TW201734002A - Substituted malonamides as insecticides - Google Patents
Substituted malonamides as insecticides Download PDFInfo
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Description
本發明係有關一種新穎之經取代之丙二醯胺類、其製法、及其於控制動物害蟲，尤指節肢動物，及特定言之昆蟲、蜘蛛類與線蟲上之用途。 The present invention relates to a novel substituted propylenediamine, a process for its preparation, and its use in controlling animal pests, particularly arthropods, and in particular insects, arachnids and nematodes.
WO2009099929說明3-{[(6-氯吡啶-3-基)甲基](吡啶-2-基)胺基}-3-側氧基苯丙酸乙酯作為殺昆蟲活性化合物。其他具有殺昆蟲性質之經取代之丙二醯胺類係自JP2013241403中已知。然而，在應用上，從文獻上已知之有些活性化合物仍有缺點，其等僅具有狹隘的應用範圍，或其可能具有未令人滿意的殺昆蟲或殺蜱蟎活性。 WO2009099929 describes ethyl 3-{[(6-chloropyridin-3-yl)methyl](pyridin-2-yl)amino}-3-oxooxyphenylpropanoate as an insecticidal active compound. Other substituted malonamides having insecticidal properties are known from JP 2013241403. However, in use, some active compounds known from the literature still have disadvantages, such as having a narrow range of applications, or they may have unsatisfactory insecticidal or acaricidal activity.
本發明之目的為提供一種化合物，其可擴大除害劑在各種不同方面之範圍及/或改善其活性。 It is an object of the present invention to provide a compound which broadens the range and/or improves the activity of the pesticide in a variety of different aspects.
現已驚人地發現，某些經取代之丙二醯胺類具有強力之殺昆蟲性質，並同時對植物有良好耐受性，對恆溫動物具有有利之毒性，及對環境具有良好相容性。根據本發明化合物迄今尚未被揭示。 It has now surprisingly been found that certain substituted malonamides have potent insecticidal properties and are well tolerated at the same time, have beneficial toxicity to warm-blooded animals, and have good compatibility with the environment. The compounds according to the invention have not heretofore been disclosed.
本發明因此提供一種通式(I)化合物
式(I)化合物同樣包含任何存在之非對映異構物或對映異構物，及E/Z異構物，亦包含式(I)化合物之鹽類與N-氧化物，及其於控制動物害蟲上之用途。 The compound of formula (I) likewise comprises any diastereomer or enantiomer present, and the E/Z isomer, also comprising the salt of the compound of formula (I) and the N-oxide, and Control the use of animal pests.
式(I)提供經取代之丙二醯胺類之一般定義。上文及下文明確說明之化學式中較佳基團定義如下。 Formula (I) provides a general definition of substituted malonamides. Preferred groups in the formulas explicitly and above are defined below.
較佳(組態2-1)係指式(I)化合物中A 代表O或S，Q 代表基團Q-1、Q-5或Q-6中之一，Y 代表苯基、吡啶基、嘧啶基、噻唑基、唑基、吡唑基、噻吩基或呋喃基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C6-烷基羰基，T 若A代表O時，則代表T1，或T 若A代表S時，則代表T2，T1 代表C1-C4-烷基、C2-C6-烯基或C2-C6-炔基，其中上述基團係經選自下列所組成群中之取代基取代：氰基、硝基、羥基、C(O)OR2、OC(O)R5、S(O)pR6、Si(R7a)(R7b)(R7c)，或T1 代表C2-C6-烯基或C2-C6-炔基，其中上述基團可視需要分別獨立經鹵素單取代至三取代或經C1-C6-烷氧基或C1-C6-鹵烷氧基單取代，或T1 代表苯基甲基、苯基乙基、苯基丙基、雙苯基甲基、吡啶基甲基、嘧啶基甲基、噻唑基甲基、唑基甲基、吡唑基甲基、噻吩基甲基、呋喃基甲基或呋喃酮基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C4-烷基羰基，或 T1 