TW201625555A - Aryl sulphide and aryl sulphoxide derivatives having C-C-attached (aza)uracils as pesticides - Google Patents
Aryl sulphide and aryl sulphoxide derivatives having C-C-attached (aza)uracils as pesticides Download PDFInfo
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
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- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
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Abstract
Description
本申請案係有關一種新穎之雜環系化合物、其製法及其於控制動物害蟲(包括節肢動物及尤指昆蟲)上之用途。 This application relates to a novel heterocyclic compound, a process for its preparation and its use for controlling animal pests, including arthropods and especially insects.
芳基硫化物及芳基亞碸衍生物及其殺昆蟲與殺蜱蟎作用已說明於文獻中,例如:WO2013/157229、WO2012/176856及WO1999/055668。 Aryl sulfides and aryl hydrazine derivatives and their insecticidal and acaricidal effects are described in the literature, for example: WO 2013/157229, WO 2012/176856 and WO 1999/055668.
作物保護劑(亦包括除害劑)必須符合許多要求,例如:與其效力、持續期、及其作用範圍及可能用途等相關方面。有關毒性及其與其他活性化合物或調配輔劑之相容性問題亦如同活性化合物所需之合成成本問題一樣扮演某種角色。此外,還會發生抗性。基於所有此等理由,認為尚未完成新穎作物保護劑之搜尋,仍然需要至少在各相關態樣上具有比已知化合物更改良性質之新穎化合物。 Crop protection agents (including pesticides) must meet many requirements, such as their effectiveness, duration, scope of action, and possible use. The toxicity and its compatibility with other active compounds or formulation adjuvants also play a role as well as the synthetic cost issues required for the active compounds. In addition, resistance can occur. For all of these reasons, it is believed that the search for novel crop protection agents has not yet been completed, and it is still necessary to have novel compounds that modify the good properties of the known compounds at least in each of the relevant aspects.
本發明之目的係提供一種化合物,其可在各種不同方面擴大除害劑作用範圍。 It is an object of the present invention to provide a compound which broadens the range of action of the pesticide in a variety of different aspects.
此目的及本文中未說明但可由相關討論中判別或推衍之其
他目的可採用新穎之式(I)化合物達成
亦已發現,該新穎式(I)化合物具有良好之除害劑效力,例如:對抗節肢動物,及尤指昆蟲與蜱蟎類,此外一般亦與植物(尤指作物) 具有極佳相容性,且/或具有有利之毒物學與/或環境相關性質。 It has also been found that the novel compounds of formula (I) have good pesticide efficacy, for example against arthropods, and especially insects and mites, in addition to plants (especially crops). It has excellent compatibility and/or has advantageous toxicological and/or environmentally relevant properties.
另一項式(I)化合物之具體實施例(具體實施例1-2)之特徵在於V1及V2 彼此分別獨立代表氧或代表硫;Q 代表經下列基團取代之碳:氫、鹵素、胺基、氰基、胺甲醯基、硝基、烷基、鹵烷基、烷基硫基、烷基亞磺醯基、烷基磺醯基、鹵烷基硫基、鹵烷基亞磺醯基、鹵烷基磺醯基、環烷基、烷基羰基、鹵烷基羰基、烷氧基羰基或烷氧基,或代表氮;R1及R2 彼此分別獨立代表氫、胺基或烷基;或代表烯基、炔基、環烷基、環烷基烷基、環烯基、氰基烷基、羥基烷基、烷基羰基、鹵烷基羰基、烷氧基烷基、鹵烷氧基烷基、烷氧基、鹵烷氧基、鹵烷基、鹵烯基或鹵炔基,其中上述基團可視需要經下列基團取代:鹵素、烷基、環烷基、氰基、硝基、烷氧基、鹵烷基或鹵烷氧基,特定言之氟、氯、(C1-C3)-烷基、(C3-C6)-環烷基、環丙基、氰基、(C1-C4)-烷氧基、(C1-C3)-鹵烷基或(C1-C3)-鹵烷氧基;或代表芳基、雜芳基、芳基烷基或雜芳基烷基,其中上述基團可視需要經下列基團取代:鹵素、烷基、環烷基、氰基、硝基、烷氧基、鹵烷基或鹵烷氧基,特定言之氟、氯、(C1-C3)-烷基、(C3-C6)-環烷基、環丙基、氰基、(C1-C4)-烷氧基、(C1-C3)-鹵烷基或(C1-C3)-鹵烷氧基;W 代表氫或鹵素;n 代表數字0、1或2;Y 代表氫、鹵素、氰基、(C1-C6)-烷基、(C3-C6)-環烷基、(C1-C6)- 鹵烷基、(C1-C6)-烷氧基或(C1-C6)-鹵烷氧基;X 代表氫、鹵素、氰基、(C1-C6)-烷基、(C1-C6)-鹵烷基或(C1-C6)-烷氧基。 Another specific embodiment of the compound of formula (I) (specific embodiment 1-2) is characterized in that V 1 and V 2 each independently represent oxygen or represent sulfur; Q represents a carbon substituted by the following groups: hydrogen, halogen , amine, cyano, amine, mercapto, nitro, alkyl, haloalkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkylthio, haloalkyl Sulfhydryl, haloalkylsulfonyl, cycloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or alkoxy, or represents nitrogen; R 1 and R 2 each independently represent hydrogen, amine Or alkyl; or represents alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cyanoalkyl, hydroxyalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxyalkyl, a haloalkoxyalkyl group, an alkoxy group, a haloalkoxy group, a haloalkyl group, a haloalkenyl group or a haloalkynyl group, wherein the above group may be substituted by the following groups: halogen, alkyl, cycloalkyl, cyanogen Alkyl, nitro, alkoxy, haloalkyl or haloalkoxy, in particular fluorine, chlorine, (C 1 -C 3 )-alkyl, (C 3 -C 6 )-cycloalkyl, cyclopropane Base, cyano group, (C 1 -C 4 )-alkoxy group, (C 1 -C 3 )-haloalkyl or (C 1 -C 3 )-haloalkoxy; or an aryl, heteroaryl, arylalkyl or heteroarylalkyl group, wherein the above groups may be optionally used Substituted by: halogen, alkyl, cycloalkyl, cyano, nitro, alkoxy, haloalkyl or haloalkoxy, in particular fluorine, chlorine, (C 1 -C 3 )-alkyl (C 3 -C 6 )-cycloalkyl, cyclopropyl, cyano, (C 1 -C 4 )-alkoxy, (C 1 -C 3 )-haloalkyl or (C 1 -C 3 )-haloalkoxy; W represents hydrogen or halogen; n represents the number 0, 1 or 2; Y represents hydrogen, halogen, cyano, (C 1 -C 6 )-alkyl, (C 3 -C 6 )- Cycloalkyl, (C 1 -C 6 )-haloalkyl, (C 1 -C 6 )-alkoxy or (C 1 -C 6 )-haloalkoxy; X represents hydrogen, halogen, cyano, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkyl or (C 1 -C 6 )-alkoxy.
由式(I)提供本發明化合物之一般定義。上文及下文所述化學式中所示基團之較佳取代基或範圍說明如下(具體實施例2-1):V1及V2分別代表氧;Q 代表氮或C-R3,其中R3 代表氫、鹵素、胺基、氰基、胺甲醯基、硝基、(C1-C6)-烷基、(C1-C6)-鹵烷基、(C1-C6)-烷基硫基、(C1-C6)-烷基亞磺醯基、(C1-C6)-烷基磺醯基、(C1-C6)-鹵烷基硫基、(C1-C6)-鹵烷基亞磺醯基、(C1-C6)-鹵烷基磺醯基、(C3-C6)-環烷基、(C1-C6)-烷基羰基、(C1-C6)-鹵烷基羰基、(C1-C6)-烷氧基羰基或(C1-C6)-烷氧基;R1及R2 彼此分別獨立代表氫、胺基或烷基;或代表烯基、炔基、環烷基、環烷基烷基、環烯基、氰基烷基、羥基烷基、烷基羰基、鹵烷基羰基、烷氧基烷基、鹵烷氧基烷基、烷氧基或鹵烷氧基,其中上述基團可視需要經取代;或代表鹵烷基、鹵烯基或鹵炔基;W 代表氫或鹵素;n 代表數字0或1;Y 代表氫、鹵素、(C1-C6)-烷基、(C3-C6)-環烷基、(C1-C6)-鹵烷基、(C1-C6)-烷氧基或(C1-C6)-鹵烷氧基;X 代表氫、鹵素、(C1-C6)-烷基、(C1-C6)-鹵烷基或(C1-C6)-烷氧基。 A general definition of a compound of the invention is provided by formula (I). Preferred substituents or ranges for the groups shown in the above formulas and hereinafter are illustrated below (specific examples 2-1): V 1 and V 2 represent oxygen, respectively; Q represents nitrogen or CR 3 , wherein R 3 represents Hydrogen, halogen, amine, cyano, amine, mercapto, nitro, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkyl, (C 1 -C 6 )-alkane thio group, (C 1 -C 6) - alkylsulfinyl acyl, (C 1 -C 6) - alkylsulfonyl group, (C 1 -C 6) - haloalkyl group, (C 1 -C 6 )-haloalkylsulfinyl, (C 1 -C 6 )-haloalkylsulfonyl, (C 3 -C 6 )-cycloalkyl, (C 1 -C 6 )-alkyl a carbonyl group, a (C 1 -C 6 )-haloalkylcarbonyl group, a (C 1 -C 6 )-alkoxycarbonyl group or a (C 1 -C 6 )-alkoxy group; R 1 and R 2 each independently represent hydrogen Or an amino group or an alkyl group; or an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkylalkyl group, a cycloalkenyl group, a cyanoalkyl group, a hydroxyalkyl group, an alkylcarbonyl group, a haloalkylcarbonyl group, an alkoxy group An alkyl group, a haloalkoxyalkyl group, an alkoxy group or a haloalkoxy group, wherein the above group may be optionally substituted; or a haloalkyl group, a haloalkenyl group or a haloalkynyl group; W represents hydrogen or a halogen; The number 0 or 1; Y stands for hydrogen, Su, (C 1 -C 6) - alkyl, (C 3 -C 6) - cycloalkyl, (C 1 -C 6) - haloalkyl, (C 1 -C 6) - alkoxy or ( C 1 -C 6 )-haloalkoxy; X represents hydrogen, halogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkyl or (C 1 -C 6 )-alkane Oxygen.
上文及下文所述化學式中所示基團之同樣較佳取代基或範圍說明如下(具體實施例2-2): V1及V2分別代表氧;Q 代表氮或C-R3,其中R3 代表氫、鹵素、胺基、氰基、胺甲醯基、硝基、(C1-C6)-烷基、(C1-C6)-鹵烷基、(C1-C6)-烷基硫基、(C1-C6)-烷基亞磺醯基、(C1-C6)-烷基磺醯基、(C1-C6)-鹵烷基硫基、(C1-C6)-鹵烷基亞磺醯基、(C1-C6)-鹵烷基磺醯基、(C3-C6)-環烷基、(C1-C6)-烷基羰基、(C1-C6)-鹵烷基羰基、(C1-C6)-烷氧基羰基或(C1-C6)-烷氧基;R1及R2 彼此分別獨立代表氫、胺基或烷基;或代表烯基、炔基、環烷基、環烷基烷基、環烯基、氰基烷基、羥基烷基、烷基羰基、鹵烷基羰基、烷氧基烷基、鹵烷氧基烷基、烷氧基或鹵烷氧基,其中上述基團可視需要經下列基團取代:鹵素、烷基、環烷基、氰基、硝基、烷氧基、鹵烷基或鹵烷氧基,特定言之氟、氯、(C1-C3)-烷基、(C3-C6)-環烷基、環丙基、氰基、(C1-C4)-烷氧基、(C1-C3)-鹵烷基或(C1-C3)-鹵烷氧基;或代表鹵烷基、鹵烯基或鹵炔基;W 代表氫或鹵素;n 代表數字0或1;Y 代表氫、鹵素、(C1-C6)-烷基、(C3-C6)-環烷基、(C1-C6)-鹵烷基、(C1-C6)-烷氧基或(C1-C6)-鹵烷氧基;X 代表氫、鹵素、(C1-C6)-烷基、(C1-C6)-鹵烷基或(C1-C6)-烷氧基。 The same preferred substituents or ranges for the groups shown in the above and below formulas are as follows (specific examples 2-2): V 1 and V 2 represent oxygen, respectively; Q represents nitrogen or CR 3 , wherein R 3 Represents hydrogen, halogen, amine, cyano, amine, mercapto, nitro, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkyl, (C 1 -C 6 )- alkylthio, (C 1 -C 6) - alkylsulfinyl acyl, (C 1 -C 6) - alkylsulfonyl group, (C 1 -C 6) - haloalkyl group, (C 1- C 6 )-haloalkylsulfinyl, (C 1 -C 6 )-haloalkylsulfonyl, (C 3 -C 6 )-cycloalkyl, (C 1 -C 6 )-alkane a carbonyl group, a (C 1 -C 6 )-haloalkylcarbonyl group, a (C 1 -C 6 )-alkoxycarbonyl group or a (C 1 -C 6 )-alkoxy group; R 1 and R 2 each independently represent Hydrogen, amine or alkyl; or represents alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cyanoalkyl, hydroxyalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxy An alkyl group, a haloalkoxyalkyl group, an alkoxy group or a haloalkoxy group, wherein the above group may be substituted by the following groups: halogen, alkyl, cycloalkyl, cyano, nitro, alkoxy , haloalkyl or haloalkoxy, Specifically, fluorine, chlorine, (C 1 -C 3 )-alkyl, (C 3 -C 6 )-cycloalkyl, cyclopropyl, cyano, (C 1 -C 4 )-alkoxy, ( C 1 -C 3 )-haloalkyl or (C 1 -C 3 )-haloalkoxy; or a haloalkyl, haloalkenyl or haloalkynyl group; W represents hydrogen or halogen; n represents the number 0 or 1 Y represents hydrogen, halogen, (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl, (C 1 -C 6 )-haloalkyl, (C 1 -C 6 )- Alkoxy or (C 1 -C 6 )-haloalkoxy; X represents hydrogen, halogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-haloalkyl or (C 1 - C 6 )-alkoxy.
式(I)化合物所示基團之更佳取代基或範圍說明如下(具體實施例3-1)。V1及V2分別代表氧;Q 代表氮或C-R3,其中 R3 代表氫、胺基、鹵素、氰基、(C1-C4)-烷基、(C1-C4)-鹵烷基、(C3-C6)-環烷基、(C1-C4)-烷基羰基、(C1-C4)-鹵烷基羰基、(C1-C4)-烷氧基羰基或(C1-C4)-烷氧基;R1及R2 彼此分別獨立代表氫、胺基、(C1-C4)-烷基、氰基-(C1-C4)-烷基、(C1-C4)-鹵烷基、(C1-C4)-烷氧基-(C1-C4)-烷基、(C1-C4)-鹵烷氧基-(C1-C4)-烷基、(C1-C4)-烷氧基或(C1-C4)-鹵烷氧基;或代表(C3-C6)-環烷基或(C3-C6)-環烷基-(C1-C2)-烷基,其中上述基團可視需要經下列基團取代:氟、氯、溴、碘、(C1-C3)-烷基、(C3-C6)-環烷基、氰基、硝基、(C1-C4)-烷氧基、(C1-C3)-鹵烷基或(C1-C3)-鹵烷氧基;W 代表氫、氯或氟;n 代表數字0或1;Y 代表鹵素、(C1-C4)-烷基、(C3-C6)-環烷基、(C1-C4)-鹵烷基、(C1-C4)-烷氧基或(C1-C4)-鹵烷氧基;X 代表氫、鹵素、(C1-C4)-烷基、(C1-C4)-鹵烷基或(C1-C4)-烷氧基。 More preferred substituents or ranges for the groups of the formula (I) are illustrated below (specific examples 3-1). V 1 and V 2 represent oxygen, respectively; Q represents nitrogen or CR 3 , wherein R 3 represents hydrogen, amine, halogen, cyano, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-halogen Alkyl, (C 3 -C 6 )-cycloalkyl, (C 1 -C 4 )-alkylcarbonyl, (C 1 -C 4 )-haloalkylcarbonyl, (C 1 -C 4 )-alkoxy Alkylcarbonyl or (C 1 -C 4 )-alkoxy; R 1 and R 2 each independently represent hydrogen, amine, (C 1 -C 4 )-alkyl, cyano-(C 1 -C 4 ) -alkyl, (C 1 -C 4 )-haloalkyl, (C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkyl, (C 1 -C 4 )-haloalkoxy -(C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or (C 1 -C 4 )-haloalkoxy; or represents (C 3 -C 6 )-cycloalkane Or (C 3 -C 6 )-cycloalkyl-(C 1 -C 2 )-alkyl, wherein the above group may be substituted by the following groups: fluorine, chlorine, bromine, iodine, (C 1 -C) 3 )-alkyl, (C 3 -C 6 )-cycloalkyl, cyano, nitro, (C 1 -C 4 )-alkoxy, (C 1 -C 3 )-haloalkyl or (C 1 -C 3 )-haloalkoxy; W represents hydrogen, chlorine or fluorine; n represents the number 0 or 1; Y represents halogen, (C 1 -C 4 )-alkyl, (C 3 -C 6 )-ring Alkyl, (C 1 -C 4 )-haloalkyl, (C 1 -C 4 )-alkoxy or (C 1 -C 4 )- Haloalkoxy; X represents hydrogen, halogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-haloalkyl or (C 1 -C 4 )-alkoxy.
式(I)化合物所示基團之特別佳取代基或範圍說明如下(具體實施例4-1)。V1及V2分別代表氧;Q 代表氮或C-R3,其中R3 代表氫、氯、甲基、乙基、甲氧基、環丙基、氰基或三氟甲基;R1及R2 彼此分別獨立代表氫、胺基、甲基、乙基、正丙基、異丙基、正丁基、第二丁基、第三丁基、CH2CH(CH3)2、CH2CN、CH2CF3、CH2CHF2、CH2CH2OCH3、環丙基、環丁基或環丙基甲基;W 代表氟; n 代表數字0或1;Y 代表氟、氯、溴、甲基、三氟甲基或甲氧基;X 代表氫、氯、氟或甲基。 Particularly preferred substituents or ranges for the groups of the compounds of formula (I) are illustrated below (specific examples 4-1). V 1 and V 2 represent oxygen, respectively; Q represents nitrogen or CR 3 , wherein R 3 represents hydrogen, chlorine, methyl, ethyl, methoxy, cyclopropyl, cyano or trifluoromethyl; R 1 and R 2 independently representing hydrogen, amine, methyl, ethyl, n-propyl, isopropyl, n-butyl, t-butyl, t-butyl, CH 2 CH(CH 3 ) 2 , CH 2 CN , CH 2 CF 3 , CH 2 CHF 2 , CH 2 CH 2 OCH 3 , cyclopropyl, cyclobutyl or cyclopropylmethyl; W represents fluorine; n represents the number 0 or 1; Y represents fluorine, chlorine, bromine , methyl, trifluoromethyl or methoxy; X represents hydrogen, chlorine, fluorine or methyl.
式(I)化合物所示基團之同樣特別佳取代基或範圍說明如下(具體實施例4-2)。V1及V2分別代表氧;Q 代表氮或C-R3,其中R3 代表氫、氯或甲基;R1及R2 彼此分別獨立代表甲基、第二丁基或胺基,較佳係分別代表甲基;W 代表氟;n 代表數字0或1;Y 代表甲基;X 代表氟或甲基。 The same particularly preferred substituents or ranges for the groups of the compounds of formula (I) are illustrated below (specific examples 4-2). V 1 and V 2 represent oxygen, respectively; Q represents nitrogen or CR 3 , wherein R 3 represents hydrogen, chlorine or methyl; and R 1 and R 2 each independently represent a methyl group, a second butyl group or an amine group, preferably Respectively represent methyl; W represents fluorine; n represents the number 0 or 1; Y represents methyl; and X represents fluorine or methyl.
式(I)化合物所示基團之同樣特別佳取代基或範圍說明如下(具體實施例4-3)。V1及V2分別代表氧;Q 代表氮;R1及R2 彼此分別獨立代表氫、胺基、甲基、乙基、正丙基、異丙基、正丁基、第二丁基、第三丁基、CH2CH(CH3)2、CH2CN、CH2CF3,CH2CHF2、CH2CH2OCH3、環丙基、環丁基或環丙基甲基;W 代表氟;n 代表數字0或1;Y 代表氟、氯、溴、甲基、三氟甲基或甲氧基; X 代表氫、氯、氟或甲基。 The same particularly preferred substituents or ranges for the groups of the compounds of formula (I) are illustrated below (specific examples 4-3). V 1 and V 2 represent oxygen, respectively; Q represents nitrogen; R 1 and R 2 each independently represent hydrogen, amine, methyl, ethyl, n-propyl, isopropyl, n-butyl, t-butyl, Third butyl, CH 2 CH(CH 3 ) 2 , CH 2 CN, CH 2 CF 3, CH 2 CHF 2 , CH 2 CH 2 OCH 3 , cyclopropyl, cyclobutyl or cyclopropylmethyl; W Represents fluorine; n represents the number 0 or 1; Y represents fluorine, chlorine, bromine, methyl, trifluoromethyl or methoxy; X represents hydrogen, chlorine, fluorine or methyl.
式(I)化合物所示基團之極特別佳取代基或範圍說明如下(具體實施例5-1)。V1及V2分別代表氧;Q 代表氮或C-R3,其中R3 代表氫;R1及R2 分別代表甲基;W 代表氟;n 代表數字0或1;Y 代表甲基;X 代表氟或甲基。 Very particularly preferred substituents or ranges for the groups of the formula (I) are illustrated below (specific examples 5-1). V 1 and V 2 represent oxygen, respectively; Q represents nitrogen or CR 3 , wherein R 3 represents hydrogen; R 1 and R 2 represent methyl respectively; W represents fluorine; n represents the number 0 or 1; Y represents a methyl group; Fluorine or methyl.
式(I)化合物所示基團之同樣極特別佳取代基或範圍說明如下(具體實施例5-2)。V1及V2分別代表氧;Q 代表氮;R1 代表甲基、乙基、異丙基或CH2CF3;R2 代表甲基、乙基或CH2CF3;W 代表氟;n 代表數字0或1;Y 代表甲基;X 代表氟或甲基。 The same very particularly preferred substituents or ranges for the groups of the compounds of formula (I) are illustrated below (specific examples 5-2). V 1 and V 2 represent oxygen, respectively; Q represents nitrogen; R 1 represents methyl, ethyl, isopropyl or CH 2 CF 3 ; R 2 represents methyl, ethyl or CH 2 CF 3 ; W represents fluorine; Represents the number 0 or 1; Y represents a methyl group; X represents a fluorine or a methyl group.
在廣義及較佳定義中,除非另有說明,否則鹵素係選自以下群組:氟、氯、溴及碘,較佳係選自氟、氯及溴之群中。 In a broad and preferred definition, unless otherwise stated, the halogen is selected from the group consisting of fluorine, chlorine, bromine and iodine, preferably selected from the group consisting of fluorine, chlorine and bromine.
在更佳及可視需要特別佳及極特別佳定義中,除非另有說 明,否則鹵素係選自以下群組:氟、氯、溴及碘,較佳係選自氟、氯及溴之群中。 In the definition of better and more visible and particularly good, unless otherwise stated Preferably, the halogen is selected from the group consisting of fluorine, chlorine, bromine and iodine, preferably selected from the group consisting of fluorine, chlorine and bromine.
經鹵素取代之基團(例如:鹵烷基)係經單鹵化或多鹵化,至多達到取代基之最高可能數量。若經多鹵化時,鹵原子可相同或相異。鹵素代表氟、氯、溴及碘,尤指氟、氯及溴。 Halogen-substituted groups (e.g., haloalkyl) are monohalogenated or polyhalogenated, up to the highest possible number of substituents. If polyhalogenated, the halogen atoms may be the same or different. Halogen represents fluorine, chlorine, bromine and iodine, especially fluorine, chlorine and bromine.
飽和或不飽和之烴基團(如:烷基或烯基)可分別為直鏈或分支鏈,若可能時,可包括與雜原子之組合,如,例如:烷氧基。 The saturated or unsaturated hydrocarbon group (e.g., alkyl or alkenyl group) may be a straight or branched chain, respectively, and may, if possible, be combined with a hetero atom such as, for example, an alkoxy group.
可視需要經取代之基團可為單取代或多取代,其中若為多取代時,取代基可相同或相異。若取代基為計畫取代基或視需要選用之取代基時,除非另有說明,否則該等取代基為:鹵素、烷基、環烷基、氰基、硝基、烷氧基、鹵烷基或鹵烷氧基,特定言之氟、氯、(C1-C3)-烷基、(C3-C6)-環烷基(尤指環丙基)、氰基、(C1-C4)-烷氧基、(C1-C3)-鹵烷基或(C1-C3)-鹵烷氧基。 The group which may be optionally substituted may be mono- or poly-substituted, and in the case of poly-substitution, the substituents may be the same or different. Where a substituent is a substituent or optionally a substituent, unless otherwise stated, the substituents are: halo, alkyl, cycloalkyl, cyano, nitro, alkoxy, halo Or haloalkoxy, in particular fluorine, chlorine, (C 1 -C 3 )-alkyl, (C 3 -C 6 )-cycloalkyl (especially cyclopropyl), cyano, (C 1 - C 4 )-alkoxy, (C 1 -C 3 )-haloalkyl or (C 1 -C 3 )-haloalkoxy.
上述通用術語或較佳範圍內之基團定義或說明亦對應地適用於終產物(包括具有下文中將說明之子結構式(I-A)及(I-B)及(I-A-1)及(I-B-1)之式(I)化合物)、及起始物與中間物。此等基團定義可依需要彼此相互組合,亦即包括個別較佳範圍之間之組合。 The definitions or descriptions of the radicals within the above general terms or preferred ranges also apply correspondingly to the final product (including substructures (IA) and (IB) and (IA-1) and (IB-1) which will be described below. The compound of formula (I)), and the starting materials and intermediates. These group definitions can be combined with each other as desired, that is, including combinations of individual preferred ranges.
較佳為根據本發明式(I)化合物中存在如上述較佳定義之組合,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1或具體實施例2-2說明之組合。 Preferably, a combination of the above-described preferred definitions is present in the compound of formula (I) according to the invention, and each of the above preferred embodiments constitutes a separate combination, in particular as embodiment 2-1 or a specific embodiment 2-2 Description of the combination.
更佳為根據本發明式(I)化合物中存在如上述更佳定義之組合,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1說明之組合。 More preferably, there is a combination of the above-defined definitions in the compound of the formula (I) according to the present invention, and each of the above-described preferred embodiments constitutes a separate combination, specifically a combination as described in the specific embodiment 3-1.
特別佳為根據本發明式(I)化合物中存在如上述特別佳定 義之組合,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1或具體實施例4-2或具體實施例4-3說明之組合。 It is particularly preferred that the compound of formula (I) according to the invention is present as described above in particular Combinations of meanings, and each of the above-described particularly preferred embodiments constitute a separate combination, specifically as described in the specific embodiment 4-1 or the combination of the specific embodiment 4-2 or the specific embodiment 4-3.
極特別佳為根據本發明式(I)化合物中存在如上述極特別佳定義之組合,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1或具體實施例5-2說明之組合。 Very particularly preferably, in accordance with the invention, a combination of the above-mentioned very particularly preferred definitions of the compounds of the formula (I), and each of the above-mentioned very particularly preferred embodiments constitute a separate combination, in particular as in the specific example 5-1 or The combination of the specific embodiments 5-2 is described.
另一項較佳具體實施例中,本發明係有關一種式(I)化合物,其中Q代表C-R3。結果產生式(I-A)化合物
結構式(I-A)所定義之式(I)化合物中,基團或結構元素R1、R2、R3、V1、V2、n、W、X及Y具有如上述定義,特定言之如具體實施例1-1(具體實施例I-A.1-1)或具體實施例1-2(具體實施例I-A.1-2)之說明。 In the compound of the formula (I) defined by the formula (IA), the group or the structural elements R 1 , R 2 , R 3 , V 1 , V 2 , n, W, X and Y have the above definitions, specifically The description is as in the specific embodiment 1-1 (specific embodiment IA.1-1) or the specific embodiment 1-2 (specific embodiment IA.1-2).
結構式(I-A)所定義之式(I)化合物中較佳為彼等其中存在如上述較佳定義組合之化合物,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1(具體實施例I-A.2-1)或具體實施例2-2(具體實施例I-A.2-2)說明之組合。 Preferred among the compounds of the formula (I) defined by the formula (IA) are those in which a combination of the above preferred definitions is present, and each of the above preferred embodiments constitutes a separate combination, specifically as specific A combination of the description of Example 2-1 (Specific Example IA.2-1) or Specific Example 2-2 (Specific Example IA.2-2).
結構式(I-A)所定義之式(I)化合物中更佳為彼等其中存在如上述更佳定義組合之化合物,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1(具體實施例I-A.3-1)說明之組合。 More preferably, among the compounds of the formula (I) defined by the formula (IA), are compounds in which a combination of the above-prepared definitions is present, and each of the above-described preferred embodiments constitutes a separate combination, specifically as specific The combination of the description of Example 3-1 (Specific Example IA.3-1).
結構式(I-A)所定義之式(I)化合物中特別佳為彼等其中存在如上述特別佳定義組合之化合物,且上述每一項特別佳具體實施例構成 獨立之組合,特定言之如具體實施例4-1(具體實施例I-A.4-1)或具體實施例4-2(具體實施例I-A.4-2)或具體實施例4-3(具體實施例I-A.4-3)說明之組合。 Particularly preferred among the compounds of the formula (I) defined by the formula (I-A) are those in which a combination of the above-mentioned particularly preferred definitions is present, and each of the above-mentioned particularly preferred embodiments constitutes Independent combination, specifically as specific embodiment 4-1 (specific embodiment IA.4-1) or specific embodiment 4-2 (specific embodiment IA.4-2) or specific embodiment 4-3 (specific A combination of the descriptions of Examples IA.4-3).
結構式(I-A)所定義之式(I)化合物中極特別佳為彼等其中存在如上述極特別佳定義組合之化合物,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1(具體實施例I-A.5-1)或具體實施例5-2(具體實施例I-A.5-2)說明之組合。 Particularly preferred among the compounds of the formula (I) defined by the formula (IA) are those in which the combinations of the above-mentioned very particularly preferred combinations are present, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination, in particular The combination as described in the specific embodiment 5-1 (specific embodiment IA.5-1) or the specific embodiment 5-2 (specific embodiment IA.5-2).
更特定言之,X及Y代表下列(Y,X)組合:(Me、F)、(Me,H)、(Me,Cl)、(Me,Me)、(Cl,Cl)、(Cl,F)、(MeO,F)、(MeO,H)、(Cl,H)、(Br,H)、(Br,F)、(F,F)、(CF3,H)、(CF3,F),特別佳為下列(Y,X)組合:(Me、F)、(Me,Me)、(Cl,Cl)。 More specifically, X and Y represent the following (Y, X) combinations: (Me, F), (Me, H), (Me, Cl), (Me, Me), (Cl, Cl), (Cl, F), (MeO, F), (MeO, H), (Cl, H), (Br, H), (Br, F), (F, F), (CF 3 , H), (CF 3 , F), particularly preferably the following (Y, X) combination: (Me, F), (Me, Me), (Cl, Cl).
式(I-A)化合物之特別佳具體實施例為彼等其中R3代表H者。結果產生式(I-A-1)化合物。 Particularly preferred embodiments of the compounds of formula (IA) are those in which R 3 represents H. As a result, a compound of the formula (IA-1) is produced.
結構式(I-A-1)所定義之式(I)化合物中,基團或結構元素R1、R2、V1、V2、n、W、X及Y具有如上述定義,特定言之如具體實施例1-1(具體實施例I-A-1.1-1)或具體實施例1-2(具體實施例I-A-1.1-2)之說明。 In the compound of the formula (I) defined by the formula (IA-1), the group or the structural elements R 1 , R 2 , V 1 , V 2 , n, W, X and Y have the definitions as defined above, specifically Description of Specific Embodiment 1-1 (Specific Example IA-1.1-1) or Specific Example 1-2 (Specific Example IA-1.1-2).
結構式(I-A-1)所定義之式(I)化合物中較佳為彼等其中存在如上述較佳定義組合之化合物,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1(具體實施例I-A-1.2-1)或具體實施例 2-2(具體實施例I-A-1.2-2)說明之組合。 Preferred among the compounds of the formula (I) defined by the formula (IA-1) are those in which a combination of the above preferred definitions is present, and each of the above preferred embodiments constitutes a separate combination, in particular Specific embodiment 2-1 (specific embodiment IA-1.2-1) or specific embodiment 2-2 (Specific Example I-A-1.2-2) A combination of the descriptions.
結構式(I-A-1)所定義之式(I)化合物中更佳為彼等其中存在如上述更佳定義組合之化合物,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1(具體實施例I-A-1.3-1)說明之組合。 More preferably, among the compounds of the formula (I) defined by the formula (IA-1), are compounds in which a combination of the above-defined definitions is more preferred, and each of the above-described preferred embodiments constitutes a separate combination, in particular A combination as described in the specific embodiment 3-1 (specific example IA-1.3-1).
結構式(I-A-1)所定義之式(I)化合物中特別佳為彼等其中存在如上述特別佳定義組合之化合物,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1(具體實施例I-A-1.4-1)或具體實施例4-2(具體實施例I-A-1.4-2)或具體實施例4-3(具體實施例I-A-1.4-3)說明之組合。 Particularly preferred among the compounds of the formula (I) defined by the formula (IA-1) are those in which a combination of the above-mentioned particularly preferred definitions is present, and each of the above-mentioned particularly preferred embodiments constitutes a separate combination, in particular Specific embodiment 4-1 (specific embodiment IA-1.4-1) or specific embodiment 4-2 (specific embodiment IA-1.4-2) or specific embodiment 4-3 (specific embodiment IA-1.4-3 ) a combination of instructions.
結構式(I-A-1)所定義之式(I)化合物中極特別佳為彼等其中存在如上述極特別佳定義組合之化合物,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1(具體實施例I-A-1.5-1)或具體實施例5-2(具體實施例I-A-1.5-2)說明之組合。 Particularly preferred among the compounds of the formula (I) as defined in the formula (IA-1) are those in which a combination of the above-mentioned extremely preferred definitions is present, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination. Specifically, a combination of the specific embodiment 5-1 (specific embodiment IA-1.5-1) or the specific embodiment 5-2 (specific embodiment IA-1.5-2) is described.
更特定言之,X及Y代表下列(Y,X)組合:(Me、F)、(Me,H)、(Me,Cl)、(Me,Me)、(Cl,Cl)、(Cl,F)、(MeO,F)、(MeO,H)、(Cl,H)、(Br,H)、(Br,F)、(F,F)、(CF3,H)、(CF3,F),特別佳為下列(Y,X)組合:(Me、F)、(Me,Me)、(Cl,Cl)。 More specifically, X and Y represent the following (Y, X) combinations: (Me, F), (Me, H), (Me, Cl), (Me, Me), (Cl, Cl), (Cl, F), (MeO, F), (MeO, H), (Cl, H), (Br, H), (Br, F), (F, F), (CF 3 , H), (CF 3 , F), particularly preferably the following (Y, X) combination: (Me, F), (Me, Me), (Cl, Cl).
另一項較佳具體實施例中,本發明係有關一種式(I)化合物,其中Q代表N。結果產生式(I-B)化合物。 In another preferred embodiment, the invention relates to a compound of formula (I) wherein Q represents N. As a result, a compound of the formula (I-B) is produced.
結構式(I-B)所定義之式(I)化合物中,基團或結構元素R1、R2、V1、V2、n、W、X及Y具有如上述定義,特定言之如具體實施例1-1(具體實施例I-B.1-1)或具體實施例1-2(具體實施例I-B.1-2)之說明。 In the compound of the formula (I) defined by the formula (IB), the group or the structural elements R 1 , R 2 , V 1 , V 2 , n, W, X and Y have the definitions as defined above, and are specifically embodied as Description of Example 1-1 (Specific Example IB.1-1) or Specific Example 1-2 (Specific Example IB.1-2).
結構式(I-B)所定義之式(I)化合物中較佳為彼等其中存在如上述較佳定義組合之化合物,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1(具體實施例I-B.2-1)或具體實施例2-2(具體實施例I-B.2-2)說明之組合。 Preferred among the compounds of the formula (I) defined by the formula (IB) are those in which a combination of the above preferred definitions is present, and each of the above preferred embodiments constitutes a separate combination, specifically as specific A combination of the description of Example 2-1 (Specific Example IB.2-1) or Specific Example 2-2 (Specific Example IB.2-2).
結構式(I-B)所定義之式(I)化合物中更佳為彼等其中存在如上述更佳定義組合之化合物,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1(具體實施例I-B.3-1)說明之組合。 More preferably, among the compounds of the formula (I) defined by the formula (IB), are compounds in which a combination of the above-defined definitions is more preferred, and each of the above-described preferred embodiments constitutes a separate combination, specifically as specific The combination of the description of Example 3-1 (Specific Example IB.3-1).
結構式(I-B)所定義之式(I)化合物中特別佳為彼等其中存在如上述特別佳定義組合之化合物,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1(具體實施例I-B.4-1)或具體實施例4-2(具體實施例I-B.4-2)或具體實施例4-3(具體實施例I-B.4-3)說明之組合。 Particularly preferred among the compounds of the formula (I) defined by the formula (IB) are those in which a combination of the above-mentioned particularly preferred definitions is present, and each of the above-mentioned particularly preferred embodiments constitutes a separate combination, specifically as specific Description of Example 4-1 (Specific Example IB.4-1) or Specific Example 4-2 (Specific Example IB.4-2) or Specific Example 4-3 (Specific Example IB.4-3) The combination.
結構式(I-B)所定義之式(I)化合物中極特別佳為彼等其中存在如上述極特別佳定義組合之化合物,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1(具體實施例I-B.5-1)或具體實施例5-2(具體實施例I-B.5-2)說明之組合。 Particularly preferred among the compounds of the formula (I) defined by the formula (IB) are those in which a combination of the above-mentioned extremely preferred definitions is present, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination, in particular The combination as described in the specific embodiment 5-1 (specific embodiment IB.5-1) or the specific embodiment 5-2 (specific embodiment IB.5-2).
更特定言之,X及Y代表下列(Y,X)組合:(Me、F)、(Me,H)、(Me,Cl)、(Me,Me)、(Cl,Cl)、(Cl,F)、(MeO,F)、(MeO,H)、(Cl,H)、(Br,H)、(Br,F)、(F,F)、(CF3,H)、(CF3,F),特別佳為下列(Y,X)組合:(Me、F)、(Me,Me)、(Cl,Cl)。 More specifically, X and Y represent the following (Y, X) combinations: (Me, F), (Me, H), (Me, Cl), (Me, Me), (Cl, Cl), (Cl, F), (MeO, F), (MeO, H), (Cl, H), (Br, H), (Br, F), (F, F), (CF 3 , H), (CF 3 , F), particularly preferably the following (Y, X) combination: (Me, F), (Me, Me), (Cl, Cl).
式(I-B)化合物之特別佳具體實施例為彼等其中R1及R2代表 甲基者。結果產生式(I-B-1)化合物。 Particularly preferred embodiments of the compounds of formula (IB) are those wherein R 1 and R 2 represent methyl. As a result, a compound of the formula (IB-1) is produced.
結構式(I-B-1)所定義之式(I)化合物中,基團或結構元素V1、V2、n、W、X及Y具有如上述定義,特定言之如具體實施例1-1(具體實施例I-B-1.1-1)或具體實施例1-2(具體實施例I-B-1.1-2)之說明。 In the compound of the formula (I) defined by the formula (IB-1), the group or the structural elements V 1 , V 2 , n, W, X and Y have the definitions as defined above, specifically as in the specific example 1-1 (Specific Example IB-1.1-1) or Description of Specific Example 1-2 (Specific Example IB-1.1-2).
結構式(I-B-1)所定義之式(I)化合物中較佳為彼等其中存在如上述較佳定義組合之化合物,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1(具體實施例I-B-1.2-1)或具體實施例2-2(具體實施例I-B-1.2-2)說明之組合。 Preferred among the compounds of the formula (I) defined by the formula (IB-1) are those in which a combination of the above preferred definitions is present, and each of the above preferred embodiments constitutes a separate combination, in particular A combination as described in the specific embodiment 2-1 (specific embodiment IB-1.2-1) or the specific embodiment 2-2 (specific embodiment IB-1.2-2).
結構式(I-B-1)所定義之式(I)化合物中更佳為彼等其中存在如上述更佳定義組合之化合物,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1(具體實施例I-B.1.3-1)說明之組合。 More preferably, among the compounds of the formula (I) defined by the formula (IB-1), are compounds in which a combination of the above-defined definitions is more preferred, and each of the above-described preferred embodiments constitutes a separate combination, in particular A combination as described in the specific embodiment 3-1 (specific embodiment IB.1.3-1).
結構式(I-B-1)所定義之式(I)化合物中特別佳為彼等其中存在如上述特別佳定義組合之化合物,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1(具體實施例I-B-1.4-1)或具體實施例4-2(具體實施例I-B-1.4-2)或具體實施例4-3(具體實施例I-B-1.4-3)說明之組合。 Particularly preferred among the compounds of the formula (I) defined by the formula (IB-1) are those in which a combination of the above-mentioned particularly preferred definitions is present, and each of the above-mentioned particularly preferred embodiments constitutes a separate combination, in particular Specific embodiment 4-1 (specific embodiment IB-1.4-1) or specific embodiment 4-2 (specific embodiment IB-1.4-2) or specific embodiment 4-3 (specific embodiment IB-1.4-3 ) a combination of instructions.
結構式(I-B-1)所定義之式(I)化合物中極特別佳為彼等其中存在如上述極特別佳定義組合之化合物,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1(具體實施例I-B-1.5-1)或具體實施例5-2(具體實施例I-B-1.5-2)說明之組合。 Particularly preferred among the compounds of the formula (I) as defined in the formula (IB-1) are those in which a combination of the above-mentioned extremely preferred definitions is present, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination. Specifically, combinations of the specific embodiments 5-1 (specific examples IB-1.5-1) or specific examples 5-2 (specific examples IB-1.5-2) are described.
更特定言之,X及Y代表下列(Y,X)組合:(Me、F)、(Me,H)、(Me,Cl)、(Me,Me)、(Cl,Cl)、(Cl,F)、(MeO,F)、(MeO,H)、(Cl,H)、(Br,H)、(Br,F)、(F,F)、(CF3,H)、(CF3,F),特別佳為下列(Y,X)組合:(Me、F)、(Me,Me)、(Cl,Cl)。 More specifically, X and Y represent the following (Y, X) combinations: (Me, F), (Me, H), (Me, Cl), (Me, Me), (Cl, Cl), (Cl, F), (MeO, F), (MeO, H), (Cl, H), (Br, H), (Br, F), (F, F), (CF 3 , H), (CF 3 , F), particularly preferably the following (Y, X) combination: (Me, F), (Me, Me), (Cl, Cl).
式(I)化合物亦可呈鹽類,特定言之酸加成鹽與金屬錯化物。式(I)化合物及其酸加成鹽與金屬錯化物具有良好效力,尤指控制動物害蟲,其包括節胺動物,及特定言之昆蟲及蜱蟎。 The compounds of formula (I) may also be in the form of a salt, in particular an acid addition salt and a metal complex. The compounds of formula (I) and their acid addition salts and metal complexes have good potency, especially for controlling animal pests, including mitochondrial animals, and in particular insects and mites.
通式(I)化合物之合適鹽類包括習知之無毒性鹽類,亦即與適當鹼類形成之鹽類及與酸之加成鹽類。較佳係與無機鹼類形成之鹽類,如:鹼金屬鹽類(例如:鈉、鉀或銫鹽類)、鹼土金屬鹽類(例如:鈣或鎂鹽類)、銨鹽類、與有機鹼形成之鹽類及與無機胺形成之鹽類(例如:三乙基銨、二環己基銨、N,N’-二苯甲基伸乙基二銨、吡啶鎓、甲基吡啶鎓或乙醇銨之鹽類)、與無機酸形成之鹽類(例如:鹽酸鹽、氫溴酸鹽、硫酸二氫鹽、硫酸三氫鹽、或磷酸鹽)、與有機羧酸或有機磺酸形成之鹽類(例如:甲酸鹽、乙酸鹽、三氟乙酸鹽、馬來酸鹽、酒石酸鹽、甲磺酸鹽、苯磺酸鹽或對甲苯磺酸鹽)、與鹼性胺基酸形成之鹽類(例如:精胺酸鹽、天冬胺酸鹽或麩胺酸鹽),等等。 Suitable salts of the compounds of the general formula (I) include the conventional non-toxic salts, that is, salts formed with suitable bases and addition salts with acids. Preferred are salts formed with inorganic bases such as alkali metal salts (for example: sodium, potassium or barium salts), alkaline earth metal salts (for example: calcium or magnesium salts), ammonium salts, and organic a salt formed by a base and a salt formed with an inorganic amine (for example, triethylammonium, dicyclohexylammonium, N,N'-dibenzylmethylethylammonium, pyridinium, methylpyridinium or ethanol) a salt of ammonium), a salt formed with an inorganic acid (for example, a hydrochloride, a hydrobromide, a dihydrogen sulfate, a trihydrogen sulfate, or a phosphate), and an organic carboxylic acid or an organic sulfonic acid. a salt (for example, formate, acetate, trifluoroacetate, maleate, tartrate, methanesulfonate, besylate or p-toluenesulfonate), formed with a basic amino acid Salts (eg, arginine, aspartate or glutamate), and the like.
式(I)化合物亦可能隨其取代基性質而定,而呈立體異構物型式,亦即幾何異構物與/或光學異構物或各種不同組成之異構物混合物型式。本發明同時提供純的立體異構物及此等異構物之任何所需混合物,但本文中通常僅討論式(I)化合物。 The compounds of formula (I) may also be in the form of stereoisomers, ie, geometric isomers and/or optical isomers or mixtures of isomers of various compositions, depending on the nature of the substituent. The present invention provides both pure stereoisomers and any desired mixtures of such isomers, but only the compounds of formula (I) are generally discussed herein.
然而,根據本發明較佳係使用式(I)化合物之光學活性立體異構型及其鹽類。 However, it is preferred according to the invention to use optically active stereoisomers of the compounds of formula (I) and salts thereof.
對映異構物特定言之可能由根據本發明式(I)化合物之對 掌性硫原子所造成。 The enantiomers are specifically described by the pair of compounds of formula (I) according to the invention Caused by palm sulfur atoms.
因此本發明係有關純的對映異構物與非對映異構物二者及其混合物,用於控制動物害蟲,包括節肢動物及尤指昆蟲及蜱蟎類。因此本發明之個別組態係有關R對映異構物(特定言之與對掌性硫原子有關者)或主要包含R對映異構物之混合物之存在,較佳係其中R對S對映異構物之比例為至少60:40,逐漸提高更佳,至少70:30、75:25、80:20、85:15及90:10。因此本發明之另一項個別組態係有關S對映異構物(特定言之與對掌性硫原子有關者)或主要包含S對映異構物之混合物之存在,較佳係其中S對R對映異構物之比例為至少60:40,逐漸提高更佳,至少70:30、75:25、80:20、85:15及90:10。 The present invention is therefore directed to both pure enantiomers and diastereomers and mixtures thereof for controlling animal pests, including arthropods and especially insects and mites. Thus, the individual configurations of the invention are related to the presence of a mixture of R enantiomers (specifically related to palm sulfur atoms) or predominantly R enantiomers, preferably wherein R to S are The ratio of the isomers is at least 60:40, and the gradual increase is better, at least 70:30, 75:25, 80:20, 85:15 and 90:10. Thus, another individual configuration of the invention relates to the presence of a mixture of the S enantiomer (specifically related to the palm sulfur atom) or predominantly the S enantiomer, preferably wherein S The ratio to the R enantiomer is at least 60:40, and is gradually improved, at least 70:30, 75:25, 80:20, 85:15 and 90:10.
式(I)化合物可能呈不同多晶型或不同多晶型之混合物。該等純的多晶型及多晶型混合物均成為本發明之主題之一部份且可根據本發明使用。 The compounds of formula (I) may be in the form of different polymorphs or different polymorphs. Such pure polymorphic and polymorphic mixtures are part of the subject matter of the present invention and can be used in accordance with the present invention.
根據本發明化合物係如式(I)之一般定義,其包括所有可能之旋轉異構物及其混合物。 The compounds according to the invention are as generally defined by formula (I) and include all possible rotamers and mixtures thereof.
根據本發明式(I)化合物可採用熟悉此相關技術者習知之方法製備。各種不同製備方法同樣地形成本發明主題之一部份,其說明於下文中。 The compounds of formula (I) according to the invention may be prepared by methods well known to those skilled in the art. A variety of different preparation methods are also costly as part of the inventive subject matter, which is described below.
根據本發明式(I)化合物可採用下列反應圖所示製程製得: The compounds of formula (I) according to the invention can be prepared by the process shown in the following reaction scheme:
製程A:
G代表氫、(C1-C6)-烷基、(C2-C6)-烯基(較佳係氫、(C1-C4)-烷基、(C2-C4)-烯基;特別佳係氫) 或B(OG)2共同形成5-或6-員環,較佳係5-員環。 G represents hydrogen, (C 1 -C 6 )-alkyl, (C 2 -C 6 )-alkenyl (preferably hydrogen, (C 1 -C 4 )-alkyl, (C 2 -C 4 )- Alkenyl; particularly preferably hydrogen) or B(OG) 2 together form a 5- or 6-membered ring, preferably a 5-membered ring .
一項本發明具體實施例中,由式(II-A)5-鹵(硫)尿嘧啶與式(III)硼酸化合物或1,3,2-二氧雜硼雜環戊烷反應,產生根據本發明式(I-Aa)化合物。 In a specific embodiment of the invention, the reaction of 5-halo(thio)uracil of formula (II-A) with a boronic acid compound of formula (III) or 1,3,2-dioxaborolane is produced according to A compound of the formula (I-Aa) according to the invention.
此類型反應(式(III)硼酸化合物或1,3,2-二氧雜硼雜環戊烷與鹵化雜環或鹵化芳香系之反應)說明於例如:WO2013/027660、 JP2007/284385或WO2007/034755。 This type of reaction (the reaction of a boronic acid compound of formula (III) or a 1,3,2-dioxaborolane with a halogenated heterocyclic ring or a halogenated aromatic system) is illustrated, for example, in WO 2013/027660, JP2007/284385 or WO2007/034755.
需要作為起始物之式(III)硼酸化合物或1,3,2-二氧雜硼雜環戊烷可自商品取得,例如:{2-氟-4-甲基-5-[(2,2,2-三氟乙基)硫基]苯基}硼酸(Aces Pharma,USA)[CAS-登錄號248270-00-0],或係自其他專利說明書中得知者,例如:來自WO 2013/157229,或其可採用文獻中已知製法合成。 The boronic acid compound of formula (III) or 1,3,2-dioxaborolane which is required as a starting material can be obtained from a commercial product, for example: {2-fluoro-4-methyl-5-[(2, 2,2-Trifluoroethyl)thio]phenyl}boronic acid (Aces Pharma, USA) [CAS-Accession No. 248270-00-0], or from other patent specifications, for example: from WO 2013 /157229, or it can be synthesized by methods known in the literature.
式(II-A)5-鹵(硫)尿嘧啶可自商品取得,例如:5-碘-1,3-二甲基尿嘧啶(Aldrich),或可採用已知製法,例如:類似Synlett 2009,(14),2309-2311說明之方法製備。5-鹵-1-胺基尿嘧啶說明於DE2801008(1979)。 Formula (II-A) 5-halo(thio)uracil can be obtained commercially, for example, 5-iodo-1,3-dimethyluracil (Aldrich), or can be obtained by a known method, for example: similar to Synlett 2009 , (14), 2309-2311 prepared by the method described. 5-Halo-1-aminouracil is described in DE2801008 (1979).
用於製備(I-8)之起始物為5-碘-6-氯-1,3-二甲基尿嘧啶[CAS-登錄號21428-30-8],係由N-碘琥珀醯亞胺與6-氯-1,3-二甲基尿嘧啶反應製得。 The starting material for the preparation of (I-8) is 5-iodo-6-chloro-1,3-dimethyluracil [CAS-Accession No. 21428-30-8], which is derived from N-iodoammonium The amine is prepared by reacting with 6-chloro-1,3-dimethyluracil.
由尿嘧啶於各種不同溶劑中使用五硫化磷形成相應4-硫-或2,4-二硫類似物之轉化法說明於例如:Synthesis 1987,256-258。 Conversion methods for the formation of the corresponding 4-sulfo- or 2,4-dithio analogs from uracil in various solvents using solvents such as: Synthesis 1987 , 256-258.
5-鹵(硫)尿嘧啶(II-A)之反應中所使用之觸媒較佳係由鈀、銅或鎳之鹽類或錯化物組成。 The catalyst used in the reaction of 5-halo(thio)uracil (II-A) is preferably composed of a salt or a complex of palladium, copper or nickel.
合適之鈀觸媒為例如:於配位體(例如:2,2'-雙(二苯基膦基)-1,1'-聯萘、9,9-二甲基-4,5-雙(二苯基膦基)呫噸或1,1'-雙(二苯基膦基)二茂絡鐵之存在下之乙酸鈀(II)、肆(三苯基膦)鈀、雙-(三苯基膦)鈀(II)氯化物、參(二亞苯甲基丙酮)二鈀(0)。 Suitable palladium catalysts are, for example, ligands (for example: 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl, 9,9-dimethyl-4,5-double Palladium(II) acetate, ruthenium (triphenylphosphine) palladium, bis-(three) in the presence of (diphenylphosphino)xanthene or 1,1'-bis(diphenylphosphino)ferrocene iron Phenylphosphine) palladium (II) chloride, ginseng (diphenylideneacetone) dipalladium (0).
合適之銅鹽類為例如:碘化亞銅(I)、氯化亞銅(I),氧化亞銅(I)、三氟甲磺酸亞銅(I)、乙酸銅(II)、三氟甲磺酸銅(II),經常在配位體(例如:二胺配位體,如:N,N‘-二甲基乙二胺、N,N-二甲基乙二胺或反式-N,N'-二甲基-1,2-環己二胺)之存在下。 Suitable copper salts are, for example, cuprous iodide (I), cuprous chloride (I), cuprous oxide (I), cuprous (III) triflate, copper (II) acetate, trifluoroacetate. Copper (II) methane sulfonate, often in a ligand (eg, a diamine ligand such as: N, N'-dimethylethylenediamine, N,N-dimethylethylenediamine or trans- In the presence of N,N'-dimethyl-1,2-cyclohexanediamine.
合適之鎳觸媒為例如:乙醯基丙酮酸鎳(II),可單獨使用或與上述磷配位體組合使用,或使用乙醯基丙酮酸鎳(II)與咪唑鎓碳烯配位體。 A suitable nickel catalyst is, for example, nickel(II) acetylacetonate, either alone or in combination with the above phosphorus ligand, or using nickel (II) acetylsulfonate and an imidazolium carbene ligand. .
觸媒之用量通常低於化學計量,較佳為相對於所使用式(II-A)5-鹵(硫)尿嘧啶之0.001-0.8當量及特別佳係0.01至0.5當量。 The amount of the catalyst is usually less than the stoichiometric amount, preferably from 0.001 to 0.8 equivalents and particularly preferably from 0.01 to 0.5 equivalents based on the 5-halo(thio)uracil of the formula (II-A) used.
式(II-A)5-鹵(硫)尿嘧啶與式(III)硼衍生物之反應較佳係在選自對主要反應條件呈惰性之習知溶劑之溶劑中進行。較佳係醚類如,例如:二烷、四氫呋喃、乙醚或1,2-二甲氧基乙烷;芳香烴類如,例如:苯、甲苯或二甲苯;脂系醇類如,例如:甲醇、乙醇或異丙醇;腈類如,例如:乙腈或丙腈;極性非質子性溶劑如:N,N-二甲基甲醯胺、二甲亞碸、N-甲基吡咯啶酮及此等溶劑與水之混合物。 The reaction of the 5-halo(thio)uracil of the formula (II-A) with the boron derivative of the formula (III) is preferably carried out in a solvent selected from the conventional solvents which are inert to the main reaction conditions. Preferred are ethers such as, for example, two Alkane, tetrahydrofuran, diethyl ether or 1,2-dimethoxyethane; aromatic hydrocarbons such as, for example, benzene, toluene or xylene; aliphatic alcohols such as, for example, methanol, ethanol or isopropanol; For example: acetonitrile or propionitrile; polar aprotic solvents such as: N,N-dimethylformamide, dimethyl hydrazine, N-methylpyrrolidone and mixtures of such solvents with water.
該反應較佳係於鹼之存在下進行。合適之鹼類為無機鹼類,特定言之鹼金屬或鹼土金屬之乙酸鹽、磷酸鹽、碳酸鹽及碳酸氫鹽。特別佳係乙酸鈉、磷酸鈉、磷酸鉀、碳酸銫、碳酸鈉、碳酸鉀、碳酸氫鈉、碳酸氫鉀。該無機鹼類亦可呈水溶液使用。 The reaction is preferably carried out in the presence of a base. Suitable bases are inorganic bases, in particular alkali metal or alkaline earth metal acetates, phosphates, carbonates and hydrogencarbonates. Particularly preferred are sodium acetate, sodium phosphate, potassium phosphate, cesium carbonate, sodium carbonate, potassium carbonate, sodium hydrogencarbonate, and potassium hydrogencarbonate. The inorganic base can also be used in an aqueous solution.
該反應可在減壓、標準壓力或加壓下,及在0至200℃之溫度下進行,較佳係在標準壓力及30至150℃之溫度下,可視需要在惰性氣體氛圍下進行反應。當進行該反應時,可視需要可能使用適合此等反應之任何市售微波裝置進行(例如:Anton Paar Monowave 300,CEM Discover S,Biotage Initiator 60)。 The reaction can be carried out under reduced pressure, standard pressure or under pressure, and at a temperature of from 0 to 200 ° C, preferably at a standard pressure and a temperature of from 30 to 150 ° C, optionally under an inert gas atmosphere. When the reaction is carried out, it may be carried out using any commercially available microwave device suitable for such reactions as desired (for example: Anton Paar Monowave 300, CEM Discover S, Biotage Initiator 60).
由步驟(a)所得之根據本發明式(I-Aa)化合物與氧化劑反應,產生根據本發明通式(I-Ab)亞碸。 The compound of the formula (I-Aa) according to the invention obtained from the step (a) is reacted with an oxidizing agent to produce a hydrazine of the formula (I-Ab) according to the invention.
該反應係類似JP2009/023910之方式進行。 This reaction was carried out in a manner similar to JP2009/023910.
所使用之氧化劑為間氯過苯甲酸,可視需要於緩衝溶液之存在下及可視需要於移相觸媒(於H2O2、含K2S2O8之硫酸或強度3-40%之過氧化氫水溶液之存在下之錸鹽類,例如:MeReO3)之存在下,可視需要於分子篩或觸媒(例如:Na2WO4二水合物或過碘酸鈉)之存在下進行。 The oxidizing agent used is m-chloroperbenzoic acid, optionally in the presence of a buffer solution and optionally in a phase shifting catalyst (in H 2 O 2 , sulfuric acid containing K 2 S 2 O 8 or 3-40% strength) In the presence of an onium salt in the presence of an aqueous hydrogen peroxide solution, for example, MeReO 3 ), it may be carried out in the presence of a molecular sieve or a catalyst (for example, Na 2 WO 4 dihydrate or sodium periodate) as needed.
該氧化反應通常在選自對主要反應條件呈惰性之習知溶劑之溶劑中進行。 The oxidation reaction is usually carried out in a solvent selected from conventional solvents which are inert to the main reaction conditions.
合適之溶劑為鹵化烴類,例如:二氯甲烷、三氯甲烷、四氯化碳、1,2-二氯乙烷或氯苯;醇類,如:甲醇或乙醇;甲酸、乙酸或丙酸。 Suitable solvents are halogenated hydrocarbons such as dichloromethane, chloroform, carbon tetrachloride, 1,2-dichloroethane or chlorobenzene; alcohols such as methanol or ethanol; formic acid, acetic acid or propionic acid .
該反應可在標準壓力或加壓下,及-10℃至80℃之溫度下進行;較佳係該反應在標準壓力及0℃至40℃之溫度下進行。 The reaction can be carried out under standard pressure or pressure, and at a temperature of from -10 ° C to 80 ° C; preferably, the reaction is carried out at a standard pressure and a temperature of from 0 ° C to 40 ° C.
有許多不同方法適合產生富集對映異構性之亞碸,如A.R.Maguire於ARKIVOC,2011(i),1-110中之說明:金屬催化之+硫醚之不對稱氧化反應,例如:鈦及釩為最常用之觸媒來源,其係呈Ti(OiPr4)及VO(acac)2型式,與對掌性配位體及氧化劑(如:第三丁基過氧化氫(TBHP)、2-苯基丙烷-2-基過氧化氫(CHP)或過氧化氫)一起使用;非金屬催化之不對稱氧化反應,其係使用對掌性氧化劑或對掌性觸媒;電化學或生物性不對稱氧化反應及亞碸之動力學解析法與親核物遷移法(依據安德森方法(Andersen's method))。 There are many different methods suitable for the production of enantiomerically enantiomers, as described in ARMaguire in ARKIVOC, 2011(i), 1-110: metal-catalyzed asymmetric oxidation of thioethers such as titanium and Vanadium is the most commonly used catalyst source, which is Ti(O i Pr 4 ) and VO(acac) 2 type, with palmitic ligands and oxidants (such as: tert-butyl hydroperoxide (TBHP), 2-Phenylpropan-2-ylhydroperoxide (CHP) or hydrogen peroxide) used together; non-metal catalyzed asymmetric oxidation, using a palmitic oxidant or a palmitic catalyst; electrochemical or biological Asymmetric oxidation reaction and kinetic analysis of hydrazine and nucleophilic migration (according to Andersen's method).
