncta, Neoleucinodes elegantalis, rice three-spotted borer (Nymphula depunctalis), winter looper moth (Operophtera brumata), European corn borer (Ostrinia nubilalis), Oxydia vesulia, grape brown cerasana (Pandemis cerasana) Pandemis heparana, Papilio demodocus, Pectinophora gossypiella, Peridroma saucia, Coffee leaf miner (Perileucoptera coffeella), Potato tuber moth (Phthorimaea) operculella, Phyllocnistis citrella, Pieris rapae, Plathypena scabra, Plodia interpunctella, Plutella xylostella, Polychrosis viteana, Prays endocarpa, Prays oleae, Pseudaletia unipuncta, Pseudoplusia includens, Rcchiplusia nu, Scirpophaga incertulas, Sesamia inferens, Sesamia nonagrioides ), nettle caterpillar (Setora nitens), wheat moth (Sitotroga cerealella), grape leaf roller moth (Sparganothis pilleriana), beet armyworm (Spodoptera exigua), grass armyworm (Spodoptera frugiperda), subtropical armyworm (Spodoptera eridania) , Thecla basilides, Tineola bisselliella, Trichoplusia ni, Tuta absoluta, Zeuzera coffeae and Zeuzera pyrina ).

於另一實施例中,式1及/或式2之分子可用於防治食毛目(Mallophaga)之害蟲。特定屬之非詳盡清單包括(但不限於)Anaticola spp.、牛羽虱屬(Bovicola spp.)、角虱屬(Chelopistes spp.)、角羽虱屬(Goniodes spp.)、體虱屬(Menacanthus spp.)及嚙毛虱屬(Trichodectes spp.)。特定物種之非詳盡清單包括(但不限於)牛毛虱(Bovicola bovis)、山羊毛虱(Bovicola caprae)、綿羊毛虱(Bovicola ovis)、火雞角虱(Chelopistes meleagridis)、雞角羽虱(Goniodes dissimilis)、大角羽虱(Goniodes gigas)、雛雞羽虱(Menacanthus stramineus)、雞短角羽虱(Menopon gallinae)及犬嚙毛虱(Trichodectes canis)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the Order Mallophaga. A non-exhaustive list of specific genera includes (but is not limited to) Anaticola spp., Bovicola spp., Chelopistes spp., Goniodes spp., Menacanthus spp.) and Trichodectes spp. A non-exhaustive list of specific species includes (but is not limited to) Bovicola bovis, Bovicola caprae, Bovicola ovis, Chelopistes meleagridis, Goniodes dissimilis , Goniodes gigas, Menacanthus stramineus, Menopon gallinae and Trichodectes canis.

於另一實施例中,式1及/或式2之分子可用於防治直翅目(Orthoptera)之害蟲。特定屬之非詳盡清單包括(但不限於)黑蝗屬(Melanoplus spp.)及Pterophylla spp.。特定物種之非詳盡清單包括(但不限於)摩門螽蟖(Anabrus simplex)、非洲螻蛄(Gryllotalpa africana)、Gryllotalpa australis、Gryllotalpa brachyptera、Gryllotalpa hexadactyla、東亞飛蝗(Locusta migratoria)、角翅螽蟖(Microcentrum retinerve)、沙漠蝗(Schistocerca gregaria)及Scudderia furcata。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Orthoptera pests. A non-exhaustive list of specific genera includes (but is not limited to) Melanoplus spp. and Pterophylla spp. A non-exhaustive list of specific species includes (but is not limited to) Mormon worm (Anabrus simplex), African mole cricket (Gryllotalpa africana), Gryllotalpa australis, Gryllotalpa brachyptera, Gryllotalpa hexadactyla, Locusta migratoria (Locusta migrarum) retinerve), desert locust (Schistocerca gregaria) and Scudderia furcata.

於另一實施例中,式1及/或式2之分子可用於防治蚤目(Siphonaptera)之害蟲。特定物種之非詳盡清單包括(但不限於)雞角葉蚤(Ceratophyllus gallinae)、黑角葉蚤(Ceratophyllus niger)、犬櫛首蚤(Ctenocephalides canis)、貓櫛首蚤(Ctenocephalides felis)及致癢蚤(Pulex irritans)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Siphonaptera pests. A non-exhaustive list of specific species includes (but is not limited to) Ceratophyllus gallinae, Ceratophyllus niger, Ctenocephalides canis, Ctenocephalides felis, and itching Fleas (Pulex irritans).

於另一實施例中,式1及/或式2之分子可用於防治纓翅目(Thysanoptera)之害蟲。特定屬之非詳盡清單包括(但不限於)巢針薊馬屬(Caliothrips spp.)、花薊馬屬(Frankliniella spp.)、硬薊馬屬(Scirtothrips spp.)及薊馬屬(Thrips spp.)。特定種之非詳盡清單包括(但不限於)菸草褐薊馬(Frankliniella fusca)、苜蓿薊馬(Frankliniella occidentalis)、梳缺花薊馬(Frankliniella schultzei)、玉米薊馬(Frankliniella williamsi)、變葉木薊馬 (Heliothrips haemorrhoidalis)、腹鉤薊馬(Rhipiphorothrips cruentatus)、橘實薊馬(Scirtothrips citri)、茶黃薊馬(Scirtothrips dorsalis)及Taeniothrips rhopalantennalis、黃胸薊馬(Thrips hawaiiensis)、豆黃薊馬(Thrips nigropilosus)、東方薊馬(Thrips orientalis)、菸薊馬(Thrips tabaci)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control Thysanoptera pests. A non-exhaustive list of specific genera includes (but is not limited to) Caliothrips spp., Frankliniella spp., Scirtothrips spp., and Thrips spp. ). A non-exhaustive list of specific species includes (but is not limited to) tobacco brown thrips (Frankliniella fusca), alfalfa thrips (Frankliniella occidentalis), comb-deficient thrips (Frankliniella schultzei), corn thrips (Frankliniella williamsi), variegated wood thistle Horses (Heliothrips haemorrhoidalis), Rhipiphorothrips cruentatus, Scirtothrips citri, Scirtothrips dorsalis and Taeniothrips rhopalantennalis, Yellow-breasted Thrips (Thrips hawaiiensis), Yellow-breasted Thrips (Thrips hawaiiensis) Thrips nigropilosus, Thrips orientalis, Thrips tabaci.