代表C3-C6-環烷基、C3-C6-環烯基、C4-C8-雙環烷基、C3-C8-環烷基-C1-C4-烷基、氮雜環丁烷基、氧雜環丁烷基、氧雜環戊烷基、氧雜環己烷基、二氧雜環己烷基、硫雜環丁烷基、側氧基硫雜環丁烷基、二側氧基硫雜環丁烷基、硫雜環戊烷基、硫雜環己烷基、四氫呋喃基、四氫硫呋喃基、側氧基四氫硫呋喃基、二側氧基四氫硫呋喃基、四氫哌喃基、四氫硫哌喃基、側氧基四氫硫哌喃基、二側氧基四氫硫哌喃基、C3-C6-環烷基甲基、C3-C6-環烷基乙基、氮雜環丁烷基甲基、氧雜環丁烷基甲基、氧雜環戊烷基甲基、硫雜環丁烷基甲基、側氧基硫雜環丁烷基甲基、二側氧基硫雜環丁烷基甲基、四氫呋喃基甲基或四氫哌喃基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C4-烷基羰基，T2 代表苯基甲基、苯基乙基、苯基丙基、吡啶基甲基、嘧啶基甲基、噻唑基甲基、唑基甲基、吡唑基甲基、噻吩基甲基、呋喃基甲基或呋喃酮基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C4-烷基羰基，或T2 代表C3-C6-環烷基、C3-C6-環烯基或C4-C8-雙環烷基，其中上述基團可視需要分別獨立經鹵素單取代至三取代或經氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基、C2-C4-烷基羰基單取 代，G 代表-C(R9)(R10)-，U 代表選自U-2、U-5、U-6、U-9、U-20與U-23所組成群中之環，Xa 代表鹵素、硝基、氰基、SF5、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷氧基-C1-C4-烷基、氰基-C1-C4-烷基、C2-C4-烯基、C3-C4-炔基、C1-C4-烷基-S(O)p-、C1-C4-烷基羰基、C1-C4-烷氧基羰基、C1-C4-烷氧基亞胺基-C1-C4-烷基或C1-C4-鹵烷基磺醯基，R1 代表鹵素、硝基、氰基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷氧基-C1-C4-烷基、氰基-C1-C4-烷基、C2-C4-烯基、C3-C4-炔基、C1-C4-烷基-S(O)p-、C1-C4-烷基羰基、C1-C4-烷氧基羰基或C1-C4-烷氧基亞胺基-C1-C4-烷基，R1a 代表C1-C4-烷基，R2 代表氫、C1-C4-烷基、C1-C4-鹵烷基、C3-C6-環烷基、C3-C6-環烷基-C1-C4-烷基、C1-C4-烷氧基-C1-C4-烷基、苯基、吡啶基、苯基甲基或吡啶基甲基，其中苯基、吡啶基、苯基甲基與吡啶基甲基可視需要經選自下列所組成群中之相同或相異取代基單取代或多取代：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基與C1-C4-鹵烷氧基，R5 代表氫、C1-C4-烷基、C1-C4-鹵烷基、C3-C6-環烷基、C3-C6-環烷基-C1-C4-烷基、苯基、吡啶基、苯基甲基或吡啶基甲基，其中苯基、吡啶基、苯基甲基與吡啶基甲基可視需要經選自下列所組成群中之相同或相異取代基單取代或多取代：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-與C1-C4-烷氧基羰基，R6 代表C1-C4-烷基、C1-C4-鹵烷基、C3-C6-環烷基、苯基或苯基甲基，其 中苯基與苯基甲基可視需要經選自下列所組成群中之相同或相異取代基單取代或多取代：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-與C1-C4-烷氧基羰基，R7a、R7b、R7c 彼此分別獨立代表C1-C4-烷基，R9 代表氫、氟、氯或C1-C4-烷基，R10 代表氫、氟、氯或C1-C4-烷基，m 代表0、1、2或3，n 代表0、1、2或3，及p 代表0、1或2。 Preferably (Configuration 2-1) means that in the compound of formula (I), A represents O or S, and Q represents one of the groups Q-1, Q-5 or Q-6, and Y represents a phenyl group, a pyridyl group, Pyrimidinyl, thiazolyl, An azolyl, pyrazolyl, thienyl or furyl group, wherein the above groups may be independently monosubstituted to trisubstituted, respectively, via the following groups: halogen, cyano, nitro, SF 5 , hydroxy, amine, C 1 - C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 6 -alkylcarbonyl, T If A represents O, it represents T 1 , or T. If A represents S, it represents T 2 , T 1 represents a C 1 -C 4 -alkyl group, a C 2 -C 6 -alkenyl group or a C 2 -C 6 -alkynyl group, wherein the above group is substituted with a substituent selected from the group consisting of cyano group, Nitro, hydroxy, C(O)OR 2 , OC(O)R 5 , S(O) p R 6 , Si(R 7a )(R 7b )(R 7c ), or T 1 represents C 2 -C 6 Alkenyl or C 2 -C 6 -alkynyl, wherein the above groups may be independently mono-substituted