根據本發明式(I-Ab)化合物之純對映異構物可由消旋物採用例如:製備性HPLC,於對掌性固定相上製得。 The pure enantiomer of the compound of formula (I-Ab) according to the invention can be prepared from the racemate using, for example, preparative HPLC on a palmitic stationary phase.
製程B:
本發明另一項具體實施例中,由式(Va)鹵代硫化物與式(IV)硼酸化合物或1,3,2-二氧雜硼雜環戊烷反應,產生根據本發明式(I-Aa)化合物。此類型反應-二羥硼酸化合物與鹵化雜環或鹵化芳香系之反應-已說明於例如:WO2012/061557。 In another embodiment of the invention, the halosulfide of formula (Va) is reacted with a boronic acid compound of formula (IV) or 1,3,2-dioxaborolane to yield formula (I) according to the invention. -Aa) compound. This type of reaction - the reaction of a diboronic acid compound with a halogenated heterocyclic ring or a halogenated aromatic system - has been described, for example, in WO 2012/061557.
需要作為起始物之式(IV)硼酸化合物或1,3,2-二氧雜硼雜環戊烷可自商品取得,例如:(1,3-二甲基-2,4-二側氧基-1,2,3,4-四氫嘧啶-5-基)硼酸(Combi-Blocks,USA)[CAS-登錄號223418-73-3]、1,3-二甲基-5-(4,4,5,5-四甲基-1,3,2-二氧雜硼雜環戊烷-2-基)嘧啶-2,4(1H,3H)-二酮(Combi-Blocks,USA)[CAS-登錄號269410-01-7],或(2,4-二硫代-1,2,3,4-四氫嘧啶-5-基)硼酸(FCH-Group,Ukraine)[CAS-登錄號125154-12-3],或自其他專利說明書中得知者,例如:來自PL185090B1,或其可採用說明於例如:J.Org.Chem.1985, 50,841-847之文獻中已知製法合成。 The boronic acid compound of formula (IV) or 1,3,2-dioxaborolane which is required as a starting material can be obtained from a commercial product, for example: (1,3-dimethyl-2,4-di-oxygen) Base-1,2,3,4-tetrahydropyrimidin-5-yl)boronic acid (Combi-Blocks, USA) [CAS-Accession No. 223418-73-3], 1,3-Dimethyl-5-(4 ,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine-2,4(1H,3H)-dione (Combi-Blocks, USA) [CAS-Accession No. 269410-01-7], or (2,4-Dithio-1,2,3,4-tetrahydropyrimidin-5-yl)boronic acid (FCH-Group, Ukraine) [CAS-Login No. 125154-12-3], or known from other patent specifications, for example, from PL185090B1, or a method known in the art such as: J. Org . Chem . 1985, 50 , 841-847. synthesis.
需要作為起始物之式(Va)鹵代芳香系可自商品取得或自許 多專利說明書中得知,例如:來自WO2013/157229、WO2012/176856或JP2009/023910。 The halogenated aromatic system of the formula (Va) which is required as a starting material can be obtained from a commodity or It is known from the multi-patent specification, for example, from WO 2013/157229, WO 2012/176856 or JP 2009/023910.
適合合成通式(Va)碘化物之起始物為具有相同通式之溴化物,其可例如:採用鹵素交換反應,根據文獻中已知方法,可視需要使用金屬觸媒進行轉化,例如:類似Chem.Lett.1985,3,411-412。 Suitable starting materials for the synthesis of the iodide of the formula (Va) are bromides of the same general formula, which can, for example, be subjected to a halogen exchange reaction, which can be converted, if desired, using a metal catalyst according to methods known in the literature, for example: analogous Chem . Lett . 1985 , 3 , 411-412.
式(IV)硼衍生物與式(Va)鹵代硫化物之反應較佳係於觸媒之存在下,可視需要於鹼之存在下,於有機溶劑中或於溶劑與水之混合物中,於環境溫度或加溫下進行,產生根據本發明式(I-Aa)化合物。 The reaction of the boron derivative of the formula (IV) with the halosulfide of the formula (Va) is preferably carried out in the presence of a catalyst, optionally in the presence of a base, in an organic solvent or in a mixture of a solvent and water. The ambient temperature or heating is carried out to produce a compound of the formula (I-Aa) according to the invention.
式(Va)鹵代硫化物之反應中所使用觸媒較佳係由鈀、銅或鎳之鹽類或錯化物組成。 The catalyst used in the reaction of the halogenated sulfide of the formula (Va) is preferably composed of a salt or a complex of palladium, copper or nickel.
合適之鈀觸媒為例如:於配位體(例如:2,2'-雙(二苯基膦基)-1,1'-聯萘、9,9-二甲基-4,5-雙(二苯基膦基)呫噸(xanthene)或1,1'-雙(二苯基膦基)二茂絡鐵)之存在下之乙酸鈀(II)、肆(三苯基膦)鈀、雙(三苯基膦)鈀(II)氯化物、參(二亞苯甲基丙酮)二鈀(0)。 Suitable palladium catalysts are, for example, ligands (for example: 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl, 9,9-dimethyl-4,5-double Palladium (II) acetate, ruthenium (triphenylphosphine) palladium in the presence of (diphenylphosphino)xanthene or 1,1'-bis(diphenylphosphino)ferrocene Bis(triphenylphosphine)palladium(II) chloride, ginseng (diphenylideneacetone) dipalladium (0).
合適之銅鹽類為例如:碘化亞銅(I)、氯化亞銅(I)、氧化亞銅(I)、三氟甲磺酸亞銅(I)、乙酸銅(II)、三氟甲磺酸銅(II),經常在配位體(例如:二胺配位體,如:N,N‘-二甲基乙二胺、N,N-二甲基乙二胺或反式-N,N'-二甲基-1,2-環己二胺)之存在下。 Suitable copper salts are, for example, cuprous iodide (I), cuprous chloride (I), cuprous oxide (I), copper (I) triflate, copper (II) acetate, trifluoroacetate. Copper (II) methane sulfonate, often in a ligand (eg, a diamine ligand such as: N, N'-dimethylethylenediamine, N,N-dimethylethylenediamine or trans- In the presence of N,N'-dimethyl-1,2-cyclohexanediamine.
合適之鎳觸媒為例如:乙醯基丙酮酸鎳(II),可單獨使用或與上述磷配位體組合使用,或使用乙醯基丙酮酸鎳(II)與咪唑鎓碳烯配位體。 A suitable nickel catalyst is, for example, nickel(II) acetylacetonate, either alone or in combination with the above phosphorus ligand, or using nickel (II) acetylsulfonate and an imidazolium carbene ligand. .
觸媒之用量通常低於化學計量,較佳為相對於所使用式(Va)鹵代硫化物之0.001-0.8當量及特別佳係0.01至0.5當量。 The amount of the catalyst is usually less than the stoichiometric amount, preferably from 0.001 to 0.8 equivalents and particularly preferably from 0.01 to 0.5 equivalents based on the halogenated sulfide of the formula (Va) used.
式(Va)鹵代硫化物與式(IV)硼衍生物之反應較佳係在選自 對主要反應條件呈惰性之習知溶劑之溶劑中進行。較佳係醚類,如,例如:二烷、四氫呋喃、乙醚或1,2-二甲氧基乙烷;芳香烴類如,例如:苯、甲苯或二甲苯;脂系醇類如,例如:甲醇、乙醇或異丙醇;腈類如,例如:乙腈或丙腈;極性非質子性溶劑,如:N,N-二甲基甲醯胺、二甲亞碸、N-甲基吡咯啶酮及此等溶劑與水之混合物。 The reaction of the halosulfide of formula (Va) with the boron derivative of formula (IV) is preferably carried out in a solvent selected from the conventional solvents which are inert to the main reaction conditions. Preferred are ethers such as, for example, two Alkane, tetrahydrofuran, diethyl ether or 1,2-dimethoxyethane; aromatic hydrocarbons such as, for example, benzene, toluene or xylene; aliphatic alcohols such as, for example, methanol, ethanol or isopropanol; For example: acetonitrile or propionitrile; polar aprotic solvents such as N,N-dimethylformamide, dimethyl hydrazine, N-methylpyrrolidone and mixtures of such solvents with water.
該反應較佳係在鹼之存在下進行。合適之鹼類為無機鹼類,特定言之鹼金屬或鹼土金屬之乙酸鹽、磷酸鹽、碳酸鹽及碳酸氫鹽。特別佳為乙酸鈉、磷酸鈉、磷酸鉀、碳酸銫、碳酸鈉、碳酸鉀、碳酸氫鈉、碳酸氫鉀。該無機鹼類亦可呈水溶液使用。 The reaction is preferably carried out in the presence of a base. Suitable bases are inorganic bases, in particular alkali metal or alkaline earth metal acetates, phosphates, carbonates and hydrogencarbonates. Particularly preferred are sodium acetate, sodium phosphate, potassium phosphate, cesium carbonate, sodium carbonate, potassium carbonate, sodium hydrogencarbonate, and potassium hydrogencarbonate. The inorganic base can also be used in an aqueous solution.
該反應可在減壓、標準壓力或加壓下,及在0至200℃之溫度下進行,較佳係在標準壓力及30至150℃之溫度下,可視需要於惰性氣體氛圍下進行反應。當進行該反應時,可視需要可能使用適合此等反應之任何市售微波裝置進行(例如:Anton Paar Monowave 300,CEM Discover S,Biotage Initiator 60)。 The reaction can be carried out under reduced pressure, standard pressure or under pressure, and at a temperature of from 0 to 200 ° C, preferably at a standard pressure and a temperature of from 30 to 150 ° C, optionally under an inert gas atmosphere. When the reaction is carried out, it may be carried out using any commercially available microwave device suitable for such reactions as desired (for example: Anton Paar Monowave 300, CEM Discover S, Biotage Initiator 60).
由製程B步驟(a)製得之根據本發明式(I-Aa)化合物係依製程A步驟(b)之說明與氧化劑反應,產生根據本發明通式(I-Ab)亞碸。 The compound of the formula (I-Aa) according to the present invention, which is obtained by the process of the step B (a), is reacted with an oxidizing agent according to the description of the step A (b) of the process A to produce a hydrazine of the formula (I-Ab) according to the invention.
製程C
本發明另一項具體實施例中,由式(II-B)6-鹵-1,2,4-三-3,5(2H,4H)-二酮與式(III)硼酸化合物或1,3,2-二氧雜硼雜環戊烷反應,產生根據本發明式(I-Ba)化合物。 In another embodiment of the invention, from the formula (II-B) 6-halo-1,2,4-three The reaction of -3,5(2H,4H)-dione with a boronic acid compound of formula (III) or 1,3,2-dioxaborolane gives the compound of formula (I-Ba) according to the invention.
用於製備(I-5)之起始物,6-溴-2,4-二甲基-1,2,4-三-3,5(2H,4H)-二酮[CAS-登錄號15870-78-7]可自商品取得(Enamine,Ukraine或Ryan Scientific,USA)或可依WO2010/006962之說明,由1,2,4-三-3,5(2H,4H)-二酮進行溴化後,進行甲基化而製得。WO1995/001965進一步說明製備式(II-B)三二酮之方法。 Starting material for the preparation of (I-5), 6-bromo-2,4-dimethyl-1,2,4-tri -3,5(2H,4H)-dione [CAS-Accession No. 15870-78-7] is available from the product (Enamine, Ukraine or Ryan Scientific, USA) or as described in WO2010/006962, by 1,2 , 4-three -3,5(2H,4H)-dione is obtained by bromination followed by methylation. WO1995/001965 further describes the preparation of formula (II-B) three The method of diketone.
式(III)硼衍生物與式(II-B)6-鹵-1,2,4-三-3,5(2H,4H)-二酮之反應較佳係於觸媒之存在下,可視需要於鹼之存在下,於有機溶劑中或於溶劑與水之混合物中,於環境溫度下或於加溫下進行,產生根據本發明式(I-Ba)化合物。 Boron derivative of formula (III) and 6-halo-1,2,4-tri3 of formula (II-B) -3,5(2H,4H)-dione is preferably reacted in the presence of a catalyst, optionally in the presence of a base, in an organic solvent or in a mixture of solvent and water, at ambient temperature or This is carried out under heating to give a compound of the formula (I-Ba) according to the invention.
式(II-B)6-鹵-1,2,4-三-3,5(2H,4H)-二酮之反應所使用觸媒較佳係由鈀、銅或鎳之鹽或錯化物組成。 Formula (II-B) 6-halo-1,2,4-three The catalyst used for the reaction of -3,5(2H,4H)-dione is preferably composed of a salt or a complex of palladium, copper or nickel.
合適之鈀觸媒為例如:於配位體(例如:2,2'-雙(二苯基膦基)-1,1'-聯萘、9,9-二甲基-4,5-雙(二苯基膦基)呫噸或1,1'-雙(二苯基膦基)二茂絡鐵)之存在下之乙酸鈀(II)、肆(三苯基膦)鈀、雙-(三苯基膦)鈀(II)氯化物、參(二亞苯甲基丙酮)二鈀(0)。 Suitable palladium catalysts are, for example, ligands (for example: 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl, 9,9-dimethyl-4,5-double Palladium (II) acetate, ruthenium (triphenylphosphine) palladium, bis-((diphenylphosphino)-xanthene or 1,1'-bis(diphenylphosphino) ferrocene) Triphenylphosphine) palladium (II) chloride, ginseng (diphenylideneacetone) dipalladium (0).
合適之銅鹽類為例如:碘化亞銅(I)、氯化亞銅(I),氧化亞銅(I)、三氟甲磺酸亞銅(I)、乙酸銅(II)、三氟甲磺酸銅(II),經常在配位體(例如:二胺配位體,如:N,N'-二甲基乙二胺、N,N-二甲基乙二胺或反式-N,N'-二甲基-1,2-環己二胺)之存在下。 Suitable copper salts are, for example, cuprous iodide (I), cuprous chloride (I), cuprous oxide (I), cuprous (III) triflate, copper (II) acetate, trifluoroacetate. Copper (II) methane sulfonate, often in a ligand (eg, a diamine ligand such as: N, N'-dimethylethylenediamine, N,N-dimethylethylenediamine or trans- In the presence of N,N'-dimethyl-1,2-cyclohexanediamine.
合適之鎳觸媒為例如:乙醯基丙酮酸鎳(II),可單獨使用或與上述磷配位體組合使用,或使用乙醯基丙酮酸鎳(II)與咪唑鎓碳烯配位體。 A suitable nickel catalyst is, for example, nickel(II) acetylacetonate, either alone or in combination with the above phosphorus ligand, or using nickel (II) acetylsulfonate and an imidazolium carbene ligand. .
觸媒之用量通常低於化學計量,較佳為相對於所使用式(II-B)鹵化氮雜尿嘧啶之0.001-0.8當量及特別佳係0.01至0.5當量。 The amount of the catalyst is usually less than the stoichiometric amount, preferably from 0.001 to 0.8 equivalents and particularly preferably from 0.01 to 0.5 equivalents based on the azadiazepine of the formula (II-B) used.
式(II-B)6-鹵-1,2,4-三-3,5(2H,4H)-二酮與式(III)硼衍生物之反應較佳係在選自對主要反應條件呈惰性之習知溶劑之溶劑中進行。較佳係醚類如,例如:二烷、四氫呋喃、乙醚或1,2-二甲氧基乙烷;芳香烴類如,例如:苯、甲苯或二甲苯;脂系醇類如,例如:甲醇、乙醇或異丙醇;腈類如,例如:乙腈或丙腈;極性非質子性溶劑,如:N,N-二甲基甲醯胺、二甲亞碸、N-甲基吡咯啶酮及此等溶劑與水之混合物。 Formula (II-B) 6-halo-1,2,4-three The reaction of the -3,5(2H,4H)-dione with the boron derivative of the formula (III) is preferably carried out in a solvent selected from the conventional solvents which are inert to the main reaction conditions. Preferred are ethers such as, for example, two Alkane, tetrahydrofuran, diethyl ether or 1,2-dimethoxyethane; aromatic hydrocarbons such as, for example, benzene, toluene or xylene; aliphatic alcohols such as, for example, methanol, ethanol or isopropanol; For example: acetonitrile or propionitrile; polar aprotic solvents such as N,N-dimethylformamide, dimethyl hydrazine, N-methylpyrrolidone and mixtures of such solvents with water.
該反應較佳係在鹼之存在下進行。合適之鹼類為無機鹼類,特定言之鹼金屬或鹼土金屬之乙酸鹽、磷酸鹽、碳酸鹽及碳酸氫鹽。特別佳為乙酸鈉、磷酸鈉、磷酸鉀、碳酸銫、碳酸鈉、碳酸鉀、碳酸氫鈉、碳 酸氫鉀。該無機鹼類亦可呈水溶液使用。 The reaction is preferably carried out in the presence of a base. Suitable bases are inorganic bases, in particular alkali metal or alkaline earth metal acetates, phosphates, carbonates and hydrogencarbonates. Particularly preferred are sodium acetate, sodium phosphate, potassium phosphate, cesium carbonate, sodium carbonate, potassium carbonate, sodium hydrogencarbonate, carbon Potassium hydrogenate. The inorganic base can also be used in an aqueous solution.
該反應可在減壓、標準壓力或加壓下,及於0至200℃之溫度下進行,較佳係在標準壓力及30至150℃之溫度下,可視需要於惰性氣體氛圍下進行反應。當進行該反應時,可視需要可能使用適合此等反應之任何市售微波裝置進行(例如:Anton Paar Monowave 300,CEM Discover S,Biotage Initiator 60)。 The reaction can be carried out under reduced pressure, standard pressure or under pressure, and at a temperature of from 0 to 200 ° C, preferably at a standard pressure and a temperature of from 30 to 150 ° C, optionally under an inert gas atmosphere. When the reaction is carried out, it may be carried out using any commercially available microwave device suitable for such reactions as desired (for example: Anton Paar Monowave 300, CEM Discover S, Biotage Initiator 60).
依製程C步驟(a)製得之根據本發明式(I-Ba)化合物係依據製程A步驟(b)之說明,使用氧化劑反應,產生根據本發明通式(I-Bb)亞碸。 The compound of the formula (I-Ba) according to the present invention, which is obtained according to Process C, step (a), is reacted with an oxidizing agent according to the description of Process A, step (b), to produce a hydrazine of the formula (I-Bb) according to the present invention.
類似DE19835943、FR2866339或Bioorg.Med.Chem.Lett.2005,15,4363-4366之製法,由式(VI)側氧基苯基乙酸衍生物與式(VII)碳 酸衍生物反應,產生根據本發明式(I-Bc)化合物。 Reaction of a pendant oxyphenylacetic acid derivative of the formula (VI) with a carbonic acid derivative of the formula (VII), in accordance with the process of DE 1983 0 493, FR 2 866 339 or Bioorg. Med. Chem. Lett. 2005 , 15 , 4363-4366, according to the invention A compound of formula (I-Bc).
式(VI)側氧基苯基乙酸衍生物與式(VII)碳酸衍生物之反應可視需要在觸媒量之酸(例如:硫酸或HCl水溶液)之存在下,較佳在在選自對主要反應條件呈惰性之習知溶劑之溶劑中進行。較佳係醚類如,例如:二烷、四氫呋喃、乙醚或1,2-二甲氧基乙烷;芳香烴類如,例如:苯、甲苯或二甲苯;脂系醇類如,例如:甲醇、乙醇或異丙醇;極性非質子性溶劑,如:二甲亞碸或N-甲基吡咯啶酮或水。 The reaction of the pendant oxyphenylacetic acid derivative of the formula (VI) with the carbonic acid derivative of the formula (VII) may be carried out in the presence of a catalytic amount of an acid (for example, an aqueous solution of sulfuric acid or HCl), preferably at a selected one. The reaction is carried out in a solvent of a conventional solvent which is inert. Preferred are ethers such as, for example, two Alkane, tetrahydrofuran, diethyl ether or 1,2-dimethoxyethane; aromatic hydrocarbons such as, for example, benzene, toluene or xylene; aliphatic alcohols such as, for example, methanol, ethanol or isopropanol; polar aprotic Solvents such as dimethyl hydrazine or N-methylpyrrolidone or water.
該反應可在減壓、標準壓力或加壓下,及於0至200℃之溫度下進行,較佳係在標準壓力及30至100℃之溫度下進行反應。 The reaction can be carried out under reduced pressure, standard pressure or under pressure, and at a temperature of from 0 to 200 ° C, preferably at a standard pressure and at a temperature of from 30 to 100 ° C.
通式(I-Bc)化合物(R2≠H)隨後進行烷化反應,產生式(I-Bd)化合物。 The compound of the formula (I-Bc) (R 2 ≠H) is subsequently subjected to an alkylation reaction to give a compound of the formula (I-Bd).
該烷化反應係依據WO2010006962之反應條件進行,亦即由(I-Bc)與R1-LG(LG=鹵素、甲磺酸根、甲苯磺酸根或三氟甲磺酸根),於例如:作為鹼之氫化鈉或第三丁醇鉀之存在下,及於作為溶劑之DMF中反應,或於光延(Mitsunobu)反應條件下,以相應醇類R1-OH及三苯基膦為起始物,於DEAD之存在下,於作為溶劑之THF或甲苯中進行。 The alkylation reaction is carried out according to the reaction conditions of WO2010006962, that is, from (I-Bc) and R 1 -LG (LG = halogen, methanesulfonate, tosylate or triflate), for example: as a base In the presence of sodium hydride or potassium t-butoxide, and in DMF as a solvent, or under the conditions of Mitsunobu reaction, starting with the corresponding alcohols R 1 —OH and triphenylphosphine, It is carried out in the presence of DEAD in THF or toluene as a solvent.
該反應可在減壓、標準壓力或加壓下,及於0至200℃之溫度下進行,較佳係在標準壓力及30至100℃之溫度下,可視需要在惰性氣體氛圍下進行反應。 The reaction can be carried out under reduced pressure, standard pressure or under pressure, and at a temperature of from 0 to 200 ° C, preferably at a standard pressure and a temperature of from 30 to 100 ° C, optionally under an inert gas atmosphere.
依製程D步驟(b)製得之根據本發明式(I-Bd)化合物係依製程A步驟(b)之說明,與氧化劑反應,產生根據本發明通式(I-Be)亞碸。 The compound of the formula (I-Bd) according to the present invention, which is obtained according to the process of the step D (b), is reacted with an oxidizing agent according to the procedure of the step A (b) of the process A to produce a hydrazine of the formula (I-Be) according to the invention.
製程D特別適合製備不對稱取代之三二酮,其中R1≠ R2。 Process D is particularly suitable for the preparation of asymmetrically substituted three Diketone, wherein R 1 ≠ R 2 .
類似Bioorg.Med.Chem.Lett.2005,15,4363-4366之製法,由式(VI)側氧基苯基乙酸衍生物與式(VIII)三唑啶酮反應,產生根據本發明式(I-Bf)化合物。 Similar to the method of Bioorg. Med. Chem. Lett. 2005 , 15 , 4363-4366, by reacting a pendant oxyphenylacetic acid derivative of formula (VI) with a triazole ketone of formula (VIII) to give a formula (I according to the invention) -Bf) compound.
如WO8600072所述,式(VIII)三唑啶酮可由相應化合物 R1-NHNH2與丙酮反應,隨後與鹼金屬氰酸鹽反應。 As described in WO8600072, the triazole ketone of formula (VIII) may be corresponding The compound R 1 -NHNH 2 is reacted with acetone and subsequently reacted with an alkali metal cyanate.
式(VI)側氧基苯基乙酸衍生物與式(VIII)三唑啶酮之反應可視需要於觸媒量之酸(例如:硫酸)之存在下,較佳在選自對主要反應條件呈惰性之習知溶劑之溶劑中進行。較佳係醚類如,例如:二烷、四氫呋喃、乙醚或1,2-二甲氧基乙烷;芳香烴類如,例如:苯、甲苯或二甲苯;脂系醇類如,例如:甲醇、乙醇或異丙醇;腈類如,例如:乙腈或丙腈;極性非質子性溶劑,如:二甲亞碸或N-甲基吡咯啶酮。 The reaction of the pendant oxyphenylacetic acid derivative of the formula (VI) with the triazole ketone of the formula (VIII) may be carried out in the presence of a catalytic amount of an acid (for example, sulfuric acid), preferably selected from the main reaction conditions. It is carried out in a solvent of a conventional solvent which is inert. Preferred are ethers such as, for example, two Alkane, tetrahydrofuran, diethyl ether or 1,2-dimethoxyethane; aromatic hydrocarbons such as, for example, benzene, toluene or xylene; aliphatic alcohols such as, for example, methanol, ethanol or isopropanol; For example: acetonitrile or propionitrile; a polar aprotic solvent such as dimethyl hydrazine or N-methylpyrrolidone.
該反應可在減壓、標準壓力或加壓下,及於0至200℃之溫度下進行,較佳係在標準壓力及30至150℃之溫度下,可視需要於惰性氣體氛圍下進行反應。。 The reaction can be carried out under reduced pressure, standard pressure or under pressure, and at a temperature of from 0 to 200 ° C, preferably at a standard pressure and a temperature of from 30 to 150 ° C, optionally under an inert gas atmosphere. .
依製程E步驟(a)製得之根據本發明式(I-Bf)化合物係依製程A步驟(b)之說明,與氧化劑反應,產生根據本發明通式(I-Bg)亞碸。 The compound of the formula (I-Bf) according to the present invention, which is obtained according to Process E, step (a), is reacted with an oxidizing agent according to the procedure of Process A, step (b), to produce a hydrazine of the formula (I-Bg) according to the present invention.
依製程E步驟(a)製得之根據本發明式(I-Bf)化合物係依製程D步驟(b)之說明,進行烷化反應,轉化成根據本發明通式(I-Bh)硫化物。 The compound of the formula (I-Bf) obtained according to the process E step (a) is subjected to an alkylation reaction according to the description of the step (b) of the process D, and converted into a sulfide of the formula (I-Bh) according to the invention. .
依製程E步驟(c)製得之根據本發明式(I-Bh)化合物係依製程A步驟(b)之說明,與氧化劑反應,產生根據本發明通式(I-Bi)亞碸。 The compound of the formula (I-Bh) according to the present invention, which is obtained according to Process E, step (c), is reacted with an oxidizing agent according to the procedure of Process A, step (b), to produce a hydrazine of the formula (I-Bi) according to the present invention.
依製程E步驟(b)製得之根據本發明式式(I-Bg)化合物係依製程D步驟(b)之說明,進行烷化反應,轉化成根據本發明通式(I-Bi)亞碸。 The compound of the formula (I-Bg) according to the process of the formula E (b) is subjected to an alkylation reaction according to the description of the step (b) of the process D, and is converted into the formula (I-Bi) according to the invention. Hey.
製程D及E使用之式(VI)側氧基苯基乙酸衍生物可以例如:由芳基鹵化物前體採用自文獻得知之方法製備,如WO2013/022818 中之說明。 The side oxyphenylacetic acid derivatives of formula (VI) used in Processes D and E can be prepared, for example, from aryl halide precursors by methods known in the literature, such as WO 2013/022818 Description in the middle.
特別值得注意本發明內容所述製程與方法中所示之中間物。此等中間物亦形成本發明之主題。除了上述中間物外,下文亦說明其他中間物。 Particular attention is given to the intermediates shown in the process and method of the present invention. These intermediates also form the subject of the present invention. In addition to the above intermediates, other intermediates are also described below.
本發明進一步提供一種式(VI)化合物,
較佳式(VI)化合物為彼等其中存在如上述較佳定義之組合,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1或2-2之說明。 Preferred compounds of formula (VI) are those in which there is a combination as defined above, and each of the above preferred embodiments constitutes a separate combination, in particular as in embodiment 2-1 or 2-2. Description.
更佳式(VI)化合物為彼等其中存在如上述更佳定義之組合,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1之說明。 More preferred compounds of formula (VI) are those in which there is a better definition as defined above, and each of the above preferred embodiments constitutes a separate combination, specifically as described in the specific example 3-1.
特別佳式(VI)化合物為彼等其中存在如上述特別佳定義之組合,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1或4-2或4-3之說明。 Particularly preferred compounds of the formula (VI) are those in which a combination of the above-mentioned particularly preferred definitions is present, and each of the above-mentioned particularly preferred embodiments constitutes a separate combination, specifically as in the specific example 4-1 or 4-2 or Description of 4-3.
極特別佳式(VI)化合物為彼等其中存在如上述極特別佳定義之組合,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1或5-2之說明。 Very particularly preferred compounds of the formula (VI) are those in which there is a very particularly preferred combination of the above, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination, in particular as in the specific examples 5-1 or 5. -2 description.
本發明提供一種式(I-Bf)化合物,
較佳式(I-Bf)化合物為彼等其中存在如上述較佳定義之組合,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1或2-2之說明。 Preferred compounds of the formula (I-Bf) are those in which there is a combination as defined above, and each of the above preferred embodiments constitutes a separate combination, in particular as in the specific example 2-1 or 2- Description of 2.
更佳式(I-Bf)化合物為彼等其中存在如上述更佳定義之組合,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1之說明。 More preferred (I-Bf) compounds are those in which there is a better definition as defined above, and each of the above preferred embodiments constitutes a separate combination, specifically as described in the specific example 3-1.
特別佳式(I-Bf)化合物為彼等其中存在如上述特別佳定義之組合,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1或4-2或4-3之說明。 Particularly preferred (I-Bf) compounds are those in which there is a combination of the above-mentioned particularly preferred definitions, and each of the above-mentioned particularly preferred embodiments constitutes a separate combination, in particular as in the specific example 4-1 or 4- Description of 2 or 4-3.
極特別佳式(I-Bf)化合物為彼等其中存在如上述極特別佳定義之組合,且上述每一項極特別佳具體實施例構成獨立之組合,特定言之如具體實施例5-1或5-2之說明。 Very particularly preferred (I-Bf) compounds are combinations in which there are very particularly well defined definitions, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination, in particular as in the specific examples 5-1 Or the description of 5-2.
本發明進一步提供一種式(I-Bg)化合物,
較佳式(I-Bg)化合物為彼等其中存在如上述較佳定義之組合,且上述每一項較佳具體實施例構成獨立之組合,特定言之如具體實施例2-1或2-2之說明。 Preferred compounds of the formula (I-Bg) are those in which there is a combination as defined above, and each of the above preferred embodiments constitutes a separate combination, in particular as in the specific example 2-1 or 2- Description of 2.
更佳式(I-Bg)化合物為彼等其中存在如上述更佳定義之組合,且上述每一項更佳具體實施例構成獨立之組合,特定言之如具體實施例3-1之說明。 More preferred (I-Bg) compounds are those in which there is a better definition as defined above, and each of the above preferred embodiments constitutes a separate combination, specifically as described in the specific example 3-1.
特別佳式(I-Bg)化合物為彼等其中存在如上述特別佳定義之組合,且上述每一項特別佳具體實施例構成獨立之組合,特定言之如具體實施例4-1或4-2或4-3之說明。 Particularly preferred (I-Bg) compounds are those in which there is a combination of the above-mentioned particularly preferred definitions, and each of the above-mentioned particularly preferred embodiments constitutes a separate combination, specifically as exemplified in Example 4-1 or 4- Description of 2 or 4-3.
極特別佳式(I-Bg)化合物為彼等其中存在如上述極特別佳定義之組合,且上述每一項極特別佳具體實施例構成獨立之組合。 Very particularly preferred (I-Bg) compounds are combinations in which there are very particularly well defined definitions, and each of the above-mentioned very particularly preferred embodiments constitutes a separate combination.
依取代基性質而定,式(I)化合物可呈幾何與/或光學活性異構物或不同組成之相應異構物混合物。此等立體異構物為例如:對映異構物、非對映異構物、阻轉異構物或幾何異構物。因此,本發明包括純立體異構物及此等異構物之任何所需混合物。 Depending on the nature of the substituent, the compound of formula (I) may be a geometrically and/or optically active isomer or a mixture of corresponding isomers of different compositions. Such stereoisomers are, for example, enantiomers, diastereomers, atropisomers or geometric isomers. Accordingly, the invention includes pure stereoisomers and any desired mixtures of such isomers.
本發明亦有關控制動物害蟲之方法,其中由式(I)化合物作用在動物害蟲與/或其棲息地上。動物害蟲之控制較佳係在農業與森林,及材料保護上進行。較佳係排除人體或動物體之手術或醫療處理之方法及在人體或動物體上進行之診斷方法。 The invention also relates to a method of controlling an animal pest in which a compound of formula (I) acts on an animal pest and/or its habitat. The control of animal pests is preferably carried out in agriculture and forests, as well as in material protection. Preferably, the method of surgical or medical treatment of the human or animal body and the diagnostic method performed on the human or animal body are excluded.
本發明亦有關一種以式(I)化合物作為除害劑,尤指作為作物保護劑之用途。 The invention also relates to the use of a compound of formula (I) as a pesticide, especially as a crop protection agent.
本申請案內容中,各例中術語"除害劑"亦總是包括術語"作物保護劑"。 In the context of the present application, the term "pesticides" in each case also always includes the term "crop protectant".
式(I)化合物具有良好之植物耐受性、對恆溫動物有利之毒性及良好之環境相容性,適合保護植物與植物器官來對抗生物性與非生物性逆境壓力,提高收成產量、改進收成材料品質、及控制動物害蟲,尤指出現在農業、園藝、動物畜養、水產養殖、森林、花園與休閒設施之昆蟲、蜘蛛、蠕蟲、線蟲與軟體動物,可用於保護庫存產品與材料,及用於衛生領域。其較佳係作為除害劑使用。其可有效對抗正常敏感性與抗性物種,及對抗所有或個別發展階段。上述害蟲包括:節肢動物門(Arthropoda),尤指蛛形綱(Arachnida)之害蟲,例如:粗腳粉蟎屬(Acarus spp.)(例如:粉塵蟎(Acarus siro))、枸杞瘤節蜱(Aceria kuko)、桔瘤節蜱(Aceria sheldoni)、刺皮癭蟎屬(Aculops spp.)、刺癭蟎屬(Aculus spp.)(例如:福氏刺節蜱(Aculus fockeui)、蘋果銹蜱(Aculus schlechtendali))、花蜱屬(Amblyomma spp.)、橫紋葉蟎(Amphitetranychus viennensis)、銳緣蜱屬(Argas spp.)、牛蜱屬(Boophilus spp.)、紅鬚蟎屬(Brevipalpus spp.)(例如:紫紅短鬚蟎(Brevipalpus phoenicis))、禾草苔蟎(Bryobia graminum)、苜蓿苔蟎(Bryobia praetiosa)、刺尾蠍屬(Centruroides spp.)、恙蟎屬(Chorioptes spp.)、雞皮刺蟎(Dermanyssus gallinae)、羽刺皮癬蟎(Dermatophagoides pteronyssinus)、美洲塵蟎(Dermatophagoides farinae)、革蜱屬(Dermacentor spp.)、始葉蟎屬(Eotetranychus spp.)(例如:核桃始葉蟎(Eotetranychus hicoriae))、梨上癭蟎(Epitrimerus pyri)、真葉蟎屬(Eutetranychus spp.)(例如:斑氏真葉蟎(Eutetranychus banksi))、癭蟎屬(Eriophyes spp.)(例如:梨癭蟎(Eriophyes pyri))、家食甜蟎(Glycyphagus domesticus)、足海鐮螯蟎(Halotydeus destructor)、半跗線蟎屬(Hemitarsonemus spp.)(例如:茶塵蟎 (Hemitarsonemus latus)(=多食細蟎(Polyphagotarsonemus latus))、璃眼蜱屬(Hyalomma spp.)、硬蜱屬(Ixodes spp.)、球腹蛛屬(Latrodectus spp.)、褐隱蛛屬(Loxosceles spp.)、秋收恙蟎(Neutrombicula autumnalis)、Nuphersa屬、小爪蟎屬(Oligonychus spp.)(例如:針葉小爪蟎(Oligonychus coniferarum)、冬青小爪蟎(Oligonychus ilicis)、甘蔗小爪蟎(Oligonychus indicus)、芒果小爪蟎(Oligonychus mangiferus)、草地小爪蟎(Oligonychus pratensis)、石榴小爪蟎(Oligonychus punicae)、樟小爪蟎(Oligonychus yothersi))、鈍緣蜱屬(Ornithodorus spp.)、巨刺蟎屬(Ornithonyssus spp.)、紅蜘蛛屬(Panonychus spp.)(例如:桔全爪蟎(Panonychus citri)(=柑桔葉蟎(Metatetranychus citri))、榆全爪蟎(Panonychus ulmi)(=歐洲葉蟎(Metatetranychus ulmi)))、橘鏽蟎(Phyllocoptruta oleivora)、雜食葉蟎(Platytetranychus multidigituli)、多食細蟎(Polyphagotarsonemus latus)、癢蟎屬(Psoroptes spp.)、扇頭蜱屬(Rhipicephalus spp.)、根蟎屬(Rhizoglyphus spp.)、人疥蟎屬(Sarcoptes spp.)、蠍(Scorpio maurus)、狹跗線蟎屬(Stenotarsonemus spp.)、稻細蟎(Steneotarsonemus spinki)、細蟎屬(Tarsonemus spp.)(例如:亂跗線蟎(Tarsonemus confusus)、仙克萊細蟎(Tarsonemus pallidus))、紅葉蟎屬(Tetranychus spp.)(例如:加拿大葉蟎(Tetranychus canadensis)、赤葉蟎(Tetranychus cinnabarinus)、土耳其斯坦葉蟎(Tetranychus turkestani)、二斑葉蟎(Tetranychus urticae))、秋蟎(Trombicula alfreddugesi)、蠍屬(Vaejovis spp.)、斜背瘤節蜱(Vasates lycopersici);唇足綱(Chilopoda),例如:地蜈蚣屬(Geophilus spp.)、蚰蜓屬(Scutigera spp.);彈尾綱或彈尾目(Collembola),例如:棘跳蟲(Onychiurus armatus);綠圓跳蟲(Sminthurus viridis); 重足綱(Diplopoda),例如:具斑馬陸(Blaniulus guttulatus);昆蟲綱(Insecta),例如:蜚蠊目(Blattodea),例如:東方蜚蠊(Blatta orientalis)、蜚蠊(Blattella asahinai)、德國蜚蠊(Blattella germanica)、馬得拉蜚蠊(Leucophaea maderae)、古巴蜚蠊屬(Panchlora spp.)、帕科蜚蠊屬(Parcoblatta spp.)、家蠊屬(Periplaneta spp.)(例如:美洲家蠊(Periplaneta americana)、澳洲家蠊(Periplaneta australasiae))、美洲家蠊(Supella longipalpa);鞘翅目(Coleoptera),例如:鑲邊黃瓜甲蟲(Acalymma vittatum)、大豆象(Acanthoscelides obtectus)、麗金龜屬(Adoretus spp.)、赤楊紫跳甲(Agelastica alni)、叩頭蟲屬(Agriotes spp.)(例如:具條叩甲(Agriotes linneatus)、小麥金針蟲(Agriotes mancus))、外米擬步行蟲(Alphitobius diaperinus)、六月金龜子(Amphimallon solstitialis)、食骸蟲(Anobium punctatum)、天牛屬(Anoplophora spp.)、棉鈴象甲屬(Anthonomus spp.)(例如:苜蓿葉象甲(Anthonomus grandis))、蠹屬(Anthrenus spp.)、梨象屬(Apion spp.)、甘蔗金龜屬(Apogonia spp.)、隱食甲屬(Atomaria spp.)(例如:甜菜隱食甲(Atomaria linearis))、小鰹節蟲屬(Attagenus spp.)、象甲(Baris caerulescens)、豆象(Bruchidius obtectus)、豆象甲屬(Bruchus spp.)(例如:豌豆象甲(Bruchus pisorum)、蠶豆象甲(Bruchus rufimanus))、金花蟲屬(Cassida spp.)、大豆葉甲(Cerotoma trifurcate)、象甲屬(Ceuthorrhynchus spp.)(例如:甘藍莢象甲(Ceutorrhynchus assimilis)、藍籽莖象甲(Ceutorrhynchus quadridens)、油菜象甲(Ceutorrhynchus rapae))、小金花蟲屬(Chaetocnema spp.)(例如:甘薯金花蟲(Chaetocnema confinis)、具齒跳甲(Chaetocnema denticulata)、玉米跳甲(Chaetocnema ectypa))、牛蒡象甲(Cleonus mendicus)、金針蟲屬(Conoderus spp.)、球莖象甲屬(Cosmopolites spp.)(例如:香蕉球莖象甲(Cosmopolites sordidus))、蠐螬(Costelytra zealandica)、叩頭蟲屬(Ctenicera spp.)、象甲屬(Curculio spp.)(例如:核桃象甲(Curculio caryae)、大栗象甲(Curculio caryatrypes)、榛子象甲(Curculio obtusus)、小栗象甲(Curculio sayi))、角胸粉扁蟲(Cryptolestes ferrugineus)、角胸扁蟲(Cryptolestes pusillus)、柳小隱喙象甲(Cryptorhynchus lapathi)、芒果象甲(Cryptorhynchus mangiferae)、莖象甲屬(Cylindrocopturus spp.)、密點細枝象甲(Cylindrocopturus adspersus)、黃杉枝象甲(Cylindrocopturus furnissi)、皮蠹屬(Dermestes spp.)、葉甲屬(Diabrotica spp.)(例如:巴西玉米根蟲(Diabrotica balteata)、北方玉米根蟲(Diabrotica barberi)、南部玉米根蟲(Diabrotica undecimpunctata howardi)、黃瓜十一星葉甲(Diabrotica undecimpunctata undecimpunctata)、玉米根蟲(Diabrotica virgifera virgifera)、墨西哥玉米根蟲(Diabrotica virgifera zeae))、蛀螟屬(Dichocrocis spp.)、水稻鐵甲蟲(Dicladispa armigera)、阿根廷兜蟲屬(Diloboderus spp.)、瓢蟲屬(Epilachna spp.)(例如:南瓜瓢蟲(Epilachna borealis)、食植瓢蟲(Epilachna varivestis))、跳甲屬(Epitrix spp.)(例如:黃瓜跳甲(Epitrix cucumeris)、茄跳甲(Epitrix fuscula)、煙草跳甲(Epitrix hirtipennis)、馬鈴薯跳甲(Epitrix subcrinita)、塊莖跳甲(Epitrix tuberis))、鑽孔蟲屬(Faustinus spp.)、麥蛛甲(Gibbium psylloides)、闊角穀盜(Gnathocerus cornutus)、菜心螟(Hellula undalis)、白蠐螬(Heteronychus arator)、天牛屬(Heteronyx spp.)、金龜子(Hylamorpha elegans)、象天牛(Hylotrupes bajulus)、苜蓿象甲(Hypera postica)、藍綠象(Hypomeces squamosus)、小蠹屬(Hypothenemus spp.)(例如:咖啡果小蠹(Hypothenemus hampei)、蘋枝小蠹(Hypothenemus obscurus)、果小蠹(Hypothenemus pubescens))、鰓角金龜(Lachnosterna consanguinea)、煙甲蟲(Lasioderma serricorne)、長首穀盜(Latheticus oryzae)、薪甲屬(Lathridius spp.)、負泥甲屬(Lema spp.)、馬鈴薯甲蟲(Leptinotarsa decemlineata)、潛葉 蛾屬(Leucoptera spp.)(例如:咖啡潛葉蛾(Leucoptera coffeella))、稻象甲(Lissorhoptrus oryzophilus)、黃象甲屬(Lixus spp.)、黃胸葉甲(Luperomorpha xanthodera)、葉甲屬(Luperodes spp.)、粉蠹屬(Lyctus spp.)、美洲葉甲屬(Megascelis spp.)、叩頭蟲屬(Melanotus spp.)(例如:奧勒岡州叩甲(Melanotus longulus oregonensis))、花粉甲(Meligethes aeneus)、吹粉金龜屬(Melolontha spp.)(例如:大栗鰓角金龜(Melolontha melolontha))、天牛屬(Migdolus spp.)、天牛屬(Monochamus spp.)、象甲(Naupactus xanthographus)、郭公蟲屬(Necrobia spp.)、金黃蛛甲(Niptus hololeucus)、犀角金龜(Oryctes rhinoceros)、鋸胸粉扁蟲(Oryzaephilus surinamensis)、稻象甲(Oryzaphagus oryzae)、深溝象甲屬(Otiorrhynchus spp.)(例如:蘋果白象甲(Otiorhynchus cribricollis)、苜蓿象甲(Otiorhynchus ligustici)、草莓根象甲(Otiorhynchus ovatus)、根象甲(Otiorhynchus rugosostriarus)、黑藤象甲(Otiorhynchus sulcatus))、銀點花金龜(Oxycetonia jucunda)、猿葉蟲(Phaedon cochleariae)、食葉蟲屬(Phyllophaga spp.)、鰓角金龜(Phyllophaga helleri)、葉蚤屬(Phyllotreta spp.)(例如:辣根跳甲(Phyllotreta armoraciae)、柔弱黑跳甲(Phyllotreta pusilla)、美條紋跳甲(Phyllotreta ramosa)、黃條葉蚤(Phyllotreta striolata))、日本麗金龜(Popillia japonica)、小象甲屬(Premnotrypes spp.)、大穀蠹(Prostephanus truncatus)、跳甲屬(Psylliodes spp.)(例如:馬鈴薯跳甲(Psylliodes affinis)、油菜蘭跳甲(Psylliodes chrysocephala)、忽布跳甲(Psylliodes punctulata))、蛛甲屬(Ptinus spp.)、黑根瓢蟲(Rhizobius ventralis)、粉長蠹蟲(Rhizopertha dominica)、米象屬(Sitophilus spp.)(例如:穀象(Sitophilus granarius)、羅望子象(Sitophilus linearis)、米象(Sitophilus oryzae)、玉米象(Sitophilus zeamais))、穀象屬(Sphenophorus spp.)、藥材甲蟲(Stegobium paniceum)、莖象屬(Sternechus spp.)(例如:豆莖象(Sternechus paludatus))、扁肩象屬(Symphyletes spp.)、象甲屬(Tanymecus spp.)(例如:玉米葉象(Tanymecus dilaticollis)、纖毛象(Tanymecus indicus)、紅豆草灰象甲(Tanymecus palliates))、粉甲(Tenebrio molitor)、穀盜(Tenebrioides mauretanicus)、擬穀盜屬(Tribolium spp.)(例如:黑粉穀盜(Tribolium audax)、擬穀盜(Tribolium castaneum)、扁擬穀盜(Tribolium confusum))、鰹節蟲屬(Trogoderma spp.)、象甲屬(Tychius spp.)、虎天牛屬(Xylotrechus spp.)、步甲屬(Zabrus spp.)(例如:玉米步甲(Zabrus tenebrioides));雙翅目(Diptera),例如:伊蚊屬(Aedes spp.)(例如:埃及斑蚊(Aedes aegypti)、白線斑蚊(Aedes albopictus)、叮刺伊蚊(Aedes sticticus)、騷擾伊蚊(Aedes vexans))、潛蠅屬(Agromyza spp.)(例如:寬額斑潛蠅(Agromyza frontella)、美洲黍潛葉蠅(Agromyza parvicornis))、按實蠅屬(Anastrepha spp.)、按蚊屬(Anopheles spp.)(例如:四斑按蚊(Anopheles quadrimaculatus)、甘比亞瘧蚊(Anopheles gambiae))、癭蚊屬(Asphondylia spp.)、實蠅屬(Bactrocera spp.)(例如:瓜實蠅(Bactrocera cucurbitae)、東方果實蠅(Bactrocera dorsalis)、橄欖果蠅(Bactrocera oleae))、毛蚊(Bibio hortulanus)、麗蠅(Calliphora erythrocephala)、紅頭麗蠅(Calliphora vicina)、地中海果實蠅(Ceratitis capitata)、搖蚊屬(Chironomus spp.)金蠅屬(Chrysomyia spp.)、斑虻屬(Chrysops spp.)、麻翅虻(Chrysozona pluvialis)、刺蚊屬(Cochliomyia spp.)、康癭蚊屬(Contarinia spp.)(例如:葡萄癭蚊(Contarinia johnsoni)、甘藍癭蚊(Contarinia nasturtii)、梨葉癭蚊(Contarinia pyrivora)、向日葵癭蚊(Contarinia schulzi)、高粱癭蚊(Contarinia sorghicola)、麥黃吸漿蟲(Contarinia tritici))、糞蠅(Cordylobia anthropophaga)、環足搖蚊(Cricotopus sylvestris)、庫蚊屬(Culex spp.)(例如:尖音庫蚊(Culex pipiens)、五帶淡色庫蚊(Culex quinquefasciatus))、庫蠓屬(Culicoides spp.)、脈毛蚊屬(Culiseta spp.)、疽蠅 屬(Cuterebra spp.)、果蠅(Dacus oleae)、癭蚊屬(Dasyneura spp.)(例如:油菜莢葉癭蚊(Dasineura brassicae))、地種蠅屬(Delia spp.)(例如:蔥地種蠅(Delia antiqua)、麥種蠅(Delia coarctata)、毛跗地種蠅(Delia florilega)、灰地種蠅(Delia platura)、甘藍地種蠅(Delia radicum))、人膚蠅(Dermatobia hominis)、猩猩蠅屬(Drosophila spp.)(例如:黑腹果蠅(Drosphila melanogaster)、鈴木果蠅(Drosphila suzukii))、象甲屬(Echinocnemus spp.)、廄蠅屬(Fannia spp.)、胃蠅屬(Gastrophilus spp.)、舌蠅屬(Glossina spp.)、麻虻屬(Haematopota spp.)、稻心蠅屬(Hydrellia spp.)、水稻潛葉蠅(Hydrellia griseola)、種蠅屬(Hylemyia spp.)、虱蠅屬(Hippobosca spp.)、皮蠅屬(Hypoderma spp.)、潛蠅屬(Liriomyza spp.)(例如:白菜斑潛蠅(Liriomyza brassicae)、南美斑潛蠅(Liriomyza huidobrensis)、蔬菜斑潛蠅(Liriomyza sativae))、綠蠅屬(Lucilia spp.)(例如:絲光綠蠅(Lucilia cuprina))、羅蛉屬(Lutzomyia spp.)、沼蚊屬(Mansonia spp.)、家蠅屬(Musca spp.)(例如:家蠅(Musca domestica)、舍蠅(Musca domestica vicina))、狂蠅屬(Oestrus spp.)、瑞典蠅(Oscinella frit)、搖蚊屬(Paratanytarsus spp.)、搖蚊(Paralauterborniella subcincta)、潛蠅屬(Pegomya spp.)(例如:甜菜潛蠅(Pegomya betae)、菠菜潛蠅(Pegomya hyoscyami)、懸鉤子潛蠅(Pegomya rubivora))、白蛉屬(Phlebotomus spp.)、蚤蠅屬(Phorbia spp.)、伏蠅屬(Phormia spp.)、酪蠅(Piophila casei)、癭蚋屬(Prodiplosis spp.)、胡蘿蔔蠅(Psila rosae)、果實蠅屬(Rhagoletis spp.)(例如:北美櫻桃實蠅(Rhagoletis cingulata)、核桃繞實蠅(Rhagoletis completa)、黑櫻桃實蠅(Rhagoletis fausta)、歐洲甜櫻桃繞實蠅(Rhagoletis indifferens)、藍橘繞實蠅(Rhagoletis mendax)、蘋果果實蠅(Rhagoletis pomonella))、肉蠅屬(Sarcophaga spp.)、蚋屬(Simulium spp.)(例如:南方蚋(Simulium meridionale))、螫蠅屬(Stomoxys spp.)、虻屬(Tabanus spp.)、直斑蠅屬 (Tetanops spp.)、大蚊屬(Tipula spp.)(例如:歐洲大蚊(Tipula paludosa)、牧場大蚊(Tipula simplex));半翅目(Hemiptera),例如:金合歡昆木虱(Acizzia acaciaebaileyanae)、木虱(Acizzia dodonaeae)、木虱(Acizzia uncatoides)、長頭蝗(Acrida turrita)、無網長管蟲牙屬(Acyrthosipon spp.)(例如:碗豆蚜(Acyrthosiphon pisum))、葉蟬屬(Acrogonia spp.)、Aeneolamia屬、隆脈木虱屬(Agonoscena spp.)、歐洲甘藍粉虱(Aleyrodes proletella)、甘蔗穴粉虱(Aleurolobus barodensis)、棉絮粉虱(Aleurothrixus floccosus)、榴蓮被榴蓮木虱(Allocaridara malayensis)、果葉蝶屬(Amrasca spp.)(例如:二點小綠葉蟬(Amrasca bigutulla)、棉葉蟬(Amrasca devastans))、飛廉短尾蚜(Anuraphis cardui)、腎圓盾介殼蟲屬(Aonidiella spp.)(例如:橘紅腎圓盾介殼蟲(Aonidiella aurantii)、橘黃腎圓盾介殼蟲(Aonidiella citrina)、木瓜腎圓盾介殼蟲(Aonidiella inornata))、梨瘤蚜(Aphanostigma piri)、蚜蟲屬(Aphis spp.)(例如:橘捲菜蚜(Aphis citricola)、豆蚜(Aphis craccivora)、黑豆蚜(Aphis fabae)、草莓根蚜(Aphis forbesi)、大豆蚜(Aphis glycines)、棉蚜(Aphis gossypii)、常春藤蚜(Aphis hederae)、葡萄蔓蚜(Aphis illinoisensis)、蚜蟲(Aphis middletoni)、鼠李馬鈴薯蚜(Aphis nasturtii)、夾竹桃蚜(Aphis nerii)、蘋果蚜(Aphis pomi)、繡線菊蚜(Aphis spiraecola)、莢蒾蚜(Aphis viburniphila))、葡萄二星斑葉蟬(Arboridia apicalis)、木虱屬(Arytainilla spp.)、小圓盾蚧屬(Aspidiella spp.)、圓盾階屬(Aspidiotus spp.)(例如:夾竹桃圓蚧(Aspidiotus nerii))、Atanus屬、馬鈴薯蚜(Aulacorthum solani)、煙草粉虱(Bemisia tabaci)、芽木虱(Blastopsylla occidentalis)、茶樹蚜木虱(Boreioglycaspis melaleucae)、光管舌尾蚜(Brachycaudus helichrysi)、微管蟲牙屬(Brachycolus spp.)、菜蚜(Brevicoryne brassicae)、梨木虱屬(Cacopsylla spp.)(例如:梨黃木虱 (Cacopsylla pyricola))、小褐稻虱(Calligypona marginata)、黃頭大葉蟬(Carneocephala fulgida)、甘蔗綿蚜(Ceratovacuna lanigera)、沫蟬科(Cercopidae)、角蠟蚧屬(Ceroplastes spp.)、草莓毛管蚜(Chaetosiphon fragaefolii)、蔗黃雪盾蚧(Chionaspis tegalensis)、茶小綠葉蟬(Chlorita onukii)、臺灣大蝗(Chondracris rosea)、核桃黑斑蚜(Chromaphis juglandicola)、柑橘褐圓蚧(Chrysomphalus ficus)、玉米葉蟬(Cicadulina mbila)、Coccomytilus halli、蚧屬(Coccus spp.)(例如:扁堅蚧(Coccus hesperidum)、長堅蚧(Coccus longulus)、桔軟蠟蟲介(Coccus pseudomagnoliarum)、黃綠蚧(Coccus viridis))、茶藨隱瘤蚜(Cryptomyzus ribis)、Cryptoneossa屬、梳木虱屬(Ctenarytaina spp.)、黃翅葉蜂屬(Dalbulus spp.)、柑桔裸粉虱(Dialeurodes citri)、柑桔木虱(Diaphorina citri)、盾蚧屬(Diaspis spp.)、草履蚧屬(Drosicha spp.)、莖蚜蟲屬(Dysaphis spp.)(例如:銹條蚜(Dysaphis apiifolia)、車前圓尾蚜(Dysaphis plantaginea)、鬱金香鱗莖蚜蟲(Dysaphis tulipae))、灰粉蚧屬(Dysmicoccus spp.)、小綠葉蟬屬(Empoasca spp.)(例如:馬鈴薯葉蟬(Empoasca abrupta)、馬鈴薯葉蟬(Empoasca fabae)、蘋果小綠葉蟬(Empoasca maligna)、茄微葉蟬(Empoasca solana)、史蒂芬氏葉蟬(Empoasca stevensi))、綿蚜屬(Eriosoma spp.)(例如:美國綿蚜(Eriosoma americanum)、蘋果綿蚜(Eriosoma lanigerum)、居梨綿蚜(Eriosoma pyricola))、斑葉蟬屬(Erythroneura spp.)、檸檬桉木虱屬(Eucalyptolyma spp.)、褐木風屬(Euphyllura spp.)、鈍鼻葉蟬(Euscelis bilobatus)、拂粉蚧屬(Ferrisia spp.)、咖啡粉蚧(Geococcus coffeae)、木虱屬(Glycaspis spp.)、銀合歡木虱(Heteropsylla cubana)、頰木虱(Heteropsylla spinulosa)、褐透翅尖頭大葉蟬(Homalodisca coagulata)、桃大尾蚜(Hyalopterus arundinis)、桃粉蚜(Hyalopterus pruni)、吹綿蚧屬(Icerya spp.)(例如:吹綿蚧(Icerya purchasi))、片角葉蟬屬(Idiocerus spp.)、綠葉蟬 屬(Idioscopus spp.)、灰飛虱(Laodelphax striatellus)、球蚧屬(Lecanium spp.)(例如:李蠟蚧(Lecanium corni)(=褐盔蠟蚧(Parthenolecanium corni))、蠣盾蚧屬(Lepidosaphes spp.)(例如:榆蠣盾蚧(Lepidosaphes ulmi))、偽菜蚜(Lipaphis erysimi)、斑衣蠟蟬(Lycorma delicatula)、長管蚜屬(Macrosiphum spp.)(例如:馬鈴薯長管蚜(Macrosiphum euphorbiae)、長管蚜(Macrosiphum lilii)、薔薇長管蚜(Macrosiphum rosae))、長針葉蟬(Macrosteles facifrons)、沫蝶屬(Mahanarva spp.)、黍蚜(Melanaphis sacchari)、Metcalfiella屬、蛾蠟蟬(Metcalfa pruinosa)、麥無網蚜(Metopolophium dirhodum)、黑緣平翅斑蚜(Monellia costalis)、胡桃黑蚜(Monelliopsis pecanis)、桃蚜屬(Myzus spp.)(例如:冬蔥瘤額蚜(Myzus ascalonicus)、李瘤蚜(Myzus cerasi)、女貞瘤額蚜(Myzus ligustri)、堇菜瘤蚜(Myzus ornatus)、桃赤蚜(Myzus persicae)、煙草蚜(Myzus nicotianae))、萵苣蚜(Nasonovia ribisnigri)、黑尾葉蟬屬(Nephotettix spp.)(例如:偽黑尾葉蟬(Nephotettix cincticeps)、黑條黑尾葉蟬(Nephotettix nigropictus))、褐飛虱(Nilaparvata lugens)、Oncometopia屬、旌蚧(Orthezia praelonga)、中華稻蝗(Oxya chinensis)、癭木虱屬(Pachypsylla spp.)、楊梅粉虱(Parabemisia myricae)、木虱屬(Paratrioza spp.)(例如:番茄木虱(Paratrioza cockerelli))、片盾蚧屬(Parlatoria spp.)、癭綿蚜屬(Pemphigus spp.)(例如:白楊癭綿蚜(Pemphigus bursarius)、多脈癭綿蚜(Pemphigus populivenae))、玉米飛虱(Peregrinus maidis)、粉蚧屬(Phenacoccus spp.)(例如:美地綿粉蚧(Phenacoccus madeirensis))、楊平翅棉蚜(Phloeomyzus passerinii)、瘤蚜(Phorodon humuli)、桃根蚜屬(Phylloxera spp.)(例如:核桃根瘤蚜(Phylloxera devastatrix)、警根瘤蚜(Phylloxera notabilis))、橘長盾蚧(Pinnaspis aspidistrae)、粉蚧屬(Planococcus spp.)(例如:柑桔粉蚧(Planococcus citri))、黃粉蚧(Prosopidopsylla flava)、梨形原棉蚧 (Protopulvinaria pyriformis)、桑白蚧(Pseudaulacaspis pentagona)、粉蚧屬(Pseudococcus spp.)(例如:柑桔棲粉蚧(Pseudococcus calceolariae)、康氏粉蚧(Pseudococcus comstocki)、長尾粉蚧(Pseudococcus longispinus)、葡萄粉蚧(Pseudococcus maritimus)、暗色粉蚧(Pseudococcus viburni))、Psyllopsis屬、木虱屬(Psylla spp.)(例如:黃楊木虱(Psylla buxi)、蘋木虱(Psylla mali)、梨木虱(Psylla pyri))、金小蜂屬(Pteromalus spp.)、飛虱屬(Pyrilla spp.)、圓蚧屬(Quadraspidiotus spp.)(例如:胡桃圓盾蚧(Quadraspidiotus juglansregiae)、正楊笠圓盾蚧(Quadraspidiotus ostreaeformis)、梨圓盾蚧(Quadraspidiotus perniciosus))、Quesada gigas、粉蚧屬(Rastrococcus spp.)、頸狀蚜屬(Rhopalosiphum spp.)(例如:玉米蚜(Rhopalosiphum maidis)、縊管蚜(Rhopalosiphum oxyacanthae)、稻麥蚜(Rhopalosiphum padi)、紅腹縊管蚜(Rhopalosiphum rufiabdominale))、硬蚧屬(Saissetia spp.)(例如:咖啡硬蚧(Saissetia coffeae)、硬蚧(Saissetia miranda、Saissetia neglecta)、工脊硬蚧(Saissetia oleae))、螻蛄(Scaphoides titanus)、麥二叉蚜(Schizaphis graminum)、盾蚧(Selenaspidus articulatus)、麥長管蚜(Sitobion avenae)、飛虱屬(Sogata spp.)、白背飛虱(Sogatella furcifera)、飛虱屬(Sogatodes spp.)、沫蟬(Stictocephala festina)、梣粉虱(Siphoninus phillyreae)、聲蚜(Tenalaphara malayensis)、Tetragonocephela屬、核桃黑蚜(Tinocallis caryaefoliae)、沫蟬屬(Tomaspis spp.)、二叉蚜屬(Toxoptera spp.)(例如:小桔蚜(Toxoptera aurantii)、大桔蚜(Toxoptera citricidus))、溫室粉虱(Trialeurodes vaporariorm)、木虱屬(Trioza spp.)(例如:棉木虱(Trioza diospyri))、紅閃小葉蟬屬(Typhlocyba spp.)、盾蚧屬(Unaspis spp.)、葡萄根瘤蚜(Viteus vitifolii)、斑點鋸蜂屬(Zygina spp.);異翅亞目(Heteroptera),例如:南瓜緣蝽(Anasa tristis)、芒果蝽屬(Antestiopsis spp.)、紅緣蝽屬(Boisea spp.)、麥長蝽屬(Blissus spp.)、盲蝽屬(Calocoris spp.)、盲蝽(Campylomma livida)、二尾蚜屬(Cavelerius spp.)、臭蟲屬(Cimex spp.)(例如:臭蟲(Cimex adjunctus)、熱帶臭蟲(Cimex hemipterus)、床蝨(Cimex lectularius)、蝠臭蟲(Cimex pilosellus))、盲蝽屬(Collaria spp.)、盲蝽(Creontiades dilutus)、胡椒緣蝽(Dasynus piperis)、二葉喙蝽(Dichelops furcatus)、胡椒網蝽(Diconocoris hewetti)、蝽象屬(Dysdercus spp.)、臭蝽屬(Euschistus spp.)