於另一實施例中,式1及/或式2之分子可用於防治纓尾目(Thysanura)之害蟲。特定屬之非詳盡清單包括(但不限於)衣魚屬(Lepisma spp.)及灶衣魚屬(Thermobia spp.)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the order Thysanura. A non-exhaustive list of specific genera includes (but is not limited to) Lepisma spp. and Thermobia spp.

於另一實施例中,式1及/或式2之分子可用於防治蜱蟎目(Acarina)之害蟲。特定屬之非詳盡清單包括(但不限於)粉蟎屬(Acarus spp.)、刺皮節蜱屬(Aculops spp.)、牛蜱屬(Boophilus spp.)、蠕形蟎屬(Demodex spp.)、矩頭蟬屬(Dermacentor spp.)、上癭蟎屬(Epitrimerus spp.)、癭蟎屬(Eriophyes spp.)、硬蜱屬(Ixodes spp.)、小爪蟎屬(Oligonychus spp.)、全爪蟎屬(Panonychus spp.)、根蟎屬(Rhizoglyphus spp.)及葉蟎屬(Tetranychus spp.)。特定物種之非詳盡清單包括(但不限於)氣管蟎(Acarapis woodi)、粗腳粉蟎(Acarus siro)、Aceria mangiferae、番茄刺皮癭蟎(Aculops lycopersici)、Aculus pelekassi、蘋刺癭蟎(Aculus schlechtendali)、美洲花蜱(Amblyomma americanum)、卵形短鬚蟎(Brevipalpus obovatus)、紫紅短鬚蟎(Brevipalpus phoenicis)、變異矩頭蜱(Dermacentor variabilis)、屋塵蟎(Dermatophagoides pteronyssinus)、鵝耳櫪始葉蟎(Eotetranychus carpini)、貓背肛蟎(Notoedres cati)、咖啡小爪蟎(Oligonychus coffeae)、Oligonychus ilicis、橘全爪蟎(Panonychus citri)、蘋果紅蜘蛛(Panonychus ulmi)、柑橘鏽蟎(Phyllocoptruta oleivora)、多食跗線蟎(Polyphagotarsonemus latus)、血紅扇頭蜱(Rhipicephalus sanguineus)、疥蟎(Sarcoptes scabiei)、Tegolophus perseaflorae、棉葉蟎(Tetranychus urticae)及狄氏瓦蟎(Varroa destructor)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the order Acarina. A non-exhaustive list of specific genera includes (but is not limited to) Acarus spp., Aculops spp., Boophilus spp., Demodex spp. , Dermacentor spp., Epitrimerus spp., Eriophyes spp., Ixodes spp., Oligonychus spp., All Claw mites (Panonychus spp.), Rhizoglyphus spp. and Tetranychus spp. A non-exhaustive list of specific species includes (but is not limited to) Acarapis woodi, Acarus siro, Aceria mangiferae, Aculops lycopersici, Aculus pelekassi, Aculus siro schlechtendali), American flower tick (Amblyomma americanum), Brevipalpus obovatus, Brevipalpus phoenicis, Dermacentor variabilis, House dust mite (Dermatophagoides pteronyssinus), Carpinus Eotetranychus carpini, Notoedres cati, Oligonychus coffeae, Oligonychus ilicis, Panonychus citri, Apple red spider (Panonychus ulmi), Citrus rust mite ( Phyllocoptruta oleivora, Polyphagotarsonemus latus, Rhipicephalus sanguineus, Sarcoptes scabiei, Tegolophus perseaflorae, Tetranychus urticae and Varro varroa.

於另一實施例中,式1及/或式2之分子可用於防治綜合目(Symphyla)之害蟲。特定種之非詳盡清單包括(但不限於)白松蟲(Scutigerella immaculata)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the order Symphyla. A non-exhaustive list of specific species includes (but is not limited to) Scutigerella immaculata.

於另一實施例中,式1及/或式2之分子可用於防治線蟲動物門之害蟲。特定屬之非詳盡清單包括(但不限於)滑刃線蟲屬(Aphelenchoides spp.)、刺線蟲屬(Belonolaimus spp.)、小環線蟲屬(Criconemella spp.)、莖線蟲屬(Ditylenchus spp.)、異皮線蟲屬(Heterodera spp.)、潛根線蟲屬(Hirschmanniella spp.)、紐帶線蟲屬(Hoplolaimus spp.)、根結線蟲屬(Meloidogyne spp.)、草地墊刃線蟲屬(Pratylenchus spp.)及內侵線蟲屬(Radopholus spp.)。特定種之非詳盡清單包括(但不限於)犬惡絲蟲(Dirofilaria immitis)、Heterodera zeae、南方根結線蟲(Meloidogyne incognita)、爪哇根結線蟲(Meloidogyne javanica)、盤尾絲蟲(Onchocerca volvulus)、香蕉穿孔線蟲(Radopholus similis)及腎形線蟲(Rotylenchulus reniformis)。 In another embodiment, the molecules of Formula 1 and/or Formula 2 can be used to control pests of the phylum Nematode. A non-exhaustive list of specific genera includes (but is not limited to) Aphelenchoides spp., Belonolaimus spp., Criconemella spp., Ditylenchus spp., Heterodera spp., Hirschmanniella spp., Hopolaimus spp., Meloidogyne spp., Pratylenchus spp. and Pratylenchus spp. Invasive nematodes (Radopholus spp.). A non-exhaustive list of specific species includes (but is not limited to) Dirofilaria immitis, Heterodera zeae, Meloidogyne incognita, Meloidogyne javanica, Onchocerca volvulus , Banana piercing nematode (Radopholus similis) and kidney-shaped nematode (Rotylenchulus reniformis).

額外的資訊可參考「Handbook of Pest Control-The Behavior,Life History,and Control of Household Pests」,Arnold Mallis著,第9版,GIE Media Inc版權所有(2004)。 For additional information, please refer to " Handbook of Pest Control-The Behavior, Life History, and Control of Household Pests", by Arnold Mallis, 9th edition, copyright GIE Media Inc (2004).