to trisubstituted or C 1 -C 6 -alkoxy or C 1 -C 6 -haloalkoxy, respectively, as desired. Monosubstituted, or T 1 represents phenylmethyl, phenylethyl, phenylpropyl, bisphenylmethyl, pyridylmethyl, pyrimidinylmethyl, thiazolylmethyl, An azolylmethyl, pyrazolylmethyl, thienylmethyl, furylmethyl or furanosylmethyl group, wherein the above groups may be independently monosubstituted to trisubstituted by the following groups, respectively: halogen, cyano, Nitro, SF 5 , hydroxy, amine, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy , C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 4 -alkylcarbonyl, or T 1 represents C 3 -C 6 -cycloalkane , C 3 -C 6 -cycloalkenyl, C 4 -C 8 -bicycloalkyl, C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, azetidinyl, oxa Cyclobutane, oxolane, oxacyclohexane, dioxanyl, thietane, oxirane, oxetane Cyclobutane, thiolanyl, thiacyclohexane, tetrahydrofuranyl, tetrahydrothiofuranyl, pendant oxytetrahydrothiofuranyl, di-tertiary tetrahydrothiofuranyl, tetrahydroper Butyl, tetrahydrothiopyranyl, pendant oxytetrahydrothiopyranyl, di- oxytetrahydrothiopyranyl, C 3 -C 6 -cycloalkylmethyl, C 3 -C 6 - ring alkyl Base, azetidinylmethyl, oxetanylmethyl, oxolylmethyl, thietanemethyl, pendant thiohedinylmethyl, a 2-sided oxetanemethyl group, a tetrahydrofuranylmethyl group or a tetrahydropyranylmethyl group, wherein the above groups may be independently monosubstituted to trisubstituted by the following groups, respectively: halogen, cyano, nitrate Base, SF5, hydroxyl, amine, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 4 -alkylcarbonyl, T 2 represents phenylmethyl, phenylethyl, benzene Propyl, pyridylmethyl, pyrimidinylmethyl, thiazolylmethyl, An azolylmethyl, pyrazolylmethyl, thienylmethyl, furylmethyl or furanosylmethyl group, wherein the above groups may be independently monosubstituted to trisubstituted by the following groups, respectively: halogen, cyano, Nitro, SF 5 , hydroxy, amine, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy , C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 4 -alkylcarbonyl, or T 2 represents C 3 -C 6 -cycloalkane a C 3 -C 6 -cycloalkenyl group or a C 4 -C 8 -bicycloalkyl group, wherein the above groups may be independently monosubstituted to trisubstituted or via cyano, nitro, SF 5 , hydroxy, Amino, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkane a group of -S(O) p -, C 2 -C 6 -alkoxycarbonyl, C 2 -C 4 -alkylcarbonyl, G represents -C(R 9 )(R 10 )-, and U represents a a ring in the group consisting of U-2, U-5, U-6, U-9, U-20 and U-23, X a represents halogen, nitro, cyano, SF 5 , C 1 -C 4 - Alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy , C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, cyano-C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 3 -C 4 -alkynyl , C 1 -C 4 -alkyl-S(O) p -, C 1 -C 4 -alkylcarbonyl, C 1 -C 4 -alkoxycarbonyl, C 1 -C 4 -alkoxyimino -C 1 -C 4 -alkyl or C 1 -C 4 -haloalkylsulfonyl, R 1 represents halogen, nitro, cyano, C 1 -C 4 -alkyl, C 1 -C 4 -halide Alkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, cyano-C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 3 -C 4 -alkynyl, C 1 -C 4 -alkyl-S(O) p -, C 1 -C 4 -alkylcarbonyl, C 1 -C 4 -alkoxycarbonyl or C 1 -C 4 -alkoxyimino-C 1 -C 4 -alkyl, R 1a represents C 1 -C 4 -alkyl, R 2 represents hydrogen, C 1- C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, C 1 - C 4 -alkoxy-C 1 -C 4 -alkyl, phenyl, pyridyl, phenylmethyl or pyridylmethyl, wherein phenyl, pyridyl, phenylmethyl and pyridylmethyl are optionally required Monosubstituted by the same or different substituents selected from the group consisting of Multi: halogen, cyano, nitro, C 1 -C 4 - alkyl, C 1 -C 4 - haloalkyl, C 1 -C 4 - alkoxy and C 1 -C 4 - haloalkoxy , R 5 represents hydrogen, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 An alkyl group, a phenyl group, a pyridyl group, a phenylmethyl group or a pyridylmethyl group, wherein the phenyl group, the pyridyl group, the phenylmethyl group and the pyridylmethyl group may be the same or a phase selected from the group consisting of the following: Monosubstituted or polysubstituted hetero-substituted: halogen, cyano, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p - and C 1 -C 4 -alkoxycarbonyl, R 6 represents C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, phenyl or phenylmethyl, wherein phenyl and phenylmethyl may optionally be the same or different substituents selected from the group consisting of Substituted or polysubstituted: halogen, cyano, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -halane alkoxy, C 1 -C 4 - alkyl -S (O) p - and C 1 -C 4 - alkoxy, Group, R 7a, R 7b, R 7c each independently of one another C 1 -C 4 - alkyl, R 9 represents hydrogen, fluorine, chlorine or C 1 -C 4 - alkyl, R 10 represents hydrogen, fluorine, chlorine, or C 1 -C 4 -alkyl, m represents 0, 1, 2 or 3, n represents 0, 1, 2 or 3, and p represents 0, 1 or 2.
同樣較佳(組態2-2)為式(I)化合物中A 代表O或S，Q 代表基團Q-1、Q-5或Q-6中之一，Y 代表苯基、吡啶基、嘧啶基、噻唑基、唑基、吡唑基、噻吩基或呋喃基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基、C2-C6-烷基羰基，T 若A代表O時，則代表T1，或T 若A代表S時，則代表T2，T1 代表C1-C4-烷基、C2-C6-烯基或C2-C6-炔基，其中上述基團係經選自下列所組成群中之取代基取代：氰基、硝基、羥基、C(O)OR2、OC(O)R5、S(O)pR6、Si(R7a)(R7b)(R7c)， 或T1 代表C2-C6-烯基或C2-C6-炔基，其中上述基團可視需要分別獨立經鹵素單取代至三取代或經C1-C6-烷氧基或C1-C6-鹵烷氧基單取代，或T1 