(例如:大豆褐蝽(Euschistus heros)、褐臭蝽(Euschistus servus)、暗淡蝽象(Euschistus tristigmus)、一點褐蝽(Euschistus variolarius))、刺蝽屬(Eurygaster spp.)、褐翅蝽象(Halyomorpha halys)、夜蛾屬(Heliopeltis spp.)、稻緣蜂(Horcias nobilellus)、豬緣蝽屬(Leptocorisa spp.)、稻緣蝽象(Leptocorisa varicornis)、西方針葉樹種子甲蟲(Leptoglossus occidentalis)、葉足緣蝽(Leptoglossus phyllopus)、麗盲蝽屬(Lygocoris spp.)(例如:原麗盲蝽(Lygocoris pabulinus))、盲蝽屬(Lygus spp.)(例如:豆莢灰盲蝽(Lygus elisus)、豆莢草盲蝽(Lygus hesperus)、美國牧草盲蝽(Lygus lineolaris))、蔗黑長蝽(Macropes excavatus)、金光綠盲蝽(Monalonion atratum)、綠蝽屬(Nezara spp.)(例如:稻綠蝽象(Nezara viridula))、盾蝽屬(Oebalus spp.)、擬配軍蟲(Piesma quadrata)、壁蝽屬(Piezodorus spp.)(例如:紅蝽(Piezodorus guildinii))、盲蝽屬(Psallus spp.)、駱梨盲蝽象(Pseudacysta persea)、紅腹獵蝽屬(Rhodnius spp.)、可哥褐盲蝽(Sahlbergella singularis)、土蝽(Scaptocoris castanea)、稻黑蝽屬(Scotinophora spp.)、梨花網蝽(Stephanitis nashi)、臭蟲屬(Tibraca spp.)、椎蝽屬(Triatoma spp.);膜翅目(Hymenoptera),例如:切葉蟻(Acromyrmex spp.)、葉蜂屬(Athalia spp.)(例如:紅角菜葉蜂(Athalia rosae))、切葉蟻屬(Atta spp.)、松葉蜂屬(Diprion spp.)(例如:歐洲赤松葉蜂(Diprion similis))、葉蜂屬(Hoplocampa spp.)(例如:櫻實葉蜂(Hoplocampa cookei)、蘋果葉蜂(Hoplocampa testudinea))、蟻屬(Lasius spp.)、阿根廷蟻(Linepithema humile)、廚蟻(Monomorium pharaonis)、樹蜂屬(Sirex spp.)、入侵紅火蟻(Solenopsis invicta)、酸臭蟻屬((Tapinoma spp.)、樹蜂(Urocerus spp.)、胡蜂屬(Vespa spp.)(例如:黃邊胡蜂(Vespa crabro))、樹蜂屬(Xeris spp.);等足目(Isopoda),例如:鼠婦(Armadillidium vulgare)、海蛆(Oniscus asellus)、球鼠婦(Porcellio scaber);等翅目(Isoptera),例如:乳白蟻屬(Coptotermes spp.)(例如:台彎家白蟻(Coptotermes formosanus))、白蟻(Cornitermes cumulans)、堆砂白蟻屬(Cryptotermes spp.)、楹白蟻屬(Incisitermes spp.)、甘蔗白蟻(Microtermes obesi)、土白蟻屬(Odontotermes spp.)、白蟻屬(Reticulitermes spp.)(例如:黃肢散白蟻(Reticulitermes flavipes)、西方犀白蟻(Reticulitermes hesperus));鱗翅目(Lepidoptera),例如:小蠟蛾(Achroia grisella)、梁劍紋夜蛾(Acronicta major)、卷葉蛾屬(Adoxophyes spp.)(例如:棉褐帶卷蛾(Adoxophyes orana))、電紋夜蛾(Aedia leucomelas)、地老虎屬(Agrotis spp.)(例如:黃地老虎(Agrotis segetum)、小地老虎(Agrotis ipsilon))、波紋夜蛾屬(Alabama spp.)(例如:棉葉波紋夜蛾(Alabama argillacea))、蘋果蠹蛾(Amyelois transitella)、條麥蛾屬(Anarsia spp.)、夜蛾屬(Anticarsia spp.)(例如:大豆夜蛾(Anticarsia gemmatalis))、黃螟屬(Argyroploce spp.)、甘藍夜蛾(Barathra brassicae)、單帶弄蝶(Borbo cinnara)、棉葉穿孔潛蛾(Bucculatrix thurberiella)、松尺蠖(Bupalus piniarius)、夜蛾屬(Busseola spp.)、卷葉蛾屬(Cacoecia spp.)、茶細蛾(Caloptilia theivora)、煙捲葉蛾(Capua reticulana)、蘋果蠹蛾(Carpocapsa pomonella)、桃蛀果蛾(Carposina niponensis)、冬尺蛾(Cheimatobia brumata)、 螟屬(Chilo spp.)(例如:稻稈螟(Chilo plejadellus)、二化螟(Chilo suppressalis))、雲杉卷葉蛾屬(Choristoneura spp.)、葡萄果蠹蛾(Clysia ambiguella)、卷螟屬(Cnaphalocerus spp.)、稻縱捲葉野螟蛾(Cnaphalocrocis medinalis)、雲卷蛾屬(Cnephasia spp.)、細蛾屬(Conopomorpha spp.)、黑象甲屬(Conotrachelus spp.)、夜蛾屬(Copitarsia spp.)、小卷蛾屬(Cydia spp.)(例如:豆莢小卷蛾(Cydia nigricana)、蘋果蠹蛾(Cydia pomonella))、夜蛾(Dalaca noctuides)、野螟屬(Diaphania spp.)、小蔗螟(Diatraea saccharalis)、埃及金剛鑽屬(Earias spp.)、柑橘果蛾(Ecdytolopha aurantium)、南美玉米苗斑螟(Elasmopalpus lignosellus)、非洲莖螟(Eldana saccharina)、粉螟屬(Ephestia spp.)(例如:烟草粉螟(Ephestia elutella)、地中海斑螟(Ephestia kuehniella))、小卷蛾屬(Epinotia spp.)、蘋果飛蛾(Epiphyas postvittana)、螟蛾屬(Etiella spp.)、巧言蟲屬(Eulia spp.)、環針單紋卷蛾(Eupoecilia ambiguella)、毒蛾屬(Euproctis spp.)(例如:棕尾毒蛾(Euproctis chrysorrhoea))、切根蟲屬(Euxoa spp.)、褐夜蛾屬(Feltia spp.)、大蠟螟(Galleria mellonella)、潛葉細蛾屬(Gracillaria spp.)、小食心蟲屬(Grapholitha spp.)(例如:桃折心蟲(Grapholita molesta)、蘋小果蠹(Grapholita prunivora))、螟蛾屬(Hedylepta spp.)、夜蛾屬(Helicoverpa spp.)(例如:番茄夜蛾(Helicoverpa armigera)、玉米夜蛾(Helicoverpa zea))、棉鈴蟲屬(Heliothis spp.)(例如:綠棉鈴蟲(Heliothis virescens))、褐織夜蛾(Hofmannophila pseudospretella)、斑螟屬(Homoeosoma spp.)、卷葉蛾屬(Homona spp.)、櫻桃巢蛾(Hyponomeuta padella)、柿食心蟲(Kakivoria flavofasciata)、黏蟲屬(Laphygma spp.)、茄黃斑螟(Leucinodes orbonalis)、潛葉蛾屬(Leucoptera spp.)(例如:咖啡潛葉蛾(Leucoptera coffeella))、細蛾屬(Lithocolletis spp.)(例如:斑幕潛葉蛾(Lithocolletis blancardella)、綠果夜蛾(Lithophane antennata))、卷蛾屬 (Lobesia spp.)(例如:葡萄莓果飛蛾(Lobesia botrana))、豆白緣切根蟲(Loxagrotis albicosta)、毒蛾屬(Lymantria spp.)(例如:舞毒蛾(Lymantria dispar))、萊氏蛾屬(Lyonetia spp.)(例如:桃潛葉蛾(Lyonetia clerkella))、金龜(Malacosoma neustria)、豆莢螟(Maruca testulalis)、甘藍夜蛾(Mamstra brassicae)、暮眼蝶(Melanitis leda)、莖夜蛾屬(Mocis spp.)、穀蛾科(Monopis obviella)、東方黏蟲(Mythimna separate)、穀蛾(Nemapogon cloacellus)、水螟屬(Nymphula spp.)、扇頭蜱屬(Oiketicus spp.)、夜蛾屬(Oria spp.)、螟蛾屬(Orthaga spp.)、玉米螟屬(Ostrinia spp.)(例如:歐洲玉米螟(Ostrinia nubilalis))、橙足負泥蟲(Oulema melanopus)、稻負泥蟲(Oulema oryzae)、小眼夜蛾(Panolis flammea)、弄蝶屬(Parnara spp.)、紅鈴蟲屬(Pectinophora spp.)(例如:棉紅鈴蟲(Pectinophora gossypiella))、潛葉蛾屬(Perileucoptera spp.)、蠹蛾屬(Phthorimaea spp.)(例如:馬鈴薯塊莖蛾(Phthorimaea operculella))、橘葉潛蛾(Phyllocnistis citrella)、細蛾屬(Phyllonorycter spp.)(例如:斑幕潛葉(Phyllonorycter blancardella)、山楂潛葉蛾(Phyllonorycter crataegella))、粉蝶屬(Pieris spp.)(例如:紋白蝶(Pieris rapae))、荷蘭石竹小卷蛾(Platynota stultana)、印度穀斑螟(Plodia interpunctella)、擬尺蠖屬(Plusia spp.)、小菜蛾(Plutella xylostella)(=小菜蛾(Plutella maculipennis))、巢蛾屬(Prays spp.)、黏蟲屬(Prodenia spp.)、天蛾屬(Protoparce spp.)、黏蟲屬(Pseudaletia spp.)(例如:星黏蟲(Pseudaletia unipuncta))、大豆夜蛾(Pseudoplusia includens)、野螟(Pyrausta nubilalis)、薄荷灰夜蛾(Rachiplusia nu)、三化螟屬(Schoenobius spp.)(例如:三化螟(Schoenobius bipunctifer))、白禾螟蛾屬(Scirpophaga spp.)(例如:稻白螟(Scirpophaga innotata))、黃地老虎(Scotia segetum)、蛀莖夜蛾屬(Sesamia spp.)(例如:稻蛀莖夜蛾(Sesamia inferens))、卷葉蛾屬(Sparganothis spp.)、 斜紋夜蛾屬(Spodoptera spp.)(例如:斜紋夜蛾(Spodoptera eradiana)、甜菜夜蛾(Spodoptera exigua)、草地斜紋夜蛾(Spodoptera frugiperda)、灰翅夜蛾(Spodoptera praefica))、舉肢蛾屬(Stathmopoda spp.)、潛葉蟲(Stomopteryx subsecivella)、透翅蛾屬(Synanthedon spp.)、馬鈴薯塊莖蛾(Tecia solanivora)、幹煞夜蛾(Thermesia gemmatalis)、軟木長角蛾(Tinea cloacella)、網衣蛾(Tinea pellionella)、袋穀蛾(Tineola bisselliella)、櫟綠卷葉蛾屬(Tortrix spp.)、毛氈衣蛾(Trichophaga tapetzella)、夜蛾屬(Trichoplusia spp.)(例如:粉紋夜蛾(Trichoplusia ni))、三化螟(Tryporyza incertulas)、番茄斑潛蠅(Tuta absoluta)、小灰蝶屬(Virachola spp.);直翅目(Orthoptera)或跳躍亞目(Saltatoria),例如:家蟋蟀(Acheta domesticus)、草蜢屬(Dichroplus spp.)、螻蛄屬(Gryllotalpa spp.)(例如:歐洲螻蛄(Gryllotalpa gryllotalpa))、蔗蝗屬(Hieroglyphus spp.)、飛蝗屬(Locusta spp.)(例如:東亞飛蝗(Locusta migratoria))、負蝗屬(Melanoplus spp.)(例如:赤地蚱蜢(Melanoplus devastator))、烏蘇裏擬寰螽(Paratlanticus ussuriensis)、群居蚱蜢(Schistocerca gregaria);毛蝨目(Phthiraptera),例如:毛蝨屬(Damalinia spp.)、豬蝨屬(Haematopinus spp.)、犬蝨屬(Linognathus spp.)、人蝨屬(Pediculus spp.)、長角羽蝨(Phylloera vastatrix)、陰蝨(Pthirus pubis)、獸鳥蝨屬(Trichodectes spp.);囓蟲目(Psocoptera),例如:齧蟲屬(Lepinatus spp.)、書蝨屬(Liposcelis spp.);蚤目(Siphonaptera),例如:鼠蚤屬(Ceratophyllus spp.)、櫛頭蚤屬(Ctenocephalides spp.)(例如:狗櫛頭蚤(Ctenocephalides canis)、貓櫛頭蚤(Ctenocephalides felis))、人蚤(Pulex irritans)、穿皮潛蚤(Tunga penetrans)、東方鼠蚤(Xenopsylla cheopis); 纓翅目(Thysanoptera),例如:玉米黃薊馬(Anaphothrips obscurus)、稻薊馬(Baliothrips biformis)、葡萄德薊馬(Drepanothris reuteri)、黃帶薊馬(Enneothrips fIavens)、花薊馬屬(Frankliniella spp.)(例如:煙褐花薊馬(Frankliniella fusca)、西方花薊馬(Frankliniella occidentalis)、梳缺花薊馬(Frankliniella schultzei)、麥花薊馬(Frankliniella tritici)、越桔花薊馬(Frankliniella vaccinii)、威廉期花薊馬(Frankliniella williamsi))、網薊馬屬(Heliothrips spp.)、溫室條籬薊馬(Hercinothrips femoralis)、葡萄薊馬(Rhipiphorothrips cruentatus)、硬薊馬屬(Scirtothrips spp.)、薊馬(Taeniothrips cardamoni)、薊馬屬(Thrips spp.)(例如:南黃薊馬(Thrips palmi)、蔥薊馬(Thrips tabaci));纓尾目(Zygentoma)(=總尾目(Thysanura)),例如:櫛衣魚屬(Ctenolepisma spp.)、西洋衣魚(Lepisma saccharina)、盜火蟲(Lepismodes inquilinus)、斑衣魚(Thermobia domestica);結合綱(Symphyla),例如:蚰蜒屬(Scutigerella spp.),例如:白松蟲(Scutigerella immaculata);軟體動物門(Mollusca),特定言之雙殼綱(Bivalva)之害蟲,例如:飾貝屬(Dreissena spp.)及腹足綱(Gastropoda),例如:蛞蝓屬(Arion spp.)(例如:紅蛞蝓(Arion ater rufus))、紅扁蜷屬(Biomphalaria spp.)、泡螺屬(Bulinus spp.)、灰蛞蝓屬(Deroceras spp.)(例如:黏液蛞蝓(Deroceras leave))、土蝸螺屬(Galba spp.)、椎實螺屬(Lymnaea spp.)、釘螺屬(Oncomelania spp.)、福壽螺屬(Pomacea spp.)、琥珀螺屬(Succinea spp.);來自扁形動物門(Platyhelminthes)與線蟲動物門(Nematoda)之動物與人類寄生蟲,例如:肺線蟲屬(Aelurostrongylus spp.)、裂口線蟲屬(Amidostomum spp.)、鉤蟲屬(Ancylostoma spp.)、住血線蟲屬(Angiostrongylus spp.)、海獸胃線蟲屬(Anisakis spp.)、裸頭絛蟲屬(Anoplocephala spp.)、蛔蟲屬(Ascaris spp.)、禽蛔屬(Ascaridia spp.)、貝利蛔蟲屬(Baylisascaris spp.)、布魯線蟲屬(Brugia spp.)、仰口線蟲屬(Bunostomum spp.)、毛細線蟲屬(Capillaria spp.)、腸線蟲屬(Chabertia spp.)、支澤吸蟲屬(Clonorchis spp.)、古柏線蟲屬(Cooperia spp.)、環體線蟲屬(Crenosoma spp.)、節蟲屬(Cyathostoma spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、網尾線蟲屬(Dictyocaulus spp.)、二葉槽蟲屬(Diphyllobothrium spp.)、瓜實絛蟲屬(Dipylidium spp.)、血直絲蟲屬(Dirofilaria spp.)、龍線蟲屬(Dracunculus spp.)、球絛蟲屬(Echinococcus spp.)、棘口吸蟲屬(Echinostoma spp.)、蟯蟲屬(Enterobius spp.)、優鞘線蟲屬(Eucoleus spp.)、吸蟲屬(Faciola spp.)、擬片形吸蟲屬(Fascioloides spp.)、薑片蟲屬(Fasciolopsis spp.)、類絲線蟲屬(Filaroides spp.)、筒線蟲屬(Gongylonema spp.)、三代蟲屬(Gyrodactylus spp.)、馬胃線蟲屬(Habronema spp.)、血矛線蟲屬(Haemonchus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、異刺線蟲屬(Heterakis spp.)、膜殼絛蟲屬(Hymenolepis spp.)、下圓線蟲屬(Hyostrongylus spp.)、光絲蟲屬(Litomosoides spp.)、羅阿絲蟲屬(Loa spp.)、後圓線蟲屬(Metastrongylus spp.)、次睾吸蟲屬(Metorchis spp.)、中殖孔屬絛蟲屬(Mesocestoides spp.)、莫尼茨絛蟲屬(Moniezia spp.)、繆勒線蟲屬(Muellerius spp.)、鉤蟲屬(Necator spp.)、細頸線蟲屬(Nematodirus spp.)、日圓線蟲屬(Nippostrongylus spp.)、結線蟲屬(Oesophagostomum spp.)、壺肛線蟲屬(Ollulanus spp.)、盤尾線蟲(Onchocerca spp.)、後睪吸蟲屬(Opisthorchis spp.)、奧斯勒絲蟲屬(Oslerus spp.)、胃絲蟲屬(Ostertagia spp.)、尖尾線蟲屬(Oxynris spp.)、毛細線蟲屬(Paracapillaria spp.)、類絲蟲屬(Parafilaria spp.)、並殖吸蟲屬(Paragonimus spp.)、雙口吸蟲屬 (Paramphistomum spp.)、副裸頭絛蟲屬(Paranoplocephala spp.)、副蛔屬(Parascaris spp.)、栓尾線蟲屬(Passalurus spp.)、原圓線蟲屬(Protostrongylus spp.)、血吸蟲屬(Schistosoma spp.)、絲狀線蟲屬(Setaria spp.)、旋尾線蟲屬(Spirocerca spp.)、冠絲蟲屬(Stephanofilaria spp.)、冠尾線蟲屬(Stephanurus spp.)、糞類圓線蟲屬(Strongyloides spp.)、圓線蟲屬(Strongylus spp.)、比翼線蟲屬(Syngamus spp.)、帶絛蟲(Taenia spp.)、牛胃絲蟲屬(Teladorsagia spp.)、吸吮線蟲屬(Thelazia spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、旋毛線蟲屬(Trichinella spp.)、毛畢屬(Trichobilharzia spp.)、毛圓線蟲屬(Trichostrongylus spp.)、鞭蟲(Trichuris spp.)、彎口線蟲屬(Uncinaria spp.)、吳策線蟲屬(Wuchereria spp.);來自線蟲動物門(Nematoda)之植物害蟲,亦即植物寄生性線蟲,特定言之:墊刃線蟲屬(Aglenchus spp.)(例如:居農野外墊刃線蟲(Aglenchus agricola))、粒癭線蟲屬(Anguina spp.)(例如:小麥粒癭線蟲(Anguina tritici))、滑刃線蟲屬(Aphelenchoides spp.)(例如:花生滑刃線蟲(Aphelenchoides arachidis)、葉芽滑刃線蟲(Aphelenchoides fragariae))、刺線蟲屬(Belonolaimus spp.)(例如:豌豆刺線蟲(Belonolaimus gracilis)、長尾刺線蟲(Belonolaimus longicaudatus)、諾頓刺線蟲(Belonolaimus nortoni))、傘滑刃線蟲屬(Bursaphelenchus spp.)(例如:椰子紅環腐線蟲(Bursaphelenchus cocophilus)、傘滑刃線蟲(Bursaphelenchus eremus)、松材線蟲(Bursaphelenchus xylophilus))、固著線蟲屬(Cacopaurus spp.)(例如:波斯固著線蟲(Cacopaurus pestis))、環紋線蟲屬(Criconemella spp.)(例如:彎曲環紋線蟲(Criconemella curvata)、環紋線蟲(Criconemella onoensis)、裝飾環紋線蟲(Criconemella ornata)、環紋線蟲(Criconemella rusium)、葡萄環紋線蟲(Criconemella xenoplax)(=環腐線蟲(Mesocriconema xenoplax))、小環線蟲屬 (Criconemoides spp.)(例如:弗尼亞小環線蟲(Criconemoides ferniae)、小環線蟲(Criconemoides onoense)、杯口小環線蟲(Criconemoides ornatum))、莖囊線蟲(Ditylenchus spp.)(例如:莖線蟲(Ditylenchus dipsaci))、錐線蟲屬(Dolichodorus spp.)、包囊線蟲屬(Globodera spp.)(例如:馬鈴薯白線蟲(Globodera pallida)、黃色馬鈴薯包囊線蟲(Globodera rostochiensis))、螺旋線蟲屬(Helicotylenchus spp.)(例如:雙宮螺旋線蟲(Helicotylenchus dihystera))、半鞘線蟲屬(Hemicriconemoides spp.)、鞘線蟲屬(Hemicycliophora spp.)、異皮線蟲屬(Heterodera spp.)(例如:禾穀異皮線蟲(Heterodera avenae)、大豆異皮線蟲(Heterodera glycines)、甜菜異皮線蟲(Heterodera schachtii))、紐帶線蟲屬(Hoplolaimus spp.)、長刺線蟲屬(Longidorus spp.)(例如:非洲長刺線蟲(Longidorus africanus))、根瘤線蟲屬(Meloidogyne spp.)(例如:奇特伍德根瘤線蟲(Meloidogyne chitwoodi)、法克斯根瘤線蟲(Meloidogyne fallax)、北方根瘤線蟲(Meloidogyne hapla)、南方根瘤線蟲(Meloidogyne incognita))、根瘤線蟲屬(Meloinema spp.)、假根瘤線蟲屬(Nacobbus spp.)、擬莖線蟲屬(Neotylenchus spp.)、擬滑刃線蟲屬(Paraphelenchus spp.)、擬毛刺線蟲屬(Paratrichodorus spp.)(例如:微小擬毛刺線蟲(Paratrichodorus minor))、短體線蟲屬(Pratylenchus spp.)(例如:穿刺短體線蟲(Pratylenchus penetrans))、假海矛線蟲屬(Pseudohalenchus spp.)、平滑墊刃線蟲屬(Psilenchus spp.)、胞囊線蟲屬(Punctodera spp.)、溝線蟲屬(Quinisulcius spp.)、穿孔線蟲屬(Radopholus spp.)(例如:柑橘穿孔線蟲(Radopholus citrophilus)、香蕉穿孔線蟲(Radopholus similis))、腎狀線蟲屬(Rotylenchulus spp.)、盤旋線蟲屬(Rotylenchus spp.)、螺旋線蟲屬(Scutellonema spp.)、粒線蟲屬(Subanguina spp.)、毛刺線蟲屬(Trichodorus spp.)(例如:鈍毛刺線蟲(Trichodorus obtusus)、原始毛刺線蟲(Trichodorus primitivus))、矮化線蟲屬(Tylenchorhynchus spp.)(例如:飾環矮化線蟲(Tylenchorhynchus annulatus))、半穿刺線蟲屬(Tylenchulus spp.)(例如:柑橘半穿刺線蟲(Tylenchulus semipenetrans))、劍線蟲屬(Xiphinema spp.)(例如:標準劍線蟲(Xiphinema index));此外,亦可控制原生動物亞界(Protozoa),球蟲目(Coccidia),例如:艾美球蟲屬(Eimeria spp.)。 The compound of formula (I) has good plant tolerance, good toxicity to warm-blooded animals and good environmental compatibility. It is suitable for protecting plants and plant organs against biotic and abiotic stresses, increasing yield and improving harvest. Material quality, and control of animal pests, especially in the fields of agriculture, horticulture, animal husbandry, aquaculture, forests, gardens and leisure facilities, insects, spiders, worms, nematodes and mollusks, can be used to protect stock products and materials, and In the field of health. It is preferably used as a pesticide. It is effective against normal sensitive and resistant species and against all or individual stages of development. The above pests include: Arthropoda, especially arachnid (Arachnida) pests, for example: Acarus spp. ) (eg: Acarus siro), Aceria kuko, Aceria sheldoni, Aculops spp. ), Acanthope (Aculus spp. ) (for example: Aculus fockeui, Aculus schlechtendali), Amblyomma spp. ), Amphitetrany sinensis (Amphitetrany sinensis), Argas spp. ), Bovineus spp. ), Red genus (Brevipalpus spp. (eg: Brevipalpus phoenicis), Bryobia graminum, Bryobia praetiosa, Centruroides spp. ), genus (Chorioptes spp. ), Dermanyssus gallinae, Dermatophagoides pteronyssinus, Dermatophagoides farinae, Dermacentor spp. ), Eotetranychus spp. ) (eg: Eotetranychus hicoriae), Epipirerus pyri, Eutetranychus spp. ) (eg Eutetranychus banksi), Eriophyes spp. ) (eg Eriophyes pyri), Glycyphagus domesticus, Halotydeus destructor, Hemitarsonemus spp. ) (for example: tea dust mites) (Hemitarsonemus latus) (= Polyphagotarsonemus latus), Hyologma spp. ), hard genus (Ixodes spp. ), the genus Arachnid (Latrodectus spp. ), Loxosceles spp. ), autumn scorpion (Neutrombicula autumnalis), Nuphersa genus, genus Oligonychus spp. (eg: Oligonychus coniferarum, Oligonychus ilicis, Oligonychus indicus, Oligonychus mangiferus, Oligonychus pratensis, Oligonychus punicae, Oligonychus yothersi, Ornithodorus spp. ), the giant genus Robinia (Ornithonyssus spp. ), Red spider genus (Panonychus spp. ) (for example: Panonychus citri (= Metatetranychus citri), Panonychus ulmi (=Metatetranychus ulmi), Phyllocoptruta oleivora ), succulent leafhopper (Platytetranychus multidigituli), Polyphagotarsonemus latus, Psoroptes spp. ), Rhipicephalus spp. ), Rhizoglyphus spp. ), human genus (Sarcoptes spp. ), Scorpio maurus, Stenotarsonemus spp. ), Steneotarsonemus spinki, Tarsonemus spp. ) (for example: Tarsonemus confusus, Tarsonemus pallidus), Tetranychus spp. (eg: Tetranychus canadensis, Tetranychus cinnabarinus, Tetranychus turkestani, Tetranychus urticae), Trimculcula alfreddugesi, Vaejovis Spp. ), Vasates lycopersici; Chilopoda, for example: Geophilus spp. ), genus (Scutigera spp. ); Collembola or Collembola, for example: Onychiurus armatus; Sminthurus viridis; Diplopoda, for example: Blanciulus guttulatus; Insecta, for example: Blattodea, for example: Blatta orientalis, Blattella asahinai, Germany Blattella germanica, Leucophaea maderae, Panchlora spp. ), Pacoblatta spp. ), family genus (Periplaneta spp. (for example: Periplaneta americana, Periplaneta australasiae), Supella longipalpa, Coleoptera, for example: Acalymma vittatum, Acanthoscelides Obtectus), Adoretus spp. ), Agelastica alni, Agitoes spp. (eg: Agriotes linneatus, Agriotes mancus), Alphitobius diaperinus, Amphimallon solstitialis, Anobium punctatum, and beetle Genus (Anoplophora spp. ), cotton boll weevil (Anthonomus spp. ) (for example: Anthonomus grandis), Anthrenus spp. ), pear genus (Apion spp. ), Sugarcane genus (Apogonia spp. ), Atomaria spp. ) (eg, Atomaria linearis), Attagenus spp. ), Baris caerulescens, Bruchidius obtectus, Bruuchus spp. ) (for example: Bruchus pisorum, Bruchus rufimanus), Cassida spp. ), soybean leaf (Cerotoma trifurcate), genus (Ceuthorrhynchus spp. (eg: Ceutorrhynchus assimilis, Ceutorrhynchus quadridens, Ceutorrhynchus rapae), Chaetocnema spp. (eg: Chaetocnema confinis, Chaetocnema denticulata, Chaetocnema ectypa), Cleonus mendicus, Conoderus spp. ), bulbous genus (Cosmopolites spp. ) (eg: Cosmopolites sordidus), Costelytra zealandica, Ctenicera Spp. ), genus Curculio spp. ) (eg: Curculio caryae, Curculio caryatrypes, Curculio obtusus, Curculio sayi), Cryptolestes ferrugineus, horn chest Cryptolestes pusillus, Cryptorhynchus lapathi, Cryptorhynchus mangiferae, Cylindrocopturus spp. ), Cylindrocopturus adspersus, Cylindrocopturus furnissi, Dermestes spp. ), A. genus (Diabrotica spp. (eg: Diabrotica balteata, Diabrotica barberi, Diabrotica undecimpunctata howardi, Diabrotica undecimpunctata undecimpunctata, Diabrotica virgifera Virgifera), Diabrotica virgifera zeae, Dichocrocis spp. ), rice iron beetle (Dicladispa armigera), Argentine genus (Diloboderus spp. ), Ladybug (Epilachna spp. ) (eg, Epilachna borealis, Epilachna varivestis), Epitrix spp. (eg: Epitrix cucumeris, Epitrix fuscula, Epitrix hirtipennis, Epitrix subcrinita, Epitrix tuberis), Botrytis ( Faustinus spp. ), Gibbium psylloides, Gnathocerus cornutus, Hellula undalis, Heteronychus arator, Heteronyx spp. ), Hylamorpha elegans, Hylotrupes bajulus, Hypera postica, Hypomeces squamosus, Hypothenemus spp. (eg: Hypothenemus hampei, Hypothenemus obscurus, Hypothenemus pubescens), Lachnosterna consanguinea, Lasioderma serricorne, Long Shougu (Latheticus oryzae), Lathridius spp. ), negative genus (Lema spp. ), potato beetle (Leptinotarsa decemlineata), leaf Moth (Leucoptera spp. ) (eg: Leucoptera coffeella), Lisorhoptrus oryzophilus, Lixus spp. ), Luperomorpha xanthodera, Luperodes spp. ), Lycium spp. ), American genus (Megascelis spp. ), the genus of the genus Melanotus spp. (eg: Melanotus longulus oregonensis), Meligethes aeneus, Melonontha spp. ) (eg: Melonontha melolontha), M. genus (Migdolus spp. ), the genus of the genus Monochamus spp. ), Napactus xanthographus, Necrobia spp. ), Niptus hololeucus, Oryctes rhinoceros, Oryzaephilus surinamensis, Oryzaphagus oryzae, Otiorrhynchus spp. (eg: Otiorhynchus cribricollis, Otiorhynchus ligustici, Otiorhynchus ovatus, Otiorhynchus rugosostriarus, Otiorhynchus sulcatus), Silver-pointed tortoise (Oxycetonia jucunda), Phaedon cochleariae, Phyllophaga spp. ), Phyllophaga helleri, Phyllotreta spp. ) (eg: Phyllotreta armoraciae, Phyllotreta pusilla, Phyllotreta ramosa, Phyllotreta striolata), Popillia japonica, small Genus (Premnotrypes spp. ), Prostephanus truncatus, Psylliodes spp. ) (eg Psylliodes affinis, Psylliodes chrysocephala, Psylliodes punctulata), Ptinus spp. ), Rhizobius ventralis, Rhizopertha dominica, Sitophilus spp. (eg: Sitophilus granarius, Sitophilus linearis, Sitophilus oryzae, Sitophilus zeamais), Sphenophorus spp. ), Stembium paniceum, Stemichus spp. ) (eg: bean stem image (Sternechus Paludatus)), scapula (Symphyletes spp. ), the genus of the genus (Tanymecus spp. (eg: Tanymecus dilaticollis, Tanymecus indicus, Tanymecus palliates), Tenebrio molitor, Tenebrioides mauretanicus, Tribolium spp . (eg: Tribolium audax, Tribolium castaneum, Tribolium confusum), Trojanderma spp. ), the genus of the genus (Tychius spp. ), Xylotrechus spp. ), the genus of the genus (Zabrus spp. ) (for example: Zabrus tenebrioides); Diptera, for example: Aedes spp. (eg: Aedes aegypti, Aedes albopictus, Aedes sticticus, Aedes vexans), Agromyza spp. ) (eg Agromyza frontella, Agromyza parvicornis), Anastrepha spp. ), Anopheles spp. (eg: Anopheles quadrimaculatus, Anopheles gambiae), Asphondylia spp. ), the fruit fly (Bactrocera spp. (eg: Bactrocera cucurbitae, Bactrocera dorsalis, Bactrocera oleae), Bibio hortulanus, Calliphora erythrocephala, Calliphora vicina , Mediterranean fruit fly (Ceratitis capitata), Chironomus spp. ) Chrysomyia spp. ), genus Chrysops spp. ), Chrysozona pluvialis, Cochliomyia spp. ), Contarinia spp. (eg: Contarinia johnsoni, Contarinia nasturtii, Contarinia pyrivora, Contarinia schulzi, Contarinia sorghicola, Contarinia) Tritici)), Cordylobia anthropophaga, Cricotopus sylvestris, Culex spp. ) (eg Culex pipiens, Culex quinquefasciatus), Culicoides spp. ), Culexeta spp. Fly Genus (Cuterebra spp. ), Drosophila (Dacus oleae), Aedes (Dasyneura spp. (eg: Dasineura brassicae), Delia spp. (eg, Delia antiqua, Delia coarctata, Delia florilega, Delia platura, Delia radicum), Dermatobia hominis, Drosophila spp. ) (eg Drosphila melanogaster, Drosphila suzukii), Echinocnemus spp. ), genus Flyfly (Fannia spp. ), the genus of the genus Gastrophilus spp. ), Glossina spp. ), genus Haematopota spp. ), genus Hydrellia spp. ), Rice leaf fly (Hydrellia griseola), Hydrangea (Hylemyia spp. ), the genus Hypobesca spp. ), the genus Hypoderma spp. ), Liriomyza spp. (eg: Liriomyza brassicae, Liriomyza huidobrensis, Liriomyza sativae), Lucilia spp. ) (eg Lucilia cuprina), Lutzomyia spp. ), the genus Mosquito (Mansonia spp. ), Musca spp. ) (eg Musca domestica, Musca domestica vicina), Oestro spp. ), Swedish fly (Oscinella frit), Chironus (Paratanytarsus spp. ), Chiarozoa (Paralauterborniella subcincta), Lepidoptera (Pegomya spp. (eg Pegomya betae, Pegomya hyoscyami, Pegomya rubivora), Phlebotomus spp. ), the genus Hypora (Phorbia spp. ), the genus Phormia spp. ), Piophila casei, Prodiplosis spp. ), Psila rosae, Rhagoletis spp. (eg, Rhagoletis cingulata, Rhagoletis completa, Rhagoletis fausta, Rhagoletis indifferens, Rhodoletis indifferens, Rhagoletis mendax ), Rhagoletis pomonella, Sarcophaga spp. ), genus (Simulium spp. ) (for example: Simulium meridionale), Stomoxys spp. ), genus (Tabanus spp. Straight (Tetanops spp. ), the genus of the genus (Tipula spp. (eg: Tipula paludosa, Tipula simplex); Hemiptera, such as: Acizzia acaciaebaileyanae, Acizzia dodonaeae, hibiscus ( Acizzia uncatoides), Acrida turrita, Acyrthosipon spp. ) (eg: Acyrthosiphon pisum), Acrogonia spp. ), Aeneolamia genus, Aragonoscena spp. ), Aleyrodes proletella, Aleurolobus barodensis, Aleurothrixus floccosus, Durian durian (Allocaridara malayensis), and genus Amrasca spp. (eg: Amrasca bigutulla, Amrasca devastans), Anuraphis cardui, Aonidiella spp. (eg: Aonidiella aurantii, Aonidiella citrina, Aonidiella inornata), Aphanostigma piri, Aphis (Aphis) Spp. (eg: Aphis citricola, Aphis craccivora, Aphis fabae, Aphis forbesi, Aphis glycines, Aphis gossypii, often Aphis hederae, Aphis illinoisensis, Aphis middletoni, Aphis nasturtii, Aphis nerii, Aphis pomi, Spiraea (Aphis) Spiraecola), Aphis viburniphila, Arboridia apicalis, Arytainilla spp. ), Aspidiella spp. ), the round shield genus (Aspidiotus spp. (eg: Aspidiotus nerii), Atanus genus, Aulacorthum solani, Bemisia tabaci, Blastopsylla occidentalis, Boreioglycaspis melaleucae, light tube Brachycaudus helichrysi, Brachycolus spp. ), Brasserie (Brevicoryne brassicae), Liriodendron (Cacopsylla spp. ) (eg: pear yellow hibiscus) (Cacopsylla pyricola)), Calligypona marginata, Carneocephala fulgida, Ceratovacuna lanigera, Cercopidae, Ceroplastes spp. ), Chaetosiphon fragaefolii, Chionaspis tegalensis, Chlorita onukii, Chondracris rosea, Chromaphis juglandicola, Chrysomphalus Ficus), Cicadulina mbila, Coccomytilus halli, Coccus spp. (eg: Coccus hesperidum, Coccus longulus, Coccus pseudomagnoliarum, Coccus viridis), Cryptomyzus ribis, Cryptoneossa Genus, Compressed genus (Ctenarytaina spp. ), Dalbulus spp. ), Dialeurodes citri, Diaphorina citri, Diaspis spp. ), Drosicha spp. ), Stem Aphid (Dysaphis spp. ) (for example: Dysaphis apiifolia, Dysaphis plantaginea, Dysaphis tulipae), Dysmicoccus spp. ), small green leaf genus (Empoasca spp. (eg: Empoasca abrupta, Emppoasca fabae, Emppoasca maligna, Emppoasca solana, Emppoasca stevensi) Genus (Eriosoma spp. (eg: Eriosoma americanum, Eriosoma lanigerum, Eriosoma pyricola), Erythroneura spp. ), Lemon Eucalyptus (Eucalyptolyma spp. ), brown wood (Euphyllura spp. ), Euscelis bilobatus, Ferrisia spp. ), coffee powder (Geococcus coffeae), hibiscus (Glycaspis spp. ), Heteropsylla cubana, Heteropsylla spinulosa, Homalodisca coagulata, Hyalopterus arundinis, Hyalopterus pruni, blown cotton Genus (Icerya spp. ) (eg, Icerya purchasi), Idiocerus spp. ), green leaves Genus (Idioscopus spp. ), Laodelphax striatellus, Lecanium spp. ) (eg Lecanium corni (Parthenolecanium corni), Lepidosaphes spp. ) (eg: Lepidosaphes ulmi), Lipaphis erysimi, Lycorma delicatula, Macrosiphum spp. (eg: Macrosiphum euphorbiae, Macrosiphum lilii, Macrosiphum rosae), Macrosteles facifrons, Mahanarva spp. ), Melanaphis sacchari, Metcalfiella, Metcalfa pruinosa, Metopolophium dirhodum, Monellia costalis, Monelliopsis pecanis, peach aphid Genus (Myzus spp. (eg: Myzus ascalonicus, Myzus cerasi, Myzus ligustri, Myzus ornatus, Myzus persicae, Tobacco) Zu (Myzus nicotianae)), lettuce 蚜 (Nasonovia ribisnigri), genus Nephotettix spp. (eg: Nephotettix cincticeps, Nephotettix nigropictus), Nilaparvata lugens, Oncometopia, Orthezia praelonga, Oxya chinensis ), Pachypsylla spp. ), Parabemisia myricae, Paratrioza spp. ) (eg: Paratrioza cockerelli), Parlatoria spp. ), 瘿 蚜 (Pemphigus spp. (eg: Pemphigus bursarius, Pemphigus populivenae), Peregrinus maidis, Phenacoccus spp. (eg: Phenacoccus madeirensis), Phloeomyzus passerinii, Phorodon humuli, Phylloxera spp. (eg: Phylloxera devastatrix, Phylloxera notabilis), Pinnaspis aspidistrae, Planococcus spp. ) (for example: Planococcus citri), Prosopidopsylla flava, pear-shaped cotton aphid (Protopulvinaria pyriformis), Pseudaulacaspis pentagona, Pseudococcus spp. (eg, Pseudococcus calceolariae, Pseudococcus comstocki, Pseudococcus longispinus, Pseudococcus maritimus, Pseudococcus viburni), Psyllopsis , hibiscus (Psylla spp. ) (for example: Psylla buxi, Psylla mali, Psylla pyri), Pteromalus spp. ), spider genus (Pyrilla spp. ), Round genus (Quadraspidiotus spp. (for example: Quadraspidiotus juglansregiae, Quadraspidiotus ostreaeformis, Quadraspidiotus perniciosus), Quesada gigas, Rastrococcus spp. ), Rhopalosiphum spp. (eg: Rhopalosiphum maidis, Rhopalosiphum oxyacanthae, Rhopalosiphum padi, Rhopalosiphum rufiabdominale), Saissetia spp. (eg: Saissetia coffeae, Saissetia miranda, Saissetia neglecta, Saissetia oleae), Scaphoides titanus, Schizaphis graminum, Shield 蚧Selenaspidus articulatus), Sitobion avenae, and Sagata spp. ), Sogatella furcifera, Sogatodes spp. ), Stictocephala festina, Siphoninus phillyreae, Tenalaphara malayensis, Tetragonocephela, Tinocallis caryaefoliae, Tomaspis spp. ), the genus of the genus (Toxoptera spp. ) (eg: Toxoptera aurantii, Toxoptera citricidus), greenhouse whitefly (Trialeurodes vaporariorm), hibiscus (Trioza spp. ) (eg Trioza diospyri), Typhlocyba spp. ), Shield genus (Unaspis spp. ), Vineus vitifolii, Zygina spp. ); Heteroptera, for example: Anasa tristis, Mantis genus Antestiopsis Spp. ), Red genus (Boisea spp. ), genus Blissus spp. ), genus Clolocoris spp. ), Campylomma livida, two-tailed genus (Cavelerius spp. ), bedbug (Cimex spp. (eg: Cimex adjunctus, Cimex hemipterus, Cimex lectularius, Cimex pilosellus), Collaria spp. ), Creontiades dilutus, Dasynus piperis, Dielops furcatus, Diconocoris hewetti, Dysdercus spp. ), skunk genus (Euschistus spp. (eg: Euschistus heros, Euschistus servus, Euschistus tristigmus, Euschistus variolarius), Eurygaster spp. ), Halyomorpha halys, Heliopeltis spp. ), Horbians nobilellus, Leptocorisa spp. ), Leptocorisa varicornis, Leptoglossus occidentalis, Leptoglossus phyllopus, Lygocoris spp. ) (for example: Lygocoris pabulinus), Lygus spp. (eg: Lygus elisus, Lygus hesperus, Lygus lineolaris), Macropes excavatus, Monalonion atratum, Green genus (Nezara spp. ) (eg: Nezara viridula), Oebalus spp. ), the proposed pest (Piesma quadrata), the genus (Pezodorus spp. ) (for example: Piezodorus guildinii), Psallus spp. ), Pearudacysta persea, Rhodonius spp. ), Sahlbergella singularis, Scaptocoris castanea, Scotinophora spp. ), Stephanitis nashi, and Tibraca spp. ), Tricusoma spp. ); Hymenoptera, for example: Acromyrmex spp. ), Athalia spp. ) (for example: Athalia rosae), Atta spp. ), Dipterus spp. ) (eg: Diprion similis), Hormone (Hoplocampa) Spp. ) (eg: Hoplocampa cookei, Hoplocampa testudinea), genus (Lasius spp. ), Argentine ants (Linepithema humile), kitchen ants (Monomorium pharaonis), tree genus (Sirex spp. ), invasive red fire ant (Solenopsis invicta), acid odorant genus ((Tapinoma spp. ), tree bee (Urocerus spp. ), Vespa (Vespa spp. ) (for example: Vespa crabro), Xeris spp. Isopoda, for example: Armadillidium vulgare, Oniscus asellus, Porcellio scaber; Isoptera, for example: Coptotermes spp. ) (for example: Coptotermes formosanus), termites (Cornitermes cumulans), and genus Quyptotermes spp. ), Termite genus (Incisitermes spp. ), sugar termites (Microtermes obesi), termite genus (Odontotermes spp. ), termite genus (Reticulitermes spp. (for example: Reticulitermes flavipes, Reticulitermes hesperus); Lepidoptera, for example: Achroia grisella, Acronicta major, leaf curl Moth (Adoxophyes spp. ) (eg: Adoxophyes orana), Aedia leucomelas, Agrotis spp. ) (eg Agrotis segetum, Agrotis ipsilon), Alabama spp. (eg: Alabama argillacea), Amyelois transitella, Anarsia spp. ), the genus Noctuidae (Anticarsia spp. ) (eg: Anticarsia gemmatalis), Astragalus spp. ), Barathra brassicae, Borbo cinnara, Bucculatrix thurberiella, Bupalus piniarius, Busseola spp. ), Cacoecia spp. ), Caloptilia theivora, Capua reticulana, Carpocapsa pomonella, Carposina niponensis, Cheimatobia brumata, Genus (Chilo spp. ) (eg Chilo plejadellus, Chilo suppressalis), Choristoneura spp. ), Clysia ambiguella, Cnaphalocerus spp. ), Cnaphalocrocis medinalis, Cnephasia spp. ), Conopomorpha spp. ), Black genus (Conotrachelus spp. ), Noctuidae (Copitarsia spp. ), Cydia spp. (eg: Cydia nigricana, Cydia pomonella), Dalaca noctuides, Diaphania spp. ), the small cane toad (Diatraea saccharalis), the Egyptian diamond genus (Earias spp. ), Ecdytolopha aurantium, Elasmopalpus lignosellus, Eldana saccharina, Ephestia spp. (eg: Ephestia elutella, Ephestia kuehniella), Epinotia spp. ), Apple moth (Epiphyas postvittana), Ethella spp. ), Elia spp. ), Eupoecilia ambiguella, Euproctis spp. ) (for example: Euproctis chrysorrhoea), cut genus (Euxoa spp. ), Heliothis sp. (Feltia spp. ), Galleria mellonella, Gracilla aria spp. ), the small heartworm (Grapholitha spp. ) (eg, Grapholita molesta, Grapholita prunivora), Hedylepta spp. ), Noctuidae (Helicoverpa spp. ) (eg: Helicoverpa armigera, Helicoverpa zea), Heliothis spp. ) (eg: Heliothis virescens), Hofmannophila pseudospretella, Homoeosoma spp. ), Homona spp. ), Hyponomeuta padella, Kakivoria flavofasciata, Laphygma spp. ), Leucinodes orbonalis, Leucoptera spp. ) (eg: Leucoptera coffeella), Lithocolletis spp. ) (for example: Lithocolletis blancardella, Lithophena antennata), Moth (Lobesia spp. ) (for example: Lobesia botrana), Loxaltis albicosta, Lymantria spp. ) (eg Lymantria dispar), Lyonetia spp. (eg, Lyonetia clerkella), Malacosoma neustria, Maruca testulalis, Mamstra brassicae, Melanitis leda, Mocis spp . ), Monopis obviella, Mythimna separate, Nemapogon cloacellus, Nymphula spp. ), genus Oiketicus spp. ), Noctuidae (Oria spp. ), Orthaga spp. ), corn genus (Ostrinia spp. (eg: Ostrinia nubilalis), Oulema melanopus, Oulema oryzae, Panolis flammea, Parnara spp. ), red bollworm (Pectinophora spp. ) (eg, Pectinophora gossypiella), Perileucoptera spp. ), genus Phthorimaea spp. ) (eg: Phthorimaea operculella), Phylcrostis citrella, Phyllonycter spp. (eg: Phyllonycter blancardella, Phyllonycter crataegella), Pieris spp. ) (eg, Pieris rapae), Platynota stultana, Plodia interpunctella, Plusia spp. ), Plutella xylostella (=Plutella maculipennis), P. rapae (Prays spp. ), the genus Mycobacterium (Prodenia spp. ), the genus Moth (Protoparce spp. ), genus Pseudaletia spp. (eg Pseudaletia unipuncta), Pseudoplusia includens, Pyrausta nubilalis, Rachiplusia nu, Schoenobius spp. ) (for example: Schoenobius bipunctifer), Scirpophaga spp. ) (eg: Scirpophaga innotata), Scotia segetum, Sesamia spp. ) (eg: Sesamia inferens), Sparganothis spp. ), Spodoptera spp. (eg, Spodoptera eradiana, Spodoptera exigua, Spodoptera frugiperda, Spodoptera praefica), Stathmopoda spp. ), Stomopteryx subsecivella, Synanthedon spp. ), Tecia solanivora, Thermesia gemmatalis, Tinea cloacella, Tinea pellionella, Tineola bisselliella, Liriodendron (Tortrix spp. ), Trichophaga tapetzella, Trichoplusia spp. ) (eg Trichoplusia ni), Tryporyza incertulas, Tuta absoluta, Virachola spp. ); Orthoptera or Saltatoria, for example: Acheta domesticus, Dichroplus spp. ), genus (Gryllotalpa spp. ) (eg: Gryllotalpa gryllotalpa), cane genus (Hieroglyphus spp. ), genus Locusta spp. ) (eg: Locusta migratoria), Melanoplus spp. (eg, Melanoplus devastator), Paratlanticus ussuriensis, Schistocerca gregaria, Phthiraptera, for example, Damalinia spp. ), genus Haematopinus spp. ), canine genus (Linognathus spp. ), human genus (Pediculus spp. ), Phylloera vastatrix, Pthirus pubis, Trichodectes spp. ); Psocoptera, for example: Lepinatus spp. ), the book genus (Liposcelis spp. ); Siphonaptera, for example: Ceratophyllus spp. ), Ctenocephalides spp. (eg: Ctenocephalides canis, Ctenocephalides felis), Pulex irritans, Tunga penetrans, Xenopsylla cheopis; Thysanoptera, for example: Anaphothrips obscurus, Baliothrips biformis, Drepanothris reuteri, Enneothrips fIavens, Frankliniella Spp. (eg: Frankliniella fusca, Frankliniella occidentalis, Frankliniella schultzei, Frankliniella tritici, Frankliniella vaccinii ), Frankliniella williamsi, and Heliothrips spp. ), Green Chestnut Horse (Hercinothrips femoralis), Rhipiphorothrips cruentatus, Hard Horse (Scirtothrips spp. ), eni马 (Taeniothrips cardamoni), 蓟 genus (Thrips spp. (eg: Thrips palmi, Thrips tabaci); Zygentoma (=Thysanura), for example: Ctenolepisma spp. ), Lepisma saccharina, Lepismodes inquilinus, Thermobia domestica; Symphyla, for example: Scutigerella spp. ), for example: Scutigerella immaculata; Mollusca, a pest of the specific bivalve (Bivalva), for example: Dreissena spp. And Gastropoda, for example: Arion spp. ) (for example: Arion ater rufus), Biomphalaria spp. ), genus Bulinus spp. ), genus genus (Deroceras spp. ) (eg: Deroceras leave), Galba spp. ), Lymnaea spp. ), Oncomelania spp. ), Pomacea spp. ), Amber snail (Succinea spp. ); animal and human parasites from the genus Platyhelminthes and Nematoda, for example: Aelurostrongylus spp. ), Nematodes (Amidostomum) Spp. ), Hookworm (Ancylostoma spp. ), live the nematode (Angiostrongylus spp. ), Sea genus Nematode (Anisakis spp. ), Anopheles genus (Anoplocephala spp. ), Ascaris spp. ), Avian genus (Ascaridia spp. ), Bailey's genus (Baylisascaris spp. ), Brugia spp. ), Anthurium genus (Bunostomum spp. ), Capillaria spp. ), Nematode (Chabertia spp. ), Clostridium spp. ), Cooperaria spp. ), C. elegans (Crenosoma spp. ), the genus Arthropod (Cyathostoma spp. ), Dicrocoelium spp. ), Dictyocaulus spp. ), Diphyllobothrium spp. ), genus Aphid (Dipylidium spp. ), Dirofilaria spp. ), Dracunculus spp. ), Echinococcus spp. ), Echinostoma spp. ), Aphid (Enterobius spp. ), Eucalyptus nematode (Eucoleus spp. ), genus genus (Faciola spp. ), Fascioloides spp. ), Ginger (Fasciolopsis spp. ), genus Nematode (Filaroides spp. ), genus Nematode (Gongylonema spp. ), the third generation of genus (Gyrodactylus spp. ), the genus Nematode (Habronema spp. ), Haemonchus spp. ), Heliconia genus (Heligmosomoides spp. ), Heterarias spp. ), membrane shell aphid (Hymenolepis spp. ), H. elegans (Hyostrongylus spp. ), Litoosoides spp. ), Loa spp. ), the genus Metastrongylus spp. ), the genus Paragonimus (Metorchis spp. ), the genus of the genus Aphis (Mesocestoides spp. ), Monizia spp. ), Muellerius spp. ), hookworm (Necator spp. ), Nematodirus spp. ), N. elegans (Nippostrongylus spp. ), Nematodes (Oesophagostomum spp. ), Anelidae (Ollulanus spp. ), Onchocerca spp. ), genus genus Opis genus (Opisthorchis spp. ), Oslerus spp. ), stomach genus (Ostertagia spp. ), Oxynris spp. ), Capreolus spp. ), Parafilaria spp. ), Paragonimus spp. Bismuth (Paramphistomum spp. ), Paranoplocephala spp. ), Parascaris spp. ), genus Nematode (Passalurus spp. ), Protostrongylus spp. ), Schistosoma spp. ), Filamentous genus (Setaria spp. ), Trichomonas (Spirocerca spp. ), Crown genus (Stephanofilaria spp. ), Coronaria genus (Stephanurus spp. ), the genus Strionics (Strongyloides spp. ), Round genus (Strongylus spp. ), genus Heteropharus (Syngamus spp. ), with aphids (Taenia spp. ), the genus Boletus (Teladorsagia spp. ), sucking nematode (Thelazia spp. ), Toxascaris spp. ), Toxoca serrata (Toxocara spp. ), Trichinella spp. ), Trichobilharzia spp. ), Trichostrongylus spp. ), whipworm (Trichuris spp. ), Uncinaria spp. ), Wucer nematode (Wuchereria spp. ); a plant pest from the Nematoda, also known as a plant-parasitic nematode, in particular: Agenchus spp. ) (eg: Aglenchus agricola), Anguina spp. ) (eg: Anguina tritici), Aphelenchoides spp. (eg: Aphelenchoides arachidis, Aphelenchoides fragariae), Nematodes (Belonolaimus spp. (eg: Belonolaimus gracilis, Belonolaimus longicaudatus, Belonolaimus nortoni), Bursaphelenchus spp. (eg: Bursaphelenchus cocophilus, Bursaphelenchus eremus, Bursaphelenchus xylophilus), Cacopaurus spp. ) (eg: Cacopaurus pestis), Criconemella spp. ) (eg: Criconemella curvata, Criconemella onoensis, Criconemella ornata, Criconemella rusium, Criconemella xenoplax (= ring rot) Nematode (Mesocriconema xenoplax), Nematode (Criconemoides spp. ) (eg, Criconemoides ferniae, Criconemoides onoense, Criconemoides ornatum), Ditylenchus spp. ) (eg Ditylenchus dipsaci), Conlichworm (Dolichodorus spp. ), cystic nematode (Globodera spp. (eg, Globodera pallida, Globodera rostochiensis), Helicopterus spp. ) (eg: Heliconicones dihystera), Hemicriconemoides spp. ), Nematode (Hemicycliophora spp. ), Heterodera spp. (eg: Heterodera avenae, Heterodera glycines, Heterodera schachtii), Hoplolaimus spp. ), Longidarus spp. ) (eg: Longidorus africanus), Meloidogyne spp. (eg: Meloidogyne chitwoodi, Meloidogyne fallax, Meloidogyne hapla, Meloidogyne incognita), Melolinema spp. ), pseudo-root nodule nematode (Nacobbus spp. ), Nematolinus spp. ), Paraphelenchus spp. ), Trichoderma genus (Paratrichodorus spp. ) (eg, Paratrichodorus minor), Pratylenchus spp. (eg puncdy nematode (Pratylenchus penetrans)), Pseudohalenchus spp. ), smoothing edge nematode (Psilenchus spp. ), cystic genus (Punctodera spp. ), Groats (Quinisulcius spp. ), perforated nematode (Radopholus spp. ) (eg Radopholus citrophilus, Radopholus similis), Rotylenchulus spp. ), the genus Nematode (Rotylenchus spp. ), Spirulina spp. ), the genus Trianguina spp. ), Trichoderma genus (Trichodorus spp. ) (eg Trichodorus obtusus, primitive burr nematode (Trichodorus) Primitivus)), dwarf nematode (Tylenchorhynchus spp. ) (for example: Tylenchorhynchus annulatus), Tylenchulus spp. ) (eg, Tylenchulus semipenetrans), Xiphinema spp. (for example: the standard Xiphinema index); in addition, it can also control the Protozoa, Coccidia, for example: Eimeria spp. ).
本文中,術語"線蟲"包括線蟲動物門(Nematoda)之所有物種及特定言之寄生在植物或真菌上(例如:來自滑刃目(Aphelenchida)、根瘤線蟲目(Meloidogyne)、墊刃目(Tylenchida)及其他之物種)或人類及動物上(例如:來自毛形亞目(Trichinellida)、墊刃目(Tylenchida)、小桿亞目(Rhabditina)及旋尾目(Spirurida)之物種)或在此等生物體中或生物體上造成傷害之寄生蟲物種,及其他寄生性蠕蟲。 As used herein, the term "nematode" includes all species of Nematoda and, in particular, plants or fungi (eg, from Aphelenchida, Meloidogyne, Tylenchida). And other species) or humans and animals (eg, species from Trichinellida, Tylenchida, Rhabditina, and Spirurida) or Parasitic species that cause damage in or on organisms, and other parasitic worms.
本文所說明用於保護作物之殺線蟲劑可以控制線蟲。 The nematicides used to protect crops described herein can control nematodes.
術語"控制線蟲"係指殺死線蟲或防止或阻礙其發展或生長,或防止或阻礙其滲透植物組織或吸食植物組織。 The term "controlling nematodes" refers to killing or preventing or hindering the development or growth of nematodes, or preventing or hindering their penetration into plant tissue or the consumption of plant tissues.
此時,化合物之效力之決定法係在經過式(I)化合物處理之植物、植株部分或經過處理之土壤與未經過處理之植物或植株部分或未經過處理之土壤(100%)之間,比較線蟲之死亡率、蟲癭之形成、囊胞之形成、每單位體積土壤之線蟲密度、每支根之線蟲密度、每單位體積土壤之線蟲卵數量、線蟲感染率。此時,與未經過處理之植物、植株部分或未經過處理之土壤比較,較佳係達成降低25-50%,更佳係降低51-79%及最佳係完全殺死或完全防止線蟲發展及生長,達降低80至100%。本文說明之線蟲控制亦包括控制線蟲繁殖(例如:囊胞與/或卵之發展)。式(I)化合物亦可用 於保持植物或動物健康,且其可用於治癒性、預防性或系統性控制線蟲。 In this case, the potency of the compound is determined between the plants treated with the compound of formula (I), the part of the plant or the treated soil and the untreated plant or part of the plant or the untreated soil (100%). Compare the mortality of nematodes, the formation of worms, the formation of cysts, the nematode density per unit volume of soil, the nematode density per root, the number of nematode eggs per unit volume of soil, and the nematode infection rate. At this time, compared with the untreated plants, part of the plants or the untreated soil, it is better to achieve a reduction of 25-50%, more preferably a reduction of 51-79% and the best system completely kills or completely prevents the development of nematodes. And growth, up to 80 to 100%. The nematode control described herein also includes control of nematode reproduction (eg, development of cysts and/or eggs). The compound of formula (I) can also be used To maintain the health of plants or animals, and it can be used for curative, prophylactic or systemic control of nematodes.