施用Apply

防治線形動物門、節肢動物門及/或軟體動物門之害蟲一般意謂減少所在地之害蟲群體、害蟲活動性或兩者。此可發生在:(a)自所在地驅逐害蟲群體;(b)使害蟲不適於所在地或周圍;或(c)消滅所在地或周圍的害蟲。 Controlling pests in the phylum Linear Animals, Arthropods, and/or Molluscs generally means reducing the local pest population, pest activity, or both. This can happen when: (a) expelling groups of pests from the location; (b) making the pests unsuitable for the location or surroundings; or (c) destroying the pests at or around the location.

當然,可存在此等結果之組合。一般而言,害蟲群體、活 動性或兩者宜減少大於50%、較佳大於90%且最佳大於98%。一般而言,所在地並非人類體內或體表;因此,所在地一般為非人類所在地。 Of course, there can be a combination of these results. Generally speaking, the pest population, activity or both should be reduced by more than 50%, preferably by more than 90%, and most preferably by more than 98%. Generally speaking, the location is not in or on the human body; therefore, the location is generally a non-human location.

於另一實施例中,施用式1及/或式2之分子的所在地可為線形動物門、節肢動物門及/或軟體動物門之害蟲棲息、或可能棲息或可能穿過的任何所在地。舉例而言,所在地可為:(a)作物、樹木、水果、穀類、飼料物種、藤本植物、草皮及/或觀賞性植物生長處;(b)家養動物居住地;(c)建築物(諸如儲存穀物之場所)之內部或外部表面;(d)建築物中所用之構築材料(諸如浸漬木材);及(e)建築物周圍的土壤。 In another embodiment, the location where the molecules of Formula 1 and/or Formula 2 are applied may be any location where pests of the phylum Nematoda, Arthropod and/or Mollusca inhabit, or may inhabit or may pass through. For example, the location may be: (a) crops, trees, fruits, cereals, fodder species, vines, turf and/or ornamental plant growth places; (b) domestic animal residence; (c) buildings (such as The internal or external surface of the place where the grain is stored); (d) the construction materials used in the building (such as impregnated wood); and (e) the soil around the building.

使用式1及/或式2之分子的特定作物區域包括蘋果、玉米、向日葵、棉花、大豆、芥花、小麥、水稻、高樑、大麥、燕麥、馬鈴薯、柑橘、苜蓿、萵苣、草莓、蕃茄、胡椒、十字花科植物、梨、菸草、杏仁、糖用甜菜、蠶豆及其他有價值作物生長或欲種植其種子的區域。當生長多種植物時,使用硫酸銨與式1及/或式2之分子亦為有利的。 Specific crop regions that use the molecules of Formula 1 and/or Formula 2 include apple, corn, sunflower, cotton, soybean, canola, wheat, rice, sorghum, barley, oats, potato, citrus, alfalfa, lettuce, strawberry, tomato , Peppers, cruciferous plants, pears, tobacco, almonds, sugar beets, broad beans and other valuable crops grow or want to plant their seeds. When growing a variety of plants, it is also advantageous to use ammonium sulfate and molecules of Formula 1 and/or Formula 2.

於另一實施例中,式1及/或式2之分子一般以每公項約0.0001公克至每公頃約5000公克之量使用以提供防治。於另一實施例中,式1及/或式2之分子較佳以每公頃約0.001公克至每公頃約500公克之量使用。於另一實施例中,式1及/或式2之分子更佳以每公頃約0.01公克至每公頃約50公克之量使用。 In another embodiment, the molecules of Formula 1 and/or Formula 2 are generally used in an amount of about 0.0001 grams per kilogram to about 5000 grams per hectare to provide control. In another embodiment, the molecules of Formula 1 and/or Formula 2 are preferably used in an amount of about 0.001 grams per hectare to about 500 grams per hectare. In another embodiment, the molecules of formula 1 and/or formula 2 are preferably used in an amount of about 0.01 g per hectare to about 50 g per hectare.

式1及/或式2之分子可單獨或與增強植物活力(例如生長較佳根系統、較佳耐受應激生長條件)之其他化合物以同時或依序施用之混合物形式使用。此類其他化合物為例如調節植物乙烯受體之化合物,最值得 注意的是1-甲基環丙烯(亦稱為1-MCP)。此外,此類分子可在害蟲活動性低的時間期間使用,諸如在生長的植物開始產生有價值的農業商品之前。此類時間包括提早種植季節,此時害蟲壓力通常較低。 The molecules of Formula 1 and/or Formula 2 can be used alone or as a mixture with other compounds that enhance plant vigor (for example, better root system growth, better stress-tolerant growth conditions) applied simultaneously or sequentially. Such other compounds are, for example, compounds that modulate plant ethylene receptors, most notably 1-methylcyclopropene (also known as 1-MCP). In addition, such molecules can be used during periods of low pest activity, such as before growing plants begin to produce valuable agricultural commodities. Such times include earlier planting seasons, when pest pressure is usually lower.

式1及/或式2之分子可施用於植物之葉面及結果部分以防治害蟲。分子將與害蟲直接接觸,或害蟲將在食用含有殺蟲劑之葉、果實或吸取含有殺蟲劑之汁液時食用殺蟲劑。式1及/或式2之分子亦可施用於土壤,且當以此方式施用時,可防治食用根及莖之害蟲。根可吸收分子,將其向上輸送至植物之葉面部分以防治地面上咀嚼及食用汁液之害蟲。 The molecules of Formula 1 and/or Formula 2 can be applied to the foliage and fruiting parts of plants to control pests. Molecules will come into direct contact with pests, or pests will consume pesticides when they eat leaves, fruits, or sap that contains pesticides. The molecules of Formula 1 and/or Formula 2 can also be applied to the soil, and when applied in this way, they can control pests of edible roots and stems. Roots can absorb molecules and transport them up to the leaf surface of the plant to prevent pests on the ground from chewing and eating sap.

一般對於誘餌而言,將誘餌置於例如白蟻可與誘鉺接觸及/或引誘至誘鉺處的地面。誘餌亦可施用於例如螞蟻、白蟻、蜚蠊及蒼蠅可與誘鉺接觸及/或引誘至誘鉺處的建築物之表面(水平、豎直或傾斜表面)。誘餌可包含式1及/或式2之分子。 Generally, for bait, the bait is placed on the ground where, for example, termites can come into contact with the bait and/or be attracted to the bait. The bait can also be applied to, for example, ants, termites, cockroaches and flies that can come into contact with the bait and/or be attracted to the surface (horizontal, vertical or inclined surface) of the building where the bait is located. The bait can include molecules of Formula 1 and/or Formula 2.