熟悉此相關技術者均習知決定線蟲死亡率、蟲癭形成、囊胞形成、每單位體積土壤之線蟲密度、每支根之線蟲密度、每單位體積土壤之線蟲卵數量、線蟲活動性之方法。 Those skilled in the art are familiar with determining nematode mortality, worm formation, cyst formation, nematode density per unit volume of soil, nematode density per root, number of nematode eggs per unit volume of soil, nematode activity. method.
使用式(I)化合物可保持植物健康,亦包括降低線蟲所造成之植物損害,及提高收成產量。 The use of the compound of formula (I) maintains plant health and also reduces plant damage caused by nematodes and increases yield.
本文中,術語"植物線蟲"係指包括所有會傷害植物之線蟲之植物線蟲。植物線蟲包括植物寄生性線蟲及土壤源性線蟲。植物寄生性線蟲包括(但不限於):體外寄生蟲,如:劍線蟲屬(Xiphinema spp.)、長刺線蟲屬(Longidorus spp.)及毛刺線蟲屬(Trichodorus spp.);半寄生蟲,如:鴕形線蟲屬(Tylenchulus spp.);遊走性體內寄生蟲,如:短體線蟲屬(Pratylenchus spp.)、穿孔線蟲屬(Radopholus spp.)及盾線蟲屬(Scutellonerna spp.);非遊走性寄生蟲,如:異皮線蟲屬(Heterodera spp.)、黃金線蟲屬(Globoderal spp.)及根瘤線蟲屬(Meloidogyne spp.),及莖與葉部之體內寄生蟲,如:莖線蟲屬(Ditylenchus spp.)、滑刃線蟲屬(Aphelenchoides spp.)及穿根線蟲屬(Hirshmaniella spp.)。特別傷害根部之寄生性土壤線蟲為例如:異皮線蟲屬(Heterodera)或黃金線蟲屬(Globodera)之包囊形成性線蟲,與/或根瘤線蟲屬(Meloidogyne)之根瘤線蟲。此等屬類之傷害性物種為例如:南方根瘤線蟲(Meloidogyne incognita)、大豆異皮線蟲(Heterodera glycines)(大豆包囊線蟲)、馬鈴薯白線蟲(Globodera pallida)及馬鈴薯黃金線蟲(Globodera rostochiensis)(黃色馬鈴薯包囊線蟲),本文所說明化合物可有效控制此等物種。然而,本文所說明化合物之用途絕未僅限於此等屬類或物種,而係亦可依相同方式沿用於其他線蟲。 As used herein, the term "plant nematode" refers to a plant nematode that includes all nematodes that can harm plants. Plant nematodes include plant-parasitic nematodes and soil-derived nematodes. Plant-parasitic nematodes include, but are not limited to, ectoparasites such as: Xiphinema spp., Longidorus spp., and Trichodorus spp.; semi-parasitic, such as : Tylenchulus spp.; migratory endoparasites, such as: Pratylinchus spp., Radoclus spp., and Scutellonerna spp.; non-walking Parasites such as Heterodera spp., Globoderal spp. and Meloidogyne spp., and endoparasites of stems and leaves, such as Ditylenchus Spp.), Aphelenchoides spp. and Hirshmaniella spp. Parasitic soil nematodes that particularly damage the roots are, for example, the cystic forming nematodes of Heterodera or Globodera, and/or the nodule nematodes of the genus Meloidogyne. Nociceptive species of these genus are, for example, Meloidogyne incognita, Heterodera glycines (soybean cyst nematode), Globodera pallida, and Globodera rostochiensis (Globodera rostochiensis) Yellow potato cyst nematode), the compounds described herein are effective in controlling these species. However, the use of the compounds described herein is by no means limited to such genus or species, but may be applied to other nematodes in the same manner.
植物線蟲包括(但不限於):例如:居農野外墊刃線蟲 (Aglenchus agricola)、小麥粒癭線蟲(Anguina tritici)、花生滑刃線蟲(Aphelenchoides arachidis)、草莓滑刃線蟲(Aphelenchoides fragaria),及滑刃線蟲屬(Aphelenchoides spp.)之莖與葉部體內寄生蟲;豌豆刺線蟲(Belonolaimus gracilis)、長尾刺線蟲(Belonolaimus longicaudatus)、諾頓刺線蟲(Belonolaimus nortoni)、椰子紅環腐線蟲(Bursaphelenchus cocophilus)、傘滑刃線蟲(Bursaphelenchus eremus)、松材線蟲(Bursaphelenchus xylophilus)及傘滑刃線蟲屬(Bursaphelenchus spp.);波斯固著線蟲(Cacopaurus pestis)、彎曲環紋線蟲(Criconemella curvata)、環紋線蟲(Criconemella onoensis)、裝飾環紋線蟲(Criconemella ornata)、環紋線蟲(Criconemella rusium)、葡萄環紋線蟲(Criconemella xenoplax)(=環腐線蟲(Mesocriconema xenoplax))及環紋線蟲屬(Criconemella spp.),弗尼亞小環線蟲(Criconemoides ferniae)、小環線蟲(Criconemoides onoense)、杯口小環線蟲(Criconemoides ornatum)及小環線蟲屬(Criconemoides spp.);馬鈴薯腐敗線蟲(Ditylenchus destructor)、莖線蟲(Ditylenchus dipsaci)、蘑菇莖線蟲(Ditylenchus myceliophagus)及莖線蟲屬(Ditylenchus spp.)之莖與葉部體內寄生蟲;異頭錐線蟲(Dolichodorus heterocephalus)、馬鈴薯白線蟲(Globodera pallida)(=馬鈴薯異皮線蟲(Heterodera pallida))、馬鈴薯黃金線蟲(Globodera rostochiensis)(黃色馬鈴薯包囊線蟲)、枯萎黃金線蟲(Globodera solanacearum)、菸草黃金線蟲(Globodera tabacum)、維吉尼亞黃金線蟲(Globodera virginia)及黃金線蟲屬(Globodera spp.)之非遊走性包囊形成性寄生蟲;雙角螺旋線蟲(Helicotylenchus digonicus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、赤色螺旋線蟲(Helicotylenchus erythrine)、多帶螺旋線蟲(Helicotylenchus multicinctus)、短小螺旋線蟲(Helicotylenchus nannus)、假強壯螺旋線蟲(Helicotylenchus pseudorobustus)及螺旋線蟲屬 (Helicotylenchus spp.);半鞘線蟲(Hemicriconemoides)、花生鞘線蟲(Hemicycliophora arenaria)、裸出鞘線蟲(Hemicycliophora nudata)、塔堅鞘線蟲(Hemicycliophora parvana)、禾穀異皮線蟲(Heterodera avenae)、十字花科異皮線蟲(Heterodera cruciferae)、大豆異皮線蟲(Heterodera glycines)(大豆包囊線蟲)、稻異皮線蟲(Heterodera oryzae)、甜菜異皮線蟲(Heterodera schachtii)、玉米異皮線蟲(Heterodera zeae)及異皮線蟲屬(Heterodera spp.)之非遊走性包囊形成性寄生蟲;細小潛根線蟲(Hirschmaniella gracilis)、稻潛根線蟲(Hirschmaniella oryzae)、刺尾潛根線蟲(Hirschmaniella spinicaudata)及潛根線蟲屬(Hirschmaniella spp.)之莖與葉部體內寄生蟲;埃及紐帶線蟲(Hoplolaimus aegyptii)、加州紐帶線蟲(Hoplolaimus californicus)、哥倫布紐帶線蟲(Hoplolaimus columbus)、帽狀紐帶線蟲(Hoplolaimus galeatus)、珍珠紐帶線蟲(Hoplolaimus indicus)、大針紐帶線蟲(Hoplolaimus magnistylus)、擬強壯紐帶線蟲(Hoplolaimus pararobustus)、非洲長刺線蟲(Longidorus africanus)、短環長刺線蟲(Longidorus breviannulatus)、橫帶長刺線蟲(Longidorus elongatus)、長刺線蟲(Longidorus laevicapitatus)、長刺線蟲(Longidorus vineacola)及長刺線蟲屬(Longidorus spp.)之體外寄生蟲;短尾根瘤線蟲(Meloidogyne acronea)、非洲根瘤線蟲(Meloidogyne africana)、花生根瘤線蟲(Meloidogyne arenaria)、花生根瘤線蟲湯氏亞種(Meloidogyne arenaria thamesi)、亞特力根瘤線蟲(Meloidogyne artiella)、奇特伍德根瘤線蟲(Meloidogyne chitwoodi)、咖啡根結線蟲(Meloidogyne coffeicola)、埃塞俄比亞根瘤線蟲(Meloidogyne ethiopica)、短小根瘤線蟲(Meloidogyne exigua)、法克斯根瘤線蟲(Meloidogyne fallax)、擬禾本科根瘤線蟲(Meloidogyne graminicola)、禾本科根瘤線蟲(Meloidogyne graminis)、北方根瘤線蟲(Meloidogyne hapla)、南方根瘤線蟲(Meloidogyne incognita)、南 方根瘤線蟲亞力塔亞種(Meloidogyne incognita acrita)、爪哇根瘤線蟲(Meloidogyne javanica)、吉庫尤根瘤線蟲(Meloidogyne kikuyensis)、小根瘤線蟲(Meloidogyne minor)、小麥根瘤線蟲(Meloidogyne naasi)、咖啡根瘤線蟲(Meloidogyne paranaensis)、泰晤士根瘤線蟲(Meloidogyne thamesi)及根瘤線蟲屬(Meloidogyne spp.)之非遊走性寄生蟲;根瘤線蟲屬(Meloinema spp.)、假根瘤線蟲(Nacobbus aberrans)、擬莖線蟲(Neotylenchus vigissi)、食菌性線蟲(Paraphelenchus pseudoparietinus)、蔥擬毛刺線蟲(Paratrichodorus allius)、擬毛刺線蟲(Paratrichodorus lobatus)、小擬毛刺線蟲(Paratrichodorus minor)、小擬毛刺線蟲(Paratrichodorus nanus)、有孔擬毛刺線蟲(Paratrichodorus porosus)、大麥光滑擬毛刺線蟲(Paratrichodorus teres)及擬毛刺線蟲屬(Paratrichodorus spp.);芹菜釘線蟲(Paratylenchus hamatus)、微小釘線蟲(Paratylenchus minutus)、突出釘線蟲(Paratylenchus projectus)及釘線蟲屬(Paratylenchus spp.);短體短體線蟲(Pratylenchus agilis)、亞倫氏短體線蟲(Pratylenchus alleni)、安第斯短體線蟲(Pratylenchus andinus)、短尾短體線蟲(Pratylenchus brachyurus)、小麥短體線蟲(Pratylenchus cerealis)、咖啡短體線蟲(Pratylenchus coffeae)、刻痕短體線蟲(Pratylenchus crenatus)、棉花短體線蟲(Pratylenchus delattrei)、吉伯氏短體線蟲(Pratylenchus giibbicaudatus)、古迪氏短體線蟲(Pratylenchus goodeyi)、漢氏短體線蟲(Pratylenchus hamatus)、六裂短體線蟲(Pratylenchus hexincisus)、盧斯短體線蟲(Pratylenchus loosi)、落選短體線蟲(Pratylenchus neglectus)、穿刺短體線蟲(Pratylenchus penetrans)、草地短體線蟲(Pratylenchus pratensis)、斯克裏布納短體線蟲(Pratylenchus scribneri)、大麥短體線蟲(Pratylenchus teres)、索氏短體線蟲(Pratylenchus thornei)、傷殘短體線蟲(Pratylenchus vulnus)、玉米短體線蟲(Pratylenchus zeae)及短體線蟲屬 (Pratylenchus spp.)之遊走性體內寄生蟲;微小假海矛線蟲(Pseudohalenchus minutus)、平滑墊刃線蟲(Psilenchus magnidens)、膨大平滑墊刃線蟲(Psilenchus tumidus)、墨西哥玉米胞囊線蟲(Punctodera chalcoensis)、五溝線蟲(Quinisulcius acutus)、柑橘穿孔線蟲(Radopholus citrophilus)、香蕉穿孔線蟲(Radopholus similis)、穿孔線蟲屬(Radopholus spp.)之遊走性體內寄生蟲;北方貝腎狀線蟲(Rotylenchulus borealis)、微小腎狀線蟲(Rotylenchulus parvus)、腎形腎狀線蟲(Rotylenchulus reniformis)及腎狀線蟲屬(Rotylenchulus spp.);直溝盤旋線蟲(Rotylenchus laurentinus)、大囊盤旋線蟲(Rotylenchus macrodoratus)、強壯盤旋線蟲(Rotylenchus robustus)、均勻盤旋線蟲(Rotylenchus uniformis)及盤旋線蟲屬(Rotylenchus spp.);小尾螺旋線蟲(Scutellonema brachyurum)、山藥螺旋線蟲(Scutellonema bradys)、卡維內斯螺旋線蟲(Scutellonema clathricaudatum)及螺旋線蟲屬(Scutellonema spp.)之遊走性體內寄生蟲;亞粒線蟲(Subanguina radiciola)、頭線蟲(Tetylenchus nicotianae)、圓桶毛刺線蟲(Trichodorus cylindricus)、微小毛刺線蟲(Trichodorus minor)、原始毛刺線蟲(Trichodorus primitivus)、普希毛刺線蟲(Trichodorus proximus)、相似毛刺線蟲(Trichodorus similis)、大蒜毛刺線蟲(Trichodorus sparsus)及毛刺線蟲屬(Trichodorus spp.)之體外寄生蟲;農田矮化線蟲(Tylenchorhynchus agri)、甘藍矮化線蟲(Tylenchorhynchus brassicae)、清亮矮化線蟲(Tylenchorhynchus clarus)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、指形矮化線蟲(Tylenchorhynchus digitatus)、伊布裏矮化線蟲(Tylenchorhynchus ebriensis)、最大矮化線蟲(Tylenchorhynchus maximus)、裸矮化線蟲(Tylenchorhynchus nudus)、普通矮化線蟲(Tylenchorhynchus vulgaris)及矮化線蟲屬(Tylenchorhynchus spp.);柑橘半穿刺線蟲(Tylenchulus semipenetrans)及半 穿刺線蟲屬(Tylenchulus spp.)之半寄生蟲;美洲劍線蟲(Xiphinema americanum)、短頸劍線蟲劍線蟲(Xiphinema brevicolle)、雙型性劍線蟲(Xiphinema dimorphicaudatum)、標準劍線蟲(Xiphinema index)及劍線蟲屬(Xiphinema spp.)之體外寄生蟲。 Plant nematodes include (but are not limited to): for example: C. elegans (Aglenchus agricola), Anguina tritici, Aphelenchoides arachidis, Aphelenchoides fragaria, and stem and leaf internal parasites of the genus Aphelenchoides spp. Belonolaimus gracilis, Belonolaimus longicaudatus, Belonolaimus nortoni, Bursaphelenchus cocophilus, Bursaphelenchus eremus, Bursaphelenchus xylophilus ) and Bursaphelenchus spp.; Cacopaurus pestis, Criconemella curvata, Criconemella onoensis, Criconemella ornata, ring Nematodes (Criconemella rusium), Criconemella xenoplax (=Mesocriconema xenoplax) and Criconemella spp., Criconemoides ferniae, Cryptocaryon elegans Criconemoides onoense), Criconemoides ornatum and C. elegans (Cri Conemoides spp.); Stem and leaf endoparasites of Ditylenchus destructor, Ditylenchus dipsaci, Ditylenchus myceliophagus, and Ditylenchus spp.; Dolichodorus heterocephalus), Globodera pallida (=Heterodera pallida), Globodera rostochiensis (yellow potato cyst nematode), Globodera solanacearum, tobacco golden nematode ( Globodera tabacum), non-walking cystic parasite of the genus Globodera virginia and Globodera spp.; Helicopterus digonicus, Helicotylenchis dihystera ), Helicotylchus erythrine, Helicoterlenchus multicinctus, Helicotyllenchus nannus, Helicotylenchus pseudorobustus, and Helicoverpa armigera (Helicotylenchus spp.); Hemicriconemoides, Hemicycliophora arenaria, Hemicycliophora nudata, Hemicycliophora parvana, Heterodera avenae, cross Heterodera cruciferae, Heterodera glycines (soybean cyst nematode), Heterodera oryzae, Heterodera schachtii, Heterodera zeae And non-walking cystic parasites of the genus Heterodera spp.; Hirschmaniella gracilis, Hirschmaniella oryzae, Hirschmaniella spinicaudata and Stem and leaf endoparasites of the genus Hirschmaniella spp.; Hoplolaimus aegyptii, Hoplolaimus californicus, Hoplolaimus columbus, Hoplolaimus galeatus , Hoplolaimus indicus, large needle nematode (Hoplolaimus magnistylu) s), Hoplolaimus pararobustus, Longidorus africanus, Longidorus breviannulatus, Longidorus elongatus, Longidorus laevicapitatus, long An ectoparasite of Longidorus vineacola and Longidorus spp.; Meloidogyne acronea, Meloidogyne africana, Meloidogyne arenaria, Peanut nodule nematode soup Meloidogyne arenaria thamesi, Meloidogyne artiella, Meloidogyne chitwoodi, Meloidogyne coffeicola, Meloidogyne ethiopica, Meloidogyne exigua ), Meloidogyne fallax, Meloidogyne graminicola, Meloidogyne graminis, Meloidogyne hapla, Meloidogyne incognita, South Meloidogyne incognita acrita, Meloidogyne javanica, Meloidogyne kikuyensis, Meloidogyne minor, Meloidogyne naasi, coffee root nodule Non-walking parasites of the genus Meloidogyne paranaensis, Meloidogyne thamesi and Meloidogyne spp.; Meloinema spp., Nacobbus aberrans, Stem nematode ( Neotylenchus vigissi), Paraphelenchus pseudoparietinus, Paratrichodorus allius, Paratrichodorus lobatus, Paratrichodorus minor, Paratrichodorus nanus, perforated Paratrichodorus porosus, Paratrichodorus teres and Paratrichodorus spp.; Paratylenchus hamatus, Paratylenchus minutus, Paratylenchus projectus ) and the genus Nematode ( Paratylenchus spp.); short-winged nematodes (Pratylenchus agilis), A. striata (Pratylenchus alleni), Andean short-lived nematodes (Pratylenchus and inus), short-tailed short-stem nematodes (Pratylenchus brachyurus), wheat short-stem nematodes ( Pratylenchus cerealis), Platylenchus coffeae, Pratylenchus crenatus, Pratylenchus delattrei, Pratylenchus giibbicaudatus, and C. elegans Pratylenchus goodeyi), Pratylenchus hamatus, Pratylenchus hexincisus, Pratylenchus loosi, Pratylenchus neglectus, Pratylenchus penetrans ), Platyllenchus pratensis, Pratylenchus scribneri, Pratylenchus teres, Pratylenchus thornei, Tradylenchus vulnus ), short-tailed nematode (Pratylenchus zeae) and short-body nematode (Pratylenchus spp.) migratory internal parasite; Pseudohalenchus minutus, Psilenchus magnidens, Psilenchus tumidus, Punctodera chalcoensis , the genus Quinisulcius acutus, Radopholus citrophilus, Radopholus similis, the vaginal parasite of the genus Radopholus spp., Rotylenchulus borealis, Rotylenchulus parvus, Rotylenchulus reniformis, and Rotylenchulus spp.; Rotylenchus laurentinus, Rotylenchus macrodoratus, T. elegans (Rotylenchus robustus), Rotylenchus uniformis and Rotylenchus spp.; Scutellonema brachyurum, Scutellonema bradys, Scutellonema clathricaudatum and spiral Nematode (Scutellonema spp.) Migratory parasites; Subanguina radiciola, Tetylenchus nicotianae, Trichodorus cylindricus, Trichodorus minor, Trichodorus primitivus, C. serrata (Trichodorus proximus), similar ectoparasites of Trichodorus similis, Trichodorus sparsus and Trichodorus spp.; Tylenchorhynchus agri, Tylenchorhynchus brassicae ), Tylenchorhynchus clarus, Tylenchorhynchus claytoni, Tylenchorhynchus digitatus, Tylenchorhynchus ebriensis, and the largest dwarf nematode (Tylenchorhynchus maximus) ), Tylenchorhynchus nudus, Tylenchorhynchus vulgaris, and Tylenchorhynchus spp.; Tylenchulus semipenetrans and half A semi-parasitic genus of the genus Tylenchulus spp.; Xiphinema americanum, Xiphinema brevicolle, Xiphinema dimorphicaudatum, Xiphinema index, and An ectoparasite of the genus Xiphinema spp.
可使用式(I)化合物控制之線蟲包括:根瘤線蟲屬(Meloidogyne)線蟲,如:南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)、北方根瘤線蟲(Meloidogyne hapla)及花生根瘤線蟲(Meloidogyne arenaria);腐敗線蟲屬(Ditylenchus)線蟲,如:馬鈴薯腐敗線蟲(Ditylenchus destructor)及莖與球莖線蟲(莖線蟲(Ditylenchus dipsaci));短體線蟲屬(Pratylenchus)線蟲,如:穗軸根腐線蟲(穿刺短體線蟲(Pratylenchus penetrans))、菊花根腐線蟲(菊花短體線蟲(Pratylenchus fallax))、咖啡根線蟲(咖啡短體線蟲(Pratylenchus coffeae))、茶樹根線蟲(盧斯短體線蟲(Pratylenchus loosi))及胡桃根腐線蟲(傷殘短體線蟲(Pratylenchus vulnus));黃金包囊線蟲屬(Globodera)線蟲,如:黃色馬鈴薯包囊線蟲(馬鈴薯黃金線蟲(Globodera rostochiensis))及白色馬鈴薯包囊線蟲(馬鈴薯白線蟲(Globodera pallida));異皮線蟲屬(Heterodera)之線蟲,如:大豆包囊線蟲(大豆異皮線蟲(Heterodera glycines))及甜菜包囊線蟲(甜菜異皮線蟲(Heterodera schachtii));滑刃線蟲屬(Aphelenchoides)線蟲,如:稻白尖病線蟲(葉芽滑刃線蟲(Aphelenchoides besseyi))、菊花線蟲(菊花滑刃線蟲(Aphelenchoides ritzemabosi))及草莓線蟲(草莓滑刃線蟲(Aphelenchoides fragariae));真滑刃線蟲屬(Aphelenchus)線蟲,如:食真菌性線蟲(燕麥真滑刃線蟲(Aphelenchus avenae));穿孔線蟲屬(Radopholus)線蟲,如:穿孔線蟲(香蕉穿孔線蟲(Radopholus similis));半穿刺線蟲屬(Tylenchulus)線蟲,如:柑橘根線蟲(柑橘半穿刺線蟲(Tylenchulus semipenetrans));腎狀線蟲屬(Rotylenchulus)線蟲,如:腎形線蟲(腎形腎狀線蟲(Rotylenchulus reniformis));鑽木線蟲,如:松材線蟲(Bursaphelenchus xylophilus)及椰子紅環腐線蟲(Bursaphelenchus cocophilus),等等之線蟲。 Nematodes that can be controlled using compounds of formula (I) include: Meloidogyne elegans such as Meloidogyne incognita, Meloidogyne javanica, Meloidogyne hapla, and Peanut root nematode ( Meloidogyne arenaria); Ditylenchus nematodes, such as: Ditylenchus destructor and stem and bulb nematodes (Ditylenchus dipsaci); genus of the genus Pratylenchus, such as: cob root rot Nematodes (Pratylenchus penetrans), Chrysanthemum root rot (Pratylenchus fallax), Coffee root nematode (Pratylenchus coffeae), Tea tree root nematode (Luss nematode) (Pratylenchus loosi)) and Walnut root rot nematode (Pratylenchus vulnus); gold cystic nematode (Globodera) nematodes, such as: yellow potato cyst nematode (Globodera rostochiensis) and white Potato cyst nematode (Globodera pallida); Nematodes of Heterodera, such as: large Nematodes (Heterodera glycines) and beet cyst nematodes (Heterodera schachtii); Aphelenchoides nematodes, such as the rice white-spotted nematode (Aphelenchoides besseyi)), Chrysanthemum nematode (Aphelenchoides ritzemabosi) and strawberry nematode (Aphelenchoides fragariae); Aphelenchus nematodes, such as: fungal nematodes (oats) Aphelenchus avenae; a nematode of the genus Radopholus, such as a perforated nematode (Radopholus similis); a nematode of the genus Tylenchulus, such as a citrus root nematode (citrus half puncture) Nematode (Tylenchulus Semipenetrans)); Rotylenchulus elegans, such as: nematode (Rotylenchulus reniformis); wood nematode, such as: Bursaphelenchus xylophilus and coconut red ring rot nematode ( Bursaphelenchus cocophilus), etc.
可使用式(I)化合物保護之植物包括下列植物,如:穀類(例如:稻、大麥、小麥、裸麥、燕麥、玉米,等等)、豆類(大豆、紅豆、豆類、蠶豆、豌豆、花生,等等)、果樹/果實(蘋果、柑橘品種、梨、葡萄、桃、日本杏、櫻桃、胡桃、杏仁、香蕉、草莓,等等)、蔬菜品種(捲心白菜、番茄、菠菜、青花菜、萵苣、洋蔥、青蔥、青椒,等等)、根部作物(胡蘿蔔、馬鈴薯、地瓜、蘿蔔、蓮藕、大頭菜,等等)、工業原料用植物(棉花、麻、構樹、三極樹、油菜、甜菜、啤酒花、甘蔗、糖甜菜、橄欖、橡膠、棕櫚樹、咖啡、菸草、茶葉,等等)、瓜類(南瓜、小黃瓜、西瓜、香瓜,等等)、草原植物(鴨茅、高粱、貓尾草、三葉草、苜蓿草,等等)、草皮(臺北草、康穗草,等等)、香料植物,等等(薰衣草、迷迭香、百里香、巴西利、胡椒、薑,等等)及花卉(菊花、玫瑰、蘭花,等等)。 Plants which can be protected with a compound of formula (I) include plants such as cereals (eg, rice, barley, wheat, rye, oats, corn, etc.), beans (soybeans, red beans, beans, broad beans, peas, peanuts). , etc.), fruit trees/fruits (apples, citrus varieties, pears, grapes, peaches, Japanese apricots, cherries, walnuts, almonds, bananas, strawberries, etc.), vegetable varieties (cabbage, tomato, spinach, broccoli) , lettuce, onions, shallots, green peppers, etc.), root crops (carrots, potatoes, sweet potatoes, radishes, lotus roots, kohlrabi, etc.), industrial raw materials (cotton, hemp, mulberry, tri-tree, rapeseed, Beets, hops, sugar cane, sugar beets, olives, rubber, palm trees, coffee, tobacco, tea, etc.), melons (pumpkins, cucumbers, watermelons, melons, etc.), grassland plants (Dactyls, sorghum, Timothy, clover, valerian, etc.), turf (Taipei grass, Kangsui grass, etc.), spice plants, etc. (lavender, rosemary, thyme, balinese, pepper, ginger, etc.) And flowers (chrysanthemums, roses, Orchid, etc.).
式(I)化合物特別適合控制咖啡線蟲,特定言之:短尾短體線蟲(Pratylenchus brachyurus)、咖啡短體線蟲(Pratylenchus coffeae)、短小根瘤線蟲(Meloidogyne exigua)、南方根瘤線蟲(Meloidogyne incognita)、咖啡根結線蟲(Meloidogyne coffeicola)、螺旋線蟲屬(Helicotylenchus spp.)及咖啡根瘤線蟲(Meloidogyne paranaensis)、盤旋線蟲屬(Rotylenchus spp.)、劍線蟲屬(Xiphinema spp.)、矮化線蟲屬(Tylenchorhynchus spp.)與螺旋線蟲屬(Scutellonema spp.)。 The compounds of formula (I) are particularly suitable for controlling coffee worms, in particular: Pratylenchus brachyurus, Pratylenchus coffeae, Meloidogyne exigua, Meloidogyne incognita, Meloidogyne coffeicola, Helicotylenchus spp. and Meloidogyne paranaensis, Rotylenchus spp., Xiphinema spp., Dylenchorhynchus Spp.) and Scutellonema spp.
式(I)化合物特別適合控制馬鈴薯線蟲,特定言之:短尾短體線蟲(Pratylenchus brachyurus)、草地短體線蟲(Pratylenchus pratensis)、斯克裏布納短體線蟲(Pratylenchus scribneri)、穿刺短體線蟲(Pratylenchus penetrans)、咖啡短體線蟲(Pratylenchus coffeae)、莖線蟲(Ditylenchus dipsaci)及亞倫氏短體線蟲(Pratylenchus alleni)、安第斯短體線蟲(Pratylenchus andinus)、小麥短體線蟲(Pratylenchus cerealis)、刻痕短體線蟲(Pratylenchus crenatus)、六裂短體線蟲(Pratylenchus hexincisus)、盧斯短體線蟲(Pratylenchus loosi)、落選短體線蟲(Pratylenchus neglectus)、大麥短體線蟲(Pratylenchus teres)、索氏短體線蟲(Pratylenchus thornei)、傷殘短體線蟲(Pratylenchus vulnus)、長尾刺線蟲(Belonolaimus longicaudatus)、圓桶毛刺線蟲(Trichodorus cylindricus)、原始毛刺線蟲(Trichodorus primitivus)、普希毛刺線蟲(Trichodorus proximus)、相似毛刺線蟲(Trichodorus similis)、大蒜毛刺線蟲(Trichodorus sparsus)、小擬毛刺線蟲(Paratrichodorus minor)、蔥擬毛刺線蟲(Paratrichodorus allius)、小擬毛刺線蟲(Paratrichodorus nanus)、大麥光滑擬毛刺線蟲(Paratrichodorus teres)、花生根瘤線蟲(Meloidogyne arenaria)、法克斯根瘤線蟲(Meloidogyne fallax)、北方根瘤線蟲(Meloidogyne hapla)、泰晤士根瘤線蟲(Meloidogyne thamesi)、南方根瘤線蟲(Meloidogyne incognita)、奇特伍德根瘤線蟲(Meloidogyne chitwoodi)、爪哇根瘤線蟲(Meloidogyne javanica)、假根瘤線蟲(Nacobbus aberrans)、馬鈴薯黃金線蟲(Globodera rostochiensis)、馬鈴薯白線蟲(Globodera pallida)、馬鈴薯腐敗線蟲(Ditylenchus destructor)、香蕉穿孔線蟲(Radopholus similis)、腎形腎狀線蟲(Rotylenchulus reniformis)、擬莖線蟲(Neotylenchus vigissi)、食菌性線蟲(Paraphelenchus pseudoparietinus)、草莓滑刃線蟲(Aphelenchoides fragariae)與根瘤線蟲屬(Meloinema spp.)。 The compounds of formula (I) are particularly suitable for controlling potato nematodes, in particular: Pratylenchus brachyurus, Pratylenchus pratensis, Pratylenchus scribneri, short-stem nematodes (Pratylenchus Penetrans), coffee larvae (Pratylenchus coffeae), stem worm (Ditylenchus dipsaci) and A. striata (Pratylenchus alleni), Andean short-stem nematode (Pratylenchus and inus), wheat short-stem nematode (Pratylenchus cerealis), nick Platylenchus crenatus, Pratylenchus hexincisus, Pratylenchus loosi, Pratylenchus neglectus, Pratylenchus teres, Soxhlet short body Nematodes (Pratylenchus thornei), Tratylenchus vulnus, Belonolaimus longicaudatus, Trichodorus cylindricus, Trichodorus primitivus, Trichodorus proximus, Similar to Trichodorus similis, Trichodorus sparsus, Paratrichodorus minor, Paratrichodorus allius, Paratrichodorus nanus, Barley smoothing burr (Paratrichodorus) Teres), peanut root nodule nematode (Meloi Dogyne arenaria), Meloidogyne fallax, Meloidogyne hapla, Meloidogyne thamesi, Meloidogyne incognita, Meloidogyne chitwoodi, Nematode nocturnal nematode (Meloidogyne javanica), Nacobbus aberrans, Globodera rostochiensis, Globodera pallida, Ditylenchus destructor, Radopholus similis, Renal nematode (Rotylenchulus reniformis), Neotylenchus vigissi, Paraphelenchus pseudoparietinus, Aphelenchoides fragariae and Melolinema spp.
式(I)化合物特別適合控制番茄線蟲,特定言之:花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、爪哇根瘤線蟲(Meloidogyne javanica)、南方根瘤線蟲(Meloidogyne incognita)、穿刺 短體線蟲(Pratylenchus penetrans)及短尾短體線蟲(Pratylenchus brachyurus)、咖啡短體線蟲(Pratylenchus coffeae)、斯克裏布納短體線蟲(Pratylenchus scribneri)、傷殘短體線蟲(Pratylenchus vulnus)、微小短體線蟲(Paratrichodorus minor)、短小根瘤線蟲(Meloidogyne exigua)、假根瘤線蟲(Nacobbus aberrans)、枯萎黃金線蟲(Globodera solanacearum)、異頭錐線蟲(Dolichodorus heterocephalus)與腎形腎狀線蟲(Rotylenchulus reniformis)。 The compounds of formula (I) are particularly suitable for controlling tomato nematodes, in particular: Meloidogyne arenaria, Meloidogyne hapla, Meloidogyne javanica, Meloidogyne incognita, puncture Pratylenchus penetrans and Pratylenchus brachyurus, Pratylenchus coffeae, Pratylenchus scribneri, Pratylenchus vulnus, tiny Paratrichodorus minor, Meloidogyne exigua, Nacobbus aberrans, Globodera solanacearum, Dolichodorus heterocephalus, and Rotylenchulus reniformis .
式(I)化合物特別適合控制胡瓜植物線蟲,特定言之:花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、爪哇根瘤線蟲(Meloidogyne javanica)、南方根瘤線蟲(Meloidogyne incognita)、腎形腎狀線蟲(Rotylenchulus reniformis)與索氏短體線蟲(Pratylenchus thornei)。 The compounds of formula (I) are particularly suitable for controlling myriad plant nematodes, in particular: Meloidogyne arenaria, Meloidogyne hapla, Meloidogyne javanica, Meloidogyne incognita, kidney Rotylenchulus reniformis and Pratylenchus thornei.
式(I)化合物特別適合控制棉花線蟲,特定言之:長尾刺線蟲(Belonolaimus longicaudatus)、南方根瘤線蟲(Meloidogyne incognita)、哥倫布紐帶線蟲(Hoplolaimus columbus)、帽狀紐帶線蟲(Hoplolaimus galeatus)與腎形腎狀線蟲(Rotylenchulus reniformis)。 The compounds of formula (I) are particularly suitable for controlling cotton nematodes, in particular: Belonolaimus longicaudatus, Meloidogyne incognita, Hoplolaimus columbus, Hoplolaimus galeatus and kidney Nematode (Rotylenchulus reniformis).
式(I)化合物特別適合控制玉米線蟲,特定言之:長尾刺線蟲(Belonolaimus longicaudatus)、小短體線蟲(Paratrichodorus minor)及短尾短體線蟲(Pratylenchus brachyurus)、棉花短體線蟲(Pratylenchus delattrei)、六裂短體線蟲(Pratylenchus hexincisus)、穿刺短體線蟲(Pratylenchus penetrans)、玉米短體線蟲(Pratylenchus zeae)、(豌豆刺線蟲(Belonolaimus gracilis))、諾頓刺線蟲(Belonolaimus nortoni)、短環長刺線蟲(Longidorus breviannulatus)、花生根瘤線蟲(Meloidogyne arenaria)、花生根瘤線蟲湯氏亞種(Meloidogyne arenaria thamesi)、禾本科根瘤線蟲(Meloidogyne graminis)、南方根瘤線蟲(Meloidogyne incognita)、南方根瘤線蟲亞力塔亞種(Meloidogyne incognita acrita)、爪哇根瘤線蟲(Meloidogyne javanica)、小麥根瘤線蟲(Meloidogyne naasi)、禾穀異皮線蟲(Heterodera avenae)、稻異皮線蟲(Heterodera oryzae)、玉米異皮線蟲(Heterodera zeae)、墨西哥玉米胞囊線蟲(Punctodera chalcoensis)、莖線蟲(Ditylenchus dipsaci)、埃及紐帶線蟲(Hoplolaimus aegyptii)、大針紐帶線蟲(Hoplolaimus magnistylus)、帽狀紐帶線蟲(Hoplolaimus galeatus)、珍珠粟槍線蟲(Hoplolaimus indicus)、雙角螺旋線蟲(Helicotylenchus digonicus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、假強壯螺旋線蟲(Helicotylenchus pseudorobustus)、美洲劍線蟲(Xiphinema americanum)、異頭錐線蟲(Dolichodorus heterocephalus)、裝飾環紋線蟲(Criconemella ornata)、環紋線蟲(Criconemella onoensis)、香蕉穿孔線蟲(Radopholus similis)、北方貝腎狀線蟲(Rotylenchulus borealis)、微小腎狀線蟲(Rotylenchulus parvus)、農田矮化線蟲(Tylenchorhynchus agri)、清亮矮化線蟲(Tylenchorhynchus clarus)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、最大矮化線蟲(Tylenchorhynchus maximus)、裸矮化線蟲(Tylenchorhynchus nudus)、普通矮化線蟲(Tylenchorhynchus vulgaris)、五溝線蟲(Quinisulcius acutus)、微小釘線蟲(Paratylenchus minutus)、塔堅鞘線蟲(Hemicycliophora parvana)、居農野外墊刃線蟲(Aglenchus agricola)、小麥粒癭線蟲(Anguina tritici)、花生滑刃線蟲(Aphelenchoides arachidis)、小尾盾線蟲(Scutellonema brachyurum)與亞粒線蟲(Subanguina radiciola)。 The compounds of formula (I) are particularly suitable for controlling corn worms, in particular: Belonolaimus longicaudatus, Paratrichodorus minor and Pratylenchus brachyurus, Pratylenchus delattrei , Pratylenchus hexincisus, Pratylenchus penetrans, Pratylenchus zeae, Belonolaimus gracilis, Belonolaimus nortoni, short loop length Longidorus breviannulatus, Meloidogyne arenaria, Meloidogyne arenaria thamesi, Graminea nematode (Meloidogyne) Graminis), Meloidogyne incognita, Meloidogyne incognita acrita, Meloidogyne javanica, Meloidogyne naasi, Heterodera avenae Heterodera oryzae, Heterodera zeae, Punctodera chalcoensis, Ditylenchus dipsaci, Hoplolaimus aegyptii, and the big needle nematode (Hoplolaimus) Magnistylus), Hoplolaimus galeatus, Hoplolaimus indicus, Helicotylenchus digonicus, Helicotylenchus dihystera, Helicotylenchus pseudorobustus, American sword Nematodes (Xiphinema americanum), Dolichodorus heterocephalus, Criconemella ornata, Criconemella onoensis, Radopholus similis, Rotylenchulus borealis, Tiny kidney Nematode (Rotylenchulus parvus), Tylenchorhynchus agri, Tylenchorhynchus clarus, Tylenchorhynchus claytoni, Tylenchorhynchus maximus, Tylenchorhynchus Nudus), Tylenchorhynchus vulgaris, Quinisulcius acutus, Paratylenchus minutus, Hemicycliophora parvana, Aglenchus agricola, wheat granules Anguina tritici, Aphelenchoides arachidis, Scutellonema brachyurum and Subanguina radiciola.
式(I)化合物特別適合控制大豆線蟲,特定言之:短尾短體線蟲(Pratylenchus brachyurus)、草地短體線蟲(Pratylenchus pratensis)、穿刺短體線蟲(Pratylenchus penetrans)、斯克裏布納短體線蟲(Pratylenchus scribneri)、長尾刺線蟲(Belonolaimus longicaudatus)、大豆異皮線蟲(Heterodera glycines)、哥倫布紐帶線蟲(Hoplolaimus columbus)及咖啡短體線蟲(Pratylenchus coffeae)、六裂短體線蟲(Pratylenchus hexincisus)、落選短體線蟲(Pratylenchus neglectus)、刻痕短體線蟲(Pratylenchus crenatus)、亞倫氏短體線蟲(Pratylenchus alleni)、短體短體線蟲(Pratylenchus agilis)、玉米短體線蟲(Pratylenchus zeae)、傷殘短體線蟲(Pratylenchus vulnus)、(豌豆刺線蟲(Belonolaimus gracilis))、花生根瘤線蟲(Meloidogyne arenaria)、南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)、北方根瘤線蟲(Meloidogyne hapla)、哥倫布紐帶線蟲(Hoplolaimus columbus)、帽狀紐帶線蟲(Hoplolaimus galeatus)與腎形腎狀線蟲(Rotylenchulus reniformis)。 The compounds of formula (I) are particularly suitable for controlling soybean nematodes, in particular: Pratylenchus brachyurus, Pratylenchus pratensis, Pratylenchus penetrans, Scribner short-body nematodes (Pratylenchus Scribneri), Belonolaimus longicaudatus, Heterodera glycines, Hoplolaimus columbus, and Pratylinchus coffeae, Pratylenchus hexincisus, unsuccessful Nematode (Pratylenchus neglectus), Platyllenchus crenatus, Pratylenchus alleni, Pratylenchus agilis, Pratylenchus zeae, disability short body Nematode (Pratylenchus vulnus), (Belonolaimus gracilis), Meloidogyne arenaria, Meloidogyne incognita, Meloidogyne javanica, Meloidogyne hapla, Columbus nucleus Nematode (Hoplolaimus columbus), Hoplolaimus galeatus and Rotylenchulus reniformis.
式(I)化合物特別適合控制菸草線蟲,特定言之:南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)及短尾短體線蟲(Pratylenchus brachyurus)、草地短體線蟲(Pratylenchus pratensis)、六裂短體線蟲(Pratylenchus hexincisus)、穿刺短體線蟲(Pratylenchus penetrans)、落選短體線蟲(Pratylenchus neglectus)、刻痕短體線蟲(Pratylenchus crenatus)、索氏短體線蟲(Pratylenchus thornei)、傷殘短體線蟲(Pratylenchus vulnus)、玉米短體線蟲(Pratylenchus zeae)、橫帶長刺線蟲(Longidorus elongatu)、擬毛刺線蟲(Paratrichodorus lobatus)、毛刺線蟲屬(Trichodorus spp.)、花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、菸草黃金線蟲(Globodera tabacum)、枯萎黃金線蟲(Globodera solanacearum)、維吉尼亞黃金線蟲(Globodera virginiae)、莖線蟲(Ditylenchus dipsaci)、盤旋線蟲屬(Rotylenchus spp.)、螺旋線蟲屬(Helicotylenchus spp.)、美洲劍線蟲(Xiphinema americanum)、環紋線蟲屬 (Criconemella spp.)、腎形腎狀線蟲(Rotylenchulus reniformis)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、釘線蟲屬(Paratylenchus spp.)與頭線蟲(Tetylenchus nicotianae)。 The compounds of formula (I) are particularly suitable for controlling tobacco nematodes, in particular: Meloidogyne incognita, Meloidogyne javanica and Pratylenchus brachyurus, Pratylenchus pratensis, Pratylenchus hexincisus, Pratylenchus penetrans, Pratylenchus neglectus, Pratylenchus crenatus, Pratylenchus thornei, disability Pratylenchus vulnus, Pratylenchus zeae, Longidorus elongatu, Paratrichodorus lobatus, Trichodorus spp., Meloidogyne arenaria ), Meloidogyne hapla, Globodera tabacum, Globodera solanacearum, Globodera virginiae, Ditylenchus dipsaci, Rotylenchus spp .), Heliconia (Helicotylenchus spp.), Americas Nematode (Xiphinema americanum), the ring Strongyloides (Criconemella spp.), Rotylenchulus reniformis, Tylenchorhynchus claytoni, Paratylenchus spp. and Tetylenchus nicotianae.
式(I)化合物特別適合控制柑橘線蟲,特定言之:咖啡短體線蟲(Pratylenchus coffeae)及短尾短體線蟲(Pratylenchus brachyurus)、傷殘短體線蟲(Pratylenchus vulnus)、長尾刺線蟲(Belonolaimus longicaudatus)、微小短體線蟲(Paratrichodorus minor)、有孔擬毛刺線蟲(Paratrichodorus porosus)、毛刺線蟲(Trichodorus)、南方根瘤線蟲(Meloidogyne incognita)、南方根瘤線蟲亞力塔亞種(Meloidogyne incognita acrita)、爪哇根瘤線蟲(Meloidogyne javanica)、大囊盤旋線蟲(Rotylenchus macrodoratus)、美洲劍線蟲(Xiphinema americanum)、短頸劍線蟲劍線蟲(Xiphinema brevicolle)、標準劍線蟲(Xiphinema index)、環紋線蟲屬(Criconemella spp.)、半鞘線蟲(Hemicriconemoides)、香蕉穿孔線蟲(Radopholus similis)與柑橘穿孔線蟲(Radopholus citrophilus)、花生鞘線蟲(Hemicycliophora arenaria)、裸出鞘線蟲(Hemicycliophora nudata)與柑橘半穿刺線蟲(Tylenchulus semipenetrans)。 The compounds of formula (I) are particularly suitable for controlling citrus nematodes, in particular: Pratylenchus coffeae and Pratylenchus brachyurus, Pratylenchus vulnus, Belonolaimus longicaudatus ), Paratrichodorus minor, Paratrichodorus porosus, Trichodorus, Meloidogyne incognita, Meloidogyne incognita acrita, Java Meloidogyne javanica, Rotylenchus macrodoratus, Xiphinema americanum, Xiphinema brevicolle, Xiphinema index, Criconemella spp .), Hemicriconemoides, Radopholus similis and Radopholus citrophilus, Hemicycliophora arenaria, Hemicycliophora nudata and Tylenchulus semipenetrans ).
式(I)化合物特別適合控制香蕉線蟲,特定言之:咖啡短體線蟲(Pratylenchus coffeae)、香蕉穿孔線蟲(Radopholus similis)及吉伯氏短體線蟲(Pratylenchus giibbicaudatus)、盧斯短體線蟲(Pratylenchus loosi)、根瘤線蟲屬(Meloidogyne spp.)、多帶螺旋線蟲(Helicotylenchus multicinctus)、雙宮螺旋線蟲(Helicotylenchus dihystera)與腎狀線蟲屬(Rotylenchulus Spp.)。 The compounds of formula (I) are particularly suitable for controlling banana nematodes, in particular: Pratylinchus coffeae, Radopholus similis and Pratylenchus giibbicaudatus, Prasylenchus Loosi), Meloidogyne spp., Helicotyllenchus multicinctus, Helicotyllenchus dihystera, and Rotylenchulus Spp.
式(I)化合物特別適合控制鳳梨線蟲,特定言之:玉米短體線蟲(Pratylenchus zeae)、草地短體線蟲(Pratylenchus pratensis)、短尾短體 線蟲(Pratylenchus brachyurus)、古迪氏短體線蟲(Pratylenchus goodeyi)、根瘤線蟲屬(Meloidogyne spp.)、腎形腎狀線蟲(Rotylenchulus reniformis)及橫帶長刺線蟲(Longidorus elongatus)、長刺線蟲(Longidorus laevicapitatus)、原始毛刺線蟲(Trichodorus primitivus)、微小毛刺線蟲(Trichodorus minor)、異皮線蟲屬(Heterodera spp.)、蘑菇莖線蟲(Ditylenchus myceliophagus)、加州紐帶線蟲(Hoplolaimus californicus)、擬強壯紐帶線蟲(Hoplolaimus pararobustus)、珍珠粟槍線蟲(Hoplolaimus indicus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、短小螺旋線蟲(Helicotylenchus nannus)、多帶螺旋線蟲(Helicotylenchus multicinctus)、赤色螺旋線蟲(Helicotylenchus erythrine)、雙型性劍線蟲(Xiphinema dimorphicaudatum)、香蕉穿孔線蟲((Radopholus similis)、指形矮化線蟲(Tylenchorhynchus digitatus)、伊布裏矮化線蟲(Tylenchorhynchus ebriensis)、微小釘線蟲(Paratylenchus minutus)、卡維內斯螺旋線蟲(Scutellonema clathricaudatum)、山藥螺旋線蟲(Scutellonema bradys)、膨大平滑墊刃線蟲(Psilenchus tumidus)、平滑墊刃線蟲(Psilenchus magnidens)、微小假海矛線蟲(Pseudohalenchus minutus)、弗尼亞小環線蟲(Criconemoides ferniae)、小環線蟲(Criconemoides onoense)與杯口小環線蟲(Criconemoides ornatum)。 The compound of formula (I) is particularly suitable for controlling pineapple nematodes, in particular: Pratylenchus zeae, Pratylenchus pratensis, short-tailed short body Nematodes (Pratylenchus brachyurus), Pratylenchus goodeyi, Meloidogyne spp., Rotylenchulus reniformis, Longidorus elongatus, and long-stem nematode ( Longidorus laevicapitatus), Trichodorus primitivus, Trichodorus minor, Heterodera spp., Ditylenchus myceliophagus, Hoplolaimus californicus, and T. elegans (Hoplolaimus pararobustus), Hoplolaimus indicus, Helicotylenchus dihystera, Helicotylenchus nannus, Helicopterchus multicinctus, Helicotylenchus erythrine, Double Xiphinema dimorphicaudatum, Radopholus similis, Tylenchorhynchus digitatus, Tylenchorhynchus ebriensis, Paratylenchus minutus, Cavanes Helix (Scutellonema clathricaudatum), Scutellonema bradys, Psilenchus tumidus, Psilenchus magnidens, Pseudohalenchus minutus, Criconemoides Ferniae), Criconemoides onoense and Criconemoides ornatum.
式(I)化合物特別適合控制葡萄藤線蟲,特定言之:傷殘短體線蟲(Pratylenchus vulnus)、花生根瘤線蟲(Meloidogyne arenaria)、南方根瘤線蟲(Meloidogyne incognita)、爪哇根瘤線蟲(Meloidogyne javanica)、美洲劍線蟲(Xiphinema americanum)、標準劍線蟲(Xiphinema index)及草地短體線蟲(Pratylenchus pratensis)、斯克裏布納短體線蟲(Pratylenchus scribneri)、落選短體線蟲(Pratylenchus neglectus)、短尾短體線蟲(Pratylenchus brachyurus)、索氏短體線蟲(Pratylenchus thornei)與柑橘半穿刺線蟲 (Tylenchulus semipenetrans)。 The compounds of formula (I) are particularly suitable for controlling grapevine nematodes, in particular: Pratylenchus vulnus, Meloidogyne arenaria, Meloidogyne incognita, Meloidogyne javanica, Xiphinema americanum, Xiphinema index, Pratylenchus pratensis, Pratylenchus scribneri, Pratylenchus neglectus, short-tailed short Nematodes (Pratylenchus brachyurus), P. striata (Pratylenchus thornei) and citrus semi-puncture nematodes (Tylenchulus semipenetrans).
式(I)化合物特別適合控制樹類作物-仁果之線蟲,特定言之穿刺短體線蟲(Pratylenchus penetrans)及傷殘短體線蟲(Pratylenchus vulnus)、橫帶長刺線蟲(Longidorus elongatus)、南方根瘤線蟲(Meloidogyne incognita)與北方根瘤線蟲(Meloidogyne hapla)。 The compounds of formula (I) are particularly suitable for controlling tree-crop-C. elegans, in particular Pratylenchus penetrans and Pratylenchus vulnus, Longidorus elongatus, Southern Meloidogyne incognita and Meloidogyne hapla.
式(I)化合物特別適合控制樹類作物-核果之線蟲,特定言之:穿刺短體線蟲(Pratylenchus penetrans)、傷殘短體線蟲(Pratylenchus vulnus)、花生根瘤線蟲(Meloidogyne arenaria)、北方根瘤線蟲(Meloidogyne hapla)、爪哇根瘤線蟲(Meloidogyne javanica)、南方根瘤線蟲(Meloidogyne incognita)、葡萄環紋線蟲(Criconemella xenoplax)及短尾短體線蟲(Pratylenchus brachyurus)、咖啡短體線蟲(Pratylenchus coffeae)、斯克裏布納短體線蟲(Pratylenchus scribneri)、玉米短體線蟲(Pratylenchus zeae)、長尾刺線蟲(Belonolaimus longicaudatus)、雙宮螺旋線蟲(Helicotylenchus dihystera)、美洲劍線蟲(Xiphinema americanum)、彎曲環紋線蟲(Criconemella curvata)、克萊頓矮化線蟲(Tylenchorhynchus claytoni)、芹菜釘線蟲(Paratylenchus hamatus)、突出釘線蟲(Paratylenchus projectus)、小尾盾線蟲(Scutellonema brachyurum)與帽狀紐帶線蟲(Hoplolaimus galeatus)。 The compounds of formula (I) are particularly suitable for controlling tree-crop nematodes, in particular: Pratylenchus penetrans, Pratylenchus vulnus, Meloidogyne arenaria, Northern nodule nematodes (Meloidogyne hapla), Meloidogyne javanica, Meloidogyne incognita, Criconemella xenoplax and Pratylenchus brachyurus, Pratylenchus coffeae, Pratylenchus scribneri, Pratylenchus zeae, Belonolaimus longicaudatus, Helicotylenchus dihystera, Xiphinema americanum, curved ringworm Criconemella curvata), Tylenchorhynchus claytoni, Paratylenchus hamatus, Paratylenchus projectus, Scutellonema brachyurum and Hoplolaimus galeatus.
式(I)化合物特別適合控制樹類作物、甘蔗與稻之線蟲,特定言之:毛刺線蟲屬(Trichodorus spp.)、環紋線蟲屬(Criconemella spp.)及短體線蟲屬(Pratylenchus spp.)、擬毛刺線蟲屬(Paratrichodorus spp.)、根瘤線蟲屬(Meloidogyne spp.)、螺旋線蟲屬(Helicotylenchus spp.)、矮化線蟲屬(Tylenchorhynchus spp.)、滑刃線蟲屬(Aphelenchoides spp.)、異皮線蟲屬(Heterodera spp.)、劍線蟲屬(Xiphinema spp.)與波斯固著線蟲(Cacopaurus pestis)。 The compounds of formula (I) are particularly suitable for controlling tree crops, sugar cane and rice worms, in particular: Trichodorus spp., Criconemella spp. and Pratylenchus spp. , Paratrichodorus spp., Meloidogyne spp., Helicopterus spp., Tylenchorhynchus spp., Aphelenchoides spp., different Heterodera spp., Xiphinema spp. and Cacopaurus pestis.
本文中,術語"線蟲"亦指會傷害人類或動物之線蟲。 As used herein, the term "nematode" also refers to nematodes that can harm humans or animals.
會傷害人類或動物之明確線蟲物種為:毛形亞目(Trichinellida),例如:毛首線蟲屬(Trichuris spp.)、毛細線蟲屬(Capillaria spp.)、毛細線蟲屬(Paracapillaria spp.),優鞘線蟲屬(Eucoleus spp.)、線蟲屬(Trichomosoides spp.)、旋毛蟲屬(Trichinella Spp.),墊刃目(Tylenchida),例如:細頸線蟲屬(Micronema spp.)、糞桿線蟲屬(Strongyloides spp.)小桿亞目(Rhabditina),例如:圓線蟲屬(Strongylus spp.)、三齒線蟲屬(Triodontophorus spp.)、食道齒線蟲屬(Oesophagodontus spp.)、毛線線蟲屬(Trichonema spp.)、輻首線蟲屬(Gyalocephalus spp.)、柱咽線蟲屬(Cylindropharynx spp.)、盆口線蟲屬(Poteriostomum spp.)、線蟲屬(Cyclococercus spp.)、杯冠線蟲屬(Cylicostephanus spp.)、食道口線蟲屬(Oesophagostomum spp.)、夏桕線蟲屬(Chabertia spp.)、冠尾線蟲屬(Stephanurus spp.)、鉤蟲屬(Ancylostoma spp.)、彎口線蟲屬(Uncinaria spp.)、鉤蟲屬(Necator spp.)、仰口線蟲屬(Bunostomum spp.)、球首線蟲屬(Globocephalus spp.)、比翼線蟲屬(Syngamus spp.)、節蟲屬(Cyathostoma spp.)、後圓線蟲屬(Metastrongylus spp.)、網尾線蟲屬(Dictyocaulus spp.)、繆勒線蟲屬(Muellerius spp.)、原圓線蟲屬(Protostrongylus spp.)、新圓線蟲屬(Neostrongylus spp.)、囊尾線蟲屬(Cystocaulus spp.)、肺圓線蟲屬(Pneumostrongylus spp.)、指尾線蟲屬(Spicocaulus spp.)、鹿圓線蟲屬(Elaphostrongylus spp.)、副麂圓線蟲屬(Parelaphostrongylus spp.)、環體線蟲屬(Crenosoma spp.)、副環體線蟲屬(Paracrenosoma spp.)、奧斯勒絲蟲屬(Oslerus spp.)、住血線蟲屬(Angiostrongylus spp.)、肺線蟲屬 (Aelurostrongylus spp.)、類絲線蟲屬(Filaroides spp.)、副類絲線蟲屬(Parafilaroides spp.)、毛圓線蟲屬(Trichostrongylus spp.)、血線蟲屬(Haemonchus spp.)、奧斯特線蟲屬(Ostertagia spp.)、牛胃絲蟲屬(Teladorsagia spp.)、馬歇爾線蟲屬(Marshallagia spp.)、古柏線蟲屬(Cooperia spp.)、日圓線蟲屬(Nippostrongylus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、細頸線蟲(Nematodirus spp.)、胃圓線蟲屬(Hyostrongylus spp.)、尖頭胃線蟲屬(Obeliscoides spp.)、裂口線蟲屬(Amidostomum spp.)、壺肛線蟲屬(Ollulanus spp.)旋尾目(Spirurida),例如:尖尾線蟲屬(Oxyuris spp.)、蟯蟲屬(Enterobius spp.)、栓尾線蟲屬(Passalurus spp.)、管狀線蟲屬(Syphacia spp.)、無刺蟯蟲屬(Aspiculuris spp.)、異刺線蟲屬(Heterakis spp.);蛔蟲屬(Ascaris spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、貝利蛔蟲屬(Baylisascaris spp.)、副蛔屬(Parascaris spp.)、海獸胃線蟲屬(Anisakis spp.)、禽蛔屬(Ascaridia spp.);棘口線蟲屬(Gnathostoma spp.)、泡翼線蟲屬(Physaloptera spp.)、吸吮線蟲屬(Thelazia spp.)、筒線蟲屬(Gongylonema spp.)、馬胃線蟲屬(Habronema spp.)、副柔絲線蟲屬(Parabronema spp.);德拉西線蟲屬(Draschia spp.)、龍線蟲屬(Dracunculus spp.);冠絲蟲屬(Stephanofilaria spp.)、類絲蟲屬(Parafilaria spp.)、絲狀線蟲屬(Setaria spp.)、羅阿絲蟲屬(Loa spp.)、血直絲蟲屬(Dirofilaria spp.)、光絲蟲屬(Litomosoides spp.)、布魯線蟲屬(Brugia spp.)、吳策絲蟲屬(Wuchereria spp.)、蟠尾絲蟲屬(Onchocerca spp.)、旋尾線蟲屬(Spirocerca spp.)。 The clear nematode species that can harm humans or animals are: Trichinellida, for example: Trichuris spp., Capillaria spp., Paracapillaria spp. Necoleus spp., Trichomosoides spp., Trichinella spp., Tylenchida, for example: Micronema spp., Fecal nematode ( Strongyloides spp.) Rhabditina, for example: Strongylus spp., Triodontophorus spp., Oesophagodontus spp., Trichonema spp. ), Gyalocephalus spp., Cylindropharynx spp., Poteriostomum spp., Cyclococercus spp., Cylicostephanus spp. Oesophagostomum spp., Chabertia spp., Stephanurus spp., Ancylostoma spp., Uncinaria spp., Hookworm (Necator spp.), Echinochloa (Bunostom) Um spp.), Globocephalus spp., Syngamus spp., Cyathostoma spp., Metastrongylus spp., Dictyocaulus spp .), Muellerius spp., Protostrongylus spp., Neostrongylus spp., Cystocaulus spp., Pneumostrongylus spp .), Spicocaulus spp., Elaphostrongylus spp., Parelaphostrongylus spp., Crenosoma spp., Parasitic nematode ( Paracrenosoma spp.), Oslerus spp., Angiostrongylus spp., L. (Aelurostrongylus spp.), Filaroides spp., Parafilaroides spp., Trichostrongylus spp., Haemonchus spp., Oster nematode Genus (Ostertagia spp.), genus Teladorsagia spp., Marshallagia spp., Cooperia spp., Nippostrongylus spp., Helicover Heligmosomoides spp.), Nematodirus spp., Hyostrongylus spp., Obeliscoides spp., Amidostomum spp., Ollulanus Spr.) Spirurida, for example: Oxyuris spp., Enterobius spp., Passalus spp., Syphacia spp., none Aspiculuris spp., Heterakis spp.; Ascaris spp., Toxascaris spp., Toxocara spp., Bailey aphid Genus (Baylisascaris spp.), Parascaris spp., Anisakis spp. ), Ascaridia spp.; Gnathostoma spp., Physaloptera spp., Thelazia spp., Gongylonema spp., horse Habronema spp., Parabronema spp.; Draschia spp., Dracunculus spp.; Stephanofilaria spp. Parafilaria spp., Setaria spp., Loa spp., Dirofilaria spp., Litomosoides spp. ), Brugia spp., Wuchereria spp., Onchocerca spp., Spirocerca spp.