式1及/或式2之分子可囊封於膠囊內部或置於膠囊表面上。膠囊之尺寸可介於奈米尺寸(約100-900奈米直徑)至微米尺寸(約10-900微米直徑)之範圍。 The molecules of Formula 1 and/or Formula 2 can be encapsulated inside the capsule or placed on the surface of the capsule. The size of the capsule can range from nanometer size (approximately 100-900 nanometer diameter) to micrometer size (approximately 10-900 microns diameter).

由於一些害蟲之卵抗某些殺蟲劑之獨特能力,故可能需要重複施用式1及/或式2之分子以防治新出現的幼蟲。 Due to the unique ability of the eggs of some pests to resist certain insecticides, it may be necessary to repeatedly apply the molecules of Formula 1 and/or Formula 2 to control newly emerging larvae.

植物中殺蟲劑之系統性移動可用於藉由將式1及/或式2之分子施用於植物之不同部分(例如藉由噴霧一定區域)而防治植物之一個部分的害蟲。舉例而言,食葉昆蟲之防治可藉由滴灌或溝施、藉由用例如種植前或種植後土壤浸液處理土壤、或藉由在種植之前處理植物種子來實現。 The systematic movement of pesticides in plants can be used to control pests in one part of the plant by applying the molecules of Formula 1 and/or Formula 2 to different parts of the plant (for example, by spraying a certain area). For example, the control of leaf-eating insects can be achieved by drip irrigation or furrow application, by treating the soil with, for example, pre-planting or post-planting soil infusion, or by treating plant seeds before planting.

種子處理可應用於全部類型之種子,包括來自經遺傳修飾以表現特定性狀之植物的將萌發的種子。代表性實例包括表現對無脊椎害 蟲具有毒性之蛋白質(諸如蘇力菌或其他殺昆蟲毒素)之種子、表現除草劑抗性之種子(諸如「Roundup Ready」種子)、或具有表現殺昆蟲毒素、除草劑抗性、營養增強、抗旱性或任何其他有益性狀之「堆疊」外源基因的種子。此外,此類使用式1及/或式2之分子的種子處理可進一步增強植物較佳耐受應激生長條件之能力。此產生更健康、更有活力的植物,可使得在收穫時間的產量較高。一般而言,每100,000個種子約1公克至約500公克式1及/或式2之分子預期提供良好效益,每100,000個種子約10公克至約100公克之量預期提供較佳效益,且每100,000個種子約25公克至約75公克之量預期提供甚至較佳效益。 Seed treatment can be applied to all types of seeds, including seeds that will germinate from plants that have been genetically modified to exhibit specific traits. Representative examples include seeds that exhibit proteins that are toxic to invertebrate pests (such as suricata or other insecticidal toxins), seeds that exhibit herbicide resistance (such as ``Roundup Ready'' seeds), or seeds that exhibit insecticidal toxins, Seeds of "stacking" foreign genes for herbicide resistance, nutritional enhancement, drought resistance or any other beneficial traits. In addition, such seed treatments using molecules of Formula 1 and/or Formula 2 can further enhance the ability of plants to better withstand stress growth conditions. This produces healthier, more vigorous plants, which can lead to higher yields at harvest time. Generally speaking, the molecules of formula 1 and/or formula 2 are expected to provide good benefits from about 1 gram to about 500 grams per 100,000 seeds, and the amount of about 10 grams to about 100 grams per 100,000 seeds is expected to provide better benefits. An amount of about 25 grams to about 75 grams of 100,000 seeds is expected to provide even better benefits.

應易於顯而易見的是,式1及/或式2之分子可用於以下植物上、內部或周圍:經遺傳修飾以表現特定性狀(諸如蘇力菌或其他殺昆蟲毒素)之植物、或表現除草劑抗性之植物、或具有表現殺昆蟲毒素、除草劑抗性、營養增強或任何其他有益性狀之「堆疊」外源基因的植物。 It should be readily apparent that the molecules of Formula 1 and/or Formula 2 can be used on, in, or around the following plants: plants that have been genetically modified to exhibit specific traits (such as threus or other insecticidal toxins), or to exhibit herbicides Resistant plants, or plants that have "stacked" foreign genes that exhibit insecticidal toxins, herbicide resistance, nutritional enhancement, or any other beneficial traits.

式1及/或式2之分子可在獸醫學領域或非人類動物飼養領域用於防治內部寄生蟲及外部寄生蟲。式1及/或式2之分子係諸如藉由以例如錠劑、膠囊、飲料、顆粒形式經口投與、藉由以例如蘸塗、噴霧、傾倒、點樣及噴粉形式經皮施用、及藉由以例如注射液形式非經腸投與來施用。 The molecules of Formula 1 and/or Formula 2 can be used to control internal parasites and external parasites in the field of veterinary medicine or non-human animal breeding. The molecules of formula 1 and/or formula 2 are such as by oral administration in the form of, for example, lozenges, capsules, beverages, granules, by, for example, transdermal application in the form of dip coating, spraying, pouring, spotting and dusting, And by parenteral administration in the form of, for example, an injection.

式1及/或式2之分子亦適宜用於家畜飼養,例如牛、羊、豬、雞及鵝。其亦適宜用於寵物,諸如馬、犬及貓。欲防治的具體害蟲將為此類動物煩惱的跳蚤及扁虱。適合之調配物與飲用水或飼料一起經口投與該等動物。適合之劑量及調配物視物種而定。 The molecules of Formula 1 and/or Formula 2 are also suitable for raising livestock, such as cattle, sheep, pigs, chickens and geese. It is also suitable for pets such as horses, dogs and cats. The specific pests to be controlled will be fleas and ticks that bother such animals. A suitable formulation is orally administered to these animals together with drinking water or feed. The appropriate dosage and formulation depend on the species.

式1及/或式2之分子亦可用於防治以上列出之動物中(尤其腸道)之寄生蠕蟲。 The molecules of Formula 1 and/or Formula 2 can also be used to control parasitic worms in the animals listed above (especially the intestinal tract).

式1及/或式2之分子亦可用於人類健康護理之治療方法。此類方法包括(但限於)以例如錠劑、膠囊、飲料、顆粒形式經口投與及藉由經皮施用。 The molecules of Formula 1 and/or Formula 2 can also be used in human health care treatment methods. Such methods include, but are limited to, oral administration in the form of, for example, lozenges, capsules, beverages, granules, and by transdermal administration.

全世界之害蟲已遷移至新環境(對於此類害蟲)且此後變成此類新環境的新侵入性物種。式1及/或式2之分子亦可用於此類新侵入性物種以在此類新環境中對其進行防治。 Pests all over the world have migrated to new environments (for such pests) and have since become new invasive species in such new environments. The molecules of Formula 1 and/or Formula 2 can also be used in such new invasive species to control them in such new environments.

式1及/或式2之分子亦可用於植物(諸如作物)生長(例如種植前、種植、收穫前)及存在少量(甚至實際不存在)可商業上損害此類植物之害蟲的區域。在此類區域中使用此類分子將益於植物在區域中生長。此類益處可包括(但不限於)改良植物健康狀況、改良植物產量(例如增加生物質量及/或增加有價值成分之含量)、改良植物活力(例如改良植物生長及/或葉子更綠)、改良植物品質(例如改良某些成分之含量或組成)及改良植物對非生物及/或生物性逆境之耐受性。 The molecules of Formula 1 and/or Formula 2 can also be used in the growth of plants (such as crops) (for example, before planting, planting, and harvesting) and areas where there are a small amount (or even non-existent) pests that can commercially damage such plants. The use of such molecules in such areas will benefit the growth of plants in the area. Such benefits may include (but are not limited to) improved plant health, improved plant yield (e.g., increased biological quality and/or increased content of valuable components), improved plant vitality (e.g. improved plant growth and/or greener leaves), Improve plant quality (for example, improve the content or composition of certain components) and improve plant tolerance to abiotic and/or biotic adversities.

在殺蟲劑可商業上使用或出售之前,此類殺蟲劑經歷多個政府當局(本地、地區、州、國家及國際)冗長的評估過程。龐大的資料要求由管理當局指定且必須由產品註冊者或由代表產品註冊者之第三方通常使用連接至全球資訊網之電腦經由資料生成及提交而寄送。此等政府當局接著審查此類資料且若得出安全性判定,則向潛在使用者或賣方提供產品註冊批准。此後,在授予且支持產品註冊之地點,此類使用者或賣方可使用或出售此類殺蟲劑。 Before pesticides can be used or sold commercially, such pesticides undergo a lengthy evaluation process by multiple government authorities (local, regional, state, national, and international). The huge data request is designated by the regulatory authority and must be sent by the product registrant or a third party on behalf of the product registrant, usually using a computer connected to the World Wide Web through data generation and submission. These government authorities then review such information and, if a safety determination is reached, provide product registration approval to potential users or sellers. Thereafter, such users or sellers may use or sell such pesticides in locations where product registration is granted and supported.

根據式1及/或式2之分子可經測試以測定其針對害蟲之功效。此外,可進行作用模式研究以確定該分子是否具有與其他殺蟲劑不同的作用模式。此後,此類獲取的資料可諸如藉由網際網路散佈至第三方。 Molecules according to Formula 1 and/or Formula 2 can be tested to determine their efficacy against pests. In addition, a mode of action study can be performed to determine whether the molecule has a different mode of action than other pesticides. Thereafter, such acquired information can be distributed to third parties, such as via the Internet.

此文件之標題僅為方便起見且不必用於解釋此處之任何部分。The title of this document is for convenience only and need not be used to explain any part here.

表格部分Form part

Figure 106137106-A0202-12-0130-64
Figure 106137106-A0202-12-0130-64

於本文中表1及表2中所揭露之根據式1及/或式2的分子(化合物)係經測試以判定其對於害蟲之功效,且通常在A類別及/或B類別顯示出活性。 The molecules (compounds) according to Formula 1 and/or Formula 2 disclosed in Table 1 and Table 2 are tested to determine their efficacy against pests, and usually show activity in Class A and/or Class B.

Figure 106137106-A0202-11-0003-5
Figure 106137106-A0202-11-0003-5

Claims (10)