許多種已知殺線蟲劑同樣對其他寄生性蠕蟲具有活性,因此可用於控制不一定屬於線蟲類之人類與動物之寄生蟲。本發明亦有關以式(I)化合物作為殺蠕蟲藥之用途。病原性體內寄生性蠕蟲包括扁形動物門 (Platyhelmintha)(例如:單殖吸蟲、絛蟲及吸蟲)、棘頭動物及舌形動物。較佳可述及下列蠕蟲:單殖吸蟲亞綱(Monogenea):例如:三代蟲屬(Gyrodactylus spp.)、指標蟲屬(Dactylogyrus spp.)、多盤吸蟲屬(Polystoma spp.);絛蟲:擬葉目(Pseudophyllidea),例如:廣節裂頭絛蟲屬(Diphyllobothrium spp.)、螺旋體蟲屬(Spirometra spp.)、裂頭絛蟲屬(Schistocephalus spp.)、舌狀絛蟲屬(Ligula spp.)、吸葉絛蟲屬(Bothridium spp.)、大複殖門絛蟲屬(Diphlogonoporus spp.);圓葉目(Cyclophyllida),例如:中殖孔屬絛蟲屬(Mesocestoides spp.)、裸頭絛蟲屬(Anoplocephala spp.)、副裸頭絛蟲屬(Paranoplocephala spp.)、莫尼茨絛蟲屬(Moniezia spp.)、隧體絛蟲屬(Thysanosoma spp.)、曲子官絛蟲屬(Thysaniezia spp.)、無卵黃腺絛蟲(Avitellina spp.)、史提拉絛蟲屬(Stilesia spp.)、錫帶絛蟲屬(Cittotaenia spp.)、安迪亞絛蟲屬(Andyra spp.)、伯特絛蟲屬(Bertiella spp.)、帶絛蟲屬(Taenia spp.)、棘球絛蟲屬(Echinococcus spp.)、泡尾絛蟲屬(Hydatigera spp.)、戴文絛蟲屬(Davainea spp.)、雷氏絛蟲屬(Raillietina spp.)、包膜絛蟲屬(Hymenolepis spp.)、瘍棘殼絛蟲屬(Echinolepis spp.)、棘葉絛蟲屬(Echinocotyle spp.)、迪克氏絛蟲屬(Diochis spp.)、瓜實絛蟲屬(Dipylidium spp.)、約優克斯絛蟲屬(Joyeuxiella spp.)、雙孔絛蟲屬(Diplopylidium spp.);吸蟲:複殖綱(Digenea),例如:複口吸蟲屬(Diplostomum spp.)、莖雙穴吸蟲屬(Posthodiplostomum spp.)、血吸蟲屬(Schistosoma spp.)、毛畢屬(Trichobilharzia spp.)、毛樣線蟲屬(Ornithobilharzia spp.)、澳畢吸蟲屬(Austrobilharzia spp.)、巨畢吸蟲屬(Gigantobilharzia spp.)、彩蚴吸蟲屬(Leucochloridium spp.)、短咽吸蟲屬(Brachylaima spp.)、棘口吸蟲屬 (Echinostoma spp.)、棘緣吸蟲屬(Echinoparyphium spp.)、棘隙吸蟲屬(Echinochasmus spp.)、低頸吸蟲屬(Hypoderaeum spp.)、肝吸蟲屬(Fasciola spp.)、擬片形吸蟲屬(Fasciolides spp.)、薑片蟲屬(Fasciolopsis spp.)、環腸吸蟲屬(Cyclocoelum spp.)、盲腔屬(Typhlocoelum spp.)、雙口吸蟲屬(Paramphistomum spp.)、杯殖吸蟲屬(Calicophoron spp.)、盤吸蟲屬(Cotylophoron spp.)、巨盤吸蟲屬(Gigantocotyle spp.)、菲策吸蟲屬(Fischoederius spp.)、腹袋吸蟲屬(Gastrothylacus spp.)、背孔吸蟲屬(Notocotylus spp.)、下彎吸蟲屬(Catatropis spp.)、斜睾吸蟲屬(Plagiorchis spp.)、前殖吸蟲屬(Prosthogonimus spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、闊盤吸蟲屬(Eurytrema spp.)、鮭吸蟲屬(Troglotrema spp.)、並殖吸蟲屬(Paragonimus spp.)、肛瘤吸蟲屬(Collyriclum spp.)、隱孔吸蟲屬(Nanophyetus spp.)、後睾吸蟲屬(Opisthorchis spp.)、支睪吸蟲屬(Clonorchis spp.)、次睾吸蟲屬(Metorchis spp.)、異形吸蟲屬(Heterophyes spp.)、後殖吸蟲屬(Metagonimus spp.);棘頭動物門(Acanthocephala):少棘目(Oligacanthorhynchida),例如:巨吻棘頭蟲屬(Macracanthorhynchus spp.)、前睾棘頭蟲屬(Prosthenorchis spp.);多形目(Polymorphida),例如:細頸棘頭蟲屬(Filicollis spp.);念珠目(Moniliformida),例如:聯珠狀棘頭蟲屬(Moniliformis spp.);棘吻目(Echinorhynchida),例如:棘頭蟲屬(Acanthocephalus spp.)、魚棘頭蟲屬(Echinorhynchus spp.)、似細吻棘頭蟲屬(Leptorhynchoides spp.);舌形動物門(Pentastoma):孔頭蟲目(Porocephalida),例如:舌形蟲屬(Linguatula spp.)。 Many known nematicides are also active against other parasitic helminths and can therefore be used to control parasites of humans and animals that are not necessarily nematodes. The invention also relates to the use of a compound of formula (I) as an anthelmintic. Pathogenic parasitic worms including flat animal gates (Platyhelmintha) (eg, monochomonas, aphids, and flukes), spines, and lingual animals. Preferably, the following helminths are mentioned: Monoogenea: for example: Gyrodactylus spp., Dactylogyrus spp., Polystoma spp.; Aphids: Pseudophyllidea, for example: Diphyllobothrium spp., Spirometra spp., Schistocephalus spp., Ligula spp. ), Bothridium spp., Diphlogonoporus spp.; Cyclophyllida, for example: Mesocestoides spp., Aphis genus Anoplocephala spp.), Paranoplocephala spp., Moniezia spp., Thysanosoma spp., Thysaniezia spp., yolk-free gland Avitellina spp., Stilesia spp., Cittotaenia spp., Andyra spp., Bertiella spp., belt Taenia spp., Echinococcus spp., Hydatigera spp .), Davainea spp., Raillietina spp., Hymenolepis spp., Echinolepis spp., Echinocotyle Spp.), Diochis spp., Dipylidium spp., Joyeuxiella spp., Diplopylidium spp.; trematode: complex Digenea, for example: Diplostomum spp., Posthodiplostomum spp., Schistosoma spp., Trichobilharzia spp., hairy Ornithobilharzia spp., Austrobilharzia spp., Gigantobilharzia spp., Leucochloridium spp., Brachylaima spp. ) (Echinostoma spp.), Echinoparyphium spp., Echinochasmus spp., Hypoderaeum spp., Fasciola spp., Fasciolides spp., Fasciolopsis spp., Cyclocoelum spp., Typhlocoelum spp., Paramphistomum spp. ), Calicophoron spp., Cotylophoron spp., Gigantocotyle spp., Fischoederius spp., Schistosoma (Gastrothylacus spp.), Notocotylus spp., Catatropis spp., Plagiorchis spp., Prosthogonimus spp. Dicrocoelium spp., Eurytrema spp., Troglotrema spp., Paragonimus spp., Collyriclum Spp.), Nanophyetus spp., Opisthorchis spp., Clonorchis spp., Metalschis spp., Alien Heterophyes spp., Metagonimus spp.; Acanthocephala: Oligacanthorhynchida, for example: Macracanthorhynchus spp. Prosthenorchis spp.; Polymorphida, for example: Filiocollis spp.; Moniliformida, for example: Moniliformis spp .); Echinorhynchida, for example: Acanthocephalus spp., Echinorhynchus spp., Leptorhynchoides spp.; (Pentastoma): Porocephalida, for example: Linguatula spp.
在獸醫與動物飼養領域中,式(I)化合物係呈合適之施用型式,採用相關技藝上已知方法投藥,直接投藥或依經腸、非經腸式、經皮 膚或經鼻投藥。該投藥法可為預防性或醫療性。 In the field of veterinary and animal husbandry, the compound of formula (I) is in a suitable application form, administered by methods known in the art, directly administered or by enteral, parenteral, transdermal Skin or nasal administration. The administration method can be prophylactic or medical.
式(I)化合物在某些濃度或施用率下,亦可視需要作為除草劑、安全劑、生長調節劑或改善植物性質之製劑、或作為殺微生物劑或殺配子劑使用,例如:殺真菌劑、抗霉劑、殺細菌劑、殺病毒劑(包括對抗類病毒之製劑)或作為對抗MLO(似黴漿菌生物體)與RLO(似立克次體生物體)之製劑。若適當時,其亦可作為合成其他活性化合物之中間物或前體使用。 The compounds of formula (I) may also be used as herbicides, safeners, growth regulators or formulations for improving the properties of plants, or as microbicides or gametocides, such as fungicides, at certain concentrations or application rates. , anti-fungal agents, bactericides, virucides (including anti-viral preparations) or as preparations against MLO (mycoplasma-like organisms) and RLO (like rickettsia organisms). If appropriate, it can also be used as an intermediate or precursor for the synthesis of other active compounds.
本發明進一步有關一種包含至少一種式(I)化合物之調配物及由其製成除害劑之施用形式,例如:浸液、滴液及噴液。有些例子中,該等施用形式可進一步包含其他除害劑與/或改良效用之佐劑,如:滲透劑,例如:植物油(例如:油菜籽油、葵花油)、礦物油(例如:石蠟油)、植物性脂肪酸之烷基酯類(例如:油菜籽油甲基酯或大豆油甲基酯)、或烷醇烷氧化物,與/或分佈劑,例如:烷基矽氧烷類,及/或鹽類,例如:有機或無機銨或鏻鹽類,例如:硫酸銨或磷酸氫二銨,與/或促進滯留劑,例如:磺基琥珀酸二辛酯或羥基丙基關華豆膠聚合物,與/或保濕劑,例如:甘油,與/或肥料,例如:含銨-、鉀-或磷之肥料。 The invention further relates to a formulation comprising at least one compound of the formula (I) and an application form from which the pesticide is made, for example, an infusion, a drip and a spray. In some instances, such application forms may further comprise other pesticides and/or improved utility adjuvants such as penetrants such as vegetable oils (eg, rapeseed oil, sunflower oil), mineral oils (eg, paraffin oil) An alkyl ester of a vegetable fatty acid (for example: rapeseed oil methyl ester or soybean oil methyl ester), or an alkanol alkoxide, and/or a distribution agent, such as an alkyl oxane, and / or salts, such as: organic or inorganic ammonium or phosphonium salts, such as: ammonium sulfate or diammonium hydrogen phosphate, and / or promote retention agents, such as: dioctyl sulfosuccinate or hydroxypropyl Guanhua gum A polymer, and/or a humectant, such as glycerin, and/or a fertilizer, such as a fertilizer containing ammonium, potassium or phosphorus.
常用調配物為例如:水溶性液體(SL)、乳化濃縮劑(EC)、水性乳液(EW)、懸浮濃縮劑(SC、SE、FS、OD)、水勻散性粒劑(WG)、粒劑(GR)及膠囊濃縮劑(CS);此等及其他可能調配物型態說明於例如:FAO/WHO農藥說明聯合會議(FAO/WHO Joint Meeting on Pesticide Specifications,2004,ISBN:9251048576)之”國際作物與農藥說明,FAO與WHO農藥發展與用法手冊,FAO植物生產與保護報告-173(Crop Life International and in Pesticide Specifications,Manual on development and use of FAO and WHO specifications for pesticides,FAO Plant Production and Protection Papers-173)”。除了一或多種式(I)化合物外,調配物中尚可視需要包含其他農化活性化合物。 Commonly used formulations are, for example, water-soluble liquid (SL), emulsified concentrate (EC), aqueous emulsion (EW), suspension concentrate (SC, SE, FS, OD), water-dispersible granules (WG), granules. Agent (GR) and capsule concentrate (CS); these and other possible formulation types are described, for example, in the FAO/WHO Joint Meeting on Pesticide Specifications (2004, ISBN: 9251048576) International Crop and Pesticides Description, FAO and WHO Pesticide Development and Usage Manual, FAO Plant Life and Development Report -173 (Crop Life International and in Pesticide Specifications, Manual on development and use Of FAO and WHO specifications for pesticides, FAO Plant Production and Protection Papers- 173)". In addition to one or more compounds of formula (I), other agrochemically active compounds may optionally be included in the formulation.
此等較佳係包含輔劑(例如:補充劑、溶劑、自發性促進劑、載劑、乳化劑、分散劑、霜害保護劑、殺生物劑、增稠劑與/或其他輔劑,例如:佐劑)之調配物或施用型式。本文中之佐劑係指可加強調配物生物效應,但本身沒有任何生物效應之組份。佐劑實例為促進滯留、分佈、附著葉表面或滲透之製劑。 These preferably comprise adjuvants (for example: supplements, solvents, spontaneous accelerators, carriers, emulsifiers, dispersants, frost protectants, biocides, thickeners and/or other adjuvants such as: The formulation or application pattern of the adjuvant). As used herein, an adjuvant refers to a component that can emphasize the biological effects of the ligand but does not have any biological effects per se. Examples of adjuvants are formulations that promote retention, distribution, attachment to leaf surfaces or penetration.
此等調配物係依已知方式製備,例如:混合式(I)化合物與輔劑,例如:補充劑、溶劑與/或固態載劑與/或其他輔劑,例如:界面活性劑。調配物係於合適設備中或於施用前或施用期間製造。 These formulations are prepared in a known manner, for example by mixing a compound of formula (I) with an adjuvant, for example a supplement, a solvent and/or a solid carrier and/or other adjuvants, for example a surfactant. Formulations are made in a suitable device or prior to or during administration.
所使用輔劑可為彼等對式(I)化合物之調配物或此等調配物所製成之施用型式(例如:現成可用之除害劑,如:噴灑液或拌種劑)賦與特殊性質,如:某些物理、技術與/或生物性質之物質。 The adjuvants used may be specially formulated for the formulation of the compound of formula (I) or the application form made of such formulations (for example: ready-to-use pesticides such as sprays or seed dressings) A property, such as a substance of some physical, technical, and/or biological nature.
合適之補充劑為例如:水、極性與非極性有機化學液體,例如:芳香系與非芳香系烴類(如:鏈烷烴、烷基苯、烷基萘、氯苯)、醇類與多元醇(若適當時,亦可經取代、醚化與/或酯化)、酮類(如:丙酮、環己酮)、酯類(包括脂肪類與油類)與(聚)醚類、未取代與經取代之胺類、醯胺類、內醯胺類(如:N-烷基吡咯啶酮)與內酯類、碸類與亞碸類(如:二甲亞碸)。 Suitable extenders are, for example, water, polar and non-polar organic chemical liquids such as aromatic and non-aromatic hydrocarbons (eg, paraffins, alkylbenzenes, alkylnaphthalenes, chlorobenzenes), alcohols and polyols. (Alternatively, substituted, etherified and/or esterified), ketones (eg acetone, cyclohexanone), esters (including fats and oils) and (poly)ethers, unsubstituted And substituted amines, guanamines, indoleamines (such as N-alkylpyrrolidone) and lactones, terpenoids and amidoxines (such as: dimethyl hydrazine).
若使用水作為補充劑時,亦可使用例如:有機溶劑作為輔助溶劑。基本上適用之液態溶劑為:芳香烴(如:二甲苯、甲苯、或烷基萘類)、氯化芳香烴或氯化脂族烴類(如:氯苯、氯化乙烯或二氯甲烷)、脂族烴類(如:環己烷或石蠟,例如:石油分餾物、礦物油與植物油)、醇類(如: 丁醇或二醇類,及其醚類與酯類)、酮類(如:丙酮、甲基乙基酮、甲基異丁基酮或環已酮)、強極性溶劑(如:二甲基甲醯胺與二甲亞碸),及水。 When water is used as a supplement, for example, an organic solvent can also be used as an auxiliary solvent. Substantially applicable liquid solvents are: aromatic hydrocarbons (eg xylene, toluene, or alkylnaphthalenes), chlorinated aromatic hydrocarbons or chlorinated aliphatic hydrocarbons (eg chlorobenzene, vinyl chloride or dichloromethane) , aliphatic hydrocarbons (such as: cyclohexane or paraffin, such as: petroleum fractions, mineral oils and vegetable oils), alcohols (such as: Butanol or glycols, and their ethers and esters), ketones (such as: acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone), strong polar solvents (such as: dimethyl Formamide and dimethyl hydrazine), and water.
原則上可能使用所有合適溶劑。合適溶劑實例為:芳香烴類(如:二甲苯、甲苯或烷基萘類)、氯化芳香烴與氯化脂族烴類(如:氯苯、氯化乙烯或二氯甲烷)、脂族烴類(如:環己烷、石蠟、石油分餾物、礦物油與植物油)、醇類(如:甲醇、乙醇、異丙醇、丁醇或二醇類及其醚類與酯類)、酮類(如:丙酮、甲基乙基酮、甲基異丁基酮或環已酮)、強極性溶劑(如:二甲亞碸),及水。 It is possible in principle to use all suitable solvents. Examples of suitable solvents are: aromatic hydrocarbons (eg xylene, toluene or alkylnaphthalenes), chlorinated aromatic hydrocarbons and chlorinated aliphatic hydrocarbons (eg chlorobenzene, vinyl chloride or dichloromethane), aliphatic Hydrocarbons (eg cyclohexane, paraffin, petroleum fractions, mineral oils and vegetable oils), alcohols (eg methanol, ethanol, isopropanol, butanol or glycols and their ethers and esters), ketones Classes (eg acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone), strong polar solvents (eg dimethyl hydrazine), and water.
原則上可能使用所有合適載劑。適用之載劑尤其包括例如:銨鹽及天然礦物磨粉,如:高嶺土、黏土、滑石、白堊、石英、矽鎂土、蒙脫土或矽藻土,及合成礦物粉末,如:高分散度矽石、氧化鋁與天然或合成矽酸鹽、樹脂、蠟類與/或固體肥料。亦可使用此等載劑之混合物。適用於粒劑之載劑包括例如:粉碎與分碎天然礦石,如:方解石、大理石、浮石、海泡石、白雲石,及無機與有機粉末之合成顆粒,及有機材料之顆粒如:鋸屑、紙、椰子殼、玉米穗軸與菸草稈。 It is possible in principle to use all suitable carriers. Suitable carriers include, for example, ammonium salts and natural mineral mills such as kaolin, clay, talc, chalk, quartz, strontium, montmorillonite or diatomaceous earth, and synthetic mineral powders such as high dispersion. Vermiculite, alumina and natural or synthetic silicates, resins, waxes and/or solid fertilizers. Mixtures of such carriers can also be used. Carriers suitable for granules include, for example, pulverized and divided natural ores such as calcite, marble, pumice, sepiolite, dolomite, and synthetic particles of inorganic and organic powders, and particles of organic materials such as sawdust, Paper, coconut shells, corn cobs and tobacco stalks.
亦可使用液化氣體補充劑或溶劑。特別適用者係彼等在標準溫度與標準壓力下呈氣態之補充劑或載劑,例如:氣霧劑推進劑氣體,如:鹵烴類及丁烷、丙烷、氮氣與二氧化碳。 Liquefied gas supplements or solvents can also be used. Particularly suitable are those supplements or carriers which are gaseous at standard temperature and standard pressure, such as: aerosol propellant gases such as halocarbons and butane, propane, nitrogen and carbon dioxide.
離子性或非離子性質乳化劑與/或泡沫形成劑、分散劑或濕化劑、或此等界面活性劑之混合物之實例為聚丙烯酸之鹽類、木質素磺酸之鹽類、苯酚磺酸或萘磺酸之鹽類、環氧乙烷與脂肪醇類或與脂肪酸或與脂肪胺、與經取代之苯酚(較佳為烷基苯酚或芳基苯酚)之聚縮合物、磺基琥珀酸酯之鹽類、牛磺酸衍生物(較佳係牛磺酸烷基酯)、聚乙氧基化醇或苯酚之磷酸酯、多元醇之脂肪酸酯,及包含硫酸根、磺酸根與磷酸根之化 合物之衍生物,例如:烷基芳基聚二醇醚類、烷基磺酸酯類、烷基硫酸酯類、芳基磺酸酯類、蛋白質水解物、木質素亞硫酸鹽廢液與甲基纖維素。若其中一種式(I)化合物與/或其中一種惰性載劑不可溶於水且當使用水施用時,宜包含界面活性劑。 Examples of ionic or nonionic emulsifiers and/or foam formers, dispersants or humidifiers, or mixtures of such surfactants are salts of polyacrylic acid, salts of lignosulfonic acid, phenolsulfonic acid Or a salt of naphthalenesulfonic acid, a polycondensate of ethylene oxide with a fatty alcohol or with a fatty acid or with an aliphatic amine, with a substituted phenol (preferably an alkylphenol or an arylphenol), sulfosuccinic acid a salt of an ester, a taurine derivative (preferably an alkyl taurate), a phosphate of a polyethoxylated alcohol or phenol, a fatty acid ester of a polyhydric alcohol, and a sulfate, a sulfonate and a phosphoric acid. Root Derivatives of the compounds, for example: alkyl aryl polyglycol ethers, alkyl sulfonates, alkyl sulfates, aryl sulfonates, protein hydrolysates, lignin sulfite waste liquids and Methylcellulose. If one of the compounds of formula (I) and/or one of the inert carriers is insoluble in water and when applied using water, it is preferred to include a surfactant.
可能存在於調配物及其所衍生之施用型式中之其他輔劑包括染劑,如:無機色素(例如:氧化鐵,氧化鈦與普魯士藍)與有機染劑(如:茜素染劑,偶氮染劑及金屬酞花青染劑),及營養素與微量營養素,如:鐵、錳、硼、銅、鈷、鉬與鋅之鹽類。 Other adjuvants that may be present in the formulation and the application form from which it is derived include dyes such as inorganic pigments (eg, iron oxide, titanium oxide and Prussian blue) and organic dyes (eg, alizarin dyes, even Nitrogen dyes and metal phthalocyanine dyes, and nutrients and micronutrients such as iron, manganese, boron, copper, cobalt, molybdenum and zinc.
其他組份可為安定劑,如:低溫安定劑、防腐劑、抗氧化劑、光安定劑或其他改善化學/物理安定性之製劑。亦可包含泡沫形成劑或消泡劑。 Other components may be stabilizers such as low temperature stabilizers, preservatives, antioxidants, light stabilizers or other agents that improve chemical/physical stability. A foam former or an antifoaming agent may also be included.
此外,調配物及其所衍生施用型式中亦可包含其他輔劑,膠黏劑,如:羧甲基纖維素、及天然與合成粉狀、粒狀或膠乳狀聚合物,如:阿拉伯膠、聚乙烯醇、聚乙酸乙烯酯,或天然磷脂類,如:腦磷脂與卵磷脂,及合成之磷脂類。其他可能輔劑為礦物油與植物油。 In addition, the formulation and its derived application form may also contain other adjuvants, such as carboxymethyl cellulose, and natural and synthetic powder, granule or latex polymers, such as: gum arabic, Polyvinyl alcohol, polyvinyl acetate, or natural phospholipids such as cephalin and lecithin, and synthetic phospholipids. Other possible adjuvants are mineral oils and vegetable oils.
調配物及其所衍生施用型式中亦可視需要包含其他輔劑。此等添加劑實例包括香料、保護性膠體、結合劑、黏著劑、增稠劑、搖變劑、滲透劑、促進滯留劑、安定劑、螯合劑、錯化劑、保濕劑、分佈劑。通常,式(I)化合物可配合調配目的,與任何常用之固態或液態添加劑組合使用。 Other adjuvants may also be included in the formulation and the forms of application from which it is derived. Examples of such additives include perfumes, protective colloids, binders, adhesives, thickeners, shakers, penetrants, retention retention agents, stabilizers, chelating agents, error agents, humectants, and distribution agents. In general, the compound of formula (I) can be used in combination with any conventional solid or liquid additive for the purpose of formulation.
適用之促進滯留劑包括所有彼等降低動力表面張力之物質,例如:磺基琥珀酸二辛酯,或提高黏彈性之物質,例如:羥基丙基關華豆膠聚合物。 Suitable promoting retention agents include all materials which reduce the dynamic surface tension, such as dioctyl sulfosuccinate, or substances which increase viscoelastic properties, such as hydroxypropyl croton gum polymers.
本文之合適滲透劑包括所有彼等常用於改善農化活性化 合物滲透進入植物中之所有物質。本文中,滲透劑之定義為其從(通常為水性)施用液體及/或從噴液層滲透進入植物表皮層並藉以提高活性化合物在表皮中移動性之能力。可採用文獻中說明之方法(Baur等人之1997,Pesticide Science 51,131-152)來測定此性質。其實例包括醇烷氧化物(如:椰子脂肪基乙氧化物(10)或異十三碳烷基乙氧化物(12))、脂肪酸酯類(例如:油菜籽油甲酯或大豆油甲酯)、脂肪胺烷氧化物(例如:獸脂胺乙氧化物(15))、或銨與/或鏻鹽類,例如:硫酸銨或磷酸氫二銨。 Suitable penetrants herein include all of them commonly used to improve agrochemical activation The compound penetrates into all the substances in the plant. As used herein, a penetrant is defined as the ability to apply a liquid from (usually aqueous) and/or from the spray layer into the plant skin layer and thereby increase the mobility of the active compound in the epidermis. This property can be determined by the method described in the literature (Baur et al. 1997, Pesticide Science 51, 131-152). Examples thereof include alcohol alkoxides (e.g., coconut fatty ethoxylate (10) or isotridecyl ethoxylate (12)), fatty acid esters (e.g., rapeseed oil methyl ester or soybean oil methyl ester) a fatty amine alkoxide (for example: tallow amine ethoxylate (15)), or an ammonium and/or phosphonium salt, for example ammonium sulphate or diammonium hydrogen phosphate.
調配物較佳係包含佔調配物重量0.00000001%至98%重量比之間之式(I)化合物,或特別佳係0.01%至95%重量比之式(I)化合物,更佳係0.5%至90%重量比之式(I)化合物。 Preferably, the formulation comprises a compound of formula (I) in an amount of from 0.00000001% to 98% by weight, based on the weight of the formulation, or particularly preferably from 0.01% to 95% by weight, based on the compound of formula (I), more preferably from 0.5% to 90% by weight of the compound of formula (I).
由調配物製成之施用型式(特定言之除害劑)中之式(I)化合物含量可在很大範圍內變化。施用型式中之式(I)化合物濃度通常佔該施用形式重量之0.00000001%至95%重量比,較佳在0.00001%至1%重量比。依適合此等施用型式之常用方式達成此應用。 The content of the compound of the formula (I) in the application form (specifically, the pesticide) made from the formulation can vary over a wide range. The concentration of the compound of the formula (I) in the application form is usually from 0.00000001% to 95% by weight, preferably from 0.00001% to 1% by weight, based on the weight of the application form. This application is achieved in the usual manner suitable for such application patterns.
式(I)化合物亦可與一種或多種合適之殺真菌劑、殺細菌劑、殺蜱蟎劑、殺軟體動物劑、殺線蟲劑、殺昆蟲劑、殺微生物劑、有利物質、除草劑、肥料、驅鳥劑、強化植物劑、不孕劑、安全劑、化學信息物質及/或植物生長調節劑形成混合物使用,藉以例如:擴大作用範圍、延長作用效期、提高作用速率、防止排斥或預防發展出抗性。此外,這種活性化合物組合可以改善植物生長及/或對非生物性因子之耐受性,例如:對高溫或低溫、對乾旱或對水份或鹽份含量上升之耐受性。亦可改善開花與結果性能、優化發芽能力與根部發展、促進收成及改善產量、影響成熟、改善所收成產物之品質與/或營養價值、為所收成產物延長儲存壽命及/或改 善可加工性。 The compound of formula (I) may also be combined with one or more suitable fungicides, bactericides, acaricides, molluscicides, nematicides, insecticides, microbicides, beneficial substances, herbicides, fertilizers Use of a mixture of bird repellents, fortified botanicals, infertility agents, safeners, chemical information substances and/or plant growth regulators, for example, to broaden the scope of action, extend the duration of action, increase the rate of action, prevent rejection or prevent Develop resistance. In addition, this combination of active compounds can improve plant growth and/or tolerance to abiotic factors, for example, to high or low temperatures, to drought or to increased moisture or salt content. It can also improve flowering and performance, optimize germination and root development, promote harvest and improve yield, affect maturity, improve the quality and/or nutritional value of harvested products, extend shelf life for harvested products and/or change Good workability.
此外,式(I)化合物可與其他活性化合物或化學信息物質(如:引誘劑與/或驅鳥劑與/或植物活化劑與/或生長調劑與/或肥料)形成混合物。同樣地,式(I)化合物可與改善植物性質(如,例如:生長、產量、及所收成材料之品質)之製劑形成混合物使用。 Furthermore, the compounds of the formula (I) may be admixed with other active compounds or chemical information substances, such as attractants and/or bird repellents and/or plant activators and/or growth regulators and/or fertilizers. Likewise, the compounds of formula (I) can be used in admixture with formulations which improve the properties of the plant, such as, for example, growth, yield, and quality of the material being harvested.
根據本發明特定具體實施例中,式(I)化合物係與其他化合物,較佳係與下文說明之化合物形成混合物而呈調配物型式或由該調配物製成之施用型式。 According to a particular embodiment of the invention, the compound of formula (I) is formed into a mixture with other compounds, preferably a compound described below, in the form of a formulation or an application form made from the formulation.
若下文述及之其中一種化合物可出現不同互變異構型,即使沒有個別出示,此等型式亦均包括在內。 If one of the compounds described below may exhibit different tautomeric forms, these forms are included even if not individually presented.
本文中以其俗名稱呼之活性化合物為已知者且說明於例如:除害劑手冊(“除害劑指南(The Pesticide Manual)”第16版,British Crop Protection Council 2012)或可參見網際網路(例如:http://www.alanwood.net/pesticides)。 Active compounds are referred to herein by their common names and are described, for example, in the Pesticides Manual ("Pesticide Manual", 16th Edition, British Crop Protection Council 2012) or can be found in the Internet (Example: http://www.alanwood.net/pesticides).
(1)乙醯基膽鹼酯酶(AChE)抑制劑,如,例如:胺甲酸酯類,例如:安利卡(alanycarb)、得滅克(aldicarb)、本得卡(bendiocarb)、本伏卡(benfuracarb)、布卡辛(butocarboxim)、丁氧布卡辛(buthoxycarboxim)、加保利(carbaryl)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、抑芬卡(ethiofencarb)、芬布卡(fenobucarb)、覆滅蟎(formetanate)、伏賽卡(furathiocarb)、滅必蝨(isoprocarb)、滅賜克(methiocarb)、納乃得(methomyl)、滅特卡(metolcarb)、歐殺滅(oxamyl)、比加普(pirimicarb)、安丹(propoxur)、硫敵克(thiodicarb)、硫芬斯(thiofanox)、三辛滅(triazamate)、三滅卡(trimethacarb)、XMC與滅爾蝨(xylylcarb);或有機磷 酸酯類,例如:歐殺松(acephate)、亞滅伏(azamethiphos)、谷速松(azinphos)-乙基、谷速松(azinphos)-甲基、卡速松(cadusafos)、氯乙松(chlorethoxyfos)、氯芬松(chlorfenvinphos)、氯滅松(chlormephos)、陶斯松(chlorpyrifos)、陶斯松(chlorpyrifos)-甲基、庫伏斯(coumaphos)、氰乃松(cyanophos)、滅賜松(demeton)-S-甲基、大利松(diazinon)、二氯松(dichlorvos)/DDVP、雙特松(dicrotophos)、大滅松(dimethoate)、大芬松(dimethylvinphos)、二硫松(disulfoton)、EPN、愛殺松(ethion)、普伏松(ethoprophos)、胺磺磷(famphur)、芬滅松(fenamiphos)、撲滅松(fenitrothion)、芬殺松(fenthion)、福賽特(fosthiazate)、飛達松(heptenophos)、抑滅伏(imicyafos)、抑伏松(isofenphos)、O-(甲氧基胺基硫代磷醯基)水楊酸異丙基酯、抑殺松(isoxathion)、馬拉松(malathion)、滅加松(mecarbam)、達馬松(methamidophos)、滅大松(methidathion)、美文松(mevinphos)、亞素靈(monocrotophos)、乃立松(naled)、歐滅松(omethoate)、歐滅賜松(oxydemeton)-甲基、巴拉松(parathion)、巴拉松(parathion)-甲基、賽達松(phenthoate)、福瑞松(phorate)、裕必松(phosalone)、益滅松(phosmet)、福賜米松(phosphamidon)、辛硫磷(phoxim)、亞特松(pirimiphos)-甲基、佈飛松(profenofos)、普丹松(propetamphos)、普硫松(prothiofos)、必伏松(pyraclofos)、必芬松(pyridaphenthion)、拜裕松(quinalphos)、速伏特(sulfotep)、特必松(tebupirimfos)、亞培松(temephos)、託福松(terbufos)、四氯松(tetrachlorvinphos)、硫滅松(thiometon)、三落松(triazophos)、三氯松(triclorfon)與繁米松(vamidothion)。 (1) Acetylcholinesterase (AChE) inhibitors, such as, for example, urethanes, for example: alanycarb, aldicarb, bendiocarb, Benfka (benfuracarb), butocarboxim, buthoxycarboxim, carbaryl, carbofuran, carbosulfan, ethiofencarb, fen Fenobucarb, formetanate, furathiocarb, isoprocarb, metiocarb, methomyl, metolcarb, killing (oxamyl), pirimicarb, propoxur, thiodicarb, thiofanox, triazamate, trimethacarb, XMC and sputum (xylylcarb); or organic phosphorus Acid esters, for example: acephate, azamethiphos, azinphos-ethyl, azinphos-methyl, cadusafos, chlorzene ( Chlorethoxyfos), chlorfenfos, chlormephos, chlorpyrifos, chlorpyrifos-methyl, coumaphos, cyanophos, demeton -S-methyl, diazinon, dichlorvos/DDVP, dicrotophos, dimethoate, dimethylvinphos, disulfoton, EPN , ethion, ethoprophos, famphur, fenamiphos, fenitrothion, fenthion, fosthiazate, fly Heptonenophos, imicyafos, isofenphos, O-(methoxyaminothiophosphonium) isopropyl salicylate, isoxathion, marathon (malathion), mecarbam, methamidophos, methidathion, mevinphos, monocrotophos, narcissus (naled), omethoate, oxydemeton-methyl, parathion, parathion-methyl, phenthoate, phorate ), phosalone, phosmet, phosphamidon, phoxim, pirimiphos-methyl, profenofos, and pudansong Propetamphos), prothiofos, pyraclofos, pyridaphenthion, quinalphos, sulfotep, tebupirimfos, temephos , terbufos, tetrachlorvinphos, thiometon, triazophos, triclofen and vamidothion.
(2)GABA-閘控之氯離子通道擷抗劑,例如:環二烯有機氯,例如:克丹(chlordane)與安殺番(endosulfan);或苯基吡唑類(飛普洛類(Fiprole)),例 如:抑普洛(ethiprole)與芬普洛(fipronil)。 (2) GABA-Gate-controlled chloride channel antagonists, for example: cyclodiene organochlorines, such as: chlordane and endosulfan; or phenylpyrazoles (feipulo ( Fiprole)), example Such as: ethiprole and fipronil.
(3)鈉通道調節劑/依賴電壓之鈉通道阻斷劑,如,例如:擬除蟲菊酯類,例如:阿納寧(acrinathrin)、丙烯菊酯(allethrin)、d-順式-反式丙烯菊酯(allethrin)、d-反式丙烯菊酯(allethrin)、畢芬寧(bifenthrin)、右亞列寧(bioallethrin)、右亞列寧(bioallethrin)S-環戊烯基異構物、必賽靈(bioresmethrin)、乙氰菊酯(cycloprothrin)、賽扶寧(cyfluthrin)、β-賽扶寧(cyfluthrin)、賽洛寧(cyhalothrin)、λ-賽洛寧(cyhalothrin)、γ-賽洛寧(cyhalothrin)、賽滅寧(cypermethrin)、α-賽滅寧(cypermethrin)、β-賽滅寧(cypermethrin)、θ-賽滅寧(cypermethrin)、ζ-賽滅寧(cypermethrin)、賽芬寧(cyphenothrin)[(1R)-反式異構物]、第滅寧(deltamethrin)、依普靈(empenthrin)[(EZ)-(1R)異構物]、益化利(esfenvalerate)、依芬寧(etofenprox)、芬普寧(fenpropathrin)、芬化利(fenvalerate)、福本賽寧(flucythrinate)、伏滅寧(flumethrin)、τ-福化利(fluvalinate)、海本斯(halfenprox)、益普靈(imiprothrin)、剋特寧(kadethrin)、百滅寧(permethrin)、芬特寧(phenothrin)[(1R)-反式異構物]、普烈靈(prallethrin)、除蟲菊酯(pyrethrins(pyrethrum))、利滅靈(resmethrin)、希拉芬(silafluofen)、特伏靈(tefluthrin)、特滅靈(tetramethrin)、特滅靈(tetramethrin)[(1R)異構物)]、泰滅寧(tralomethrin)與參伏靈(transfluthrin);或DDT;或美克氯(methoxychlor)。 (3) Sodium channel modulators/voltage-dependent sodium channel blockers, such as, for example, pyrethroids, for example: acrinathrin, allethrin, d-cis-trans Allethrin, allethrin, bifenthrin, bioallethrin, bioallethrin S-cyclopentenyl isomer, biscitron Bioresmethrin), cycloprothrin, cyfluthrin, cyfluthrin, cyhalothrin, cy- cyhalothrin, γ-cylonin ), cypermethrin, cypermethrin, cypermethrin, cypermethrin, cypermethrin, cyphenothrin ) [(1R)-trans isomer], deltamethrin, emtemphrin [(EZ)-(1R) isomer], esfenvalerate, efenine ( Etofenprox), fenpropathrin, fenvalerate, flucythrinate, flumethrin, τ-fuvalinate, halfenprox, Yipu (imiprothrin), kadethrin, permethrin, phenothrin [(1R)-trans isomer], prallethrin, pyrethrins (pyrethrins) Pyrethrum)), resmethrin, silafluofen, tefluthrin, tetramethrin, tetramethrin [(1R) isomer), typhine (tralomethrin) and transfluthrin; or DDT; or methoxychlor.
(4)菸鹼激導性乙醯基膽鹼受體(nAChR)促效劑,例如:類新菸鹼類,例如:乙醯普(acetamiprid)、克利定(clothianidin)、第諾芬(dinotefuran)、益達胺(imidacloprid)、尼普爛(nitenpyram)、硫克比(thiacloprid)與賽速安(thiamethoxam);或尼古丁或碸蟲啶(sulfoxaflor)。 (4) Nicotine-induced acetylcholine receptor (nAChR) agonists, such as neonicotinoids, for example: acetamiprid, clothianidin, dinotefuran ), imidacloprid, nitenpyram, thiacloprid and thiamethoxam; or nicotine or sulfoxaflor.
(5)菸鹼激導性乙醯基膽鹼受體(nAChR)之異位性活化劑,例如:賜諾殺類 (Spinosyns)、例如:賜諾特(spinetoram)與賜諾殺(spinosad)。 (5) Atopic activators of nicotine-induced acetylcholine receptor (nAChR), for example: (Spinosyns), for example: spinetoram and spinosad.
(6)氯離子通道活化劑,例如:抑滅克定類(avermectins)/美保黴素(milbemycin),例如:艾滅克定(abamectin)、抑滅克定(emamectin)苯甲酸鹽、利滅克定(lepimectin)與美保克定(milbemectin)。 (6) Chloride channel activators, for example: avermectins/milbemycin, for example: abamectin, emamectin benzoate, benefit Lepimectin and milbemectin.
(7)幼保激素擬似物,例如:幼保激素類似物,例如:赫普靈(hydroprene)、克普靈(kinoprene)與滅普靈(methoprene);或吩克卡(fenoxycarb);或必普芬(pyriproxyfen)。 (7) a juvenile hormone mimetic, such as a juvenile hormone analog, such as: hydroprene, kinoprene and metoprene; or fenoxycarb; Pypriroxyfen.
(8)作用機轉未知或非專一性之活性化合物,例如:烷基鹵化物,例如:甲基溴及其他烷基鹵化物;或氯吡靈(chloropicrin);或硫醯氟;或硼砂(borax);或酒石酸銻鉀鹽(tartar emetic)。 (8) active compounds which are undesired or non-specific, such as alkyl halides such as methyl bromide and other alkyl halides; or chloropicrin; or thiopurine; or borax ( Borax); or tartar emetic.
(9)選擇性抗攝食劑,例如:必滅辛(pymetrozine)或伏卡滅(flonicamid)。 (9) Selective antifeeding agents, for example, pymetrozine or flonicamid.
(10)蟎生長抑制劑,例如:克芬辛(clofentezine)、海賽唑(hexythiazox)與地伏辛(diflovidazin)或抑特唑(etoxazole)。 (10) Indole growth inhibitors, for example: clofentezine, hexythiazox and diflovidazin or etoxazole.
(11)昆蟲腸膜之微生物瓦解劑,例如:蘇雲金芽胞桿菌以色列亞種(Bacillus thuringiensis subspecies israelensis)、球形芽孢桿菌(Bacillus sphaericus)、蘇雲金芽胞桿菌鮎澤亞種(Bacillus thuringiensis subspecies aizawai)、蘇雲金芽胞桿菌庫斯塔基亞種(Bacillus thuringiensis subspecies kurstaki)、蘇雲金芽胞桿菌殺蟲亞種(Bacillus thuringiensis subspecies tenebrionis)與BT植物蛋白質:Cry1Ab、Cry1Ac、Cry1Fa、Cry2Ab、mCry3A、Cry3Ab、Cry3Bb、Cry34/35Ab1。 (11) Microbial resolving agents for insect intestinal membranes, for example, Bacillus thuringiensis subspecies israelensis , Bacillus sphaericus , Bacillus thuringiensis subspecies aizawai , Bacillus thuringiensis Bacillus thuringiensis subspecies kurstaki , Bacillus thuringiensis subspecies tenebrionis and BT plant proteins: Cry1Ab, Cry1Ac, Cry1Fa, Cry2Ab, mCry3A, Cry3Ab, Cry3Bb, Cry34/35Ab1.
(12)氧化性磷酸化反應抑制劑,ATP瓦解劑,例如:地芬能(diafenthiuron);或有機錫化合物,例如:亞賽錫(azocyclotin)、賽赫錫(cyhexatin)與芬塔錫(fenbutatin)氧化物;或歐蟎多(propargite)或特達芬(tetradifon)。 (12) oxidative phosphorylation inhibitor, ATP disintegrator, for example: diafenthiuron; or organotin compounds such as azocyclotin, cyhexatin and fenbutatin Oxide; or propargite or tetradifon.
(13)干擾H-質子梯度之氧化性磷酸化反應去偶合劑,例如:克芬吡 (chlorfenapyr)、DNOC與氟蟲胺(sulfluramid)。 (13) Oxidative phosphorylation reaction decoupling agent that interferes with the H-proton gradient, for example: kefenpyr (chlorfenapyr), DNOC and sulfluramid.
(14)菸鹼激導性乙醯基膽鹼受體擷抗劑,例如:本速達(bensultap)、培丹(cartap)鹽酸鹽、硫克蘭(thiocylam)與硫速伏(thiosultap)-鈉。 (14) Nicotine-induced acetylcholine receptor antagonists, for example, bensultap, cartap hydrochloride, thiocylam, and thiosultap- sodium.
(15)幾丁質生合成抑制劑,第0型,例如:必賽伏(bistrifluron)、克伏能(chlofluazuron)、地伏能(diflubenzuron)、福環脲(flucycloxuron)、氟芬隆(flufenoxuron)、赫姆能(hexaflumuron)、利芬能(lufenuron)、利化能(novaluron)、諾化能(noviflumuron)、特速能(teflubenzuron)與三伏能(triflumuron)。 (15) Chitin biosynthesis inhibitors, type 0, for example: bistrifluron, chlofluazuron, diflubenzuron, flucycloxuron, flufenoxuron, Hexaflumuron, lufenuron, novaluron, noviflumuron, teflubenzuron and triflumuron.
(16)幾丁質生合成抑制劑,第1型,例如:佈芬辛(buprofezin)。 (16) Chitin biosynthesis inhibitor, type 1, for example, buprofezin.
(17)蛻變抑制劑(特定言之雙翅目,亦即雙翅目昆蟲),如,例如:賽麻辛(cyromazine)。 (17) A mutated inhibitor (specifically, a Diptera, that is, a Diptera insect), such as, for example, cyromazine.
(18)脫皮激素受體促效劑,例如:可芬諾(chromafenozide)、赫芬賽(halofenozide)、甲氧芬賽(methoxyfenozide)與特芬賽(tebufenozide)。 (18) Opioid receptor agonists, for example, chromafenozide, hafenfenzide, methoxyfenozide, and tebufenozide.
(19)章魚胺激導性促效劑,例如:三亞蟎(amitraz)。 (19) Octopamine-induced agonist, for example: amitraz.
(20)複合物-III電子傳遞抑制劑,例如:海滅能(hydramethylnone)或亞克希(acequinocyl)或伏克靈(fluacrypyrim)。 (20) Complex-III electron transport inhibitors, for example, hydramethylnone or acequinocyl or fluacrypyrim.
(21)複合物-I電子傳遞抑制劑,例如:METI殺蟎劑,例如:芬殺蟎(fenazaquin)、芬普蟎(fenpyroximate)、普靈芬(pyrimidifen)、畢達本(pyridaben)、達芬必(tebufenpyrad)與特芬必(tolfenpyrad);或魚藤精(rotenone)(Derris)。 (21) Complex-I electron transport inhibitors, for example: METI acaricides, for example: fenazaquin, fenpyroximate, pyrimidifen, pyridaben, up to Tebufenpyrad and tolfenpyrad; or rotenone (Derris).
(22)電壓閘控之鈉通道阻斷劑,例如:因得克(indoxacarb)或滅伏美松(metaflumizone)。 (22) Voltage-gated sodium channel blockers, such as indoxacarb or metaflumizone.
(23)乙醯基-Co-A羧酸酶之抑制劑,例如:季酮酸與吡咯酮酸衍生物,例如:螺克芬(spirodiclofen)、螺滅芬(spiromesifen)與賜派滅(spirotetramat)。 (23) Inhibitors of acetyl-Co-A carboxylases, for example, quaternary keto acids and pyrrolidone derivatives, such as: spirodiclofen, spiromesifen, and spirotetramat ).
(24)複合物-IV電子傳遞抑制劑,例如:膦類,例如:磷化鋁、磷化鈣、膦與磷化鋅;或氰化物。 (24) Complex-IV electron transport inhibitors, for example: phosphines such as: aluminum phosphide, calcium phosphide, phosphine and zinc phosphide; or cyanide.
(25)複合物-II電子傳遞抑制劑,例如:氰必吩(cyenopyrafen)與賽芬蟎(cyflumetofen)。 (25) Complex-II electron transport inhibitors, for example, cyenopyrafen and cyflumetofen.
(28)蘭尼鹼(Ryanodine)受體效應劑,例如:二醯胺類,例如:氯蒽吡咯(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)與表氟蟲胺(flubendiamide),其他活性成份,例如:艾特本(afidopyropen)、查得定(azadirachtin)、苯克賽(benclothiaz)、苯賽滅(benzoximate)、必芬賽(bifenazate)、新殺蟎(bromomethylate)、蟎離丹(chinomethionat)、克利得(cryolite),大克蟎(dicofol)、氟蟎四嗪(diflovidazin)、氟速吩(fluensulfone)、氟喹啉(flometoquin)、伏吩靈(flufenerim)、氟菌蟎酯(flufenoxystrobin)、丁烯氟蟲腈(flufiprole)、氟吡菌醯胺(fluopyram)、伏達隆(flupyradifurone)、呋喃蟲醯肼(fufenozide)、氯氟醚菊酯(heptafluthrin)、氯噻啉(imidaclothiz)、依普同(iprodione)、氯氟醚菊酯(meperfluthrin)、哌蟲啶(paichongding)、必伏拜(pyflubumide)、必伏松(pyrifluquinazon)、嘧蟎胺(pyriminostrobin)、四氟醚菊酯(tetramethylfluthrin)與碘甲烷;及基於堅強芽孢桿菌(Bacillus firmus)之製劑(I-1582,BioNeem,Votivo),與下列化合物:3-溴-N-{2-溴-4-氯-6-[(1-環丙基乙基)胺甲醯基]苯基}-1-(3-氯吡啶-2-基)-1H-吡唑-5-羧醯胺(自WO2005/077934中已知)與1-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)亞磺醯基]苯基}-3-(三氟甲基)-1H-1,2,4-三唑-5-胺(自WO2006/043635中已知)、{1'-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]-5-氟螺[吲哚-3,4'-哌啶]-1(2H)-基}(2-氯吡啶-4-基)甲酮(自WO2003/106457中已知)、2-氯-N-[2-{1-[(2E)-3-(4-氯苯基)丙-2-烯-1-基]哌啶-4-基}-4-(三氟甲基)苯基]異菸鹼醯胺(自 WO2006/003494中已知)、3-(2,5-二甲基苯基)-4-羥基-8-甲氧基-1,8-重氮螺[4.5]癸-3-烯-2-酮(自WO2009/049851中已知)、碳酸3-(2,5-二甲基苯基)-8-甲氧基-2-側氧基-1,8-重氮螺[4.5]癸-3-烯-4-基-乙基酯(自WO2009/049851中已知)、4-(丁-2-炔-1-基氧)-6-(3,5-二甲基哌啶-1-基)-5-氟嘧啶(自WO2004/099160中已知)、4-(丁-2-炔-1-基氧)-6-(3-氯苯基)嘧啶(自WO2003/076415中已知)、PF1364(CAS登錄號1204776-60-2)、4-[5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基]-2-甲基-N-{2-側氧基-2-[(2,2,2-三氟乙基)胺基]乙基}苯甲醯胺(自WO2005/085216中已知)、4-{5-[3-氯-5-(三氟甲基)苯基]-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基}-N-{2-側氧基-2-[(2,2,2-三氟乙基)胺基]乙基}-1-萘甲醯胺(自WO2009/002809中已知)、2-[2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)-5-氯-3-甲基苯甲醯基]-2-甲基肼羧酸甲酯(自WO2005/085216中已知)、2-[2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)-5-氰基-3-甲基苯甲醯基]-2-乙基肼羧酸甲酯(自WO2005/085216中已知)、2-[2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)-5-氰基-3-甲基苯甲醯基]-2-甲基肼羧酸甲酯(自WO2005/085216中已知)、2-[3,5-二溴-2-({[3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-基]羰基}胺基)苯甲醯基]-2-乙基肼羧酸甲酯(自WO2005/085216中已知)、1-(3-氯吡啶-2-基)-N-[4-氰基-2-甲基-6-(甲基胺甲醯基)苯基]-3-{[5-(三氟甲基)-2H-四唑-2-基]甲基}-1H-吡唑-5-羧醯胺(自WO2010/069502中已知)、N-[2-(5-胺基-1,3,4-噻二唑-2-基)-4-氯-6-甲基苯基]-3-溴-1-(3-氯吡啶-2-基)-1H-吡唑-5-羧醯胺(自CN102057925中已知)、3-氯-N-(2-氰基丙烷-2-基)-N-[4-(1,1,1,2,3,3,3-七氟丙烷-2-基)-2-甲基苯基]酞醯胺(自WO2012/034472中已知)、8-氯-N-[(2-氯-5-甲氧基苯基)磺醯基]-6-(三氟甲基)咪唑并[1,2-a]吡啶-2-羧醯胺(自WO2010/129500中已知)、 4-[5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基]-2-甲基-N-(1-氧離子基硫雜環丁烷-3-基)苯甲醯胺(自WO2009/080250中已知)、4-[5-(3,5-二氯苯基)-5-(三氟甲基)-4,5-二氫-1,2-唑-3-基]-2-甲基-N-(1-氧離子基硫雜環丁烷-3-基)苯甲醯胺(自WO2012/029672中已知)、1-[(2-氯-1,3-噻唑-5-基)甲基]-4-側氧基-3-苯基-4H-吡啶并[1,2-a]嘧啶-1-鎓-2-醇酸鹽(自WO2009/099929中已知)、1-[(6-氯吡啶-3-基)甲基]-4-側氧基-3-苯基-4H-吡啶并[1,2-a]嘧啶-1-鎓-2-醇酸鹽(自WO2009/099929中已知)、(5S,8R)-1-[(6-氯吡啶-3-基)甲基]-9-硝基-2,3,5,6,7,8-六氫-1H-5,8-環氧咪唑并[1,2-a]氮雜環庚烯(自WO2010/069266中已知)、(2E)-1-[(6-氯吡啶-3-基)甲基]-N'-硝基-2-亞戊基肼甲脒(自WO2010/060231中已知)、4-(3-{2,6-二氯-4-[(3,3-二氯丙-2-烯-1-基)氧]苯氧基}丙氧基)-2-甲氧基-6-(三氟甲基)嘧啶(自CN101337940中已知)、N-[2-(第三丁基胺甲醯基)-4-氯-6-甲基苯基]-1-(3-氯吡啶-2-基)-3-(氟甲氧基)-1H-吡唑-5-羧醯胺(自WO2008/134969中已知)。 (28) Ryanodine receptor effector, for example, diamines, for example, chlorantraniliprole, cyantraniliprole and flubendiamide, other active ingredients, For example: afidopyropen, azadirachtin, benclothiaz, benzoximate, bifenazate, bromomethylate, chinomethionat , cryolite, dicofol, diflovidazin, fluensulfone, flometoquin, flufenerim, flufenoxystrobin , flufiprole, fluopyram, flupyradifurone, fufenozide, heptafluthrin, imidaclothiz, Iprodione, meperfluthrin, paichongding, pyflubumide, pyrifluquinazon, pyriminostrobin, tetrafluthrin Tetramethylfluthrin) with methyl iodide; and based on Bacillus firm Us) formulation (I-1582, BioNeem, Votivo), with the following compound: 3-bromo-N-{2-bromo-4-chloro-6-[(1-cyclopropylethyl)aminecarbamyl] Phenyl}-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide (known in WO2005/077934) and 1-{2-fluoro-4-methyl-5 -[(2,2,2-trifluoroethyl)sulfinyl]phenyl}-3-(trifluoromethyl)-1H-1,2,4-triazole-5-amine (from WO2006/ Known in 043635), {1'-[(2E)-3-(4-chlorophenyl)prop-2-en-1-yl]-5-fluorospiro[吲哚-3,4'-piperidine -1(2H)-yl}(2-chloropyridin-4-yl)methanone (known from WO2003/106457), 2-chloro-N-[2-{1-[(2E)-3- (4-Chlorophenyl)prop-2-en-1-yl]piperidin-4-yl}-4-(trifluoromethyl)phenyl]isonicotinamide (known from WO2006/003494) , 3-(2,5-Dimethylphenyl)-4-hydroxy-8-methoxy-1,8-diazospiro[4.5]indole-3-en-2-one (from WO 2009/049851) 3-(2,5-Dimethylphenyl)-8-methoxy-2-oxo-1,8-diazospiro[4.5]indol-3-yl-4-yl carbonate -ethyl ester (known from WO 2009/049851), 4-(but-2-yn-1-yloxy)-6-(3,5-dimethylpiperidin-1-yl)-5-fluoro Pyrimidine (known from WO2004/099160), 4-(but-2-yn-1-yloxy)-6-(3-chlorophenyl)pyrimidine (known from WO2003/076415), PF 1364 (CAS Accession No. 1204776-60-2), 4-[5-(3,5-Dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2- Zyrid-3-yl]-2-methyl-N-{2-p-oxy-2-[(2,2,2-trifluoroethyl)amino]ethyl}benzamide (from WO2005/ Known in 085216), 4-{5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2- Zyrid-3-yl}-N-{2-p-oxy-2-[(2,2,2-trifluoroethyl)amino]ethyl}-1-naphthylguanamine (from WO 2009/002809) Known), 2-[2-({[3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazol-5-yl]carbonyl}amino)-5-chloro-3- Methyl benzhydryl]-2-methylindolecarboxylate (known in WO2005/085216), 2-[2-({[3-bromo-1-(3-chloropyridin-2-yl) -1H-pyrazol-5-yl]carbonyl}amino)-5-cyano-3-methylbenzylidene]-2-ethylindolecarboxylic acid methyl ester (known from WO2005/085216) 2-[2-({[3-Bromo-1-(3-chloropyridin-2-yl)-1H-pyrazol-5-yl]carbonyl}amino)-5-cyano-3-methyl Methyl benzhydryl]-2-methylindolecarboxylate (known in WO2005/085216), 2-[3,5-dibromo-2-({[3-bromo-1-(3-chloro) Methyl pyridin-2-yl)-1H-pyrazol-5-yl]carbonyl}amino)benzimidyl]-2-ethylindolecarboxylate (known from WO2005/085216), 1-(3) -chloropyridin-2-yl)-N-[4-cyano-2-methyl-6-(methylamine-mercapto)phenyl]-3-{[5-(trifluoromethyl)-2H -tetrazol-2-yl]methyl}-1H-pyrazole-5-carboxamide (known from WO2010/069502), N-[2-(5-amino-1,3,4-thia Diazol-2-yl)-4-chloro-6-methylphenyl]-3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxamide (from CN102057925 in Know), 3-chloro-N-(2-cyanopropan-2-yl)-N-[4-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)-2- Methylphenyl]decylamine (known from WO2012/034472), 8-chloro-N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl) Imidazo[1,2-a]pyridine-2-carboxamide (known from WO2010/129500), 4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl) )-4,5-dihydro-1,2- Zyrid-3-yl]-2-methyl-N-(1-oxo-oxathiolan-3-yl)benzamide (known in WO2009/080250), 4-[5-( 3,5-dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2- Zyrid-3-yl]-2-methyl-N-(1-oxo-oxathiolan-3-yl)benzamide (known from WO2012/029672), 1-[(2- Chloro-1,3-thiazol-5-yl)methyl]-4-oxo-3-phenyl-4H-pyrido[1,2-a]pyrimidin-1-indole-2-alkanoate ( Known from WO2009/099929), 1-[(6-chloropyridin-3-yl)methyl]-4-oxo-3-phenyl-4H-pyrido[1,2-a]pyrimidine- 1-non-2-alkanoate (known from WO2009/099929), (5S,8R)-1-[(6-chloropyridin-3-yl)methyl]-9-nitro-2,3 ,5,6,7,8-hexahydro-1H-5,8-epoxyimidazo[1,2-a]azepane (known from WO2010/069266), (2E)-1- [(6-chloropyridin-3-yl)methyl]-N'-nitro-2-pentanylguanidinium (known from WO2010/060231), 4-(3-{2,6-di Chloro-4-[(3,3-dichloroprop-2-en-1-yl)oxy]phenoxy}propoxy)-2-methoxy-6-(trifluoromethyl)pyrimidine Known in CN101337940), N-[2-(t-butylaminomethylmercapto)-4-chloro-6-methylphenyl]-1-(3-chloropyridin-2-yl)-3-( Fluoromethoxy)-1H-pyrazole-5-carboxamide (known in WO 2008/134969).
本文中以其俗名稱呼之活性化合物為已知者且說明於例如:“除害劑指南(The Pesticide Manual)“或網際網路(例如:http://www.alanwood.net/pesticides)。 Active compounds which are referred to herein by their common names are known and are described, for example, in "The Pesticide Manual" or the Internet (for example: http://www.alanwood.net/pesticides).
(1)麥角固醇生合成抑制劑,例如:(1.1)艾狄莫(aldimorph)、(1.2)阿克唑(azaconazole)、(1.3)拜坦諾(bitertanol)、(1.4)布康唑(bromuconazole)、(1.5)西普康唑(cyproconazole)、(1.6)二氯丁唑(diclobutrazole)、(1.7)地吩康唑(difenoconazole)、(1.8)地康唑(diniconazole)、(1.9)地康唑-M(diniconazole-M)、(1.10)得莫(dodemorph)、(1.11)得莫乙酸鹽(dodemorph acetate)、(1.12)環氧克唑(epoxiconazole)、(1.13)抑達唑 (etaconzole)、(1.14)芬利莫(fenarimol)、(1.15)芬康唑(fenbuconazole)、(1.16)吩醯胺(fenhexamide)、(1.17)芬普定(fenpropidin)、(1.18)芬普福(fenpropimorph)、(1.19)伏克康唑(fluquinconazole)、(1.20)伏米得(flurprimidol)、(1.21)護矽得(flusilazole)、(1.22)護汰芬(flutriafol)、(1.23)伏康唑(furconazole)、(1.24)順式伏康唑(furconazole-cis))、(1.25)赫康唑(hexaconazole)、(1.26)依滅列(imazalil)、(1.27)依滅列硫酸鹽(imazalil sulphate)、(1.28)抑本康唑(imibenconazole)、(1.29)抑普康唑(ipconazole)、(1.30)滅康唑(metconazole)、(1.31)麥克坦尼(myclobutanil)、(1.32)納得吩(naftifin)、(1.33)紐莫(nuarimol)、(1.34)康唑(oxpoconazole)、(1.35)巴克素(paclobutrazole)、(1.36)比菲唑(pefurazoate)、(1.37)本康唑(penconazole)、(1.38)哌布靈(piperalin)、(1.39)撲克樂(prochloraz)、(1.40)普克利(propiconazole)、(1.41)普賽康唑(prothioconazole)、(1.42)必達克(pyributicarb)、(1.43)比芬斯(pyrifenox)、(1.44)克康唑(quinconazole)、(1.45)辛康唑(simeconazole)、(1.46)賜必安(spiroxamine)、(1.47)得克利(tebuconazole)、(1.48)特本吩(terbinafin)、(1.49)特康唑(tetraconazole)、(1.50)三泰芬(triadimefon)、(1.51)三泰隆(triadimenol)、(1.52)賽得莫(tridemorph)、(1.53)三伏唑(triflumizol)、(1.54)賽福寧(triforine)、(1.55)三狄康唑(triticonazole)、(1.56)優康唑(uniconazole)、(1.57)優康唑-P(uniconazol-P)、(1.58)芬克唑(viniconazole)、(1.59)福康唑(voriconazole)、(1.60)1-(4-氯苯基)-2-(1H-1,2,4-三唑-1-基)環庚醇、(1.61)1-(2,2-二甲基-2,3-二氫-1H-茚-1-基)-1H-咪唑-5-羧酸甲酯、(1.62)N'-{5-(二氟甲基)-2-甲基-4-[3-(三甲基矽烷基)丙氧基]苯基}-N-乙基-N-甲基甲脒、(1.63)N-乙基-N-甲基-N'-{2-甲基-5-(三氟甲基)-4-[3-(三甲基矽烷基)丙氧基]苯基}甲脒與 (1.64)O-[1-(4-甲氧基苯氧基)-3,3-二甲基丁烷-2-基]-1H-咪唑-1-硫代甲酸酯、(1.65)啶菌唑(pyrisoxazole)。 (1) ergosterol biosynthesis inhibitors, for example: (1.1) aldimorph, (1.2) azaconazole, (1.3) bitertanol, (1.4) butoconazole (bromuconazole), (1.5) cyproconazole, (1.6) diclobutrazole, (1.7) difenoconazole, (1.8) diconazole, (1.9) Diconicon-M, (1.10) dodemorph, (1.11) dodemorph acetate, (1.12) epoxiconazole, (1.13) statazole ( Etaconzole), (1.14) fenarimol, (1.15) fenbuconazole, (1.16) fenhexamide, (1.17) fenpropidin, (1.18) fenfluz ( Fenpropimorph), (1.19) fluquinconazole, (1.20) flurprimidol, (1.21) flusilazole, (1.22) flutriafol, (1.23) fluconazole (furconazole), (1.24) fluconazole-cis, (1.25) hexaconazole, (1.26) imazalil, (1.27) ima sulphate (imazalil sulphate) ), (1.28) imibenconazole, (1.29) fepconazole (ipcon) Azole, (1.30) metconazole, (1.31) myclobutanil, (1.32) naftifin, (1.33) nuarimol, (1.34) Oxpoconazole, (1.35) paclobutrazole, (1.36) pefurazoate, (1.37) penconazole, (1.38) piperalin, (1.39) poker (prochloraz), (1.40) propiconazole, (1.41) prothioconazole, (1.42) pyributicarb, (1.43) pyrifenox, (1.44) claconazole ( Quinconazole), (1.45) simeconazole, (1.46) spiroxamine, (1.47) tebuconazole, (1.48) terbinafin, (1.49) terconazole ), (1.50) triadimefon, (1.51) triadimenol, (1.52) tridemorph, (1.53) triflumizol, (1.54) triforine, (1.55) triticonazole, (1.56) uniconazole, (1.57) euconazole-P (uniconazol-P), (1.58) viniconazole, (1.59) Fukang Voriconazole, (1.60) 1-(4-chlorophenyl)-2-(1H-1,2,4-triazol-1-yl)cycloheptanol, (1.61) 1-(2,2- Methyl dimethyl-2,3-dihydro-1H-indol-1-yl)-1H-imidazole-5-carboxylate, (1.62) N'-{5-(difluoromethyl)-2-methyl Base-4-[3-(three矽alkyl)propoxy]phenyl}-N-ethyl-N-methylformamidine, (1.63) N-ethyl-N-methyl-N'-{2-methyl-5-(trifluoro Methyl)-4-[3-(trimethyldecyl)propoxy]phenyl}formamidine with (1.64)O-[1-(4-methoxyphenoxy)-3,3-di Methylbutan-2-yl]-1H-imidazole-1-thioformate, (1.65) pyrisoxazole.
(2)呼吸抑制劑(呼吸鏈抑制劑),例如:(2.1)必賽吩(bixafen)、(2.2)保卡利(boscalid)、(2.3)卡布辛(carboxin)、(2.4)地伏滅靈(diflumetorim)、(2.5)芬伏爛(fenfuram)、(2.6)護派楠(fluopyram)、(2.7)護坦尼(flutolanil)、(2.8)護賽保(fluxapyroxad)、(2.9)福滅普(furametpyr)、(2.10)福滅克(furmecyclox)、(2.11)抑本散(isopyrazam)之順-差向異構體消旋物1RS,4SR,9RS與反-差向異構體消旋物1RS,4SR,9SR混合物、(2.12)抑本散(isopyrazam)(反-差向異構體消旋物)、(2.13)抑本散(isopyrazam)(反-差向異構體對映異構物1R,4S,9S)、(2.14)抑本散(isopyrazam)(反-差向異構體對映異構物1S,4R,9R)、(2.15)抑本散(isopyrazam)(順-差向異構體消旋物1RS,4SR,9RS)、(2.16)抑本散(isopyrazam)(順-差向異構體對映異構物1R,4S,9R)、(2.17)抑本散(isopyrazam)(順-差向異構體對映異構物1S,4R,9S)、(2.18)米普尼(mepronil)、(2.19)嘉得信(oxycarboxin)、(2.20)本福吩(penflufen)、(2.21)本賽能(penthiopyrad)、(2.22)速達散(sedaxane)、(2.23)地伏醯胺(thifluzamid)、(2.24)1-甲基-N-[2-(1,1,2,2-四氟乙氧基)苯基]-3-(三氟甲基)-1H-吡唑-4-羧醯胺、(2.25)3-(二氟甲基)-1-甲基-N-[2-(1,1,2,2-四氟乙氧基)苯基]-1H-吡唑-4-羧醯胺、(2.26)3-(二氟甲基)-N-[4-氟-2-(1,1,2,3,3,3-六氟丙氧基)苯基]-1-甲基-1H-吡唑-4-羧醯胺、(2.27)N-[1-(2,4-二氯苯基)-1-甲氧基丙烷-2-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(2.28)5,8-二氟-N-[2-(2-氟-4-{[4-(三氟甲基)吡啶-2-基]氧}苯基)乙基]喹唑啉-4-胺、(2.29)苯索伏比(benzovindiflupyr)、(2.30)N-[(1S,4R)-9-(二氯亞甲基)-1,2,3,4-四氫-1,4-甲撐基萘-5-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺與(2.31)N-[(1R,4S)-9-(二氯亞甲基)-1,2,3,4-四氫-1,4-甲撐基萘-5-基]-3-(二氟 甲基)-1-甲基-1H-吡唑-4-羧醯胺、(2.32)3-(二氟甲基)-1-甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(2.33)1,3,5-三甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(2.34)1-甲基-3-(三氟甲基)-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(2.35)1-甲基-3-(三氟甲基)-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.36)1-甲基-3-(三氟甲基)-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.37)3-(二氟甲基)-1-甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.38)3-(二氟甲基)-1-甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.39)1,3,5-三甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.40)1,3,5-三甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(2.41)麥鏽靈(benodanil)、(2.42)2-氯-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)吡啶-3-羧醯胺、(2.43)抑吩滅(isofetamid)。 (2) Respiratory inhibitors (respiratory chain inhibitors), for example: (2.1) bixafen, (2.2) boscalid, (2.3) carboxin, (2.4) Diflumetorim, (2.5) fenfuram, (2.6) fluopyram, (2.7) flutolanil, (2.8) fluxapyroxad, (2.9) Furametpyr, (2.10) furmecyclox, (2.11) isoprozol cis-epimer racemate 1RS, 4SR, 9RS and anti-epimer elimination Spin 1RS, 4SR, 9SR mixture, (2.12) isopyrazam (trans-epimer racemate), (2.13) isopyrazam (anti-epimer alignment) Isomers 1R, 4S, 9S), (2.14) Isoprozam (anti-epimer enantiomers 1S, 4R, 9R), (2.15) Isoproza (isopyrazam) - Epimer racemate 1RS, 4SR, 9RS), (2.16) Isoprozam (cis-epimomer enantiomers 1R, 4S, 9R), (2.17) Isopyrazam (cis-epimomer enantiomers 1S, 4R, 9S), (2.18) mepronil, (2.19) oxycarboxin, (2.20) Benfu (penflufen), (2.21) this game (penthio Pyrad), (2.22) sedaxane, (2.23) flufluzamid, (2.24) 1-methyl-N-[2-(1,1,2,2-tetrafluoroethoxy) Phenyl]-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide, (2.25) 3-(difluoromethyl)-1-methyl-N-[2-(1, 1,2,2-tetrafluoroethoxy)phenyl]-1H-pyrazole-4-carboxamide, (2.26) 3-(difluoromethyl)-N-[4-fluoro-2-(1) ,1,2,3,3,3-hexafluoropropoxy)phenyl]-1-methyl-1H-pyrazole-4-carboxamide, (2.27) N-[1-(2,4- Dichlorophenyl)-1-methoxypropan-2-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide, (2.28) 5,8- Difluoro-N-[2-(2-fluoro-4-{[4-(trifluoromethyl)pyridin-2-yl]oxy}phenyl)ethyl]quinazolin-4-amine, (2.29) Benzovindiflupyr, (2.30) N-[(1S,4R)-9-(dichloromethylene)-1,2,3,4-tetrahydro-1,4-methylenenaphthalene- 5-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide and (2.31) N-[(1R,4S)-9-(dichloromethylene )-1,2,3,4-tetrahydro-1,4-methylenenaphthalen-5-yl]-3-(difluoro Methyl)-1-methyl-1H-pyrazole-4-carboxamide, (2.32) 3-(difluoromethyl)-1-methyl-N-(1,1,3-trimethyl- 2,3-Dihydro-1H-indol-4-yl)-1H-pyrazole-4-carboxamide, (2.33) 1,3,5-trimethyl-N-(1,1,3-three Methyl-2,3-dihydro-1H-indol-4-yl)-1H-pyrazole-4-carboxamide, (2.34) 1-methyl-3-(trifluoromethyl)-N-( 1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl)-1H-pyrazole-4-carboxamide, (2.35) 1-methyl-3-(trifluoro) Methyl)-N-[(3R)-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.36 1-methyl-3-(trifluoromethyl)-N-[(3S)-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H- Pyrazole-4-carboxyguanamine, (2.37) 3-(difluoromethyl)-1-methyl-N-[(3S)-1,1,3-trimethyl-2,3-dihydro- 1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.38) 3-(difluoromethyl)-1-methyl-N-[(3R)-1,1,3- Trimethyl-2,3-dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.39) 1,3,5-trimethyl-N-[(3R) -1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.40) 1,3,5-trimethyl -N-[(3S)-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.41) wheat rust Spirit (benodanil), (2.42) 2-chloro-N-(1,1,3-trimethyl -2,3-Dihydro-1H-indol-4-yl)pyridine-3-carboxamide, (2.43) isofetamid.
(3)作用於呼吸鏈複合物III之呼吸抑制劑(呼吸鏈抑制劑),例如:(3.1)辛唑嘧菌胺(ametoctradin)、(3.2)安美速(amisulbrom)、(3.3)亞托敏(azoxystrobin)、(3.4)賽發滅(cyazofamid)、(3.5)甲香菌酯(coumethoxystrobin)、(3.6)丁香菌酯(coumoxystrobin)、(3.7)醚菌胺(dimoxystrobin)、(3.8)烯肟菌酯(enestroburin)、(3.9)芬色丹(famoxadone)、(3.10)芬滅酮(fenamidone)、(3.11)吩嘧菌酯(flufenoxystrobin)、(3.12)氟嘧菌酯(fluoxastrobin)、(3.13)甲基醚菌酯(kresoxim-methyl)、(3.14)苯氧菌胺(metominostrobin)、(3.15)肟醚菌胺(orysastrobin)、(3.16)啶氧菌酯(picoxystrobin)、(3.17)唑菌胺酯(pyraclostrobin)、(3.18)唑胺菌酯(pyrametostrobin)、(3.19)唑菌酯(pyraoxystrobin)、(3.20)吡菌苯威(pyribencarb)、(3.21)三氯比(triclopyricarb)、(3.22)三氟敏(trifloxystrobin)、 (3.23)(2E)-2-(2-{[6-(3-氯-2-甲基苯氧基)-5-氟嘧啶-4-基]氧}苯基)-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.24)(2E)-2-(甲氧基亞胺基)-N-甲基-2-(2-{[({(1E)-1-[3-(三氟甲基)苯基]亞乙基}胺基)氧]甲基}苯基)乙醯胺、(3.25)(2E)-2-(甲氧基亞胺基)-N-甲基-2-{2-[(E)-({1-[3-(三氟甲基)苯基]乙氧基}亞胺基)甲基]苯基}乙醯胺、(3.26)(2E)-2-{2-[({[(1E)-1-(3-{[(E)-1-氟-2-苯基乙烯基]氧}苯基)亞乙基]胺基}氧)甲基]苯基}-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.27)(2E)-2-{2-[({[(2E,3E)-4-(2,6-二氯苯基)亞丁-3-烯-2-基]胺基}氧)甲基]苯基}-2-(甲氧基亞胺基)-N-甲基乙醯胺、(3.28)2-氯-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)吡啶-3-羧醯胺、(3.29)5-甲氧基-2-甲基-4-(2-{[({(1E)-1-[3-(三氟甲基)苯基]亞乙基}胺基)氧]甲基}苯基)-2,4-二氫-3H-1,2,4-三唑-3-酮、(3.30)(2E)-2-{2-[({環丙基[(4-甲氧基苯基)亞胺基]甲基}硫基)甲基]苯基}-3-甲氧基丙-2-烯酸甲酯、(3.31)N-(3-乙基-3,5,5-三甲基環己基)-3-(甲醯基胺基)-2-羥基苯甲醯胺、(3.32)2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺。 (3) Respiratory inhibitors (breathing chain inhibitors) acting on the respiratory chain complex III, for example: (3.1) ametoctradin, (3.2) amisulbrom, (3.3) atoramine (azoxystrobin), (3.4) cyazofamid, (3.5) coumethoxystrobin, (3.6) coumoxystrobin, (3.7) dimoxystrobin, (3.8) olefin Essence (enestroburin), (3.9) famoxadone, (3.10) fenamidone, (3.11) flufenoxystrobin, (3.12) fluoxastrobin, (3.13) Kresoxim-methyl, (3.14) methotrexate, (3.15) orysastrobin, (3.16) picoxystrobin, (3.17) pyraclostrobin Ester (pyraclostrobin), (3.18) pyramitostrobin, (3.19) pyraoxystrobin, (3.20) pyridencarb, (3.21) triclopyricarb, (3.22) Trifloxystrobin, (3.23) (2E)-2-(2-{[6-(3-Chloro-2-methylphenoxy)-5-fluoropyrimidin-4-yl]oxy}phenyl)-2-(methoxy Iminoamino)-N-methylacetamide, (3.24) (2E)-2-(methoxyimino)-N-methyl-2-(2-{[({(1E)-) 1-[3-(Trifluoromethyl)phenyl]ethylidene]amino)oxy]methyl}phenyl)acetamide, (3.25)(2E)-2-(methoxyimino) -N-methyl-2-{2-[(E)-({1-[3-(trifluoromethyl)phenyl]ethoxy}imido)methyl]phenyl}acetamide, (3.26) (2E)-2-{2-[({[(1E)-1-(3-{[(E)-1-fluoro-2-phenylvinyl]oxy)phenyl)ethylidene) ]amino}oxy)methyl]phenyl}-2-(methoxyimino)-N-methylacetamide, (3.27)(2E)-2-{2-[({[(2E) ,3E)-4-(2,6-dichlorophenyl)butylene-3-en-2-yl]amino}oxy)methyl]phenyl}-2-(methoxyimino)-N -methylacetamide, (3.28) 2-chloro-N-(1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl)pyridine-3-carboxamide, (3.29) 5-Methoxy-2-methyl-4-(2-{[({(1E)-1-[3-(trifluoromethyl)phenyl]ethylidene))oxy)] Methyl}phenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one, (3.30)(2E)-2-{2-[({cyclopropyl[(4) -Methoxyphenyl)imido]methyl}thio)methyl]phenyl}-3-methoxyprop-2-enoate, (3.31 N-(3-ethyl-3,5,5-trimethylcyclohexyl)-3-(carbamimidino)-2-hydroxybenzamide, (3.32) 2-{2-[( 2,5-Dimethylphenoxy)methyl]phenyl}-2-methoxy-N-methylacetamide.
(4)有絲分裂與細胞分化之抑制劑,例如:(4.1)免賴德(benomyl)、(4.2)卡苯辛(carbendazim)、(4.3)氯吩唑(chlorfenazole)、(4.4)地吩卡(diethofencarb)、(4.5)噻唑菌胺(ethaboxam)、(4.6)氟吡菌胺(fluopicolide)、(4.7)伏塔唑(fuberidazole)、(4.8)賓克隆(pencycuron)、(4.9)腐絕(thiabendazole)、(4.10)甲基多保淨(thiophanate-methyl)、(4.11)多保淨(thiophanate)、(4.12)索醯胺(zoxamide)、(4.13)5-氯-7-(4-甲基哌啶-1-基)-6-(2,4,6-三氟苯基)[1,2,4]三唑并[1,5-a]嘧啶與(4.14)3-氯-5-(6-氯吡啶-3-基)-6-甲基-4-(2,4,6-三氟苯基)嗒。 (4) Inhibitors of mitosis and cell differentiation, for example: (4.1) benomyl, (4.2) carbendazim, (4.3) chlorfenazole, (4.4) Diethofencarb), (4.5) ethaboxam, (4.6) fluopicolide, (4.7) fuberidazole, (4.8) pencycuron, (4.9) thiabendazole ), (4.10) thiophanate-methyl, (4.11) thiophanate, (4.12) zoxamide, (4.13) 5-chloro-7-(4-methyl Piperidin-1-yl)-6-(2,4,6-trifluorophenyl)[1,2,4]triazolo[1,5-a]pyrimidine with (4.14)3-chloro-5- (6-chloropyridin-3-yl)-6-methyl-4-(2,4,6-trifluorophenyl)anthracene .
(5)具有多重位點活性之化合物,例如:(5.1)波爾多(Bordeaux)混合物、(5.2)四氯丹(captafol)、(5.3)蓋普丹(captan)、(5.4)四氯異苯腈(chlorothalonil)、(5.5) 銅製劑,如:氫氧化銅、(5.6)萘甲酸銅、(5.7)氧化銅、(5.8)鹼性氯氧化銅、(5.9)硫酸銅、(5.10)益發靈(dichlofluanid)、(5.11)腈硫醌(dithianon)、(5.12)多寧(dodine)、(5.13)多寧游離鹼、(5.14)富爾邦(ferbam)、(5.15)護福爾培(fluorfolpet)、(5.16)福爾培(folpet)、(5.17)免熱淨(guazatine)、(5.18)免熱淨乙酸鹽(guazatine acetate)、(5.19)抑克定(iminoctadine)、(5.20)抑克定苯烷磺酸鹽(iminoctadine albesilate)、(5.21)抑克定(iminoctadine)三乙酸鹽、(5.22)錳銅(mancopper)、(5.23)錳粉克(mancozeb)、(5.24)錳乃浦(maneb)、(5.25)滅得賴(metiram)、(5.26)滅得賴鋅鹽、(5.27)快得寧(copper-oxine)、(5.28)丙氧苯脒(propamidine)、(5.29)甲基鋅乃浦(propineb)、(5.30)硫與硫製劑,如,例如:多硫化鈣、(5.31)得恩地(thiram)、(5.32)特伏奈(tolylfluanid)、(5.33)鋅乃浦(zineb)、(5.34)益穗(ziram)與(5.35)敵菌靈(anilazine)。 (5) Compounds having multiple site activities, for example: (5.1) Bordeaux mixture, (5.2) captafol, (5.3) captan, (5.4) tetrachloroisophthalonitrile (chlorothalonil), (5.5) Copper preparations such as: copper hydroxide, (5.6) copper naphthoate, (5.7) copper oxide, (5.8) basic copper oxychloride, (5.9) copper sulfate, (5.10) dichlofluanid, (5.11) nitrile Dithianon, (5.12) dodine, (5.13) tannin free base, (5.14) ferbam, (5.15) fluorfolpet, (5.16) fore (folpet), (5.17) guazatine, (5.18) guazatine acetate, (5.19) iminoctadine, (5.20) succinyl sulfonate (iminoctadine) Albesilate), (5.21) iminoctadine triacetate, (5.22) manganese (mancopper), (5.23) manganese powder (mancozeb), (5.24) manganese iripy (maneb), (5.25) Met (metiram), (5.26) 得 锌 zinc salt, (5.27) copper-oxine, (5.28) propamidine, (5.29) methyl zinc propimb (propineb), ( 5.30) Sulfur and sulfur preparations such as, for example, calcium polysulfide, (5.31) thiram, (5.32) tolylfluanid, (5.33) zinc napu (zineb), (5.34) Ziram) and (5.35) anilazine.
(6)抗性誘發劑,例如:(6.1)阿拉酸式苯(acibenzolar)-S-甲基、(6.2)異噻菌胺(isotianil)、(6.3)撲殺熱(probenazole)、(6.4)地得尼(tiadinil)與(6.5)昆布多醣(laminarin)。 (6) Resistance-inducing agents, for example: (6.1) acibenzolar-S-methyl, (6.2) isotianil, (6.3) probenazole, (6.4) Tiadinil and (6.5) laminarin.
(7)胺基酸與蛋白質生合成抑制劑,如,例如:(7.1)、(7.2)保米黴素(blasticidin-S)、(7.3)嘧菌環胺(cyprodinil)、(7.4)賜黴素(kasugamycin)、(7.5)賜黴素鹽酸鹽水合物(kasugamycin hydrochloride hydrate)、(7.6)米本靈(mepanipyrim)、(7.7)比坦尼(pyrimethanil)、(7.8)3-(5-氟-3,3,4,4-四甲基-3,4-二氫異喹啉-1-基)喹啉、與(7.9)土黴素(oxytetracycline)與(7.10)鏈黴素(streptomycin)。 (7) Amino acids and protein biosynthesis inhibitors, for example, (7.1), (7.2) blasticidin-S, (7.3) cyprodinil, (7.4) Kasugamycin, (7.5) kasugamycin hydrochloride hydrate, (7.6) mepanipyrim, (7.7) pyrimethanil, (7.8) 3-(5-fluoro -3,3,4,4-tetramethyl-3,4-dihydroisoquinolin-1-yl)quinoline, and (7.9) oxytetracycline and (7.10) streptomycin .
(8)ATP生產抑制劑,如,例如:(8.1)三苯醋錫(fentin acetate)、(8.2)三苯氯錫(fentin chloride)、(8.3)三苯錫氫氧化物(fentin hydroxide)與(8.4)矽硫吩(silthiofam)。 (8) ATP production inhibitors such as, for example, (8.1) fentin acetate, (8.2) fentin chloride, (8.3) fentin hydroxide and (8.4) Silthiofam.
(9)細胞壁合成抑制劑,例如:(9.1)苯賽卡(benthiavalicarb)、(9.2)地滅莫 (dimethomorph)、(9.3)伏莫(flumorph)、(9.4)抑發利(iprovalicarb)、(9.5)曼普胺(mandipropamid)、(9.6)保粒黴素(polyoxins)、(9.7)保粒靈(polyoxorim)、(9.8)瓦利黴素(validamycin A)、(9.9)發利列(valifenalate)與(9.10)保粒黴素(polyoxin)B。 (9) Cell wall synthesis inhibitors, for example: (9.1) benthiavalicarb, (9.2) (dimethomorph), (9.3) flumorph, (9.4) iprovalicarb, (9.5) mandipropamid, (9.6) polyoxins, (9.7) Baolingling (polyoxorim), (9.8) validamycin A, (9.9) valifenalate and (9.10) polyoxin B.
(10)脂質與膜合成抑制劑,例如:(10.1)聯苯、(10.2)地茂散(chloroneb)、(10.3)大克爛(dicloran)、(10.4)護粒松(edifenphos)、(10.5)依得利(etridiazole)、(10.6)碘卡(iodocarb)、(10.7)丙基喜樂松(iprobenfos)、(10.8)亞賜普醇烷(isoprothiolane)、(10.9)普莫卡(propamocarb)、(10.10)普莫卡鹽酸鹽(propamocarb hydrochloride)、(10.11)硫菌威(prothiocarb)、(10.12)白粉松(pyrazophos)、(10.13)五氯硝苯(quintozene)、(10.14)四氯硝苯(tecnazene)與(10.15)特克斯-甲基(tolclofos-methyl)。 (10) Lipid and membrane synthesis inhibitors, for example: (10.1) biphenyl, (10.2) chloroneb, (10.3) dicloran, (10.4) edifenphos, (10.5) ) etridiazole, (10.6) iodocarb, (10.7) iprobenfos, (10.8) isoprothiolane, (10.9) propamocarb, (10.10) propamocarb hydrochloride, (10.11) prothiocarb, (10.12) pyrazophos, (10.13) quintozene, (10.14) tetrachloronitrate Benzene (tecnazene) and (10.15) tolclofos-methyl.
(11)黑色素生合成抑制劑,例如:(11.1)卡普醯胺(capropamid))、(11.2)地克賽(diclocymet)、(11.3)芬散尼(fenoxanil)、(11.4)太得(fthalide)、(11.5)百快隆(pyroquilon)、(11.6)三賽唑(tricyclazole)與(11.7){3-甲基-1-[(4-甲基苯甲醯基)胺基]丁烷-2-基}胺甲酸2,2,2-三氟乙基酯。 (11) melanin synthesis inhibitors, for example: (11.1) capellamid (), (11.2) diccoymet, (11.3) fenoxanil, (11.4) fthalide ), (11.5) pyroquilon, (11.6) tricyclazole and (11.7) {3-methyl-1-[(4-methylbenzhydryl)amino]butane- 2-Base} 2,2,2-trifluoroethyl carbamate.
(12)核酸合成抑制劑,例如:(12.1)本達樂(benalaxyl)、(12.2)本達樂-M(benalaxyl-M)(克拉利(kiralaxyl))、(12.3)布滅莫(bupirimate)、(12.4)克拉肯(clozylacon)、(12.5)地滅利(dimethirimol)、(12.6)抑利莫(ethirimol)、(12.7)伏拉希(furalaxyl)、(12.8)殺紋寧(hymexazol)、(12.9)滅達樂(metalaxyl)、(12.10)滅達樂-M(metalaxyl-M)(滅芬散(mefenoxam))、(12.11)歐弗斯(ofurace)、(12.12)歐殺斯(oxadixyl)、(12.13)啉酸(oxolinic acid)與(12.14)歐奇農(octhilinone)。 (12) Inhibitors of nucleic acid synthesis, for example: (12.1) benalaxyl, (12.2) benalaxyl-M (kiralaxyl), (12.3) bupirimate (12.4) clozylacon, (12.5) dimethirimol, (12.6) ethirimol, (12.7) furaxax, (12.8) hymexazol, (12.9) metalaxyl, (12.10) metalaxyl-M (mefenoxam), (12.11) ofofce, (12.12) oxadixyl ), (12.13) oxolinic acid and (12.14) octhilinone.
(13)訊號轉導抑制劑,例如:(13.1)氯唑內(chlozolinate)、(13.2)拌種咯(fenpiclonil)、(13.3)護汰寧(fludioxonil)、(13.4)依普同(iprodione)、(13.5)撲 滅寧(procymidone)、(13.6)快諾芬(quinoxyfen)、(13.7)免克寧(vinclozolin)與(13.8)丙氧喹啉(proquinazid)。 (13) Signal transduction inhibitors, for example: (13.1) chlozolinate, (13.2) fenpiclonil, (13.3) fludioxonil, (13.4) iprodione (13.5) Procymidone, (13.6) quinoxyfen, (13.7) vinclozolin and (13.8) proquinazid.
(14)去偶合劑,例如:(14.1)百蟎克(binapacryl)、(14.2)白粉克(dinocap)、(14.3)富米松(ferimzone)、(14.4)扶吉胺(fluazinam)與(14.5)敵蟎普(meptyldinocap)。 (14) Decoupling agents, for example: (14.1) binapacryl, (14.2) dinocap, (14.3) ferimzone, (14.4) fluazinam and (14.5) Meptyldinocap.
(15)其他化合物,例如:(15.1)本塞唑(benthizole)、(15.2)苯(bethoxazine)、(15.3)卡普黴素(capsimycin)、(15.4)卡吩(carvone)、(15.5)喹啉甲硫胺酸鹽(quinomethionat)、(15.6)必伏農(pyriofenone)(克吩農(chlazafenon))、(15.7)庫發尼(cufraneb)、(15.8)賽伏醯胺(cyflufenamid)、(15.9)西莫尼(cymoxanil)、(15.10)環丙磺草胺(cyprosulfamide)、(15.11)邁隆(dazomet)、(15.12)迪布卡(debacarb)、(15.13)二氯吩(dichlorophen)、(15.14)地克美辛(diclomezine)、(15.15)地吩唑克(difenzoquat)、(15.16)地吩唑克甲基硫酸鹽、(15.17)二苯基胺、(15.18)抑克滅(EcoMate)、(15.19)吩普胺(fenpyrazamine)、(15.20)伏特夫(flumetover)、(15.21)氟菌丹(fluoromid)、(15.22)護硫醯胺(flusulphamide)、(15.23)噻菌淨(flutianil)、(15.24)福賽得鋁(fosetyl-aluminium)、(15.25)福賽得鈣(fosetyl-calcium)、(15.26)福賽得鈉(fosetyl-sodium)、(15.27)六氯苯、(15.28)依麻黴素(irumamycin)、(15.29)滅速卡(methasulfocarb)、(15.30)異硫氰酸甲酯、(15.31)滅奇吩(metrafenone)、(15.32)米德黴素(mildiomycin)、(15.33)納坦黴素(natamycin)、(15.34)二甲基二硫代胺甲酸鎳、(15.35)硝基太(nitrothal)-異丙基、(15.36)歐奇農(octhilinone)、(15.37)歐賽保(oxamocarb)、(15.38)歐芬汀(oxyfenthiin)、(15.39)五氯酚與其鹽類、(15.40)酚丁滅蝨(phenothrin)、(15.41)磷酸與其鹽類、(15.42)霜黴威乙膦酸鹽(propamocarb-fosetylate)、(15.43)普辛(propanosine)-鈉、(15.44)丁吡嗎啉 (pyrimorph)、(15.45)(2E)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎啉-4-基)丙-2-烯-1-酮、(15.46)(2Z)-3-(4-第三丁基苯基)-3-(2-氯吡啶-4-基)-1-(嗎啉-4-基)丙-2-烯-1-酮、(15.47)吡咯靈(pyrrolnitrin)、(15.48)美爾奎寧(tebufloquin)、(15.49)特克爛(tecloftalam)、(15.50)特伏尼(tolnifanid)、(15.51)三唑氧(triazoxide)、(15.52)三氯醯胺(trichlamide)、(15.53)奇利醯胺(zarilamid)、(15.54)2-甲基丙酸(3S,6S,7R,8R)-8-苯甲基-3-[({3-[(異丁醯基氧)甲氧基]-4-甲氧基吡啶-2-基}羰基)胺基]-6-甲基-4,9-二側氧基-1,5-二氧雜環壬烷-7-基酯、(15.55)1-(4-{4-[(5R)-5-(2,6-二氟苯基)-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.56)1-(4-{4-[(5S)-5-(2,6-二氟苯基)-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.57)1-(4-{4-[5-(2,6-二氟苯基)-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)-2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙酮、(15.58)1H-咪唑-1-羧酸1-(4-甲氧基苯氧基)-3,3-二甲基丁烷-2-基酯、(15.59)2,3,5,6-四氯-4-(甲基磺醯基)吡啶、(15.60)2,3-二丁基-6-氯噻吩并[2,3-d]嘧啶-4(3H)-酮、(15.61)2,6-二甲基-1H,5H-[1,4]二硫并[2,3-c:5,6-c']二吡咯-1,3,5,7(2H,6H)-四酮、(15.62)2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]-1-(4-{4-[(5R)-5-苯基-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)乙酮、(15.63)2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]-1-(4-{4-[(5S)-5-苯基-4,5-二氫-1,2-唑-3-基]-1,3-噻唑-2-基}哌啶-1-基)乙酮、(15.64)2-[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]-1-{4-[4-(5-苯基-4,5-二氫-1,2-唑-3-基)-1,3-噻唑-2-基]哌啶-1-基}乙酮、(15.65)2-丁氧基-6-碘-3-丙基-4H-色烯-4-酮、(15.66)2-氯-5-[2-氯-1-(2,6-二氟-4-甲氧基苯基)-4-甲基-1H-咪唑-5-基]吡啶、(15.67)2-苯基苯酚與鹽類、(15.68)3-(4,4,5-三氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、 (15.69)3,4,5-三氯吡啶-2,6-二甲腈、(15.70)3-氯-5-(4-氯苯基)-4-(2,6-二氟苯基)-6-甲基嗒、(15.71)4-(4-氯苯基)-5-(2,6-二氟苯基)-3,6-二甲基嗒、(15.72)5-胺基-1,3,4-噻二唑-2-硫醇、(15.73)5-氯-N'-苯基-N'-(丙-2-炔-1-基)噻吩-2-亞硫羧基醯肼、(15.74)5-氟-2-[(4-氟苯甲基)氧]嘧啶-4-胺、(15.75)5-氟-2-[(4-甲基苯甲基)氧]嘧啶-4-胺、(15.76)5-甲基-6-辛基[1,2,4]三唑并[1,5-a]嘧啶-7-胺、(15.77)(2Z)-3-胺基-2-氰基-3-苯基丙烯酸乙酯、(15.78)N'-(4-{[3-(4-氯苯甲基)-1,2,4-噻二唑-5-基]氧}-2,5-二甲基苯基)-N-乙基-N-甲基甲脒、(15.79)N-(4-氯苯甲基)-3-[3-甲氧基-4-(丙-2-炔-1-基氧)苯基]丙醯胺、(15.80)N-[(4-氯苯基)(氰基)甲基]-3-[3-甲氧基-4-(丙-2-炔-1-基氧)苯基]丙醯胺、(15.81)N-[(5-溴-3-氯吡啶-2-基)甲基]-2,4-二氯菸醯胺、(15.82)N-[1-(5-溴-3-氯吡啶-2-基)乙基]-2,4-二氯菸醯胺、(15.83)N-[1-(5-溴-3-氯吡啶-2-基)乙基]-2-氟-4-碘菸醯胺、(15.84)N-{(E)-[(環丙基甲氧基)亞胺基][6-(二氟甲氧基)-2,3-二氟苯基]甲基}-2-苯基乙醯胺、(15.85)N-{(Z)-[(環丙基甲氧基)亞胺基][6-(二氟甲氧基)-2,3-二氟苯基]甲基}-2-苯基乙醯胺、(15.86)N'-{4-[(3-第三丁基-4-氰基-1,2-噻唑-5-基)氧]-2-氯-5-甲基苯基}-N-乙基-N-甲基甲脒、(15.87)N-甲基-2-(1-{[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-N-(1,2,3,4-四氫萘-1-基)-1,3-噻唑-4-羧醯胺、(15.88)N-甲基-2-(1-{[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-N-[(1R)-1,2,3,4-四氫萘-1-基]-1,3-噻唑-4-羧醯胺、(15.89)N-甲基-2-(1-{[5-甲基-3-(三氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-N-[(1S)-1,2,3,4-四氫萘-1-基]-1,3-噻唑-4-羧醯胺、(15.90){6-[({[(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2-基}胺甲酸戊酯、(15.91)吩-1-羧酸、(15.92)喹啉-8-醇、(15.93)喹啉-8-醇硫酸鹽(2:1)、(15.94){6-[({[(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2- 基}胺甲酸第三丁基酯、(15.95)1-甲基-3-(三氟甲基)-N-[2'-(三氟甲基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.96)N-(4'-氯聯苯-2-基)-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.97)N-(2',4'-二氯聯苯-2-基)-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.98)3-(二氟甲基)-1-甲基-N-[4'-(三氟甲基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.99)N-(2',5'-二氟聯苯-2-基)-1-甲基-3-(三氟甲基)-1H-吡唑-4-羧醯胺、(15.100)3-(二氟甲基)-1-甲基-N-[4'-(丙-1-炔-1-基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.101)5-氟-1,3-二甲基-N-[4'-(丙-1-炔-1-基)聯苯-2-基]-1H-吡唑-4-羧醯胺、(15.102)2-氯-N-[4'-(丙-1-炔-1-基)聯苯-2-基]菸醯胺、(15.103)3-(二氟甲基)-N-[4'-(3,3-二甲基丁-1-炔-1-基)聯苯-2-基]-1-甲基-1H-吡唑-4-羧醯胺、(15.104)N-[4'-(3,3-二甲基丁-1-炔-1-基)聯苯-2-基]-5-氟-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.105)3-(二氟甲基)-N-(4'-乙炔基聯苯-2-基)-1-甲基-1H-吡唑-4-羧醯胺、(15.106)N-(4'-乙炔基聯苯-2-基)-5-氟-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.107)2-氯-N-(4'-乙炔基聯苯-2-基)菸醯胺、(15.108)2-氯-N-[4'-(3,3-二甲基丁-1-炔-1-基)聯苯-2-基]菸醯胺、(15.109)4-(二氟甲基)-2-甲基-N-[4'-(三氟甲基)聯苯-2-基]-1,3-噻唑-5-羧醯胺、(15.110)5-氟-N-[4'-(3-羥基-3-甲基丁-1-炔-1-基)聯苯-2-基]-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.111)2-氯-N-[4'-(3-羥基-3-甲基丁-1-炔-1-基)聯苯-2-基]菸醯胺、(15.112)3-(二氟甲基)-N-[4'-(3-甲氧基-3-甲基丁-1-炔-1-基)聯苯-2-基]-1-甲基-1H-吡唑-4-羧醯胺、(15.113)5-氟-N-[4'-(3-甲氧基-3-甲基丁-1-炔-1-基)聯苯-2-基]-1,3-二甲基-1H-吡唑-4-羧醯胺、(15.114)2-氯-N-[4'-(3-甲氧基-3-甲基丁-1-炔-1-基)聯苯-2-基]菸醯胺、(15.115)(5-溴-2-甲氧基-4-甲基吡啶-3-基)(2,3,4-三甲氧基-6-甲基苯基)甲酮、(15.116)N-[2-(4-{[3-(4-氯苯基)丙-2-炔-1-基]氧}-3-甲氧基苯基)乙基]-N2-(甲基磺醯基)纈醯胺、(15.117)4-側氧基-4-[(2-苯基乙基)胺基]丁酸、 (15.118){6-[({[(Z)-(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2-基}胺甲酸丁-3-炔-1-基酯、(15.119)4-胺基-5-氟嘧啶-2-醇(互變異構型:4-胺基-5-氟嘧啶-2(1H)-酮)、(15.120)3,4,5-三羥基苯甲酸丙酯、(15.121)1,3-二甲基-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1H-吡唑-4-羧醯胺、(15.122)1,3-二甲基-N-[(3R)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(15.123)1,3-二甲基-N-[(3S)-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1H-吡唑-4-羧醯胺、(15.124)[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-唑-4-基](吡啶-3-基)甲醇、(15.125)(S)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-唑-4-基](吡啶-3-基)甲醇、(15.126)(R)-[3-(4-氯-2-氟苯基)-5-(2,4-二氟苯基)-1,2-唑-4-基](吡啶-3-基)甲醇、(15.127)2-{[3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.128)硫代氰酸1-{[3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑-5-基酯、(15.129)5-(烯丙基硫基)-1-{[3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑、(15.130)2-[1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.131)2-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.132)2-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.133)硫代氰酸1-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑-5-基酯、(15.134)硫代氰酸1-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑-5-基酯、(15.135)5-(烯丙基硫基)-1-{[rel(2R,3S)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2-基]甲基}-1H-1,2,4-三唑、(15.136)5-(烯丙基硫基)-1-{[rel(2R,3R)-3-(2-氯苯基)-2-(2,4-二氟苯基)環氧乙烷-2- 基]甲基}-1H-1,2,4-三唑、(15.137)2-[(2S,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.138)2-[(2R,4S,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.139)2-[(2R,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.140)2-[(2S,4R,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.141)2-[(2S,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.142)2-[(2R,4S,5R)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.143)2-[(2R,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.144)2-[(2S,4R,5S)-1-(2,4-二氯苯基)-5-羥基-2,6,6-三甲基庚烷-4-基]-2,4-二氫-3H-1,2,4-三唑-3-硫酮、(15.145)2-氟-6-(三氟甲基)-N-(1,1,3-三甲基-2,3-二氫-1H-茚-4-基)苯甲醯胺、(15.146)2-(6-苯甲基吡啶-2-基)喹唑啉、(15.147)2-[6-(3-氟-4-甲氧基苯基)-5-甲基吡啶-2-基]喹唑啉、(15.148)3-(4,4-二氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.149)脫落酸(abscisic acid)、(15.150)3-(二氟甲基)-N-甲氧基-1-甲基-N-[1-(2,4,6-三氯苯基)丙烷-2-基]-1H-吡唑-4-羧醯胺、(15.151)N'-[5-溴-6-(2,3-二氫-1H-茚-2-基氧)-2-甲基吡啶-3-基]-N-乙基-N-甲基甲脒、(15.152)N'-{5-溴-6-[1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.153)N'-{5-溴-6-[(1R)-1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.154)N'-{5-溴-6-[(1S)-1-(3,5-二氟苯基)乙氧基]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.155)N'-{5-溴-6-[(順式-4-異丙基環己基)氧]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.156)N'-{5-溴-6-[(反式-4-異丙基環己基) 氧]-2-甲基吡啶-3-基}-N-乙基-N-甲基甲脒、(15.157)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.158)N-環丙基-N-(2-環丙基苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.159)N-(2-第三丁基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.160)N-(5-氯-2-乙基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.161)N-(5-氯-2-異丙基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.162)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-氟苯甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.163)N-環丙基-3-(二氟甲基)-5-氟-N-(5-氟-2-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.164)N-環丙基-N-(2-環丙基-5-氟苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.165)N-(2-環戊基-5-氟苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.166)N-環丙基-3-(二氟甲基)-5-氟-N-(2-氟-6-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.167)N-環丙基-3-(二氟甲基)-N-(2-乙基-5-甲基苯甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.168)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基-5-甲基苯甲基)-1-甲基-1H-吡唑-4-羧醯胺、(15.169)N-環丙基-N-(2-環丙基-5-甲基苯甲基)-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.170)N-(2-第三丁基-5-甲基苯甲基)-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.171)N-[5-氯-2-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.172)N-環丙基-3-(二氟甲基)-5-氟-1-甲基-N-[5-甲基-2-(三氟甲基)苯甲基]-1H-吡唑-4-羧醯胺、(15.173)N-[2-氯-6-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.174)N-[3-氯-2-氟-6-(三氟甲基)苯甲基]-N-環丙基-3-(二氟甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.175)N-環丙基-3-(二氟甲基)-N-(2-乙基-4,5-二甲 基苯甲基)-5-氟-1-甲基-1H-吡唑-4-羧醯胺、(15.176)N-環丙基-3-(二氟甲基)-5-氟-N-(2-異丙基苯甲基)-1-甲基-1H-吡唑-4-羧硫醯胺、(15.177)3-(二氟甲基)-N-(7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基)-1-甲基-1H-吡唑-4-羧醯胺、(15.178)3-(二氟甲基)-N-[(3R)-7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1-甲基-1H-吡唑-4-羧醯胺、(15.179)3-(二氟甲基)-N-[(3S)-7-氟-1,1,3-三甲基-2,3-二氫-1H-茚-4-基]-1-甲基-1H-吡唑-4-羧醯胺、(15.180)N'-(2,5-二甲基-4-苯氧基苯基)-N-乙基-N-甲基甲脒、(15.181)N'-{4-[(4,5-二氯-1,3-噻唑-2-基)氧]-2,5-二甲基苯基}-N-乙基-N-甲基甲脒、(15.182)N-(4-氯-2,6-二氟苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺。所有第(1)至(15)類所述之混合組份依據其官能基而定,可視需要與合適酸或鹼形成鹽類。 (15) Other compounds, for example: (15.1) benzizole, (15.2) benzene (bethoxazine), (15.3) cappmycin (capsimycin), (15.4) carvone, (15.5) quinoline thioacetate (quinethionat), (15.6) pyrofenone (pyriofenone) (chlazafenon), (15.7) cufraneb, (15.8) cyflufenamid, (15.9) cymoxanil, (15.10) cyprosulfamide, ( 15.11) dazomet, (15.12) debacarb, (15.13) dichlorophen, (15.14) dimlomezine, (15.15) difenzoquat, ( 15.16) morphazole methyl sulfate, (15.17) diphenylamine, (15.18) espressan (EcoMate), (15.19) fenpyrazamine, (15.20) flumetover, (15.21) ) fluoromid, (15.22) flusulphamide, (15.23) flutianil, (15.24) fosetyl-aluminium, (15.25) forsythia calcium ( Fosetyl-calcium), (15.26) fosetyl-sodium, (15.27) hexachlorobenzene, (15.28) irumamycin, (15.29) methasulfocarb, (15.30) Methyl thiocyanate, (15.31) metrafenone, (15.32) medemycin (m Ildiomycin), (15.33) natamycin, (15.34) nickel dimethyldithiocarbamate, (15.35) nitrothal-isopropyl, (15.36) octhilinone (15.37) oxamocarb, (15.38) oxyfenthiin, (15.39) pentachlorophenol and its salts, (15.40) phenothrin, (15.41) phosphate and its salts, (15.42) propamocarb-fosetylate, (15.43) propanosine-sodium, (15.44) pyrymorph, (15.45)(2E)-3-(4- Tert-butylphenyl)-3-(2-chloropyridin-4-yl)-1-(morpholin-4-yl)prop-2-en-1-one, (15.46)(2Z)-3- (4-tert-butylphenyl)-3-(2-chloropyridin-4-yl)-1-(morpholin-4-yl)prop-2-en-1-one, (15.47) pyrroline ( Pyrrolnitrin), (15.48) tebufloquin, (15.49) tecloftalam, (15.50) tolnifanid, (15.51) triazoxide, (15.52) trichloropurine Tricholide, (15.53) zarilamid, (15.54) 2-methylpropionic acid (3S,6S,7R,8R)-8-benzyl-3-[({3-[( Isobutyryloxy)methoxy]-4-methoxypyridin-2-yl}carbonyl)amino]-6-methyl-4,9-di-oxy-1 ,5-dioxan-7-yl ester, (15.55) 1-(4-{4-[(5R)-5-(2,6-difluorophenyl)-4,5-dihydrol -1,2- Zyrid-3-yl]-1,3-thiazol-2-yl}piperidin-1-yl)-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl Ethyl ketone, (15.56) 1-(4-{4-[(5S)-5-(2,6-difluorophenyl)-4,5-dihydro-1,2- Zyrid-3-yl]-1,3-thiazol-2-yl}piperidin-1-yl)-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl Ethylketone, (15.57) 1-(4-{4-[5-(2,6-difluorophenyl)-4,5-dihydro-1,2- Zyrid-3-yl]-1,3-thiazol-2-yl}piperidin-1-yl)-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl Ethyl ketone, (15.58) 1H-imidazol-1-carboxylic acid 1-(4-methoxyphenoxy)-3,3-dimethylbutan-2-yl ester, (15.59) 2,3, 5,6-tetrachloro-4-(methylsulfonyl)pyridine, (15.60) 2,3-dibutyl-6-chlorothieno[2,3-d]pyrimidin-4(3H)-one, (15.61) 2,6-Dimethyl-1H,5H-[1,4]disulfide And [2,3-c:5,6-c']dipyrrole-1,3,5,7(2H,6H)-tetraone, (15.62)2-[5-methyl-3-(trifluoro Methyl)-1H-pyrazol-1-yl]-1-(4-{4-[(5R)-5-phenyl-4,5-dihydro-1,2- Zyrid-3-yl]-1,3-thiazol-2-yl}piperidin-1-yl)ethanone, (15.63) 2-[5-methyl-3-(trifluoromethyl)-1H-pyridyl Zin-1-yl]-1-(4-{4-[(5S)-5-phenyl-4,5-dihydro-1,2- Zyrid-3-yl]-1,3-thiazol-2-yl}piperidin-1-yl)ethanone, (15.64) 2-[5-methyl-3-(trifluoromethyl)-1H-pyridyl Zin-1-yl]-1-{4-[4-(5-phenyl-4,5-dihydro-1,2- Zyridin-3-yl)-1,3-thiazol-2-yl]piperidin-1-yl}ethanone, (15.65) 2-butoxy-6-iodo-3-propyl-4H-chromene- 4-ketone, (15.66) 2-chloro-5-[2-chloro-1-(2,6-difluoro-4-methoxyphenyl)-4-methyl-1H-imidazol-5-yl] Pyridine, (15.67) 2-phenylphenol and salts, (15.68) 3-(4,4,5-trifluoro-3,3-dimethyl-3,4-dihydroisoquinolin-1-yl Quinoline, (15.69) 3,4,5-trichloropyridine-2,6-dicarbonitrile, (15.70) 3-chloro-5-(4-chlorophenyl)-4-(2,6-di Fluorophenyl)-6-methyloxime , (15.71) 4-(4-chlorophenyl)-5-(2,6-difluorophenyl)-3,6-dimethylhydrazine , (15.72) 5-amino-1,3,4-thiadiazole-2-thiol, (15.73) 5-chloro-N'-phenyl-N'-(prop-2-yn-1-yl Thiophene-2-sulfinyl hydrazine, (15.74) 5-fluoro-2-[(4-fluorobenzyl)oxy]pyrimidine-4-amine, (15.75) 5-fluoro-2-[(4- Methylbenzyloxy)pyrimidine-4-amine, (15.76) 5-methyl-6-octyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine, ( 15.77) (2Z)-3-Amino-2-cyano-3-phenylethyl acrylate, (15.78) N'-(4-{[3-(4-chlorobenzyl)-1,2, 4-thiadiazol-5-yl]oxy}-2,5-dimethylphenyl)-N-ethyl-N-methylformamidine, (15.79)N-(4-chlorobenzyl)- 3-[3-methoxy-4-(prop-2-yn-1-yloxy)phenyl]propanamine, (15.80) N-[(4-chlorophenyl)(cyano)methyl] -3-[3-methoxy-4-(prop-2-yn-1-yloxy)phenyl]propanamine, (15.81) N-[(5-bromo-3-chloropyridin-2-yl) )methyl]-2,4-dichloroshitamine, (15.82) N-[1-(5-bromo-3-chloropyridin-2-yl)ethyl]-2,4-dichloroshitamine , (15.83) N-[1-(5-bromo-3-chloropyridin-2-yl)ethyl]-2-fluoro-4-iodoguanidine, (15.84) N-{(E)-[( Cyclopropylmethoxy)imido][6-(difluoromethoxy)-2,3-difluorophenyl]methyl}-2-phenylacetamide, (15.85) N-{( Z)-[(cyclopropylmethoxy)imido][6-(difluoromethoxy) )-2,3-difluorophenyl]methyl}-2-phenylacetamidine, (15.86) N'-{4-[(3-tert-butyl-4-cyano-1,2- Thiazol-5-yl)oxy]-2-chloro-5-methylphenyl}-N-ethyl-N-methylformamidine, (15.87) N-methyl-2-(1-{[5- Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethenyl}piperidin-4-yl)-N-(1,2,3,4-tetrahydronaphthalene-1- -1,3-1,3-thiazol-4-carboxamide, (15.88) N-methyl-2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazole-1 -yl]ethinyl}piperidin-4-yl)-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-1,3-thiazole-4-carboxyguanamine , (15.89) N-methyl-2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethenyl}piperidin-4-yl) -N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]-1,3-thiazole-4-carboxyguanamine, (15.90){6-[({[(1- Methyl-1H-tetrazol-5-yl)(phenyl)methylene]amino}oxy)methyl]pyridin-2-yl}ammonium formate, (15.91) phene 1-carboxylic acid, (15.92) quinoline-8-ol, (15.93) quinoline-8-ol sulfate (2:1), (15.94) {6-[({[(1-methyl-1H) -tetrazol-5-yl)(phenyl)methylene]amino}oxy)methyl]pyridin-2-yl}carbamic acid tert-butyl ester, (15.95) 1-methyl-3-(three Fluoromethyl)-N-[2'-(trifluoromethyl)biphenyl-2-yl]-1H-pyrazole-4-carboxamide, (15.96) N-(4'-chlorobiphenyl-2 -yl)-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide, (15.97) N-(2',4'-dichlorobiphenyl-2-yl) -3-(Difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide, (15.98) 3-(difluoromethyl)-1-methyl-N-[4'-( Trifluoromethyl)biphenyl-2-yl]-1H-pyrazole-4-carboxamide, (15.99) N-(2',5'-difluorobiphenyl-2-yl)-1-methyl -3-(trifluoromethyl)-1H-pyrazole-4-carboxamide, (15.100) 3-(difluoromethyl)-1-methyl-N-[4'-(prop-1-yne) -1-yl)biphenyl-2-yl]-1H-pyrazole-4-carboxyguanamine, (15.101) 5-fluoro-1,3-dimethyl-N-[4'-(prop-1- Alkyn-1-yl)biphenyl-2-yl]-1H-pyrazole-4-carboxamide, (15.102) 2-chloro-N-[4'-(prop-1-yn-1-yl) Benz-2-yl]nicotinamine, (15.103) 3-(difluoromethyl)-N-[4'-(3,3-dimethylbut-1-yn-1-yl)biphenyl-2 -yl]-1-methyl-1H-pyrazole-4-carboxyguanamine, (15.104) N-[4'-(3,3-di Butyl-1-yn-1-yl)biphenyl-2-yl]-5-fluoro-1,3-dimethyl-1H-pyrazole-4-carboxamide, (15.105) 3-(difluoro Methyl)-N-(4'-ethynylbiphenyl-2-yl)-1-methyl-1H-pyrazole-4-carboxamide, (15.106) N-(4'-ethynylbiphenyl- 2-yl)-5-fluoro-1,3-dimethyl-1H-pyrazole-4-carboxamide, (15.107) 2-chloro-N-(4'-ethynylbiphenyl-2-yl) Nicotinamide, (15.108) 2-chloro-N-[4'-(3,3-dimethylbut-1-yn-1-yl)biphenyl-2-yl]nicotamine, (15.109)4 -(Difluoromethyl)-2-methyl-N-[4'-(trifluoromethyl)biphenyl-2-yl]-1,3-thiazole-5-carboxamide, (15.110) 5- Fluorine-N-[4'-(3-hydroxy-3-methylbut-1-yn-1-yl)biphenyl-2-yl]-1,3-dimethyl-1H-pyrazole-4- Carboxylamidine, (15.111) 2-chloro-N-[4'-(3-hydroxy-3-methylbut-1-yn-1-yl)biphenyl-2-yl]nicotamine, (15.112) 3-(Difluoromethyl)-N-[4'-(3-methoxy-3-methylbut-1-yn-1-yl)biphenyl-2-yl]-1-methyl-1H -pyrazole-4-carboxyguanamine, (15.113) 5-fluoro-N-[4'-(3-methoxy-3-methylbut-1-yn-1-yl)biphenyl-2-yl ]-1,3-Dimethyl-1H-pyrazole-4-carboxamide, (15.114) 2-chloro-N-[4'-(3-methoxy-3-methylbut-1-yne) -1-yl)biphenyl-2-yl]nicotamine, (15.115) (5-bromo-2-methoxy-4-methylpyridinium -3-yl)(2,3,4-trimethoxy-6-methylphenyl)methanone, (15.116) N-[2-(4-{[3-(4-chlorophenyl)propene- 2-alkyn-1-yl]oxy}-3-methoxyphenyl)ethyl]-N2-(methylsulfonyl)decylamine, (15.117) 4-sided oxy-4-[(2 -Phenylethyl)amino]butyric acid, (15.118){6-[({[(Z)-(1-methyl-1H-tetrazol-5-yl)(phenyl)methylene]amine) (yloxy)methyl]pyridin-2-yl}carbamic acid but-3-yn-1-yl ester, (15.119) 4-amino-5-fluoropyrimidin-2-ol (tautomeric form: 4- Amino-5-fluoropyrimidine-2(1H)-one), (15.120) propyl 3,4,5-trihydroxybenzoate, (15.121)1,3-dimethyl-N-(1,1, 3-trimethyl-2,3-dihydro-1H-indol-4-yl)-1H-pyrazole-4-carboxamide, (15.122)1,3-dimethyl-N-[(3R) -1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (15.123)1,3-dimethyl-N -[(3S)-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (15.124) [3-( 4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)-1,2- Zin-4-yl](pyridin-3-yl)methanol, (15.125)(S)-[3-(4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)- 1,2- Zin-4-yl](pyridin-3-yl)methanol, (15.126)(R)-[3-(4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)- 1,2- Zin-4-yl](pyridin-3-yl)methanol, (15.127) 2-{[3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxirane-2 -yl]methyl}-2,4-dihydro-3H-1,2,4-triazole-3-thione, (15.128) 1-{[3-(2-chlorophenyl)thiocyanate -2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazol-5-yl ester, (15.129) 5-(allyl Thiothio)-1-{[3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-1,2, 4-triazole, (15.130) 2-[1-(2,4-dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-di Hydrogen-3H-1,2,4-triazole-3-thione, (15.131)2-{[rel(2R,3S)-3-(2-chlorophenyl)-2-(2,4-di Fluorophenyl)oxiran-2-yl]methyl}-2,4-dihydro-3H-1,2,4-triazole-3-thione, (15.132)2-{[rel(2R) , 3R)-3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-2,4-dihydro-3H-1, 2,4-triazole-3-thione, (15.133) thiocyanate 1-{[rel(2R,3S)-3-(2-chlorophenyl)-2-(2,4-difluorobenzene) Ethylene oxide-2-yl]methyl}-1H-1,2,4-triazol-5-yl ester, (15.134) thiocyanate 1-{[rel(2R,3R)-3 -(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazol-5-yl ester, (15.135) 5-(allyl -1{[rel(2R,3S)-3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H -1,2,4-triazole, (15.136) 5-(allylthio)-1-{[rel(2R,3R)-3-(2-chlorophenyl)-2-(2,4 -difluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazole, (15.137)2-[(2S,4S,5S)-1-(2,4 -dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole-3-thione , (15.138) 2-[(2R,4S,5S)-1-(2,4-Dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2 ,4-dihydro-3H-1,2,4-triazole-3-thione, (15.139) 2-[(2R,4R,5R)-1-(2,4-dichlorophenyl)-5 -hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole-3-thione, (15.140) 2-[( 2S,4R,5R)-1-(2,4-dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H- 1,2,4-triazole-3-thione, (15.141) 2-[(2S,4S,5R)-1-(2,4-dichlorophenyl)-5-hydroxy-2,6,6 -trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole-3-thione, (15.142)2-[(2R,4S,5R)-1 -(2,4-dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole -3-thione, (15.143) 2-[(2R,4R,5S)-1-(2,4-dichlorophenyl)-5-hydroxy-2,6,6- Trimethylheptane-4-yl]-2,4-dihydro-3H-1,2,4-triazole-3-thione, (15.144)2-[(2S,4R,5S)-1- (2,4-dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole- 3-thione, (15.145) 2-fluoro-6-(trifluoromethyl)-N-(1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl)benzene Formamide, (15.146) 2-(6-benzylpyridin-2-yl)quinazoline, (15.147) 2-[6-(3-fluoro-4-methoxyphenyl)-5- Pyridin-2-yl]quinazoline, (15.148) 3-(4,4-difluoro-3,3-dimethyl-3,4-dihydroisoquinolin-1-yl)quinoline, 15.149) Abscisic acid, (15.150) 3-(difluoromethyl)-N-methoxy-1-methyl-N-[1-(2,4,6-trichlorophenyl)propane -2-yl]-1H-pyrazole-4-carboxamide, (15.151) N'-[5-bromo-6-(2,3-dihydro-1H-indol-2-yloxy)-2- Methylpyridin-3-yl]-N-ethyl-N-methylformamidine, (15.152) N'-{5-bromo-6-[1-(3,5-difluorophenyl)ethoxy ]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine, (15.153) N'-{5-bromo-6-[(1R)-1-(3,5- Difluorophenyl)ethoxy]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine, (15.154) N'-{5-bromo-6-[(1S) 1-(3,5-difluorophenyl)ethoxy]-2-methylpyridin-3-yl}-N-ethyl-N-A Formazan, (15.155) N'-{5-bromo-6-[(cis-4-isopropylcyclohexyl)oxy]-2-methylpyridin-3-yl}-N-ethyl-N- Methylformamidine, (15.156) N'-{5-bromo-6-[(trans-4-isopropylcyclohexyl)oxy]-2-methylpyridin-3-yl}-N-ethyl- N-methylformamidine, (15.157) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(2-isopropylbenzyl)-1-methyl-1H-pyridyl Azole-4-carboxamide, (15.158) N-cyclopropyl-N-(2-cyclopropylbenzyl)-3-(difluoromethyl)-5-fluoro-1-methyl-1H- Pyrazole-4-carboxyguanamine, (15.159) N-(2-t-butylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl- 1H-pyrazole-4-carboxyguanamine, (15.160) N-(5-chloro-2-ethylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1 -methyl-1H-pyrazole-4-carboxyguanamine, (15.161) N-(5-chloro-2-isopropylbenzyl)-N-cyclopropyl-3-(difluoromethyl)- 5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.162) N-cyclopropyl-3-(difluoromethyl)-N-(2-ethyl-5-fluorobenzene Methyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.163) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(5 -fluoro-2-isopropylbenzyl)-1-methyl-1H-pyrazole-4-carboxamide, (15.164) N-cyclopropyl-N-(2-cyclopropyl-5-fluoro Benzyl)-3-( Fluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.165) N-(2-cyclopentyl-5-fluorobenzyl)-N-cyclopropyl -3-(Difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.166) N-cyclopropyl-3-(difluoromethyl)-5- Fluorine-N-(2-fluoro-6-isopropylbenzyl)-1-methyl-1H-pyrazole-4-carboxamide, (15.167) N-cyclopropyl-3-(difluoromethyl) -N-(2-ethyl-5-methylbenzyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.168) N-cyclopropyl-3 -(Difluoromethyl)-5-fluoro-N-(2-isopropyl-5-methylbenzyl)-1-methyl-1H-pyrazole-4-carboxamide, (15.169)N -cyclopropyl-N-(2-cyclopropyl-5-methylbenzyl)-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxyindole Amine, (15.170) N-(2-tert-butyl-5-methylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H- Pyrazole-4-carboxamide, (15.171) N-[5-chloro-2-(trifluoromethyl)benzyl]-N-cyclopropyl-3-(difluoromethyl)-5-fluoro -1-methyl-1H-pyrazole-4-carboxamide, (15.172) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-N-[5-A Benzyl-2-(trifluoromethyl)benzyl]-1H-pyrazole-4-carboxamide, (15.173) N-[2-chloro-6-(trifluoromethyl)benzyl]-N -cyclopropyl-3-(difluoro 5-)fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.174) N-[3-chloro-2-fluoro-6-(trifluoromethyl)benzyl]- N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.175) N-cyclopropyl-3-(difluoromethyl) -N-(2-ethyl-4,5-dimethylbenzyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (15.176) N-cyclopropane 3-(difluoromethyl)-5-fluoro-N-(2-isopropylbenzyl)-1-methyl-1H-pyrazole-4-carboxythioguanamine, (15.177)3- (difluoromethyl)-N-(7-fluoro-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl)-1-methyl-1H-pyrazole- 4-carboxyguanamine, (15.178) 3-(difluoromethyl)-N-[(3R)-7-fluoro-1,1,3-trimethyl-2,3-dihydro-1H-indole- 4-yl]-1-methyl-1H-pyrazole-4-carboxamide, (15.179) 3-(difluoromethyl)-N-[(3S)-7-fluoro-1,1,3- Trimethyl-2,3-dihydro-1H-indol-4-yl]-1-methyl-1H-pyrazole-4-carboxamide, (15.180) N'-(2,5-dimethyl -4-phenoxyphenyl)-N-ethyl-N-methylformamidine, (15.181) N'-{4-[(4,5-dichloro-1,3-thiazol-2-yl) Oxy]-2,5-dimethylphenyl}-N-ethyl-N-methylformamidine, (15.182) N-(4-chloro-2,6-difluorophenyl)-4-(2 -Chloro-4-fluorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine. All of the mixed components described in the above categories (1) to (15) are depending on their functional groups, and may form a salt with a suitable acid or base as needed.