一種化合物,其係選自於具有下式之化合物:
Figure 106137106-A0305-02-0135-1
其中:(A)Ar1係選自(1)呋喃基、苯基、噠嗪基(pyridazinyl)、吡啶基、嘧啶基或噻吩基;或(2)經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基;其中所述經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基係具有一或多個獨立地選自由以下組成之群的取代基:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的 取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(B)Het為5員或6員之飽和或不飽和雜環,其含有獨立地選自氮、硫或氧之一或多個雜原子,且其中Ar1及Ar2係不彼此相鄰(但可相間或相對,諸如,對於5員環其為1,3,而對於6員環其為1,3或1,4),且其中該雜環亦可經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、側氧基、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、 S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(C)Ar2係選自(1)呋喃基、苯基、噠嗪基、吡啶基、嘧啶基或噻吩基;或(2)經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基;其中所述經取代之呋喃基、經取代之苯基、經取代之噠嗪基、經取代之吡啶基、經取代之嘧啶基或經取代之噻吩基係具有一或多個獨立地選自由以下組成之群的取代基:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8) 鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;(D)L為選自以下之連接基團:(1)一飽和或不飽和、經取代或未經取代之直鏈(C1-C4)烴基連接基團;及(2)一飽和或不飽和、經取代或未經取代之環狀(C3-C8)烴基連接基團;其中所述連接基團中之每一者係將Ar2與-NH-連接,且其中所述經取代之直鏈(C1-C4)烴基連接基團及經取代之環狀(C3-C8)烴基連接基團係具有一或多個獨立地選自R8、R9、R10、R11及R12的取代基,其中R8、R9、R10、R11及R12每一者係選自F、Cl、Br、I、CN、側氧基、(C1-C6)烷基、(C2-C6)烯基、(C2-C6)鹵烯基、(C2-C6)炔基、(C1-C6)鹵烷基、(C3-C6)環烷基、(C3-C6)環烯基、(C3-C6)鹵環烷基、(C1-C6)烷氧基、(C1-C6)鹵烷氧基或苯基;(H)R3係選自由以下所組成之群:(C3-C8)環烷基、苯基、(C1-C8)烷基苯基、(C1-C8)烷基-O-苯基、(C2-C8)烯基-O-苯基、(Het-1)、(C1-C8)烷基-(Het-1)及(C1-C8)烷基-O-(Het-1); 其中烷基、環烷基、烯基、苯基及(Het-1)每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、NRxRy、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C1-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、O-(C1-C8)烷基、S-(C1-C8)烷基、(C1-C8)烷基-O-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基、苯氧基及(Het-1);(J)R5、R6及R7係各獨立地選自由以下組成之群:H、F、Cl、Br、I、CN、OH、NO2、側氧基、硫基(thioxo)、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及(Het-1);(K)Rx及Ry係各獨立地選自由以下組成之群:H、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)H、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基 -S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及(C1-C8)烷基苯基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及烷基苯基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)H、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及(Het-1);(L)(Het-1)為一個5員或6員之飽和或不飽和雜環,其含有獨立地選自氮、硫或氧之一或多個雜原子;其中該雜環係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取代:H、F、Cl、Br、I、CN、NO2、側氧基、(C1-C8)烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、OSO2-(C1-C8)烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;其中烷基、環烷基、烷氧基、烯基、炔基、苯基及苯氧基取代基每一者係可選擇性地經一或多個獨立地選自由以下組成之群的取代基取 代:H、F、Cl、Br、I、CN、NO2、(C1-C8)烷基、(C1-C8)鹵烷基、(C3-C8)環烷基、(C1-C8)烷氧基、(C1-C8)鹵烷氧基、(C2-C8)烯基、(C2-C8)炔基、S(O)n-(C1-C8)烷基、S(O)n-(C1-C8)鹵烷基、OSO2-(C1-C8)烷基、OSO2-(C1-C8)鹵烷基、C(O)-NRxRy、(C1-C8)烷基-NRxRy、C(O)-(C1-C8)烷基、C(O)O-(C1-C8)烷基、C(O)-(C1-C8)鹵烷基、C(O)O-(C1-C8)鹵烷基、C(O)-(C3-C8)環烷基、C(O)O-(C3-C8)環烷基、C(O)-(C2-C8)烯基、C(O)O-(C2-C8)烯基、(C1-C8)烷基-O-(C1-C8)烷基、(C1-C8)烷基-S(O)n-(C1-C8)烷基、C(O)-(C1-C8)烷基-C(O)O-(C1-C8)烷基、苯基及苯氧基;且(M)n係各獨立地為0、1或2;以及其等之農業上可接受之酸加成鹽、同位素、解析的立體異構體及互變異構物。
A compound selected from compounds having the following formula:
Figure 106137106-A0305-02-0135-1
Wherein: (A) Ar 1 is selected from (1) furyl, phenyl, pyridazinyl, pyridyl, pyrimidinyl or thienyl; or (2) substituted furyl, substituted phenyl , Substituted pyridazinyl, substituted pyridinyl, substituted pyrimidinyl or substituted thienyl; wherein the substituted furanyl, substituted phenyl, substituted pyridazinyl, substituted The pyridyl group, substituted pyrimidinyl group or substituted thienyl group has one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl , C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, ( C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O )-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; wherein alkyl, cycloalkyl, alkoxy, alkenyl, Each of the alkynyl, phenyl, and phenoxy substituents can be optionally substituted with one or more substituents independently selected from the group consisting of: H, F, Cl, Br, I, CN, NO 2. (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 ) Haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -( C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O) )O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 ) Alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1- C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; (B) Het is a 5-membered or 6-membered saturated or unsaturated heterocyclic ring, which Contain one or more heteroatoms independently selected from nitrogen, sulfur or oxygen, and wherein Ar 1 and Ar 2 are not adjacent to each other (but may be alternately or opposite to each other, such as 1, 3 for a 5-membered ring, and For a 6-membered ring it is 1,3 or 1,4), and the heterocyclic ring may also be substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , pendant oxy, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl , (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O) -(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O- (C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1- C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; wherein alkyl, Each of the cycloalkyl, alkoxy, alkenyl, alkynyl, phenyl, and phenoxy substituents may be optionally substituted with one or more substituents independently selected from the group consisting of: H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 ) alkyl, (C 1 -C 8 ) haloalkyl, (C 3 -C 8 ) cycloalkyl, (C 1 -C 8 ) Alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 ) Alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C( O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C( O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O) )O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 ) Alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; (C) Ar 2 is selected from (1) furyl, phenyl, pyridazine Or (2) substituted furyl, substituted phenyl, substituted pyridazinyl, substituted pyridyl, substituted pyrimidyl or substituted thiophene Group; wherein the substituted furyl, substituted phenyl, substituted pyridazinyl, substituted pyridinyl, substituted pyrimidinyl or substituted thienyl system has one or more independently selected Substituents free from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 ) Alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 ) alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O -(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-( C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 ) Alkyl, phenyl and phenoxy; wherein each of the alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, phenyl and phenoxy substituents can be optionally substituted by one or more Substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 ) haloalkyl, ( C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1- C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1- C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )Cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 ) Alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl , C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; (D) L is a linking group selected from the following Group: (1) a saturated or unsaturated, substituted or unsubstituted linear (C 1 -C 4 ) hydrocarbyl linking group; and (2) a saturated or unsaturated, substituted or unsubstituted ring A (C 3 -C 8 ) hydrocarbyl linking group; wherein each of the linking groups connects Ar 2 to -NH-, and wherein the substituted straight chain (C 1 -C 4 ) The hydrocarbyl linking group and the substituted cyclic (C 3 -C 8 ) hydrocarbyl linking group have one or more substituents independently selected from R 8 , R 9 , R 10 , R 11 and R 12 , wherein Each of R 8 , R 9 , R 10 , R 11 and R 12 is selected from F, Cl, Br, I, CN, pendant oxy, (C 1 -C 6 ) alkyl, (C 2 -C 6 )Alkenyl, (C 2 -C 6 )haloalkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )haloalkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 )cycloalkenyl, (C 3 -C 6 )halocycloalkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )haloalkoxy or phenyl; (H) R 3 is selected from the group consisting of: (C 3 -C 8 )cycloalkyl, phenyl, (C 1 -C 8 )alkylphenyl, (C 1 -C 8 )alkyl-O-phenyl , (C 2 -C 8 )alkenyl-O-phenyl, (Het-1), (C 1 -C 8 )alkyl-(Het-1) and (C 1 -C 8 )alkyl-O-(Het-1); wherein each of alkyl, cycloalkyl, alkenyl, phenyl, and (Het-1) can be selectively treated by one or more independently Substituent substitution selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , NR x R y , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkane Group, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2- C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkane Group, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)H, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O )-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O- (C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 1 -C 8 )cycloalkyl, C(O)-( C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, O-(C 1 -C 8 )alkyl, S-(C 1 -C 8 )alkyl, ( C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkane Group, phenyl, phenoxy and (Het-1); (J) R 5 , R 6 and R 7 are each independently selected from the group consisting of H, F, Cl, Br, I, CN, OH , NO 2 , pendant oxy group, thioxo, (C 1 -C 8 ) alkyl, (C 1 -C 8 ) haloalkyl, (C 3 -C 8 ) cycloalkyl, (C 1- C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 ) alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C (O)H, C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkane Group, C(O)O-(C 1 -C 8 )haloalkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O -(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkane基-C(O)O-(C 1 -C 8 )alkyl, phenyl and (Het-1); (K) R x and R y are each independently selected from the group consisting of: H, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )alkyl, C(O)H, C(O)-(C 1 -C 8 )alkyl, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C (O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkane Group, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-( C 1 -C 8 )alkyl, phenyl and (C 1 -C 8 )alkylphenyl; wherein alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, phenyl and alkylphenyl are each One is optionally substituted with one or more substituents independently selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 ) Alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)H, C(O)-(C 1 -C 8 )alkyl, C(O) O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl, C(O)- (C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-( C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)- (C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and (Het-1); (L) (Het-1) is a 5-member or 6-member The saturated or unsaturated heterocyclic ring contains one or more heteroatoms independently selected from nitrogen, sulfur or oxygen; wherein the heterocyclic ring system can be optionally selected from one or more independently selected from the group consisting of Substituent substitution: H, F, Cl, Br, I, CN, NO 2 , pendant oxy, (C 1 -C 8 )alkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )Alkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynyl, S(O) n -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )Alkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkyl, C(O)O- (C 1 -C 8 )alkyl, C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C(O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1- C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 ) Alkyl, phenyl, and phenoxy; wherein each of the alkyl, cycloalkyl, alkoxy, alkenyl, alkynyl, phenyl, and phenoxy substituents can optionally be substituted by one or more independent Substituents selected from the group consisting of H, F, Cl, Br, I, CN, NO 2 , (C 1 -C 8 )alkyl, (C 1 -C 8 )haloalkyl, (C 3 -C 8 )cycloalkyl, (C 1 -C 8 )alkoxy, (C 1 -C 8 )haloalkoxy, (C 2 -C 8 )alkenyl, (C 2 -C 8 )alkynes Group, S(O) n -(C 1 -C 8 )alkyl, S(O) n -(C 1 -C 8 )haloalkyl, OSO 2 -(C 1 -C 8 )alkyl, OSO 2 -(C 1 -C 8 )haloalkyl, C(O)-NR x R y , (C 1 -C 8 )alkyl-NR x R y , C(O)-(C 1 -C 8 )alkane Group, C(O)O-(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )haloalkyl, C(O)O-(C 1 -C 8 )haloalkyl , C(O)-(C 3 -C 8 )cycloalkyl, C(O)O-(C 3 -C 8 )cycloalkyl, C(O)-(C 2 -C 8 )alkenyl, C( O)O-(C 2 -C 8 )alkenyl, (C 1 -C 8 )alkyl-O-(C 1 -C 8 )alkyl, (C 1 -C 8 )alkyl-S(O) n -(C 1 -C 8 )alkyl, C(O)-(C 1 -C 8 )alkyl-C(O)O-(C 1 -C 8 )alkyl, phenyl and phenoxy; And (M) n is each independently 0, 1 or 2; and agriculturally acceptable acid addition salts, isotopes, resolved stereoisomers, and tautomers thereof.