式(I)化合物可與生物性除害劑組合。 The compound of formula (I) can be combined with a biological pesticide.
生物性除害劑特別包括細菌、真菌、酵母、植物抽出物及由微生物形成之產物,包括蛋白質與二次代謝物。 Biological pesticides include, in particular, bacteria, fungi, yeast, plant extracts and products formed by microorganisms, including proteins and secondary metabolites.
生物性除害劑包括細菌,如:形成孢子之細菌、定殖在根部之細菌及具有生物性殺昆蟲劑、殺真菌劑或殺線蟲劑作用之細菌。 Biological pesticides include bacteria such as bacteria that form spores, bacteria that colonize the roots, and bacteria that have biological insecticides, fungicides, or nematicides.
此等可用為生物性除害劑之細菌實例為:液化澱粉芽孢桿菌(Bacillus amyloliquefaciens)菌株FZB42(DSM 231179),或仙人掌桿菌(Bacillus cereus),特定言之仙人掌桿菌(B.cereus)菌株CNCM I-1562或堅強芽胞桿菌(Bacillus firmus)菌株I-1582(登錄號CNCM I-1582)或短小芽胞桿菌(Bacillus pumilus),特定言之菌株GB34(登錄號ATCC 700814)與菌株QST2808(登錄號NRRL B-30087),或枯草桿菌(Bacillus subtilis),特定言之菌株GB03(登錄號ATCC SD-1397),或枯草桿 菌(Bacillus subtilis)菌株QST713(登錄號NRRL B-21661)或枯草桿菌(Bacillus subtilis)菌株OST 30002(登錄號NRRL B-50421)、蘇雲金芽孢桿菌(Bacillus thuringiensis),特定言之蘇雲金芽胞桿菌以色列亞種(B.thuringiensis subspecies israelensis)(血清型H-14),菌株AM65-52(登錄號ATCC 1276),或蘇雲金芽胞桿菌鮎澤亞種(B.thuringiensis subsp.aizaaai),特定言之菌株ABTS-1857(SD-1372),或蘇雲金芽胞桿菌庫斯塔基亞種(B.thuringiensis subsp.kurstaki)菌株HD-1,或蘇雲金芽胞桿菌殺蟲亞種(B.thuringiensis subsp.tenebrionis)菌株NB 176(SD-5428)、穿刺巴斯德菌(Pasteuria penetrans)、巴斯德菌屬(Pasteuria spp.)(腎形腎狀線蟲(Rotylenchulus reniformis))-PR3(登錄號ATCC SD-5834)、細黃鏈黴菌(Streptomyces microflavus)菌株AQ6121(=QRD 31.013、NRRL B-50550)、鮮黃鏈黴菌(Streptomyces galbus)菌株AQ 6047(登錄號NRRL 30232)。 These bacteria can be used as biological pesticides of example are: liquefaction of starch Bacillus (Bacillus amyloliquefaciens) strain FZB42 (DSM 231179), or Bacillus cereus (Bacillus cereus), specific words cereus (B. cereus) strain CNCM I -1562 or Bacillus firmus strain I-1582 (accession number CNCM I-1582) or Bacillus pumilus , specifically strain GB34 (accession number ATCC 700814) and strain QST2808 (accession number NRRL B) -30087), or Bacillus subtilis , specific strain GB03 (accession number ATCC SD-1397), or Bacillus subtilis strain QST713 (accession number NRRL B-21661) or Bacillus subtilis Strain OST 30002 (accession number NRRL B-50421), Bacillus thuringiensis , specifically B. thuringiensis subspecies israelensis (serotype H-14), strain AM65-52 (login number ATCC 1276), or Bacillus thuringiensis aizawai (B.thuringiensis subsp.aizaaai), specific words strain ABTS-1857 (SD-1372) , or Bacillus thuringiensis Costa Nokia species (B.thuringiensis subsp.kurstaki) strain HD-1, or Bacillus thuringiensis subsp Insecticidal (B.thuringiensis subsp. Tenebrionis) strain NB 176 (SD-5428), Pasteurella puncture (of Pasteuria Penetrans ), Pasteuria spp . ( Rotylenchulus reniformis ) -PR3 (accession number ATCC SD-5834), Streptomyces microflavus strain AQ6121 (=QRD 31.013, NRRL B-50550), Streptomyces galbus strain AQ 6047 (accession number NRRL 30232).
此等已用為或可用為生物性殺蟲劑之真菌及酵母實例為:巴氏蠶白僵菌(Beauveria bassiana),特定言之菌株ATCC 74040;微坦盾殼黴(Coniothyrium minitans),特定言之菌株CON/M/91-8(登錄號DSM-9660);輪枝菌屬(Lecanicillium spp.),特定言之菌株HRO LEC 12;蠟蚧輪枝菌(Lecanicillium lecanii)(過去稱為Verticillium lecanii),特定言之菌株KV01;黑殭菌(Metarhizium anisopliae),特定言之菌株F52(DSM3884/ATCC 90448);核果梅奇酵母(Metschnikowia fructicola),特定言之菌株NRRL Y-30752;玫煙色擬青霉(Paecilomyces fumosoroseus)(現在稱為:玫烟色棒束孢(Isaria fumosorosea)),特定言之菌株IFPC 200613,或菌株Apopka 97(登錄號ATCC 20874);淡紫色擬青霉(Paecilomyces lilacinus),特定言之淡紫色擬青霉(P.lilacinus)菌株251(AGAL 89/030550);大孢籃狀菌(Talaromyces flavus),特定言之菌株V117b;深綠木黴 (Trichoderma atroviride),特定言之菌株SC1(登錄號CBS 122089);哈茨木黴(Trichoderma harzianum),特定言之哈茨木黴(T.harzianum rifai)T39(登錄號CNCM I-952)。 Examples of such fungi and yeasts that have been or can be used as biological insecticides are: Beauveria bassiana , specifically strain ATCC 74040; Coniothyrium minitans , specific words The strain CON/M/91-8 (accession number DSM-9660); Verticillium spp ., specifically the strain HRO LEC 12; Lecanicillium lecanii (formerly known as Verticillium lecanii) ), specifically strain KV01; Metarhizium anisopliae , specifically strain F52 (DSM3884/ATCC 90448); Metschnikowia fructicola , specific strain NRRL Y-30752; Paecilomyces fumosoroseus (now known as: Isaria fumosorosea ), specifically strain IFPC 200613, or strain Apopka 97 (accession number ATCC 20874); Paecilomyces lilacinus , specifically, P. lilacinus strain 251 (AGAL 89/030550); Talaromyces flavus , specifically strain V117b; Trichoderma atroviride , specific words Bacteria Strain SC1 (accession number CBS 122089); Trichoderma harzianum , specifically T. harzianum rifai T39 (accession number CNCM I-952).
此等已用為或可用為生物性殺蟲劑之病毒實例為:棉褐帶卷蛾(Adoxophyes orana)顆粒體病毒(GV)、蘋果蠹蛾(Cydia pomonella)顆粒體病毒(GV)、番茄夜蛾(Helicoverpa armigera)(棉蛉蟲)核型多角體病毒(NPV)、甜菜夜蛾(Spodoptera exigua)mNPV、草地斜紋夜蛾(Spodoptera frugiperda)mNPV、棉貪夜蛾(Spodoptera littoralis)NPV。 Examples of such viruses that have been or can be used as biological insecticides are: Adoxophyes orana granulosis virus (GV), Cydia pomonella granulosis virus (GV), tomato night Helicoverpa armigera (cotton mites) nuclear polyhedrosis virus (NPV), Spodoptera exigua mNPV, Spodoptera frugiperda mNPV, Spodoptera littoralis NPV.
亦包括以細菌與真菌作為'菌種'加至植物或植株部分或植物器官中,並利用其特殊性質,促進植物生長與植物健康。其實例包括:土壤桿菌屬(Agrobacterium spp.)、甘藍固氮根瘤菌(Azorhizobium caulinodans)、固氮螺菌屬(Azospirillum spp.)、固氮菌屬(Azotobacter spp.)、慢生根瘤菌屬(Bradyrhizobium spp.)、伯克氏菌屬(Burkholderia spp.)(尤指洋蔥伯克氏菌(Burkholderia cepacia)(過去稱為洋蔥假單胞菌(Pseudomonas cepacia)))、巨孢球囊黴屬(Gigaspora spp.)或單孢巨孢球囊黴(Gigaspora monosporum)、菌根菌屬(Glomus spp.)、蠟蘑菌屬(Laccaria spp.)、布氏乳桿菌(Lactobacillus buchneri)、類球囊黴屬(Paraglomus spp.)、豆包菌(Pisolithus tinctorus)、假單胞菌屬(Pseudomonas spp.)、根瘤菌屬(Rhizobium spp.)(尤指三葉草根瘤菌(Rhizobium trifolii))、松露屬(Rhizopogon spp.)、硬皮馬勃菌屬(Scleroderma spp.)、乳牛肝菌屬(Suillus spp.)、鏈黴菌屬(Streptomyces spp.)。 It also includes the addition of bacteria and fungi as 'bacteria' to plants or plant parts or plant organs, and uses its special properties to promote plant growth and plant health. Examples include: Agrobacterium spp ., Azorhizobium caulinodans , Azospirillum spp ., Azotobacter spp ., Bradyrhizobium spp . ), Burkholderia spp . (especially Burkholderia cepacia (formerly known as Pseudomonas cepacia )), Gigaspora spp . Or Gigaspora monosporum , Glomus spp ., Laccaria spp ., Lactobacillus buchneri , Paraglomus Spp .), Pisolithus tinctorus , Pseudomonas spp ., Rhizobium spp . (especially Rhizobium trifolii ), Rhizopogon spp . Scleroderma spp ., Suillus spp ., Streptomyces spp .
已用為或可用為生物性除害劑之植物抽出物及由微生物形成之產物(包括蛋白質與二次代謝物)實例為:大蒜(Allium sativum)、中亞苦蒿(Artemisia absinthium)、印楝素 (azadirachtin)、Biokeeper WP、肉桂(Cassia nigricans)、苦皮藤(Celastrus angulatus)、臭杏(Chenopodium anthelminticum)、幾丁質、Armour-Zen、歐洲鱗毛蕨(Dryopteris filix-mas)、問荊草(Equisetum arvense)、Fortune Aza、Fungastop、Heads Up(藜麥(Chenopodium quinoa)皂苷抽出物)、除蟲菊/除蟲菊酯、苦木(Quassia amara)、櫟屬(Quercus)、皂樹(Quillaja)、虎杖抽出物(Regalia)、"RequiemTM Insecticide"、魚藤酮、魚尼丁(ryania)/雷諾丁(ryanodine)、聚合草(Symphytum officinale)、菊蒿(Tanacetum vulgare)、百里酚、Triact 70、TriCon、金蓮花(Tropaeulum majus)、大蕁麻(Urtica dioica)、藜蘆鹼(Veratrin)、槲寄生(Viscum album)、十字花科抽出物,特定言之油菜籽粉或芥末粉。 Examples of plant extracts that have been or can be used as biological pesticides and products formed by microorganisms, including proteins and secondary metabolites, are: Allium sativum, Artemisia absinthium, Neem Azadirachtin, Biokeeper WP, Cassia nigricans, Celastrus angulatus, Chenopodium anthelminticum, chitin, Armour-Zen, Dryopteris filix-mas, phoenix Equisetum arvense, Fortune Aza, Fungastop, Heads Up (Chenopodium quinoa saponin extract), pyrethrum/pyremethrin, Quasisia amara, Quercus, soap tree Quillaja), Regalia, "Requiem TM Insecticide", rotenone, ryania / ryanodine, Symphytum officinale, Tanacetum vulgare, thymol, Triact 70, TriCon, Tropaeulum majus, Urtica dioica, Veratrin, Viscum album, Cruciferous extract, specifically rapeseed meal or mustard powder.
式(I)化合物可與安全劑組合,例如:解草酮(benoxacor)、解毒喹(cloquintocet(-mexyl))、解草胺腈(cyometrinil)、環丙磺草胺(cyprosulfamide)、二氯丙烯胺(dichlormid)、解草唑(fenchlorazole)(-ethyl)、解草啶(fenclorim)、解草安(flurazole)、氟草肟(fluxofenim)、解草唑(furilazole)、雙苯唑酸(isoxadifen(-ethyl))、吡唑解草酯(mefenpyr(-diethyl))、萘甲酸酐、解草腈(oxabetrinil)、2-甲氧基-N-({4-[(甲基胺甲醯基)胺基]苯基}磺醯基)苯甲醯胺(CAS 129531-12-0)、4-(二氯乙醯基)-1-氧雜-4-氮雜螺[4.5]癸烷(CAS 71526-07-3)、2,2,5-三甲基-3-(二氯乙醯基)-1,3-唑啶(CAS 52836-31-4)。 The compound of formula (I) may be combined with a safener, for example: benoxacor, cloquintocet (-mexyl), cyometrinil, cyprosulfamide, dichloropropene Dichlormid, fenchlorazole (-ethyl), fenclorim, flurazole, fluxofenim, turfgrass Furilazole, diphenyl Isozoic acid (isethyldifen (-ethyl)), mefenpyr (-diethyl), naphthalic anhydride, oxabetrinil, 2-methoxy-N-({4-[(methyl) Aminomethyl)amino]phenyl}sulfonyl)benzamide (CAS 129531-12-0), 4-(dichloroethenyl)-1-oxa-4-azaspiro[4.5 ] decane (CAS 71526-07-3), 2,2,5-trimethyl-3-(dichloroethenyl)-1,3- Azole (CAS 52836-31-4).
所有植物與植株部份均可根據本發明處理。此時,咸瞭解植物係指所有植物及植物族群,如:需要及不需要之野生植物或作物(包括天然作物),例如:穀類(小麥、稻、硬粒小麥、大麥、裸麥、燕麥)、玉 米、大豆、馬鈴薯、甜菜、甘蔗、番茄、豆與其他蔬菜類、棉花、菸草、油菜、與果實植物(蘋果、梨、柑橘類果實與葡萄)。作物可為得自依傳統育種法與最適化方法或利用生物技術與遺傳工程法或此等方法之組合所取得者,包括轉殖基因植物,及包括受植物育種者權益保護或未受保護之植物栽培品種。咸瞭解,植株部份意指植物之所有地上及地下部份與器官,如:芽、葉、花與根,其實例可述及:闊葉、針葉、莖、樹幹、花、果實體、果實與種子,及根、球莖、與根莖。植株部份亦包括收成之植物,及無性與有性繁殖材料,例如:扦插、球莖、根莖、插枝與種子。 All plant and plant parts can be treated in accordance with the present invention. At this time, the salty plant refers to all plants and plant groups, such as wild plants or crops (including natural crops) that are needed and not needed, for example: cereals (wheat, rice, durum wheat, barley, rye, oats) ,jade Rice, soybeans, potatoes, beets, sugar cane, tomatoes, beans and other vegetables, cotton, tobacco, canola, and fruit plants (apples, pears, citrus fruits and grapes). Crops may be obtained from traditional breeding methods and optimization methods or using biotechnology and genetic engineering methods or combinations of such methods, including genetically modified plants, and including protected or unprotected by plant breeders' rights. Plant cultivars. It is understood that plant parts mean all above-ground and underground parts and organs of plants, such as buds, leaves, flowers and roots. Examples can be described as: broadleaf, needles, stems, trunks, flowers, fruit bodies, Fruits and seeds, and roots, bulbs, and rhizomes. The plant parts also include harvested plants, as well as vegetative and sexually propagated materials such as cuttings, bulbs, rhizomes, cuttings and seeds.
根據本發明使用式(I)化合物處理植物與植株部份之方法係依習用之處理法直接處理或使化合物作用在其周圍、環境或庫存空間,例如:浸泡、噴灑、蒸發、霧化、撒播、塗刷、注射,且若處理繁殖材料時,特定言之處理種子時,亦可施加一層或多層包衣。 The method of treating plants and plant parts using the compounds of formula (I) according to the invention is carried out according to conventional treatments or by acting on the surrounding, environmental or stock space, for example: soaking, spraying, evaporating, atomizing, spreading , brushing, injecting, and when processing the propagation material, one or more layers of coating may also be applied when the seed is treated specifically.
如上述,根據本發明亦可處理所有植物與其部份植株。較佳具體實施例中係處理野生植物品種與植物栽培品種或彼等由傳統生物育種法(如:交配法或原生質融合法)取得者,與其部份植株。另一項較佳具體實施例中,係處理由遺傳工程方法(若適當時,可併用傳統方法)得到之轉殖基因植物與植物栽培品種(基因改造生物),及其部份植株。術語"部份"或"植株部份"或"部份植株"已如上述說明。特別佳者,本發明係處理自商品取得或使用中之植物栽培品種之植物。咸瞭解,植物栽培品種意指經由傳統育種法、誘變法或重組DNA技術得到之具有新穎性質("性狀")之植物。其可為栽培品種、變異種、生物型或基因型。 As mentioned above, all plants and parts thereof can also be treated according to the invention. In a preferred embodiment, wild plant varieties and plant cultivars or those obtained by conventional biological breeding methods (e.g., mating method or protoplast fusion method) are treated with some of the plants. In another preferred embodiment, the transgenic plants and plant cultivars (genetically modified organisms) obtained by genetic engineering methods (and, if appropriate, conventional methods), and parts thereof are treated. The terms "part" or "plant part" or "partial plant" have been described above. Particularly preferred, the present invention is a plant that processes plant cultivars obtained or used in the art. It is understood that plant cultivars mean plants having novel properties ("traits") obtained by conventional breeding methods, mutagenesis methods or recombinant DNA techniques. It can be a cultivar, a variant, a biotype or a genotype.
根據本發明處理之較佳轉殖基因植物或植物栽培品種(彼等由遺傳工程取得者)包括所有透過基因改造過程,接受賦與特別有利性 質(”性狀”)之遺傳物質之植物。此等性質實例為改善植物生長、提高對高溫或低溫之耐受性、提高對乾旱或對水含量或土壤鹽含量之耐受性、提高開花率、簡化收成、加速成熟、提高收成量、提高所收成產品之品質與/或提高營養價值、所收成產品之更佳儲存壽命與/或提高可加工性。其他及特別強調之此等性質實例為提高植物對抗動物害蟲與有害微生物之防禦性,如:由例如:植物內所形成之毒素,特定言之由來自蘇雲金芽孢桿菌(Bacillus thuringiensis)之遺傳物質(例如:基因CryIA(a)、CryIA(b)、CryIA(c)、CryIIA、CryIIIA、CryIIIB2、Cry9c Cry2Ab、Cry3Bb與CryIF及其組合)於植物中產生之毒素來對抗昆蟲、蜘蛛、線蟲、蟎類、蛞蝓與蝸牛,進一步利用例如:後天取得之全株抗性(SAR)、系統素(systemin)、植物抗毒素(phytoalexins)、誘發素(elicitors)與抗性基因,及相應表現之蛋白質與毒素,提高植物對抗植物病原性真菌、細菌與/或病毒之抗性,亦提高植物對某些除草活性化合物,例如:咪唑啉酮類、磺醯脲類、嘉磷塞(glyphosata)或草銨膦(phosphonotricin)之耐受性(例如:"PAT"基因)。此等賦與所需性狀之基因亦可相互組合進入轉殖基因植物中。轉殖基因植物實例包括重要作物,如:穀類(小麥、稻、硬粒小麥、大麥、裸麥、燕麥)、玉米、大豆、馬鈴薯、甜菜、甘蔗、番茄、豌豆及其他蔬菜品種、棉花、菸草、油菜與果實植物(生產蘋果、梨、柑橘類水果與葡萄),特別著重於玉米、大豆、小麥、稻、馬鈴薯、棉花、甘蔗、番茄與油菜。特別強調之性質(”性狀”)為提高植物對抗昆蟲、蜘蛛、線蟲、蛞蝓與蝸牛之抗性。 Preferred transgenic plants or plant cultivars (which are acquired by genetic engineering) treated in accordance with the present invention, including all through genetic modification processes, receive special endowment A plant of genetic material ("trait"). Examples of such properties are to improve plant growth, increase tolerance to high or low temperatures, increase tolerance to drought or water content or soil salt content, increase flowering rate, simplify harvest, accelerate ripening, increase harvest, and increase The quality of the harvested product and/or improved nutritional value, better shelf life of the harvested product and/or improved processability. Other and particularly emphasized examples of such properties are the enhancement of the defensiveness of plants against animal pests and harmful microorganisms, such as, for example, toxins formed in plants, in particular by genetic material from Bacillus thuringiensis ( For example: the genes CryIA (a), CryIA (b), CryIA (c), CryIIA, CryIIIA, CryIIIB2, Cry9c Cry2Ab, Cry3Bb and CryIF and combinations thereof to produce toxins in plants against insects, spiders, nematodes, mites , cockroaches and snails, further utilizing, for example, acquired whole plant resistance (SAR), systemin, phytoalexins, elicitors and resistance genes, and corresponding proteins and toxins, Increasing the resistance of plants to phytopathogenic fungi, bacteria and/or viruses, and also increasing the herbicidal activity of certain compounds, such as imidazolinones, sulfonylureas, glyphosata or glufosinate ( Tolerance of phosphonotricin) (eg "PAT" gene). These genes, which confer the desired trait, can also be combined into a transgenic plant. Examples of genetically modified plants include important crops such as: cereals (wheat, rice, durum wheat, barley, rye, oats), corn, soybeans, potatoes, sugar beets, sugar cane, tomatoes, peas and other vegetable varieties, cotton, tobacco , rapeseed and fruit plants (production of apples, pears, citrus fruits and grapes), with particular emphasis on corn, soybeans, wheat, rice, potatoes, cotton, sugar cane, tomatoes and canola. A special emphasis on the nature ("traits") is to increase the resistance of plants to insects, spiders, nematodes, mites and snails.
使用式(I)化合物處理植物與植株部份之方法係依習用之處理法直接處理或使化合物作用在其周圍、棲息地或庫存空間,例如:浸泡、噴灑、噴霧、灌注、蒸發、撒粉、霧化、撒播、起泡、塗刷、散播、 注射、澆水(澆淋)、滴灌,若處理繁殖材料時,特定言之處理種子時,可進一步為供乾式處理種子之粉末、濕式處理種子之溶液、漿式處理種子之水溶性粉末、包殼、塗佈一層或多層包衣,等等。亦可進一步採用超低體積法施用式(I)化合物或取施用型式或式(I)化合物本身注射至土壤中。 The method of treating plants and plant parts using a compound of formula (I) is carried out by conventional treatment or by applying the compound to its surroundings, habitat or stock space, for example: soaking, spraying, spraying, pouring, evaporating, dusting , atomization, spreading, foaming, painting, spreading, Injection, watering (pouring), drip irrigation, when the propagation material is treated, in particular, when the seed is treated, the powder for dry treatment, the solution of the wet treated seed, the water-soluble powder of the pulp treated seed, Encapsulating, coating one or more layers of coating, and the like. The compound of formula (I) may also be further applied by ultra low volume method or by injection of the compound of formula or formula (I) into the soil.
植物之較佳直接處理法為葉部施用法,亦即讓式(I)化合物施用在葉部,其中處理頻率及施用率應配合所針對害蟲之感染程度來調整。 A preferred direct treatment of plants is the foliar application method, i.e., the compound of formula (I) is applied to the leaves, wherein the frequency of treatment and the rate of application are adjusted to match the degree of infection of the pest in question.
若為全株作用性活性化合物時,式(I)化合物亦可經由根系到達植物。因此可藉由式(I)化合物對植物所在地之作用來處理植物。其作法可為例如:浸泡或混合至土壤或營養液中,亦即在植物所在地(例如:土壤或水耕系統)浸入液體型式之式(I)化合物,或藉由土壤施用法,亦即將式(I)化合物以固體型式(例如:呈粒劑型式)加至植物所在地。若為水稻作物時,其作法為量取式(I)化合物固體施用型式(例如:粒劑)加至水稻田中。 In the case of a whole plant active compound, the compound of formula (I) can also reach the plant via the root system. The plant can thus be treated by the action of the compound of formula (I) on the locus of the plant. The method can be, for example, immersion or mixing into soil or nutrient solution, that is, immersing in the liquid form of the compound of formula (I) at the plant site (for example, soil or hydroponic system), or by soil application method, (I) The compound is added to the locus of the plant in a solid form (for example, in the form of a granule). In the case of a rice crop, the method is to measure the solid application form of the compound of formula (I) (for example, granules) and add it to the paddy field.
長久以來已知藉由處理植物種子來控制動物害蟲且仍在改良中。然而,處理種子時,經常出現一些無法以令人滿意之方式解決之問題。因此需要發展一種保護種子及發芽植物之方法,其可以在儲存期間、播種後或植物發芽後免除或至少顯著減少另外施用除害劑。亦需要使活性化合物以最適當用量提供種子及發芽植物最佳保護程度,以免動物害蟲侵害,且不受所使用活性化合物傷害植物本身。特定言之,處理種子之方法亦應考量可抵抗或耐受害蟲之轉殖基因植物固有之殺昆蟲或殺線蟲性質,以便在最低之除害劑用量下,對種子及發芽植物達最佳保護程度。 It has long been known to control animal pests by treating plant seeds and still in the process of improvement. However, when dealing with seeds, there are often problems that cannot be solved in a satisfactory manner. There is therefore a need to develop a method of protecting seeds and germinating plants which can dispense with, or at least significantly reduce, the additional application of pesticides during storage, after sowing or after germination of the plants. It is also desirable to provide the active compound with optimum protection of the seed and the germinating plant in an optimum amount to avoid infestation by the animal pest and not to damage the plant itself by the active compound used. In particular, the method of seed treatment should also consider the insecticidal or nematicidal properties inherent in plants that are resistant or resistant to pests, so as to provide optimal protection of seeds and germinating plants at the lowest pesticide dosage. degree.
特定言之,本發明因此亦有關使用一種式(I)化合物處理種 子,以保護種子與發芽植物免於害蟲侵害之方法。根據本發明保護種子與發芽植物對抗害蟲侵害之方法亦包括以式(I)化合物與混合組份在一次操作中同時處理或依序處理之方法。亦包括以式(I)化合物與混合組份在不同時間處理種子之方法。 In particular, the invention therefore also relates to the use of a compound of formula (I) for treating species A method to protect seeds and germinating plants from pests. The method for protecting a seed from a germinating plant against pests according to the present invention also comprises a method of simultaneously treating or sequentially treating the compound of the formula (I) with the mixed component in one operation. Also included are methods of treating seeds with the compound of formula (I) and the mixed components at different times.
本發明同樣係有關一種以式(I)化合物於處理種子上之用途,以保護種子與所長成植物免於動物害蟲侵害。 The invention is also related to the use of a compound of formula (I) for treating seed to protect the seed from the grown plant from animal pests.
此外,本發明係有關一種已經過式(I)化合物處理之種子,以保護免於動物害蟲侵害。本發明亦係有關一種經過式(I)化合物與混合組份同時處理之種子。本發明亦有關一種經過式(I)化合物與混合組份在不同時間點處理之種子。若為經過式(I)化合物與混合組份在不同時間點處理之種子時,該等個別物質可存在於種子之不同覆層中。此時,包含式(I)化合物之覆層與包含混合組份之覆層可視需要利用中間層分隔。本發明亦係有關一種已經過式(I)化合物與混合組份作為包衣之一部份或作為包衣以外之另一層或多層塗覆之種子。 Furthermore, the invention relates to a seed which has been treated with a compound of formula (I) to protect against animal pests. The invention also relates to a seed which is treated simultaneously with a compound of formula (I) and a mixed component. The invention also relates to a seed treated at a different point in time via a compound of formula (I) and a mixed component. If the seed of the compound of formula (I) and the mixed component are treated at different time points, the individual substances may be present in different coatings of the seed. In this case, the coating comprising the compound of formula (I) and the coating comprising the mixed component may optionally be separated by an intermediate layer. The invention is also directed to a seed which has been subjected to the compound of formula (I) and the mixed component as part of the coating or as another layer or layers coated other than the coating.
此外,本發明係有關一種種子,其在經過式(I)化合物處理後,再經過包膜衣製程,以防止種子被塵粉磨損。 Furthermore, the present invention relates to a seed which, after being treated with a compound of formula (I), is subjected to a coating process to prevent the seed from being worn by the dust.
式(I)化合物之全株作用性化合物之優點之一在於經過此等處理之種子不僅可保護種子本身,而且可保護種子出土後所長成植株,對抗動物害蟲侵害。依此方式,即不需要在播種期間或播種後短時間內立即處理作物。 One of the advantages of the whole plant-active compound of the compound of the formula (I) is that the seed treated by such treatment not only protects the seed itself, but also protects the seed from growing into a plant after the seed is unearthed, against the pest of the animal. In this way, it is not necessary to treat the crop immediately during sowing or shortly after sowing.
另一項優點在於透過式(I)化合物處理種子,可促進該經過處理之種子發芽及出土。 Another advantage is that the treatment of the seed through the compound of formula (I) promotes germination and emergence of the treated seed.
同樣可視為優點之處在於式(I)化合物亦可特別用於轉殖基因種子。 It can also be considered to be advantageous in that the compounds of the formula (I) can also be used in particular for the transfer of genetic seeds.
此外,式(I)化合物亦可與訊號轉導技術組成物組合使用,結果可以改善與共生菌(如,例如:根瘤菌、菌根菌與/或內生細菌或真菌)之定殖,及/或達最佳固氮作用。 In addition, the compounds of formula (I) can also be used in combination with signal transduction technology compositions to improve colonization with commensal bacteria such as, for example, rhizobium, mycorrhizal and/or endophytic bacteria or fungi, and / or up to the best nitrogen fixation.
式(I)化合物適合保護任何用於農業、溫室、森林或園藝之植物栽培品種之種子。更特定言之,其包括穀類(例如:小麥、大麥、裸麥、燕麥與小米)、玉米、棉花、大豆、稻、馬鈴薯、葵花、咖啡、菸草、芥花、油菜、甜菜(例如:製糖用甜菜與飼料用甜菜)、花生、蔬菜(如:番茄、胡瓜、豆、十字花科蔬菜、洋蔥與萵苣)、果實植物、草皮與觀賞植物之種子。特別重要為處理穀類(如:小麥、大麥、裸麥與燕麥)、玉米、大豆、棉花、芥花、油菜與稻之種子。 The compounds of formula (I) are suitable for protecting any seed of plant cultivars used in agriculture, greenhouses, forests or horticulture. More specifically, it includes cereals (eg, wheat, barley, rye, oats and millet), corn, cotton, soybeans, rice, potatoes, sunflowers, coffee, tobacco, canola, canola, and beets (eg, for sugar production) Beets and fodder beets), peanuts, vegetables (eg tomatoes, courgettes, beans, cruciferous vegetables, onions and lettuce), fruit plants, turf and ornamental plants. Of particular importance is the treatment of cereals (eg wheat, barley, rye and oats), corn, soybeans, cotton, canola, canola and rice seeds.
亦如上述,式(I)化合物對轉殖基因種子之處理法亦特別重要。此時該植物種子通常包含至少一種可以控制特定言之具有殺昆蟲性質與/或殺線蟲性質之多肽表現之異源基因。該轉殖基因種子中之此等異源基因可源自下列微生物屬種,如:芽胞桿菌(Bacillus)、根瘤菌(Rhizobium)、假單胞菌(Pseudomonas)、沙雷氏菌(Serratia)、木黴(Trichoderma)、棒形桿菌(Clavibacter)、菌根菌(Glomus)或黏帚黴(Gliocladium)。本發明特別適合處理包含至少一種來自芽胞桿菌屬(Bacillus sp.)之異源基因之轉殖基因種子。更佳為該異源基因係來自蘇雲金芽胞桿菌(Bacillus thuringiensis)。 As also mentioned above, the compounds of formula (I) are also of particular importance for the treatment of genetically engineered seeds. At this point the plant seed typically comprises at least one heterologous gene that can control the expression of a polypeptide having insecticidal properties and/or nematicidal properties in particular. The transfected gene seed colonization of these heterologous genes may be derived from the following species of microorganisms, such as: Bacillus (Bacillus), Rhizobium (with Rhizobium), Pseudomonas (of Pseudomonas), Serratia (SERRATIA), Trichoderma (Trichoderma), rod-shaped bacilli (Clavibacter), mycorrhizal fungi (Glomus) or sticky broom mildew (Gliocladium). The invention is particularly suitable for treating seed of a transgenic gene comprising at least one heterologous gene from Bacillus sp . More preferably, the heterologous gene line is derived from Bacillus thuringiensis .
本發明內容中,式(I)化合物係施用至種子上。接受處理之種子最好處於充份穩定狀態,以免在處理過程中損傷。通常,可在收穫至播種期間任何時間點處理種子。所採用之種子通常已與植株分離且已脫除軸、殼、稈、包衣、穗或果肉。因此例如:可採用已經過採收、清潔且乾燥至可以儲存之水份含量之種子。或者亦可使用乾燥後再例如:經過水處理後再度乾燥之種子,例如:底層處理。處理稻種子時,亦可使用例如: 已吸水至特定階段(雞胸型階段)之種子,以改善發芽及較一致之出土。 In the context of the present invention, the compound of formula (I) is applied to the seed. The seed to be treated is preferably in a sufficiently stable state to avoid damage during processing. Typically, the seed can be treated at any point during harvesting to sowing. The seeds used have generally been separated from the plant and have been removed from the shaft, shell, stalk, coating, ear or pulp. Thus, for example, seeds that have been harvested, cleaned and dried to a moisture content that can be stored can be used. Alternatively, it may be used after drying, for example, a seed which has been dried after being treated with water, for example, a bottom treatment. When dealing with rice seeds, you can also use, for example: Seeds that have been absorbed to a specific stage (chicken-chest stage) to improve germination and more consistent emergence.
當處理種子時,通常必需小心選擇施用至種子之式(I)化合物與/或其他添加劑之施用量,以免破壞種子發芽,或不致於傷害所長成之植物。尤其當活性化合物在特定施用率下可能具有植物毒性時,必需確保此點。 When treating seeds, it is usually necessary to carefully select the amount of the compound of formula (I) and/or other additives applied to the seed so as not to damage the seed germination or to damage the grown plant. This must be ensured especially when the active compound may be phytotoxic at a particular application rate.
通常,式(I)化合物係呈合適調配物施用至種子上。處理種子之合適調配物與方法係習此相關技藝之人士習知者。 Typically, the compound of formula (I) is applied to the seed in a suitable formulation. Suitable formulations and methods for treating seeds are well known to those skilled in the art.
式(I)化合物可轉換成常用拌種調配物,如:溶液、乳液、懸浮液、粉劑、發泡劑、漿物或種子之其他包衣組成物,與ULV調配物。 The compound of formula (I) can be converted to conventional seed dressing formulations such as solutions, emulsions, suspensions, powders, foaming agents, other coating compositions of seeds or seeds, and ULV formulations.
此等調配物可依已知方式製造,混合式(I)化合物與常用之添加劑,例如:常用之補充劑,及溶劑或稀釋劑、染劑、濕化劑、分散劑、乳化劑、消泡劑、防腐劑、二次增稠劑、膠黏劑、赤霉素,及水。 These formulations may be prepared in a known manner by admixing the compound of formula (I) with conventional additives, such as: conventionally used supplements, and solvents or diluents, dyes, wetting agents, dispersing agents, emulsifiers, defoaming agents. Agents, preservatives, secondary thickeners, adhesives, gibberellins, and water.
根據本發明可使用之拌種調配物中可包含之適用染劑為此等目的常用之所有染劑。此時,可使用難溶於水之色素,或可使用水溶性染劑。可述及之實例包括彼等已知名稱為若丹明B(Rhodamin B)、C.I.紅色(Pigment Red)112號與C.I.溶劑紅(Solvent Red)1號之染劑。 Suitable dyes which may be included in the seed dressing formulations which may be used in accordance with the invention are generally used for such purposes. At this time, a pigment which is hardly soluble in water may be used, or a water-soluble dye may be used. Examples which may be mentioned include those known by the names Rhodamin B, C.I. Red (Pigment Red) No. 112 and C.I. Solvent Red No. 1.
根據本發明可使用之拌種調配物中可包含之適用濕化劑為可促進濕化及調配農化活性化合物時常用之所有物質。較佳為使用萘磺酸烷基酯類,如:萘磺酸二異丙基酯或-二異丁基酯。 Suitable moisturizing agents which may be included in the seed dressing formulations which can be used in accordance with the invention are all materials which are customary for promoting wetting and agrochemically active compounds. It is preferred to use alkyl naphthalenesulfonates such as diisopropyl naphthalenesulfonate or di-isobutyl ester.
根據本發明可使用之拌種調配物中可包含之適用分散劑與/或乳化劑為調配農化活性化合物時常用之所有非離子性、陰離子性與陽離子性分散劑。較佳為使用非離子性或陰離子性分散劑或非離子性或陰離子性分散劑之混合物。合適之非離子性分散劑尤其包括環氧乙烷/氧化丙烯嵌段聚合物、烷基苯酚聚二醇醚與三苯乙烯苯酚聚二醇醚,及其磷酸 化或硫酸化衍生物。合適之陰離子性分散劑尤其指木質素磺酸鹽、聚丙烯酸鹽與芳基磺酸鹽/甲醛縮合物。 Suitable dispersing agents and/or emulsifiers which may be included in the seed dressing formulations which can be used according to the invention are all nonionic, anionic and cationic dispersing agents which are customary in the formulation of agrochemically active compounds. It is preferred to use a mixture of a nonionic or anionic dispersant or a nonionic or anionic dispersant. Suitable nonionic dispersants include, in particular, ethylene oxide/propylene oxide block polymers, alkylphenol polyglycol ethers and tristyrylphenol polyglycol ethers, and their phosphoric acid Chemical or sulfated derivatives. Suitable anionic dispersants are especially referred to as lignosulfonates, polyacrylates and arylsulfonate/formaldehyde condensates.
根據本發明可使用之拌種調配物中可包含之消泡劑為調配農化活性化合物時常用之所有抑制泡沫物質。較佳為使用聚矽氧消泡劑與硬脂酸鎂。 Defoamers which may be included in the seed dressing formulations which can be used in accordance with the invention are all foam inhibiting substances which are conventionally used in the formulation of agrochemically active compounds. Preferably, a polyfluorene defoamer and magnesium stearate are used.
根據本發明可使用之拌種調配物中可包含之防腐劑為農化組成物中為了此等目的常用之所有物質。其實例包括二氯吩(dichlorophen)與苯甲醇半縮甲醛。 Preservatives which may be included in the seed dressing formulations which may be employed in accordance with the invention are all materials commonly used in agrochemical compositions for such purposes. Examples thereof include dichlorophen and benzyl alcohol hemiformal.
根據本發明可使用之拌種調配物中可包含之二次增稠劑為農化組成物中為了此等目的常用之所有物質。較佳實例包括:纖維素衍生物、丙烯酸衍生物、黃原膠、改質黏土與高分散性矽石。 Secondary thickeners which may be included in the seed dressing formulations which may be employed in accordance with the invention are all materials commonly used in agrochemical compositions for such purposes. Preferred examples include cellulose derivatives, acrylic acid derivatives, xanthan gum, modified clay and highly dispersible vermiculite.
根據本發明可使用之拌種調配物中可包含之適用膠黏劑為拌種產品中所有常用之結合劑。較佳實例包括聚乙烯基吡咯啶酮、聚乙酸乙烯酯、聚乙烯醇,與纖基乙酸鈉(tylose)。 Suitable adhesives which may be included in the seed dressing formulations which can be used in accordance with the invention are all commonly used binders in the seed dressing product. Preferred examples include polyvinylpyrrolidone, polyvinyl acetate, polyvinyl alcohol, and tylose.
根據本發明可使用之拌種調配物中可包含之赤霉素較佳為赤霉素A1、A3(=赤霉酸)、A4與A7;以使用赤霉酸特別佳。該赤霉素係已知者(參見R.Wegler“作物保護劑與除害劑之化學(Chemie der Pflanzenschutz-und Schädlingsbekämpfungsmittel)”,Vol.2,Springer Verlag,1970,pp.401-412)。 The gibberellins which may be included in the seed dressing formulations which can be used according to the invention are preferably gibberellins A1, A3 (=gibberellic acid), A4 and A7; particularly preferred for the use of gibberellic acid. This gibberellin is known (see R. Wegler "Chemie der Pflanzenschutz-und Schädlings bekämpfungsmittel", Vol. 2, Springer Verlag, 1970, pp. 401-412).
根據本發明可使用之拌種調配物可直接使用或加水稀釋後使用,用於處理各種不同種子。例如:該濃縮劑或其加水稀釋後所得之製劑可用於包覆穀類(如:小麥、大麥、裸麥、燕麥與硬粒小麥)之種子,及玉米、稻、油菜、豌豆、豆類、棉花、葵花、大豆及甜菜之種子,或各 種不同蔬菜之種子。可根據本發明使用之拌種調配物或其稀釋之施用型式亦可用於包覆轉殖基因植物之種子。 The seed dressing formulations which can be used in accordance with the invention can be used directly or after dilution with water for the treatment of various seeds. For example, the concentrate or its diluted water-added preparation can be used to coat seeds of cereals (eg, wheat, barley, rye, oats, and durum wheat), and corn, rice, canola, peas, beans, cotton, Sunflower, soybean and beet seeds, or each Seeds of different vegetables. Seed dressing formulations which may be used in accordance with the invention or their diluted application forms may also be used to coat seeds of transgenic plants.
根據本發明可使用之拌種調配物或其所製成施用型式用於處理種子時,可使用所有常用於拌種之合適混合裝置。明確言之,進行該拌種過程時,將種子置入混合機中,依分批或連續操作方式,添加所需拌種調配物特定用量,可直接添加或先加水稀釋後添加,混合直到調配物均勻分佈在種子上為止。若適當時可接著進行乾燥過程。 When the seed dressing formulations which can be used according to the invention or the application forms thereof are used for the treatment of the seed, all suitable mixing devices which are customary for seed dressing can be used. Specifically, when the seed dressing process is carried out, the seed is placed in a mixer, and the specific amount of the desired seed dressing is added according to batch or continuous operation, and can be directly added or diluted with water and added, mixed until blending The matter is evenly distributed on the seed. The drying process can then be carried out if appropriate.
根據本發明可使用之拌種調配物之施用率可在相當大範圍內變化。其依據調配物中式(I)化合物之特定含量及依據種子而變化。式(I)化合物之施用率通常在每公斤種子0.001至50克之間,較佳為每公斤種子0.01至15克之間。 The application rate of the seed dressing formulations which can be used in accordance with the invention can vary over a considerable range. It varies depending on the particular amount of the compound of formula (I) in the formulation and on the basis of the seed. The application rate of the compound of the formula (I) is usually between 0.001 and 50 g per kg of seed, preferably between 0.01 and 15 g per kg of seed.
在動物健康領域(亦即獸醫學領域),式(I)化合物可活性對抗動物寄生蟲,特定言之體外寄生蟲或體內寄生蟲。術語"體內寄生蟲"尤其包括蠕蟲與原蟲,如:球蟲目(Coccidia)。體外寄生蟲通常且較佳為節肢動物,尤指昆蟲與蜱蟎類。 In the field of animal health (ie, the field of veterinary medicine), the compounds of formula (I) are active against animal parasites, in particular ectoparasites or endoparasites. The term "endoparasite" includes, inter alia, helminths and protozoa, such as Coccidia. Extracorporeal parasites are usually and preferably arthropods, especially insects and mites.
在獸醫學領域中,對恆溫動物具有有利毒性之式(I)化合物適合在畜牧、養殖動物、動物園動物、實驗室動物、實驗動物與家畜動物中控制出現在動物養殖及動物畜養中之寄生蟲。其可活性對抗寄生蟲之所有或特定發展階段。 In the field of veterinary medicine, the compound of formula (I) which is advantageously toxic to warm-blooded animals is suitable for controlling parasites present in animal husbandry and animal husbandry in livestock, farm animals, zoo animals, laboratory animals, laboratory animals and livestock animals. . It can be active against all or specific stages of development of the parasite.
農業牲畜包括例如:哺乳動物,如:綿羊、山羊、馬、驢、駱駝、水牛、兔子、馴鹿、黇鹿及尤指牛與豬;禽類,如:火雞、鴨、鵝,及尤指雞;魚類與甲殼類,例如:水產養殖,及昆蟲,如:蜜蜂。 Agricultural livestock include, for example, mammals such as sheep, goats, horses, donkeys, camels, buffalos, rabbits, reindeer, elk and especially cattle and pigs; poultry such as turkeys, ducks, geese, and especially chickens Fish and crustaceans, such as: aquaculture, and insects such as bees.
家畜動物包括例如:哺乳動物,如:倉鼠、天竺鼠,大鼠、 小鼠、栗鼠、雪貂,及特定言之狗、貓、籠內的鳥、爬蟲類、兩棲類或水族箱內的魚。 Livestock animals include, for example, mammals such as hamsters, guinea pigs, rats, Mice, chinchillas, ferrets, and specific dogs, cats, birds in cages, reptiles, amphibians, or fish in aquaria.
較佳具體實施例中,式(I)化合物係投與哺乳動物。 In a preferred embodiment, the compound of formula (I) is administered to a mammal.
另一項較佳具體實施例中,式(I)化合物係投與鳥類,亦即籠內的鳥,且尤指禽類。 In another preferred embodiment, the compound of formula (I) is administered to birds, i.e., birds in a cage, and especially to birds.
使用式(I)化合物控制動物寄生蟲,係計畫降低或防止生病、死亡例及下降之效能(指肉品、乳品、毛、皮、蛋、蜂蜜,等等),因此可以達到更經濟及更簡單之動物管理及更佳之動物效益。 The use of a compound of formula (I) to control animal parasites is intended to reduce or prevent the onset of illness, death and decline (referred to as meat, dairy, wool, hide, egg, honey, etc.), thereby achieving a more economical Simpler animal management and better animal benefits.
在動物健康之相關領域中,術語"控制"或"防治"係指式(I)化合物可有效降低特定寄生蟲在感染此等寄生蟲之動物中之發病率,使此等寄生蟲降至無害程度。更明確言之,本文所採用之"控制"係指式(I)化合物可以有效殺死各寄生蟲、抑制其生長或抑制其繁殖。 In the field of animal health, the term "control" or "control" means that the compound of formula (I) is effective in reducing the incidence of specific parasites in animals infected with such parasites, rendering such parasites harmless. degree. More specifically, "control" as used herein refers to a compound of formula (I) that is effective in killing, inhibiting, or inhibiting the growth of various parasites.
節肢動物包括:蝨目(Anoplurida),例如:盲蝨屬(Haematopinus spp.)、長顎蝨屬(Linognathus spp.)、蝨蟎屬(Pediculus spp.)、陰蝨屬(Phtirus spp.)、管蝨屬(Solenopotes spp.);食毛目(Mallophagida)及鈍角亞目(Amblycerina)與細角亞目(Ischnocerina),例如:毛鳥蝨屬(Trimenopon spp.)、雞蝨屬(Menopon spp.)、巨毛蝨屬(Trinoton spp.)、羽蝨屬(Bovicola spp.)、嚼蝨屬(Werneckiella spp.)、毛虱屬(Lepikentron spp.)、食蟲虻屬(Damalina spp.)、獸鳥蝨屬(Trichodectes spp.)、貓羽蝨屬(Felicola spp.);雙翅目(Diptera)及長角亞目(Nematocerina)與短角亞目(Brachycerina),例如:伊蚊屬(Aedes spp.)、按蚊屬(Anopheles spp.)、庫蚊屬(Culex spp.)、蚋蚊屬(Simulium spp.)、真蚋屬(Eusimulium spp.)、白蛉屬(Phlebotomus spp.)、沙蠅屬(Lutzomyia spp.)、蚊屬(Culicoides spp.)、斑虻屬(Chrysops spp.)、蚋屬(Odagmia spp.)、維蚋屬(Wilhelmia spp.)、瘤 虻屬(Hybomitra spp.)、黃虻屬(Atylotus spp.)、虻屬(Tabanus spp.)、麻翅虻屬(Haematopota spp.)、Philipomyia屬、蜂虱屬(Braula spp.)、家蠅屬(Musca spp.)、齒股蠅屬(Hydrotaea spp.)、螫蠅屬(Stomoxys spp.)、血蠅屬(Haematobia spp.)、莫蠅屬(Morellia spp.)、廄蠅屬(Fannia spp.)、舌蠅屬(Glossina spp.)、麗蠅屬(Calliphora spp.)、綠蠅屬(Lucilia spp.)、金蠅屬(Chrysomyia spp.)、肉蠅屬(Wohlfahrtia spp.)、麻蠅屬(Sarcophaga spp.)、狂蠅屬(Oestrus spp.)、皮蠅屬(Hypoderma spp.)、胃蠅屬(Gasterophilus spp.)、蝨蠅屬(Hippobosca spp.)、蝨蠅屬(Lipoptena spp.)、羊蝨蠅屬(Melophagus spp.)、鼻狂蠅屬(Rhinoestrus spp.)、大蚊屬(Tipula spp.);蚤目(Siphonapterida),例如:蚤屬(Pulex spp.)、櫛頭蚤屬(Ctenocephalides spp.)、潛蚤屬(Tunga spp.)、鼠蚤屬(Xenopsylla spp.)、角葉蚤屬(Ceratophyllus spp.);異翅目(Heteropterida),例如:臭蟲屬(Cimex spp.)、錐蝽屬(Triatoma spp.)、紅腹獵蝽屬(Rhodnius spp.)、金圓蝽屬(Panstrongylus spp.);及蜚蠊目(Blattaria)之擾人及衛生害蟲。 Arthropods include: Anoplurida, for example: Haematopinus spp., Linognathus spp., Pediculus spp., Phtirus spp., tube Solenopotes spp.; Mallophagida and Amblycerina and Ischnocerina, for example: Trimenopon spp., Menopon spp. , Trinoton spp., Bovicola spp., Werneckiella spp., Lepikentron spp., Damalina spp., ostrich Genus (Trichodectes spp.), Felicola spp.; Diptera and Nematocerina and Brachycerina, for example: Aedes spp. , Anopheles spp., Culex spp., Simulium spp., Eusimulium spp., Phlebotomus spp., Sand fly genus Lutzomyia spp.), Culicoides spp., Chrysops spp., Odagmia spp., Wilhelmia spp., tumor Hybomitra spp., Atylotus spp., Tabanus spp., Haematopota spp., Philipomyia, Braula spp., Musca domestica (Musca spp.), Hydrotaea spp., Stomoxys spp., Haematobia spp., Morellia spp., Fannia spp. ), Glossina spp., Calliphora spp., Lucilia spp., Chrysomyia spp., Wohlfahrtia spp., genus Sarcophaga spp.), Oestrus spp., Hypoderma spp., Gasterophilus spp., Hippotosca spp., Lipoptena spp. Melophagus spp., Rhinoestrus spp., Tipula spp.; Siphonapterida, for example: Pulex spp., genus Ctenocephalides spp.), Tunga spp., Xenopsylla spp., Ceratophyllus spp.; Heteropterida, for example, Cimex spp. Triatoma spp., Rhododendron genus (R Hodnius spp.), Panstrongylus spp.; and Blattaria are disturbing and sanitary pests.
節肢動物進一步包括:蜱蟲(Acari)之亞綱(蜱蟎亞綱(Acarina))及後氣亞目(Metastigmata),例如:軟蜱科(Argasidae),如:銳緣蜱屬(Argas spp.)、鈍緣蜱屬(Ornithodorus spp.)、殘緣蜱屬(Otobius spp.);硬蜱科(Ixodidae),如:硬蜱屬(Ixodes spp.)、花蜱屬(Amblyomma spp.)、扇頭蜱(Rhipicephalus(牛蜱(Boophilus))屬、革蜱屬(Dermacentor spp.)、血蜱屬(Haemophysalis spp.)、璃眼蜱屬(Hyalomma spp.)、扇頭蜱屬(Rhipicephalus spp.)(多重宿主蜱之原始屬種);中氣亞目(Mesostigmata),如:刺皮蟎屬(Dermanyssus spp.)、禽刺蟎屬(Ornithonyssus spp.)、肺刺蟎屬(Pneumonyssus spp.)、耳蟎屬(Raillietia spp.)、肺刺蟎屬 (Pneumonyssus spp.)、胸孔蟎屬(Sternostoma spp.)、瓦蟎屬(Varroa spp.)、蜂蟎屬(Acarapis spp.);光芒蟲亞目(Actinedida)(前氣亞目(Prostigmata)),例如:蜂蟎屬(Acarapis spp.)、姬蟄蟎屬(Cheyletiella spp.)、禽螫蟎屬(Ornithocheyletia spp.)、肉蟎屬(Myobia spp.)、綿羊疥蟎屬(Psorergates spp.)、脂蟎屬(Demodex spp.)、恙蟎屬(Trombicula spp.)、新恙蟎屬(Neotrombicula spp.)、螫蟎屬(Listrophorus spp.);及粉蟎亞目(Acaridida)(無氣亞目(Astigmata)),例如:粉蟎屬(Acarus spp.)、食酪蟎屬(Tyrophagus spp.)、嗜木蟎屬(Caloglyphus spp.)、皮頸下蟎屬(Hypodectes spp.)、翼蟎屬(Pterolichus spp.)、癢蟎屬(Psoroptes spp.)、皮蟎屬(Chorioptes spp.)、耳蟎屬(Otodectes spp.)、疥蟎屬(Sarcoptes spp.)、耳蟎屬(Notoedres spp.)、鳥疥蟎屬(Knemidocoptes spp.)、雞蟎屬(Cytodites spp.)、雞雛蟎屬(Laminosioptes spp.)。 Arthropods further include: Acari subfamily (Acarina) and Metastigmata, for example: Argasidae, such as Argas spp. ), Ornithodorus spp., Otobius spp.; Ixodidae, such as: Ixodes spp., Amblyomma spp., fan Rhipicephalus (Boophilus) genus, Dermacentor spp., Haemophysalis spp., Hyalomma spp., Rhipicephalus spp. (the original genus of the genus genus); Mesostigmata, such as: Dermanyssus spp., Ornithonyssus spp., Pneumonyssus spp. Railietia spp., lung locust (Pneumonyssus spp.), Sternostoma spp., Varroa spp., Acarapis spp.; Actinedida (Prostigmata) For example, Acarapis spp., Cheyletiella spp., Ornithocheyletia spp., Myobia spp., Psorergates spp. , Demodex spp., Trombula spp., Neotrombicula spp., Listrophorus spp.; and Acaridida (no gas (Astigmata), for example: Acarus spp., Tyrophagus spp., Caloglyphus spp., Hypodectes spp., pterygium Genus (Pterolichus spp.), Psoroptes spp., Chorioptes spp., Otodectes spp., Sarcoptes spp., Notoedres spp. ), genus Knemidocoptes spp., Cytodites spp., Laminosioptes spp.
寄生性原蟲實例包括:鞭毛門(Mastigophora)(鞭毛動物綱(Flagellata)),例如:錐蟲科(Trypanosomatidae),例如:布氏錐蟲(Trypanosoma b.brucei)、布氏剛比亞錐蟲(T.b.gambiense)、布氏羅德西亞錐蟲(T.b.rhodesiense)、剛果錐蟲(T.congolense)、克氏錐蟲(T.cruzi)、伊氏錐蟲(T.evansi)、馬錐蟲(T.equinum)、路易氏錐蟲(T.lewisi)、鱸魚錐蟲(T.percae)、猿猴錐蟲(T.simiae)、活動錐蟲(T.vivax)、巴西利什曼原蟲(Leishmania brasiliensis)、杜氏利什曼原蟲(L.donovani)、熱帶利什曼原蟲(L.tropica),例如:毛滴蟲科(Trichomonadidae),例如:藍氏賈第鞭毛蟲(Giardia lamblia)、犬賈第鞭毛蟲(G.canis)肉質鞭毛蟲門(Sarcomastigophora)(根足蟲綱(Rhizopoda)),如:內阿米巴科(Entamoebidae),例如:溶組織內阿米巴(Entamoeba histolytica)、哈曼原蟲科(Hartmanellidae),例如:棘阿米巴屬(Acanthamoeba sp.)、哈曼原蟲屬 (Harmanella sp.)頂複合器門(Apicomplexa)(孢子蟲綱(Sporozoa)),如:艾美球蟲科(Eimeridae),例如:雞球蟲(Eimeria acervulina)、腺樣艾美球蟲(E.adenoides)、阿拉巴艾美爾球蟲(E.alabamensis)、鴨艾美耳球蟲(E.anatis)、鵝艾美球蟲(E.anseris)、阿氏艾美球蟲(E.arloingi)、阿洛尼氏艾美球蟲(E.ashata)、奧本艾美球蟲(E.auburnensis)、牛艾美球蟲(E.bovis)、波氏艾美球蟲(E.brunetti)、犬艾美球蟲(E.canis)、栗鼠艾美球蟲(E.chinchillae)、鯡魚艾美球蟲(E.clupearum)、鴿艾美球蟲(E.columbae)、扭轉艾美球蟲(E.contorta)、槌狀艾美球蟲(E.crandalis)、狄氏艾美球蟲(E.debliecki)、分散艾美球蟲(E.dispersa)、橢圓艾美球蟲(E.ellipsoidales)、鐮形艾美球蟲(E.falciformis)、福氏艾美球蟲(E.faurei)、黃色艾美球蟲(E.flavescens)、加洛帕沃尼艾美球蟲(E.gallopavonis)、哈氏艾美球蟲(E.hagani)、腸艾美球蟲(E.intestinalis)、易洛魁艾美球虫(E.iroquoina)、伊氏艾美球虫(E.irresidua)、拉本艾美球虫(E.labbeana)、留氏艾美球蟲(E.leucarti)、大型艾美球蟲(E.magna)、巨型艾美球蟲(E.maxima)、中型艾美球蟲(E.media)、火雞艾美球蟲(E.meleagridis)、火雞和緩艾美球蟲(E.meleagrimitis)、和緩艾美球蟲(E.mitis)、毒害艾美球蟲(E.necatrix)、雅氏艾美球蟲(E.ninakohlyakimovae)、羊艾美球蟲(E.ovis)、小型艾美球蟲(E.parva)、孔雀艾美球蟲(E.pavonis)、穿孔艾美球蟲(E.perforans)、法森艾美球蟲(E.phasani)、梨形艾美球蟲(E.piriformis)、早熟艾美球蟲(E.praecox)、艾美球蟲(E.residua)、粗糙艾美球蟲(E.scabra)、艾美球蟲屬(E.spec.)、斯氏艾美球蟲(E.stiedai)、豬艾美球蟲(E.suis)、柔嫩艾美球蟲(E.tenella)、樹艾美球蟲(E.truncata)、特魯特艾美球蟲(E.truttae)、朱氏艾美球蟲(E.zuernii)、球蟲屬(Globidium spec.)、貝氏等孢球蟲(Isospora belli)、犬等孢 球蟲(I.canis)、貓等孢球蟲(I.felis)、俄亥俄等孢球蟲(I.ohioensis)、芮氏等孢球蟲(I.rivolta)、等孢球蟲屬(I.spec.)、豬等孢球蟲(I.suis)、囊等孢球蟲屬(Cystisospora spec.)、隱孢子蟲屬(Cryptosporidium spec.),特定言之小隱孢子蟲(C.parvum);如:弓形蟲科(Toxoplasmadidae),例如:鼠弓形蟲(Toxoplasma gondii)、哈芒球蟲(Hammondia heydornii)、犬新孢子蟲(Neospora caninum)、貝內特貝斯諾孢子蟲(Besnoitia besnoitii);如:肉孢子蟲科(Sarcocystidae),例如:牛犬肉孢子蟲(Sarcocystis bovicanis)、牛人肉孢子蟲(S.bovihominis)、羊犬肉孢子蟲(S.ovicanis)、羊貓肉孢子蟲(S.ovifelis)、神經肉孢子蟲(S.neurona)、肉孢子蟲屬(S.spec.)、豬人肉孢子蟲(S.suihominis);如:白細胞蟲科(Leucozoidae),例如:西氏住白細胞蟲(Leucozytozoon simondi);如:瘧原蟲科(Plasmodiidae),例如:柏格氏鼠瘧原蟲(Plasmodium berghei)、惡性瘧原蟲(P.falciparum)、三日瘧原蟲(P.malariae)、卵形瘧原蟲(P.ovale)、間日瘧原蟲(P.vivax)、瘧蟲屬(P.spec.);如:焦蟲目(Piroplasmea),例如:阿根廷巴貝蟲(Babesia argentina)、牛巴貝蟲(B.bovis)、犬巴貝蟲(B.canis)、巴貝蟲屬(B.spec.)、小泰勒蟲(Theileria parva)、泰勒蟲屬(Theileria spec.);如:匿蟲亞目(Adeleina),例如:犬肝簇蟲(Hepatozoon canis)、肝簇蟲屬(H.spec.)。 Examples of parasitic protozoa include: Mastigophora (Flagellata), for example: Trypanosomatidae, for example: Trypanosoma b. brucei, Trypanosoma brucei (Tbgambiense), Tbrhodesiense, T. congolense, T. cruzi, T. evansi, and trypanosomes (T. convanolense) T. equinum), T. lewisi, T. percae, T. simiae, T. vivax, Leishmania Brasiliensis), L. donovani, L. tropica, for example: Trichomonadidae, for example: Giardia lamblia, G. canis Sarcomastigophora (Rhizopoda), such as Entamoebidae, for example: Entamoeba histolytica , Hartmanellidae, for example: Acanthamoeba sp., Harman prototheca (Harmanella sp.) Apicomplexa (Sporozoa), such as: Eimeridae, such as: Eimeria acervulina, Adenoid Eimeria (E .adenoides), E. alabamensis, E. anatis, E. anseris, E. arloingi ), E. ashata, E. auburnensis, E. bovis, E. brunetti , E. canis, E. chinchillae, E. clupearum, E. columbae, reversal of Eimeria (E. contorta), E. crandalis, E. debliecki, E. dispersa, E. ellipsoidales ), E. falciformis, E. faurei, E. flavescens, E. gallopavonis ), E. hagani, E. intestinalis, E. iroquoina, E. irresidua, E. labbeana, E. leucarti, E. magna, giant Emerald E. maxima, E. media, E. meleagridis, turkey and E. meleagrimitis, and Eimeria (E. coli) .mitis), E. necatrix, E. ninakohlyakimovae, E. ovis, E. parva, Peacock E. pavonis, E. perforans, E. phasani, E. piriformis, early maturing Eimeria (E. praecox), E. residua, E. scabra, E. spec., E. stiedai , E. suis, E. tenella, E. truncata, E. truttae, Zhu Ai E.zuernii, Globidium spec., Isospora belli, canine I. canis, I. felis, genus I. ohioensis, I. rivolta, etc., Isospora (I. Spec.), I. suis, genus Cystisospora spec., Cryptosporidium spec., specifically C. parvum; For example: Toxoplasmadidae, for example: Toxoplasma gondii, Hammondia heydornii, Neospora caninum, Besnoitia besnoitii; : Sarcocystidae, for example: Sarcocystis bovicanis, S. bovihominis, S. ovicanis, and sheep sarcocystis (S. Ovifelis), S.neurona, S. spec., S. suihominis; for example: Leucozoidae, for example, S. cerevisiae (Leucozytozoon simondi); for example: Plasmodiidae, for example: Plasmodium berghei, P. falciparum, three days Plasmodium (P. malariae), Plasmodium falciparum (P.ovale), Plasmodium vivax (P. vivax), Plasmodium (P. spec.); eg, Piroplasmea, For example: Babesia argentina, B. bovis, B. canis, B. spec., Theileria parva, Theileria spec.; for example: Adeleina, for example: Hepatozoon canis, H. spec.
病原性體內寄生蟲為蠕蟲,包括:扁形動物門(Platyhelmintha)(例如:單殖吸蟲、絛蟲及吸蟲)、線蟲、棘頭動物與舌形動物,包括:單殖吸蟲亞綱(Monogenea):例如:三代蟲屬(Gyrodactylus spp.)、指標蟲屬(Dactylogyrus spp.)、多盤吸蟲屬(Polystoma spp.);絛蟲:擬葉目(Pseudophyllidea),例如:廣節裂頭絛蟲屬(Diphyllobothrium spp.)、螺旋體蟲屬(Spirometra spp.)、裂頭絛蟲屬(Schistocephalus spp.)、舌 狀絛蟲屬(Ligula spp.)、吸葉絛蟲屬(Bothridium spp.)、大複殖門絛蟲屬(Diphlogonoporus spp.);圓葉目(Cyclophyllida),例如:中殖孔屬絛蟲屬(Mesocestoides spp.)、裸頭絛蟲屬(Anoplocephala spp.)、副裸頭絛蟲屬(Paranoplocephala spp.)、莫尼茨絛蟲屬(Moniezia spp.)、隧體絛蟲屬(Thysanosoma spp.)、曲子官絛蟲屬(Thysaniezia spp.)、無卵黃腺絛蟲(Avitellina spp.)、史提拉絛蟲屬(Stilesia spp.)、錫帶絛蟲屬(Cittotaenia spp.)、安迪亞絛蟲屬(Andyra spp.)、伯特絛蟲屬(Bertiella spp.)、帶絛蟲屬(Taenia spp.)、棘球絛蟲屬(Echinococcus spp.)、泡尾絛蟲屬(Hydatigera spp.)、戴文絛蟲屬(Davainea spp.)、雷氏絛蟲屬(Raillietina spp.)、包膜絛蟲屬(Hymenolepis spp.)、瘍棘殼絛蟲屬(Echinolepis spp.)、棘葉絛蟲屬(Echinocotyle spp.)、迪克氏絛蟲屬(Diochis spp.)、瓜實絛蟲屬(Dipylidium spp.)、約優克斯絛蟲屬(Joyeuxiella spp.)、雙孔絛蟲屬(Diplopylidium spp.);吸蟲:複殖綱(Digenea),例如:複口吸蟲屬(Diplostomum spp.)、莖雙穴吸蟲屬(Posthodiplostomum spp.)、血吸蟲屬(Schistosoma spp.)、毛畢屬(Trichobilharzia spp.)、毛樣線蟲屬(Ornithobilharzia spp.)、澳畢吸蟲屬(Austrobilharzia spp.)、巨畢吸蟲屬(Gigantobilharzia spp.)、彩蚴吸蟲屬(Leucochloridium spp.)、短咽吸蟲屬(Brachylaima spp.)、棘口吸蟲屬(Echinostoma spp.)、棘緣吸蟲屬(Echinoparyphium spp.)、棘隙吸蟲屬(Echinochasmus spp.)、低頸吸蟲屬(Hypoderaeum spp.)、肝吸蟲屬(Fasciola spp.)、擬片形吸蟲屬(Fasciolides spp.)、薑片蟲屬(Fasciolopsis spp.)、環腸吸蟲屬(Cyclocoelum spp.)、盲腔屬(Typhlocoelum spp.)、雙口吸蟲屬(Paramphistomum spp.)、杯殖吸蟲屬(Calicophoron spp.)、盤吸蟲屬(Cotylophoron spp.)、巨盤吸蟲屬(Gigantocotyle spp.)、菲策吸蟲屬 (Fischoederius spp.)、腹袋吸蟲屬(Gastrothylacus spp.)、背孔吸蟲屬(Notocotylus spp.)、下彎吸蟲屬(Catatropis spp.)、斜睾吸蟲屬(Plagiorchis spp.)、前殖吸蟲屬(Prosthogonimus spp.)、雙腔吸蟲屬(Dicrocoelium spp.)、闊盤吸蟲屬(Eurytrema spp.)、鮭吸蟲屬(Troglotrema spp.)、並殖吸蟲屬(Paragonimus spp.)、肛瘤吸蟲屬(Collyriclum spp.)、隱孔吸蟲屬(Nanophyetus spp.)、後睾吸蟲屬(Opisthorchis spp.)、支睪吸蟲屬(Clonorchis spp.)、次睾吸蟲屬(Metorchis spp.)、異形吸蟲屬(Heterophyes spp.)、後殖吸蟲屬(Metagonimus spp.);線蟲:毛形亞目(Trichinellida),例如:毛首線蟲屬(Trichuris spp.)、毛細線蟲屬(Capillaria spp.)、毛細線蟲屬(Paracapillaria spp.)、優鞘線蟲屬(Eucoleus spp.)、線蟲屬(Trichomosoides spp.)、旋毛蟲屬(Trichinella spp.);墊刃目(Tylenchida),例如:細頸線蟲屬(Micronema spp.)、糞桿線蟲屬(Strongyloides spp.);小桿亞目(Rhabditina),例如:圓線蟲屬(Strongylus spp.)、三齒線蟲屬(Triodontophorus spp.)、食道齒線蟲屬(Oesophagodontus spp.)、毛線線蟲屬(Trichonema spp.)、輻首線蟲屬(Gyalocephalus spp.)、柱咽線蟲屬(Cylindropharynx spp.)、盆口線蟲屬(Poteriostomum spp.)、線蟲屬(Cyclococercus spp.)、杯冠線蟲屬(Cylicostephanus spp.)、食道口線蟲屬(Oesophagostomum spp.)、夏桕線蟲屬(Chabertia spp.)、冠尾線蟲屬(Stephanurus spp.)、鉤蟲屬(Ancylostoma spp.)、彎口線蟲屬(Uncinaria spp.)、鉤蟲屬(Necator spp.)、仰口線蟲屬(Bunostomum spp.)、球首線蟲屬(Globocephalus spp.)、比翼線蟲屬(Syngamus spp.)、節蟲屬(Cyathostoma spp.)、後圓線蟲屬(Metastrongylus spp.)、網尾線蟲屬(Dictyocaulus spp.)、繆勒線蟲屬(Muellerius spp.)、原圓線蟲屬(Protostrongylus spp.)、新圓線蟲 屬(Neostrongylus spp.)、囊尾線蟲屬(Cystocaulus spp.)、肺圓線蟲屬(Pneumostrongylus spp.)、指尾線蟲屬(Spicocaulus spp.)、鹿圓線蟲屬(Elaphostrongylus spp.)、副麂圓線蟲屬(Parelaphostrongylus spp.)、環體線蟲屬(Crenosoma spp.)、副環體線蟲屬(Paracrenosoma spp.)、奧斯勒絲蟲屬(Oslerus spp.)、住血線蟲屬(Angiostrongylus spp.)、肺線蟲屬(Aelurostrongylus spp.)、類絲線蟲屬(Filaroides spp.)、副類絲線蟲屬(Parafilaroides spp.)、毛圓線蟲屬(Trichostrongylus spp.)、血線蟲屬(Haemonchus spp.)、奧斯特線蟲屬(Ostertagia spp.)、牛胃絲蟲屬(Teladorsagia spp.)、馬歇爾線蟲屬(Marshallagia spp.)、古柏線蟲屬(Cooperia spp.)、日圓線蟲屬(Nippostrongylus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、細頸線蟲(Nematodirus spp.)、胃圓線蟲屬(Hyostrongylus spp.)、尖頭胃線蟲屬(Obeliscoides spp.)、裂口線蟲屬(Amidostomum spp.)、壺肛線蟲屬(Ollulanus spp.);旋尾目(Spirurida),例如:尖尾線蟲屬(Oxyuris spp.)、蟯蟲屬(Enterobius spp.)、栓尾線蟲屬(Passalurus spp.)、管狀線蟲屬(Syphacia spp.)、無刺蟯蟲屬(Aspiculuris spp.)、異刺線蟲屬(Heterakis spp.);蛔蟲屬(Ascaris spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、貝利蛔蟲屬(Baylisascaris spp.)、副蛔屬(Parascaris spp.)、海獸胃線蟲屬(Anisakis spp.)、禽蛔屬(Ascaridia spp.);棘口線蟲屬(Gnathostoma spp.)、泡翼線蟲屬(Physaloptera spp.)、吸吮線蟲屬(Thelazia spp.)、筒線蟲屬(Gongylonema spp.)、馬胃線蟲屬(Habronema spp.)、副柔絲線蟲屬(Parabronema spp.)、德拉西線蟲屬(Draschia spp.)、龍線蟲屬(Dracunculus spp.);冠絲蟲屬(Stephanofilaria spp.)、類絲蟲屬(Parafilaria spp.)、絲狀線蟲屬(Setaria spp.)、羅阿絲蟲屬(Loa spp.)、血直絲蟲屬(Dirofilaria spp.)、光絲蟲屬(Litomosoides spp.)、布魯線蟲屬 (Brugia spp.)、吳策絲蟲屬(Wuchereria spp.)、蟠尾絲蟲屬(Onchocerca spp.)、旋尾線蟲屬(Spirocerca spp.);棘頭動物門(Acantocephala):少棘目(Oligacanthorhynchida),例如:巨吻棘頭蟲屬(Macracanthorhynchus spp.)、前睾棘頭蟲屬(Prosthenorchis spp.);多形目(Polymorphida),例如:細頸棘頭蟲屬(Filicollis spp.);念珠目(Moniliformida),例如:聯珠狀棘頭蟲屬(Moniliformis spp.);棘吻目(Echinorhynchida),例如:棘頭蟲屬(Acanthocephalus spp.)、魚棘頭蟲屬(Echinorhynchus spp.)、似細吻棘頭蟲屬(Leptorhynchoides spp.);舌形動物門(Pentastoma):孔頭蟲目(Porocephalida),例如:舌形蟲屬(Linguatula spp.)。 Pathogenic endoparasites are helminths, including: flat phylum (Platyhelmintha) (eg, monogonim, aphid, and trematode), nematodes, echinoderms, and lingual animals, including: Monogenea): for example: Gyrodactylus spp., Dactylogyrus spp., Polystoma spp.; Aphid: Pseudophyllidea, for example: Aphididae Genus (Diphyllobothrium spp.), Spirometra spp., Schistocephalus spp., tongue Ligula spp., Bothridium spp., Diphlogonoporus spp.; Cyclophyllida, for example, Mesocestoides spp. ), Anoplocephala spp., Paranoplocephala spp., Moniezia spp., Thysanosoma spp., Thysaniezia Spp.), Avitellina spp., Stilesia spp., Cittotaenia spp., Andyra spp., Burt's genus (Bertiella spp.), Taenia spp., Echinococcus spp., Hydatigera spp., Davainea spp., Aphis genus Raillietina spp.), Hymenolepis spp., Echinolepis spp., Echinocotyle spp., Diochis spp., Aphis genus (Dipylidium spp.), Joyeuxiella spp., Diplopylidium spp.; fluke: Digenea, for example: Diplostomum spp., Posthodiplostomum spp., Schistosoma spp., Trichobilharzia spp., hair Ornithobilharzia spp., Austrobilharzia spp., Gigantobilharzia spp., Leucochloridium spp., Brachylaima spp .), Echinostoma spp., Echinoparyphium spp., Echinochasmus spp., Hypoderaeum spp., liver fluke Genus (Fasciola spp.), Fasciolides spp., Fasciolopsis spp., Cyclocoelum spp., Typhlocoelum spp., double Paramphistomum spp., Calicophoron spp., Cotylophoron spp., Gigantocotyle spp., Phytophthora (Fischoederius spp.), Gastrothylacus spp., Notocotylus spp., Catatropis spp., Plagiorchis spp. Prosthogonimus spp., Dicrocoelium spp., Eurytrema spp., Troglotrema spp., Paragonimus Spp.), Collyriclum spp., Nanophyetus spp., Opisthorchis spp., Clonorchis spp., subtestis Metorchis spp., Heterophyes spp., Metagonimus spp.; Nematode: Trichinellida, for example: Trichuris spp. ), Capillaria spp., Paracapillaria spp., Eucoleus spp., Trichomosa spp., Trichinella spp.; (Tylenchida), for example: Micronema spp., Strongyloides spp.; Rhabditina, for example: round wire Strongylus spp., Triodontophorus spp., Oesophagodontus spp., Trichonema spp., Gyalocephalus spp., Nematode Cylindropharynx spp., Poteriostomum spp., Cyclococercus spp., Cylicostephanus spp., Oesophagostomum spp., Summer locust genus Chabertia spp.), Stephanurus spp., Ancylostoma spp., Uncinaria spp., Necator spp., Bunostomum spp. , Globocephalus spp., Syngamus spp., Cyathostoma spp., Metastrongylus spp., Dictyocaulus spp., 缪Muellerius spp., Protostrongylus spp., New round nematode Genus (Neostrongylus spp.), Cystocaulus spp., Pneumostrongylus spp., Spicocaulus spp., Elaphostrongylus spp. Nematode (Parelaphostrongylus spp.), Crenosoma spp., Paracrenosoma spp., Oslerus spp., Angiostrongylus spp. , Aelurostrongylus spp., Filaroides spp., Parafilaroides spp., Trichostrongylus spp., Haemonchus spp. Ostertagia spp., Teladorsagia spp., Marshallagia spp., Cooperia spp., Nippostrongylus spp. Heliconia (Heligmosomoides spp.), Nematodirus spp., Hyostrongylus spp., Obeliscoides spp., Amidostomum spp., anal sphincter Ollulanus spp.; Spirurida, example Such as: Oxyuris spp., Enterobius spp., Passalus spp., Syphacia spp., Aspiculuris spp. Heterakis spp.; Ascaris spp., Toxascaris spp., Toxocara spp., Baylisascaris spp., deputy Genus (Parascaris spp.), Anisakis spp., Ascaridia spp.; Gnathostoma spp., Physaloptera spp., Nematode Thelazia spp.), Gongylonema spp., Habronema spp., Parabronema spp., Draschia spp., and genus Dracunculus spp.); Stephanofilaria spp., Parafilaria spp., Setaria spp., Loa spp., Drosophila Genus (Dirofilaria spp.), Litomosoides spp., Brucella (Brugia spp.), Wuchereria spp., Onchocerca spp., Spirocerca spp.; Acantocephala: Oligacanthorhynchida For example: Macracanthorhynchus spp., Prosthenorchis spp.; Polymorphida, for example: Filiocollis spp.; Rosary (Moniliformida), for example: Moniliformis spp.; Echinorhynchida, for example: Acanthocephalus spp., Echinorhynchus spp., like Leptorhynchoides spp.; Pentastoma: Porocephalida, for example, Linguatula spp.
在獸醫與動物飼養領域中,式(I)化合物係呈合適之製劑型式,採用相關技藝上已知方法投藥,如:經腸、非經腸式、經皮膚或經鼻途徑投藥。該投藥法可為預防性或醫療性。 In the field of veterinary and animal feeding, the compound of formula (I) is in a suitable formulation and is administered by methods known in the art, such as enteral, parenteral, transdermal or nasal routes. The administration method can be prophylactic or medical.
因此,本發明一項具體實施例係指以式(I)化合物作為醫藥之用途。 Thus, a specific embodiment of the invention refers to the use of a compound of formula (I) as a medicament.
另一態樣係指一種以式(I)化合物作為抗體內寄生蟲劑,特定言之殺蠕蟲劑或抗原蟲劑之用途。式(I)化合物適合在例如:動物畜養、動物養殖、畜牧建築及衛生領域中作為抗體內寄生蟲劑,尤指殺蠕蟲劑或抗原蟲劑使用。 Another aspect refers to the use of a compound of formula (I) as an endoparasite, in particular an anthelmintic or antiprotozoal agent. The compounds of the formula (I) are suitable for use as an endoparasite, in particular an anthelmintic or antiprotozoal agent, in the field of animal husbandry, animal husbandry, animal husbandry and hygiene.
另一態樣係有關一種以式(I)化合物作為抗體外寄生蟲劑,特定言之殺節肢動物劑,如:殺昆蟲劑或殺蜱蟎劑之用途。另一態樣係指一種以式(I)化合物在例如:動物畜養、動物養殖、畜牧建築及衛生領域中作為抗體外寄生蟲劑,特定言之殺節肢動物劑,如:殺昆蟲劑或殺蜱蟎劑之用途。 Another aspect relates to the use of a compound of formula (I) as an antibody ectoparasite, in particular an arthropodicide, such as an insecticide or an acaricide. Another aspect refers to a compound of formula (I) as an antibody ectoparasite in animal breeding, animal husbandry, animal husbandry and health, for example, arthropodicides such as insecticides or killing agents. The use of tincture.
式(I)化合物亦可用於控制病媒。本發明內容中,病媒係會從帶原者(植物、動物、人類,等等)傳播病原菌(例如:病毒、蠕蟲、單細胞生物與細菌)給宿主之節肢動物,尤指昆蟲或蜘蛛類。該病原菌可經由機械式傳播至宿主(例如:經由非叮咬性蠅傳播之沙眼)或經由注入傳播至宿主(例如:由蚊子傳播之瘧疾寄生蟲)。 The compounds of formula (I) can also be used to control vectors. In the context of the present invention, a disease vector system transmits pathogenic bacteria (eg, viruses, worms, single-celled organisms, and bacteria) from the original (plants, animals, humans, etc.) to the host arthropods, especially insects or spiders. class. The pathogen can be transmitted mechanically to the host (eg, trachoma via non-bite flies) or via injection to a host (eg, malaria parasite transmitted by mosquitoes).
病媒及其所傳播之疾病或病原菌之實例為:1)蚊子- 按蚊(Anopheles):瘧疾、絲蟲病;- 庫蚊(Culex):日本腦炎、絲蟲病、其他病毒疾病、蠕蟲之傳播;- 伊蚊(Aedes):黃熱病、登革熱、絲蟲病、其他病毒疾病;- 蚋科(Simuliidae):傳播蠕蟲,特定言之,盤尾線蟲(Onchocerca volvulus);2)蝨:皮膚傳染病、流行性斑疹傷寒;3)跳蚤:疫病、鼠型斑疹傷寒;4)蠅:昏睡病(錐蟲病);霍亂、其他細菌性疾病;5)蟎:家畜疥癣病、流行性斑疹傷寒、立克次痘疹(rickettsialpox)、兔熱病(tularamia)、聖路易腦炎(Saint-Louis encephalitis)、蜱傳播性腦炎(TBE)、克里米亞-剛果惡性血液疾病(Krim-Kongo haematologic fever)、疏螺旋體病;6)蜱:疏螺旋體病(borelliosis),如:杜通氏螺旋體(Borrelia duttoni)、蜱傳播性腦炎、Q熱(貝氏考克斯菌(Coxiella burnetii))、焦蟲症(犬焦蟲症(Babesia canis canis))。 Examples of vectors and diseases or pathogens transmitted by them are: 1) mosquitoes - Anopheles: malaria, filariasis; - Culex: Japanese encephalitis, filariasis, other viral diseases, creeps Propagation of insects; - Aedes: yellow fever, dengue fever, filariasis, other viral diseases; - Simuliidae: spread worms, specifically, Onchocerca volvulus; 2) : skin infections, epidemic typhus; 3) fleas: blight, mouse-type typhus; 4) flies: sleeping sickness (trypanosis); cholera, other bacterial diseases; 5) cockroaches: livestock rickets , epidemic typhus, rickettsialpox, tularamia, Saint-Louis encephalitis, tick-borne encephalitis (TBE), Crimean-Congo blood Krim-Kongo haematologic fever, Borrelia; 6) 蜱: Borelliosis, such as: Borrelia duttoni, sputum-transmitted encephalitis, Q-heat (C. faecalis) (Coxiella burnetii)), coccidiosis (Babesia canis canis).
本發明內容中之病媒實例為昆蟲,例如:會傳播植物病毒 給植物之蚜蟲、蠅、葉蟬或薊馬。其他會傳播植物病毒之病媒為蜘蛛蟎、蝨、甲蟲與線蟲。 An example of a vector in the context of the present invention is an insect, for example, a plant virus is transmitted. Aphids, flies, leafhoppers or thrips that give plants. Other vectors that transmit plant viruses are spider mites, mites, beetles and nematodes.
本發明內容中之其他病媒實例為昆蟲與蜘蛛類,如:蚊子,尤指會傳播病原菌給動物與/或人類之伊蚊(Aedes)、按蚊(Anopheles),例如:甘比亞按蚊(A.gambiae)、阿拉伯按蚊(A.arabiensis)、致死按蚊(A.funestus)、大劣按蚊(A.dirus)(瘧疾)與庫蚊(Culex)、蝨、跳蚤、蠅、蟎、與蜱。 Examples of other vectors in the context of the present invention are insects and arachnids, such as: mosquitoes, especially Aedes, Anopheles, Anopheles, etc., which transmit pathogens to animals and/or humans, for example: Anopheles gambiae (A.gambiae), A. arabiensis, A. funestus, A. dirus (malaria) and Culex, cockroaches, fleas, flies, cockroaches And 蜱.
亦可能使用突破抗性之式(I)化合物控制病媒。 It is also possible to use a compound of formula (I) that breaks through resistance to control the vector.
式(I)化合物適用於預防由病媒傳播之疾病與/或病原菌。因此本發明另一態樣係以式(I)化合物於控制病媒之用途,例如:用於農業、園藝、花園與休閒活動設施,及亦用於保護材料與庫存產品。 The compounds of formula (I) are useful for the prevention of diseases and/or pathogenic bacteria transmitted by vectors. Thus, another aspect of the invention is the use of a compound of formula (I) for controlling a vector, for example, for use in agricultural, horticultural, garden and recreational activities, and also for protecting materials and stock products.
式(I)化合物適用於保護工業材料,對抗昆蟲之侵害或破壞,例如:鞘翅目(Coleoptera)、膜翅目(Hymenoptera)、等翅目(Isoptera)、鱗翅目(Lepidoptera)、囓蟲目(Psocoptera)與總尾目(Zygentoma)。 The compounds of formula (I) are suitable for the protection of industrial materials against insect damage or destruction, for example: Coleoptera, Hymenoptera, Isoptera, Lepidoptera, Diptera (Lepidoptera) Psocoptera) and total tail (Zygentoma).
咸了解,本文所指之工業材料為無生命材料,如:較佳為塑膠、膠黏劑、膠水、紙張與紙板、皮革、木料、加工木製品與塗料組成物。本發明用途特別適合保護木料。 It is understood that the industrial materials referred to herein are inanimate materials, such as: plastics, adhesives, glues, paper and cardboard, leather, wood, processed wood products and coatings. The use of the invention is particularly suitable for protecting wood.
另一項具體實施例中,式(I)化合物係與至少一種其他殺昆蟲劑與/或至少一種殺真菌劑共同使用。 In another embodiment, the compound of formula (I) is used in combination with at least one other insecticide and/or at least one fungicide.
另一項具體實施例中,式(I)化合物係呈即用型除害劑,亦即其不需要進一步修飾即可施用在所需材料上。合適之其他殺昆蟲劑或殺真菌劑特定言之係如上述說明者。 In another embodiment, the compound of formula (I) is a ready-to-use pesticide, i.e., it can be applied to the desired material without further modification. Suitable other insecticides or fungicides are specifically described above.
亦已驚人地發現,式(I)化合物可用於保護與鹽水或鹹水接 觸之物品,特定言之船體、隔板、編網、建築物、繫船設備及訊號系統,防止污塞。同樣地,式(I)化合物可單獨使用或與其他活性化合物組合,作為抗污塞劑使用。 It has also surprisingly been found that the compounds of formula (I) can be used to protect from salt water or salt water. Touch items, specific hulls, partitions, nets, buildings, mooring equipment and signal systems to prevent contamination. Likewise, the compounds of formula (I) can be used alone or in combination with other active compounds as anti-sick plugs.
式(I)化合物適合在衛生領域中控制動物害蟲。更特定言之,本發明可應用在居家領域、衛生領域及保護庫存產品中,尤其控制出現在如:住家、廠房、辦公室、車廂等封閉空間之昆蟲、蜘蛛與蟎類。式(I)化合物可單獨使用或與其他活性化合物與/或輔劑組合用於控制動物害蟲。其等較佳係家庭用殺昆蟲劑產品。式(I)化合物可有效對抗敏感性及抗性品種,並對抗所有發展階段。 The compounds of formula (I) are suitable for controlling animal pests in the hygiene sector. More specifically, the present invention can be applied to home, health, and inventory protection products, especially insects, spiders, and mites that appear in closed spaces such as homes, factories, offices, and cars. The compounds of formula (I) may be used alone or in combination with other active compounds and/or adjuvants for controlling animal pests. These are preferably household insecticide products. The compounds of formula (I) are effective against sensitive and resistant varieties and are resistant to all stages of development.
此等害蟲包括例如:蜘蛛綱(Arachnida),蠍目(Scorpiones)、蜘蛛目(Araneae)與盲蛛目(Opiliones);唇足綱(Chilopoda)與重足綱(Diplopoda);昆蟲綱,蜚蠊目(Blattodea)、鞘翅目(Coleoptera)、革翅目(Dermaptera)、雙翅目(Diptera)、異翅目(Heteroptera)、膜翅目(Hymenoptera)、等翅目(Isoptera)、鱗翅目(Lepidoptera)、毛蝨目(Phthiraptera)、囓蟲目(Psocoptera)、跳躍亞目(Saltatoria)或直翅目(Orthoptera)、蚤目(Siphonaptera)與總尾目(Zygentoma),及軟甲綱(Malacostraca)等足目(Isopoda)。 Such pests include, for example, Arachnida, Scorpiones, Araneae and Opiliones; Chilopoda and Diplopoda; Insecta, 蜚蠊(Blattodea), Coleoptera, Dermaptera, Diptera, Heteroptera, Hymenoptera, Isoptera, Lepidoptera ), Phthiraptera, Psocoptera, Saltatoria or Orthoptera, Siphonaptera and Zygentoma, and Malacostraca Isopoda.
其可呈例如:氣霧劑、無壓力噴灑產品,例如:泵壓及霧化噴灑器、自動噴霧系統、霧化器、發泡物、凝膠、使用由纖維素或塑膠製成之蒸發片之蒸發器產品、液體蒸發器、凝膠及膜式蒸發器、螺漿驅動式蒸發器、無能源或被動式蒸發系統、防蟲紙、防蟲袋及防蟲膠,呈粒狀或塵粉,用於撒播式誘餌或用於誘餌台等形式使用。 It may be, for example, an aerosol, a pressureless spray product such as: a pump and atomizer sprayer, an automatic spray system, an atomizer, a foam, a gel, using a vaporized sheet made of cellulose or plastic. Evaporator products, liquid evaporators, gel and membrane evaporators, screw-driven evaporators, energy-free or passive evaporation systems, insect-proof paper, insect-proof bags and insect-repellent glue, in the form of granules or dust particles. Used in the form of a spread bait or in a bait table.
下列製法與應用實例說明本發明,但未加以限制。採用1H-NMR或13C-NMR光譜儀與/或LC-MS(氣相層析法-質譜儀)判別產物特徵。 The following preparations and application examples illustrate the invention, but are not limited. The product characteristics were discriminated by 1H-NMR or 13C-NMR spectrometer and/or LC-MS (gas chromatography-mass spectrometer).
logP值測定法係依據EEC Directive 79/831 Annex V.A8,採用HPLC(高效液相層析法),使用逆相管柱(C18),依下列方法進行: The logP value method is based on EEC Directive 79/831 Annex V.A8, using HPLC (High Performance Liquid Chromatography), using reverse phase column (C18), according to the following method:
[a]LC-MS測定法係在pH 2.7之酸性範圍內,使用0.1%甲酸水溶液及乙腈(含0.1%甲酸)作為溶離劑,依10%乙腈至95%乙腈之線性梯度進行。表中以logP(HCOOH)表示。 [a] The LC-MS assay was carried out in a pH range of 2.7 using a 0.1% aqueous formic acid solution and acetonitrile (containing 0.1% formic acid) as the dissolving agent, with a linear gradient from 10% acetonitrile to 95% acetonitrile. The table is represented by logP (HCOOH).
[b]LC-MS測定法係在pH 7.8之中性範圍內,使用0.001莫耳濃度碳酸氫銨水溶液與乙腈作為溶離劑,依10%乙腈至95%乙腈之線性梯度進行。表中以logP(中性)表示。 [b] The LC-MS assay was carried out in a neutral range of pH 7.8 using a linear gradient of 10% acetonitrile to 95% acetonitrile using a 0.001 molar aqueous solution of ammonium bicarbonate and acetonitrile as the dissolving agent. The table is represented by logP (neutral).
採用具有已知logP-值之未分支之烷-2-酮類(具有3至16個碳原子)進行校正(在兩種連續烷酮之間使用滯留時間之線性內插法測定logP值)。 Calibration was performed using unbranched alkan-2-ones (having 3 to 16 carbon atoms) with known logP-values (logP values were determined using linear interpolation of residence time between two consecutive alkanones).
λ-最大值係採用200nm至400nm之UV光譜測定層析訊號之最大值。 The λ-maximum is the maximum value of the chromatographic signal measured by UV spectroscopy from 200 nm to 400 nm.
所選定實例之NMR數據係依習用方式列表(δ值,氫原子數,裂峰多重性)或列出NMR波峰。 The NMR data for the selected examples are listed by convention (δ value, number of hydrogen atoms, split peak multiplicity) or NMR peaks.
NMR光譜中之溶劑係於各例中分別提示。 The solvents in the NMR spectrum are presented separately in each case.
製備實例1:5-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)亞磺醯基]苯基}-1,3-二甲基嘧啶-2,4(1H,3H)-二酮(I-1)Preparation Example 1: 5-{2-Fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenyl}-1,3-dimethylpyrimidine-2 ,4(1H,3H)-dione (I-1)
1H-NMR(D6-DMSO)δ ppm:8.02(s,1H),7.88-7.86(m,1H),7.35-7.32(m,1H),4.24-4.13(m,1H),4.02-3.90(m,1H),3.39(s,3H),3.24(s,3H),2.41(s,3H) 1H-NMR (D6-DMSO) δ ppm: 8.02 (s, 1H), 7.88-7.86 (m, 1H), 7.35-7.32 (m, 1H), 4.24 - 4.13 (m, 1H), 4.02-3.90 (m) , 1H), 3.39 (s, 3H), 3.24 (s, 3H), 2.41 (s, 3H)
logP(HCOOH):1.81 logP(中性):1.77 logP(HCOOH): 1.81 logP (neutral): 1.77
製備實例2:5-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)硫基]苯基}-1,3-二甲基嘧啶-2,4(1H,3H)-二酮(I-2)Preparation Example 2: 5-{2-Fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)thio]phenyl}-1,3-dimethylpyrimidine-2,4 (1H,3H)-dione (I-2)
1H-NMR(D6-DMSO)δ ppm:7.94(s,1H),7.60-7.58(m,1H),7.25-7.22(m,1H),3.91-3.83(q,2H),3.38(s,3H),3.23(s,3H),2.43(s,3H) 1H-NMR (D 6 -DMSO) δ ppm: 7.94 (s, 1H), 7.60-7.58 (m, 1H), 7.25-7.22 (m, 1H), 3.91-3.83 (q, 2H), 3.38 (s, 3H), 3.23 (s, 3H), 2.43 (s, 3H)
logP(HCOOH):2.81 logP(中性):2.72 logP(HCOOH): 2.81 logP (neutral): 2.72
製備實例3:6-氯-5-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)亞磺醯基]苯基}-1,3-二甲基嘧啶-2,4(1H,3H)-二酮(I-3)Preparation Example 3: 6-chloro-5-{2-fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenyl}-1,3-dimethyl Pyrimidine-2,4(1H,3H)-dione (I-3)
1H-NMR(D6-DMSO)δ ppm:7.80-7.78(m,1H),7.40-7.37(m,1H),4.32-4.20(m,1H),3.97-3.84(m,1H),3.56/3.55(s,3H),3.24/3.23(s,3H),2.42(s,3H)(因阻轉異構性產生之非對映異構物) 1H-NMR (D6-DMSO) δ ppm: 7.80-7.78 (m, 1H), 7.40-7.37 (m, 1H), 4.32-4.20 (m, 1H), 3.97-3.84 (m, 1H), 3.56/3.55 (s, 3H), 3.24/3.23 (s, 3H), 2.42 (s, 3H) (diastereomers due to atropisomerism)
logP(HCOOH):2.21 logP(中性):2.18 logP(HCOOH): 2.21 logP (neutral): 2.18
製備實例4:5-{2,4-二甲基-5-[(2,2,2-三氟乙基)硫基]苯基}-1,3-二甲基嘧啶-2,4(1H,3H)-二酮(I-4)Preparation Example 4: 5-{2,4-Dimethyl-5-[(2,2,2-trifluoroethyl)thio]phenyl}-1,3-dimethylpyrimidine-2,4 ( 1H,3H)-dione (I-4)
1H-NMR(D6-DMSO)δ ppm:7.74(s,1H),7.31(s,1H),7.15(s,1H),3.89-3.81(q,2H),3.36(s,3H),3.23(s,3H),2.37(s,3H),2.11(s,3H) 1H-NMR (D 6 -DMSO) δ ppm: 7.74 (s, 1H), 7.31 (s, 1H), 7.15 (s, 1H), 3.89-3.81 (q, 2H), 3.36 (s, 3H), 3.23 (s, 3H), 2.37 (s, 3H), 2.11 (s, 3H)
logP(HCOOH):2.97 logP(中性):2.88 logP(HCOOH): 2.97 logP (neutral): 2.88
製備實例5:6-{2,4-二甲基-5-[(2,2,2-三氟乙基)硫基]苯基}-2,4-二甲基-1,2,4-三 -3,5(2H,4H)-二酮(I-5) Preparation Example 5: 6-{2,4-Dimethyl-5-[(2,2,2-trifluoroethyl)thio]phenyl}-2,4-dimethyl-1,2,4 -three -3,5(2H,4H)-dione (I-5)
1H-NMR(D6-DMSO)δ ppm:7.49(s,1H),7.21(s,1H),3.85-3.78(q,2H),3.57(s,3H),3.23(s,3H),2.40(s,3H),2.19(s,3H) 1H-NMR (D 6 -DMSO) δ ppm: 7.49 (s, 1H), 7.21 (s, 1H), 3.85-3.78 (q, 2H), 3.57 (s, 3H), 3.23 (s, 3H), 2.40 (s, 3H), 2.19 (s, 3H)
logP(HCOOH):3.38 logP(中性):3.29 logP(HCOOH): 3.38 logP (neutral): 3.29
製備實例6:6-{2-氟-4-甲基-5-[(2,2,2-三氟乙基)亞磺醯基]苯基}-2,4-二甲基-1,2,4-三 -3,5(2H,4H)-二酮(I-6) Preparation Example 6: 6-{2-Fluoro-4-methyl-5-[(2,2,2-trifluoroethyl)sulfinyl]phenyl}-2,4-dimethyl-1, 2,4-three -3,5(2H,4H)-dione (I-6)
1H-NMR(D6-DMSO)δ ppm:7.98-7.97(m,1H),7.43-7.40(m,1H),4.27-4.18(m,1H),3.99-3.93(m,1H),3.60(s,3H),3.24(s,3H),2.43(s,3H) 1H-NMR (D6-DMSO) δ ppm: 7.98-7.97 (m, 1H), 7.43-7.40 (m, 1H), 4.27-4.18 (m, 1H), 3.99-3.93 (m, 1H), 3.60 (s) , 3H), 3.24 (s, 3H), 2.43 (s, 3H)
logP(HCOOH):2.06 logP(中性):2.04 logP(HCOOH): 2.06 logP (neutral): 2.04
製備實例7:4-乙基-6-[2-氟-4-甲基-5-(2,2,2-三氟乙基硫基)苯基]-2-甲基-1,2,4-三 -3,5-二酮(I-15) Preparation Example 7: 4-ethyl-6-[2-fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfanyl)phenyl]-2-methyl-1,2, 4-three -3,5-dione (I-15)
1H-NMR(CDCl3,400MHz)δ ppm:7.68(d,1H),7.07(d,1H),4.07(q,2H),3.72(s,3H),3.35(q,2H),2.53(s,3H),1.30(t,3H) 1H-NMR (CDCl 3 , 400MHz) δ ppm: 7.68 (d, 1H), 7.07 (d, 1H), 4.07 (q, 2H), 3.72 (s, 3H), 3.35 (q, 2H), 2.53 (s) , 3H), 1.30(t, 3H)
logP(HCOOH):3.52 logP(HCOOH): 3.52
製備實例8:4-乙基-6-[2-氟-4-甲基-5-(2,2,2-三氟乙基亞磺醯基)苯基]-2-甲基-1,2,4-三 -3,5-二酮(I-18) Preparation Example 8: 4-ethyl-6-[2-fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfinyl)phenyl]-2-methyl-1, 2,4-three -3,5-dione (I-18)
1H-NMR(CDCl3,400MHz)δ ppm:8.12(d,1H),7.10(d,1H),4.07(q,2H),3.72(s,3H),3.53-3.40(m,2H),2.45(s,3H),1.30(t,3H) 1H-NMR (CDCl 3 , 400MHz) δ ppm: 8.12 (d, 1H), 7.10 (d, 1H), 4.07 (q, 2H), 3.72 (s, 3H), 3.53-3.40 (m, 2H), 2.45 (s, 3H), 1.30 (t, 3H)
logP(HCOOH):2.38 logP(HCOOH): 2.38
類似該等實例及依據上述製法,可得到下列式(I-A)化合物:
測定化合物I-11之一種對映異構物之比旋光度。因此,其為如下示之R對映異構物(I-12)。 The specific optical rotation of one enantiomer of Compound I-11 was determined. Therefore, it is the R enantiomer (I-12) shown below.
類似該等實例及依據上述製法,可得到下列式(I-B)化合物:
NMR波峰列表方法NMR peak list method
所選定實例之1H NMR數據係以1H NMR-波峰列表型式出示。每個訊號峰先以δ-值(ppm)表示,然後訊號強度則列於圓括號中。所列出不同訊號峰之每對δ-值-訊號強度之間以分號作為分隔符號。 The 1H NMR data for the selected examples are presented as a 1H NMR-peak list. Each signal peak is first expressed in δ-values (ppm), and then the signal strength is listed in parentheses. A semicolon is used as a separator between each pair of δ-value-signal strengths of the different signal peaks listed.
因此某一實例之波峰列表型式為:δ1(強度1);δ2(強度2);......;δi(強度i);......;δn(強度n) Therefore, the peak list type of an example is: δ 1 (intensity 1 ); δ 2 (intensity 2 ); ...; δ i (intensity i ); ...; δ n (intensity n )
陡峰訊號強度係與印出之NMR光譜實例中訊號高度(以cm計)呈相關性,且顯示訊號強度之真實比例關係。在寬峰訊號中,則可出示複數個峰或中間訊號及其相較於光譜中最高強度訊號之相對強度。 The steep signal intensity is correlated with the height of the signal (in cm) in the printed NMR spectrum example and shows the true proportional relationship of the signal strength. In the wide-peak signal, a plurality of peaks or intermediate signals and their relative intensities relative to the highest intensity signal in the spectrum can be produced.
採用四甲基矽烷與/或溶劑之化學位移(尤其在DMSO中測定光譜時)校準1H NMR光譜之化學位移。因此四甲基矽烷峰有可能但不一定會出現在NMR波峰列表中。 The chemical shift of the 1H NMR spectrum was calibrated using chemical shifts of tetramethylnonane and/or solvent, especially when the spectrum was measured in DMSO. Therefore, the tetramethylnonane peak is possible but not necessarily present in the NMR peak list.
1H NMR波峰列表類似印出之典型1H NMR圖,因此通常包含列於典型NMR解讀中之所有波峰。 The 1H NMR peak list is similar to the typical 1H NMR map printed, and therefore typically contains all of the peaks listed in a typical NMR interpretation.
此外,可如同印出之典型1H NMR圖,其亦顯示溶劑訊號、目標化合物之立體異構物(其同時為本發明主題之一部份)訊號及/或雜質之波峰。 In addition, as with the typical 1H NMR image printed, it also shows the solvent signal, the stereoisomer of the target compound (which is also part of the subject matter of the invention), and the peak of the signal and/or impurity.
在溶劑與/或水之δ-範圍內顯示化合物訊號時,吾等之1H NMR波峰列表會出示一般溶劑波峰(例如:DMSO-D6中之DMSO波峰)及水之波峰,其通常以高強度平均值表示。 When the compound signal is displayed in the δ-range of solvent and/or water, our 1H NMR peak list will show the general solvent peak (eg DMSO peak in DMSO-D 6 ) and the water peak, which is usually high intensity. The average value is expressed.
目標化合物之立體異構物波峰與/或雜質波峰之平均強度通常低於目標化合物(例如:純度>90%)之波峰強度。 The average intensity of the stereoisomer peaks and/or impurity peaks of the target compound is generally lower than the peak intensity of the target compound (eg, purity >90%).
此等立體異構物與/或雜質係典型出現在特定製法中。因此其波峰有助於藉由“副產物指印”辨識吾等製法之再現性。 Such stereoisomers and/or impurities are typically found in a particular process. Therefore, its peak helps to identify the reproducibility of our system by "byproduct fingerprinting."
可以採用已知方法(MestreC,ACD-模擬法,但亦採用實驗性分析之預期數值)計算目標化合物波峰之專家可依需要另外採用其他強度濾波器,單離出目標化合物之波峰。此單離法即類似典型1H NMR解讀中相關波峰挑選法。 Experts who can use known methods (MestreC, ACD-simulation, but also use the expected values of experimental analysis) to calculate the peak of the target compound can additionally use other intensity filters to separate the peaks of the target compound. This singularity method is similar to the relevant peak selection method in a typical 1H NMR interpretation.
有關1H NMR波峰列表之進一步詳細內容可參見:Research Disclosure Database Number 564025。 Further details regarding the 1H NMR peak list can be found in Research Disclosure Database Number 564025.
NMR數據與logP值:logP(HCOOH)=logP[a]logP(中性)=logP[b] NMR data and logP values: logP(HCOOH)=logP[a]logP(neutral)=logP[b]
6-[2-氟-4-甲基-5-(2,2,2-三氟乙基硫基)苯基]-2-甲基-1,2,4-三 -3,5-二酮(I-Bf-1) 6-[2-Fluoro-4-methyl-5-(2,2,2-trifluoroethylthio)phenyl]-2-methyl-1,2,4-tri -3,5-dione (I-Bf-1)
步驟1:1-(1-乙氧基乙烯基)-2-氟-4-甲基-5-(2,2,2-三氟乙基硫基)苯Step 1: 1-(1-ethoxyvinyl)-2-fluoro-4-methyl-5-(2,2,2-trifluoroethylthio)benzene
步驟2:2-[2-氟-4-甲基-5-(2,2,2-三氟乙基硫基)表基]-2-側氧基乙酸(VI-1)Step 2: 2-[2-Fluoro-4-methyl-5-(2,2,2-trifluoroethylthio)epi]-2-oxoacetic acid (VI-1)
1H-NMR(D6-DMSO,400MHz)δ ppm:7.94(d,1H),7.31(d,1H),3.89(q,2H),2.47(s,3H) 1H-NMR (D 6 -DMSO, 400MHz) δ ppm: 7.94 (d, 1H), 7.31 (d, 1H), 3.89 (q, 2H), 2.47 (s, 3H)
步驟3:6-[2-氟-4-甲基-5-(2,2,2-三氟乙基硫基)苯基]-2-甲基-1,2,4-三 -3,5-二酮(I-Bf-1) Step 3: 6-[2-Fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfanyl)phenyl]-2-methyl-1,2,4-tri -3,5-dione (I-Bf-1)
1H-NMR(CDCl3,400MHz)δ ppm:8.83(b,1H),7.79(d,1H),7.07(d,1H),3.71(s,3H),3.35(q,2H),2.53(s,3H) 1H-NMR (CDCl 3 , 400MHz) δ ppm: 8.83 (b, 1H), 7.79 (d, 1H), 7.07 (d, 1H), 3.71 (s, 3H), 3.35 (q, 2H), 2.53 (s) , 3H)
logP(HCOOH):2.62 logP(HCOOH): 2.62
6-[2-氟-4-甲基-5-(2,2,2-三氟乙基亞磺醯基)苯基]-2-甲基-1,2,4-三 -3,5-二酮(I-Bg-1) 6-[2-Fluoro-4-methyl-5-(2,2,2-trifluoroethylsulfinyl)phenyl]-2-methyl-1,2,4-tri -3,5-dione (I-Bg-1)
1H-NMR(CDCl3,400MHz)δ ppm:9.00(b,1H),8.14(d,1H),7.10(d,1H), 3.71(s,3H),3.56-3.41(m,2H),2.45(s,3H) 1H-NMR (CDCl 3 , 400MHz) δ ppm: 9.00 (b, 1H), 8.14 (d, 1H), 7.10 (d, 1H), 3.71 (s, 3H), 3.56-3.41 (m, 2H), 2.45 (s, 3H)
logP(HCOOH):1.72 logP(HCOOH): 1.72
類似該等實例及依據上述製法,可得到下列式(I-Bf)或(I-Bg)化合物:
NMR數據與logP值:logP(HCOOH)=logP[a]logP(中性)=logP[b] NMR data logP values: logP (HCOOH) = logP [ a] logP ( neutral) = logP [b]
微小牛蜱(Boophilus microplus)-注射試驗Boophilus microplus - injection test
溶劑:二甲亞碸 Solvent: dimethyl hydrazine
製造合適之活性化合物製劑時,取10mg活性化合物與0.5ml溶劑混合,使用溶劑稀釋該濃縮液至所需濃度。 When a suitable active compound preparation is made, 10 mg of the active compound is mixed with 0.5 ml of the solvent, and the concentrate is diluted with a solvent to the desired concentration.
取1μl活性化合物溶液注射至5隻充血之雌性微小牛蜱(Boophilus microplus)成蟲腹部。將動物移至培養皿,保持在人工氣候室內。 1 μl of the active compound solution was injected into the abdomen of 5 adult females of Boophilus microplus. The animals were transferred to a Petri dish and kept in an artificial climate chamber.
7天後,由所產下可孵化的卵來分析效力。無法目視觀察孵化力之卵係存放在人工氣候室內,直到約42天後孵化為止。100%之效力意指沒有牛蜱產下任何有孵化力之卵,0%意指所有卵均有孵化力。 After 7 days, the potency was analyzed from the eggs that were hatched. Eggs that are not visually observable for hatching are stored in an artificial climate chamber until they hatch after about 42 days. 100% effectiveness means that no burdock produces any hatching eggs, 0% means that all eggs have hatching power.
本試驗中,例如:下列製備實例之化合物在20μg/隻動物之施用率下顯示100%之效力:I-1、I-2、I-6、I-7、I-9、I-10 In this test, for example, the compounds of the following preparation examples showed 100% potency at an application rate of 20 μg/animal: I-1, I-2, I-6, I-7, I-9, I-10
南方根瘤線蟲(Meloidogyne incognita)試驗Meloidogyne incognita test
溶劑:125.0份重量比丙酮 Solvent: 125.0 parts by weight acetone
製造合適之活性化合物製劑時,取1份重量比之活性化合物與上述量溶劑混合,並加水稀釋該濃縮液至所需濃度。 In the preparation of a suitable active compound preparation, one part by weight of the active compound is mixed with the above amount of solvent and the concentrate is diluted with water to the desired concentration.
在容器中填充砂子、活性化合物溶液、南方根瘤線蟲(Meloidogyne incognita)之卵/幼蟲懸浮液及萵苣種子。讓萵苣種子發芽及長成植物。在根部形成蟲癭。 The container is filled with sand, active compound solution, egg/larva suspension of Meloidogyne incognita and lettuce seeds. Let the lettuce seeds germinate and grow into plants. Forming insects at the roots.
14天後,依據所形成之蟲癭決定殺線蟲之效力%。100%意指沒有出現蟲癭;0%意指處理組植物之蟲癭數相當於未處理對照組。 After 14 days, the potency of nematicidal was determined based on the formed insects. 100% means that no insects appeared; 0% means that the number of insects in the treated group was equivalent to the untreated control.
本試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示100%之效力:I-22 In this test, for example, the following preparation examples show a 100% potency at an application rate of 20 ppm: I-22
本試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示90%之效力:I-1、I-21 In this test, for example, the compounds of the following preparation examples showed 90% efficacy at an application rate of 20 ppm: I-1, I-21
桃赤蚜(Myzus persicae)-噴灑試驗Myzus persicae - spray test
溶劑:78.0份重量比丙酮 Solvent: 78.0 parts by weight acetone
1.5份重量比二甲基甲醯胺 1.5 parts by weight of dimethylformamide
乳化劑:烷基芳基聚二醇醚 Emulsifier: alkyl aryl polyglycol ether
製備合適之活性化合物製劑時,使用指定份數重量比之溶劑溶解1份重量比活性化合物,並補充包含1000ppm乳化劑濃度之水直到達到所需濃度為止。再使用包含乳化劑之水稀釋,進一步製成其他試驗濃度。 When preparing a suitable active compound preparation, the active compound is dissolved in a proportion by weight of the solvent in a specified portion by weight, and water containing 1000 ppm emulsifier concentration is added until the desired concentration is reached. It was further diluted with water containing an emulsifier to further prepare other test concentrations.
在感染所有階段之桃赤蚜(Myzus persicae)之捲心白菜(Brassica pekinensis)葉圓片上噴灑所需濃度之活性化合物製劑。 The active compound preparation of the desired concentration is sprayed onto the leaf disc of Brassica pekinensis of Myzus persicae at all stages of infection.
6天後,測定效力%。100%表示所有蚜蟲均死亡;0%表示沒有任何蚜蟲死亡。 After 6 days, the potency was determined. 100% means that all mites have died; 0% means that no mites have died.
本試驗中,例如:下列製備實例之化合物在500g/ha之施用率下展現100%之效力:I-7 In this test, for example, the following preparation examples show a 100% potency at an application rate of 500 g/ha: I-7
猿葉蟲(Phaedon cochleariae)-噴灑試驗Phaedon cochleariae - spray test
溶劑:78.0份重量比丙酮 Solvent: 78.0 parts by weight acetone
1.5份重量比二甲基甲醯胺 1.5 parts by weight of dimethylformamide
乳化劑:烷基芳基聚二醇醚 Emulsifier: alkyl aryl polyglycol ether
製備合適之活性化合物製劑時,使用指定份數重量比之溶劑溶解1份重量比活性化合物,並補充含1000ppm乳化劑濃度之水直到達到所需濃度為止。再使用含乳化劑之水稀釋該製劑,進一步製成其他試驗濃度。 When preparing a suitable active compound preparation, the active compound is dissolved in a specified proportion by weight of the solvent and the water containing 1000 ppm emulsifier concentration is added until the desired concentration is reached. The preparation was further diluted with water containing an emulsifier and further prepared to other test concentrations.
以所需濃度之活性化合物製劑噴灑捲心白菜(Brassica pekinensis)葉圓片,乾燥後,接種猿葉蟲(Phaedon cochleariae)幼蟲。 Cabbage leaves of Brassica pekinensis are sprayed with the active compound preparation at the desired concentration, dried and inoculated with larvae of Phaedon cochleariae .
7天後,測定效力%。100%意指所有猿葉蟲幼蟲均死亡;0%意指沒有猿葉蟲幼蟲死亡。 After 7 days, the potency % was determined. 100% means that all locust larvae die; 0% means that no locust larvae die.
本試驗中,例如:下列製備實例之化合物在500g/ha之施用率下顯示100%之效力:I-2、I-9、I-16、I-21 In this test, for example, the compounds of the following preparation examples showed 100% potency at an application rate of 500 g/ha: I-2, I-9, I-16, I-21
本試驗中,例如:下列製備實例之化合物在500g/ha之施用率下顯示83%之效力:I-6 In this test, for example, the following preparation examples show an efficacy of 83% at an application rate of 500 g/ha: I-6
紅葉蟎(Tetranychus urticae)-噴灑試驗,OP-抗性Tetranychus urticae - spray test, OP-resistant
溶劑:78.0份重量比丙酮 Solvent: 78.0 parts by weight acetone
1.5份重量比二甲基甲醯胺 1.5 parts by weight of dimethylformamide
乳化劑:烷基芳基聚二醇醚 Emulsifier: alkyl aryl polyglycol ether
製備合適之活性化合物製劑時,使用指定份數重量比之溶劑溶解1份重量比活性化合物,並補充含1000ppm乳化劑濃度之水直到達到所需濃度為止。使用含乳化劑之水稀釋該製劑,進一步製成其他試驗濃度。 When preparing a suitable active compound preparation, the active compound is dissolved in a specified proportion by weight of the solvent and the water containing 1000 ppm emulsifier concentration is added until the desired concentration is reached. The preparation was diluted with water containing an emulsifier and further prepared to other test concentrations.
以所需濃度之活性化合物製劑噴灑已感染所有階段之溫室紅葉蟎(Tetranychus urticae)之菜豆(Phaseolus vulgaris)葉圓片。 In preparation of the desired concentration of active compound is sprayed infection at all stages of the greenhouse spider mite (Tetranychus urticae) of kidney bean (Phaseolus vulgaris) leaf discs.
6天後,測定效力%。100%意指所有蜘蛛蟎均死亡;0%意指沒有任何蜘蛛蟎死亡。 After 6 days, the potency was determined. 100% means that all spider mites die; 0% means that no spider mites die.
本試驗中,例如:下列製備實例之化合物在500g/ha之施用率下顯示100%之效力:I-1、I-2、I-6、I-7、I-8、I-9、I-10、I-11、I-13、I-14、I-15、I-16、I-17、I-18 In this test, for example, the compounds of the following preparation examples showed 100% potency at an application rate of 500 g/ha: I-1, I-2, I-6, I-7, I-8, I-9, I -10, I-11, I-13, I-14, I-15, I-16, I-17, I-18
本試驗中,例如:下列製備實例之化合物在500g/ha之施用率下顯示90%之效力:I-5、I-12、I-19、I-20、I-21、I-22 In this test, for example, the compounds of the following preparation examples showed 90% potency at an application rate of 500 g/ha: I-5, I-12, I-19, I-20, I-21, I-22
紅葉蟎(Tetranychus urticae)-噴灑試驗,OP-抗性Tetranychus urticae - spray test, OP-resistant
溶劑:7份重量比二甲基甲醯胺 Solvent: 7 parts by weight of dimethylformamide
乳化劑:烷基芳基聚二醇醚 Emulsifier: alkyl aryl polyglycol ether
製備合適之活性化合物製劑時,使用指定份數重量比之溶劑溶解1份重量比活性化合物,並補充含1000ppm乳化劑濃度之水直到達到所需濃度為止。使用含乳化劑之水稀釋該製劑,進一步製成其他試驗濃度。若需要添加銨鹽與/或滲透劑時,則其分別添加1000ppm濃度至該製劑溶液中。 When preparing a suitable active compound preparation, the active compound is dissolved in a specified proportion by weight of the solvent and the water containing 1000 ppm emulsifier concentration is added until the desired concentration is reached. The preparation was diluted with water containing an emulsifier and further prepared to other test concentrations. If it is desired to add an ammonium salt and/or a penetrant, it is separately added to the formulation solution at a concentration of 1000 ppm.
在受到所有階段溫室紅葉蟎(Tetranychus urticae)嚴重感染之豆科植物(Phaseolus vulgaris)上噴灑所需濃度之活性化合物製劑。 The active compound preparation of the desired concentration is sprayed on the leguminous plant ( Phenolus vulgaris ) which is severely infected by the greenhouse, Tetranychus urticae .
7天後,測定效力%。100%意指所有紅葉蟎均死亡;0%意指沒有任何紅葉蟎死亡。 After 7 days, the potency % was determined. 100% means that all red leafhoppers die; 0% means that there is no death of any red leafhopper.
本試驗中,例如:下列製備實例之化合物在20ppm之施用率下顯示100%之效力:I-4 In this test, for example, the compounds of the following preparation examples show 100% efficacy at an application rate of 20 ppm: I-4
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