如請求項1之化合物,其中至少一個H為2H或至少一個C為14C。 The compound of claim 1, wherein at least one H is 2 H or at least one C is 14 C. 一種化合物,其係選自於具有下式之化合物:
Figure 106137106-A0305-02-0141-2
其中:(A)Ar1為經取代之苯基,其中所述經取代之苯基係具有一或多個獨立地選自(C1-C6)鹵烷基及(C1-C6)鹵烷氧基之取代基;(B)Het為1,2,4-三唑基;(C)Ar2為苯基或經取代之苯基,其中所述經取代之苯基係具有一或多個獨立地選自F、Cl、Br、I及(C1-C6)烷基之取代基; (F)R3為苯基,其中所述苯基係可選擇性地經一或多個獨立地選自由F、Cl、Br、I、(C1-C6)烷基及(C1-C6)烷氧基組成之群的取代基取代;(J)R5、R6及R7每一者係選自H、F、Cl、Br、I、CN、OH、(C1-C6)烷基及側氧基;以及(L)L為選自以下之連接基團:(1)一飽和或不飽和、經取代或未經取代之直鏈(C1-C4)烴基連接基團;及(2)一飽和或不飽和、經取代或未經取代之環狀(C3-C8)烴基連接基團;其中所述連接基團中之每一者係將Ar2與-NH-連接,且其中所述經取代之直鏈(C1-C4)烴基連接基團及經取代之環狀(C3-C8)烴基連接基團係具有一或多個獨立地選自R8、R9、R10、R11及R12的取代基,其中R8、R9、R10、R11及R12每一者係選自F、Cl、Br、I、CN、側氧基、(C1-C6)烷基、(C2-C6)烯基、(C2-C6)鹵烯基、(C2-C6)炔基、(C1-C6)鹵烷基、(C3-C6)環烷基、(C3-C6)環烯基、(C3-C6)鹵環烷基及苯基;以及其等之互變異構物。
A compound selected from compounds having the following formula:
Figure 106137106-A0305-02-0141-2
Wherein: (A) Ar 1 is a substituted phenyl group, wherein the substituted phenyl group has one or more independently selected from (C 1 -C 6 ) haloalkyl and (C 1 -C 6 ) Substituents of haloalkoxy; (B) Het is 1,2,4-triazolyl; (C) Ar 2 is phenyl or substituted phenyl, wherein said substituted phenyl has one or A plurality of substituents independently selected from F, Cl, Br, I, and (C 1 -C 6 ) alkyl; (F) R 3 is a phenyl group, wherein the phenyl group may be selectively subjected to one or more A substituent independently selected from the group consisting of F, Cl, Br, I, (C 1 -C 6 )alkyl and (C 1 -C 6 )alkoxy; (J) R 5 , R 6 and Each of R 7 is selected from H, F, Cl, Br, I, CN, OH, (C 1 -C 6 )alkyl and pendant oxy; and (L) L is a linking group selected from: (1) A saturated or unsaturated, substituted or unsubstituted linear (C 1 -C 4 ) hydrocarbyl linking group; and (2) a saturated or unsaturated, substituted or unsubstituted cyclic ( C 3 -C 8 ) a hydrocarbyl linking group; wherein each of the linking groups connects Ar 2 to -NH-, and wherein the substituted linear (C 1 -C 4 ) hydrocarbyl group is connected The group and the substituted cyclic (C 3 -C 8 ) hydrocarbyl linking group has one or more substituents independently selected from R 8 , R 9 , R 10 , R 11 and R 12 , wherein R 8 , R 9 , R 10 , R 11 and R 12 are each selected from F, Cl, Br, I, CN, pendant oxy, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkene Group, (C 2 -C 6 )haloalkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )haloalkyl, (C 3 -C 6 )cycloalkyl, (C 3 -C 6 ) Cycloalkenyl, (C 3 -C 6 )halocycloalkyl and phenyl; and their tautomers.
一種化合物,其係選自於以下所列之化合物:
Figure 106137106-A0305-02-0142-4
Figure 106137106-A0305-02-0143-5
Figure 106137106-A0305-02-0144-6
Figure 106137106-A0305-02-0145-7
Figure 106137106-A0305-02-0146-8
Figure 106137106-A0305-02-0147-9
Figure 106137106-A0305-02-0148-10
Figure 106137106-A0305-02-0149-11
Figure 106137106-A0305-02-0150-12
Figure 106137106-A0305-02-0151-13
Figure 106137106-A0305-02-0152-14
Figure 106137106-A0305-02-0153-15
Figure 106137106-A0305-02-0154-16
Figure 106137106-A0305-02-0155-17
Figure 106137106-A0305-02-0156-18
Figure 106137106-A0305-02-0157-19
Figure 106137106-A0305-02-0158-20
Figure 106137106-A0305-02-0159-21
Figure 106137106-A0305-02-0160-22
Figure 106137106-A0305-02-0161-23
Figure 106137106-A0305-02-0162-24
Figure 106137106-A0305-02-0163-25
Figure 106137106-A0305-02-0164-26
Figure 106137106-A0305-02-0165-27
Figure 106137106-A0305-02-0166-28
Figure 106137106-A0305-02-0167-29
Figure 106137106-A0305-02-0168-30
Figure 106137106-A0305-02-0169-31
Figure 106137106-A0305-02-0170-32
Figure 106137106-A0305-02-0171-33
Figure 106137106-A0305-02-0172-35
A compound selected from the following compounds:
Figure 106137106-A0305-02-0142-4
Figure 106137106-A0305-02-0143-5
Figure 106137106-A0305-02-0144-6
Figure 106137106-A0305-02-0145-7
Figure 106137106-A0305-02-0146-8
Figure 106137106-A0305-02-0147-9
Figure 106137106-A0305-02-0148-10
Figure 106137106-A0305-02-0149-11
Figure 106137106-A0305-02-0150-12
Figure 106137106-A0305-02-0151-13
Figure 106137106-A0305-02-0152-14
Figure 106137106-A0305-02-0153-15
Figure 106137106-A0305-02-0154-16
Figure 106137106-A0305-02-0155-17
Figure 106137106-A0305-02-0156-18
Figure 106137106-A0305-02-0157-19
Figure 106137106-A0305-02-0158-20
Figure 106137106-A0305-02-0159-21
Figure 106137106-A0305-02-0160-22
Figure 106137106-A0305-02-0161-23
Figure 106137106-A0305-02-0162-24
Figure 106137106-A0305-02-0163-25
Figure 106137106-A0305-02-0164-26
Figure 106137106-A0305-02-0165-27
Figure 106137106-A0305-02-0166-28
Figure 106137106-A0305-02-0167-29
Figure 106137106-A0305-02-0168-30
Figure 106137106-A0305-02-0169-31
Figure 106137106-A0305-02-0170-32
Figure 106137106-A0305-02-0171-33
Figure 106137106-A0305-02-0172-35
一種用於防治一害蟲之方法,該方法包括將如請求項1至4中任一項之化合物以足夠防治該害蟲的量施用於一所在地,其中該所在地並非在人類或動物內或人類或動物上。 A method for controlling a pest, the method comprising applying the compound of any one of claims 1 to 4 in an amount sufficient to control the pest to a locus, wherein the locus is not in humans or animals or humans or animals superior. 如請求項5之方法,其中所述害蟲為甜菜夜蛾(beet armyworm,BAW)、粉紋夜蛾(cabbage looper,CL)或黃熱病蚊(YFM)。 The method of claim 5, wherein the pest is beet armyworm (BAW), cabbage looper (CL) or yellow fever mosquito (YFM). 一種組成物,其包括有如請求項1至4中任一項之化合物以及至少一個具有殺蟲、除草、殺蟎、殺線蟲或殺真菌活性之其他化合物。 A composition comprising the compound of any one of claims 1 to 4 and at least one other compound having insecticidal, herbicidal, acaricidal, nematicidal or fungicidal activity. 一種組成物,其包括有如請求項1至4中任一項之化合物以及一載劑。 A composition comprising the compound of any one of claims 1 to 4 and a carrier. 一種用於防治一害蟲之方法,該方法包括將如請求項1至4中任一項之化合物施用於一已經過基因改造以表現一或多種特殊性狀之基因改造植物或基因改造種子。 A method for controlling a pest, the method comprising applying a compound according to any one of claims 1 to 4 to a genetically modified plant or genetically modified seed that has been genetically modified to exhibit one or more special traits. 一種如請求項1至4中任一項之化合物於製造一藥物之用途,該藥物係用於防治一非人類的動物之體內寄生蟲、體外寄生蟲或此二者。 A use of a compound according to any one of claims 1 to 4 in the manufacture of a medicine for controlling endoparasites, ectoparasites or both of a non-human animal.
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CN103826452A (en) * 2011-07-12 2014-05-28 陶氏益农公司 Pesticidal compositions and processes related thereto
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