代表苯基甲基、苯基乙基、苯基丙基、雙苯基甲基、吡啶基甲基、嘧啶基甲基、噻唑基甲基、唑基甲基、吡唑基甲基、噻吩基甲基、呋喃基甲基或呋喃酮基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C2-C4-烯基、C1-C4-鹵烷基、C1-C4-氰基烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C4-烷基羰基，或T1 代表C3-C6-環烷基、C3-C6-環烯基、C4-C8-雙環烷基、C3-C8-環烷基-C1-C4-烷基、氮雜環丁烷基、氧雜環丁烷基、氧雜環戊烷基、氧雜環己烷基、二氧雜環己烷基、硫雜環丁烷基、側氧基硫雜環丁烷基、二側氧基硫雜環丁烷基、硫雜環戊烷基、四氫呋喃基、四氫硫呋喃基、側氧基四氫硫呋喃基、二側氧基四氫硫呋喃基、四氫哌喃基、四氫硫哌喃基、側氧基四氫硫哌喃基、二側氧基四氫硫哌喃基、C3-C6-環烷基甲基、C3-C6-環烷基乙基、氮雜環丁烷基甲基、氧雜環丁烷基甲基、氧雜環戊烷基甲基、硫雜環丁烷基甲基、側氧基硫雜環丁烷基甲基、二側氧基硫雜環丁烷基甲基、四氫呋喃基甲基或四氫哌喃基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C4-烷基羰基，T2 代表苯基甲基、苯基乙基、苯基丙基、吡啶基甲基、嘧啶基甲基、噻 唑基甲基、唑基甲基、吡唑基甲基、噻吩基甲基、呋喃基甲基或呋喃酮基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：鹵素、氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基或C2-C4-烷基羰基，或T2 代表C3-C6-環烷基、C3-C6-環烯基或C4-C8-雙環烷基，其中上述基團可視需要分別獨立經鹵素單取代至三取代或經氰基、硝基、SF5、羥基、胺基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基、C2-C4-烷基羰基單取代，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-4、U-5、U-6、U-9、U-20、U-23、U-24與U-25所組成群中之環，Xa 代表鹵素、硝基、氰基、SF5、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷氧基-C1-C4-烷基、氰基-C1-C4-烷基、C2-C4-烯基、C3-C4-炔基、C1-C4-烷基-S(O)p-、C1-C4-烷基羰基、C1-C4-烷氧基羰基、C1-C4-烷氧基亞胺基-C1-C4-烷基或C1-C4-鹵烷基磺醯基，R1 代表鹵素、硝基、氰基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷氧基-C1-C4-烷基、氰基-C1-C4-烷基、C2-C4-烯基、C3-C4-炔基、C1-C4-烷基-S(O)p-、C1-C4-烷基羰基、C1-C4-烷氧基羰基或C1-C4-烷氧基亞胺基-C1-C4-烷基，R1a 代表C1-C4-烷基，R2 代表氫、C1-C4-烷基、C1-C4-鹵烷基、C3-C6-環烷基、C3-C6-環烷基-C1-C4- 烷基、C1-C4-烷氧基-C1-C4-烷基、苯基、吡啶基、苯基甲基或吡啶基甲基，其中苯基、吡啶基、苯基甲基與吡啶基甲基可視需要經選自下列所組成群中之相同或相異取代基單取代或多取代：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基與C1-C4-鹵烷氧基，R5 代表氫、C1-C4-烷基、C1-C4-鹵烷基、C3-C6-環烷基、C3-C6-環烷基-C1-C4-烷基、苯基、吡啶基、苯基甲基或吡啶基甲基，其中苯基、吡啶基、苯基甲基與吡啶基甲基可視需要經選自下列所組成群中之相同或相異取代基單取代或多取代：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-與C1-C4-烷氧基羰基，R6 代表C1-C4-烷基、C1-C4-鹵烷基、C3-C6-環烷基、苯基或苯基甲基，其中苯基與苯基甲基可視需要經選自下列所組成群中之相同或相異取代基單取代或多取代：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-與C1-C4-烷氧基羰基，R7a、R7b、R7c 彼此分別獨立代表C1-C4-烷基，R9 代表氫、氟、氯或C1-C4-烷基，R10 代表氫、氟、氯或C1-C4-烷基，m 代表0、1、2或3，n 代表0、1、2或3，及p 代表0、1或2。 Also preferably (Configuration 2-2) is that in the compound of formula (I), A represents O or S, and Q represents one of the groups Q-1, Q-5 or Q-6, and Y represents a phenyl group, a pyridyl group, Pyrimidinyl, thiazolyl, An azolyl, pyrazolyl, thienyl or furyl group, wherein the above groups may be independently monosubstituted to trisubstituted, respectively, via the following groups: halogen, cyano, nitro, SF 5 , hydroxy, amine, C 1 - C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl, C 2 -C 6 -alkylcarbonyl, T If A represents O, it represents T 1 , or T. If A represents S, it represents T 2 , T 1 represents a C 1 -C 4 -alkyl group, a C 2 -C 6 -alkenyl group or a C 2 -C 6 -alkynyl group, wherein the above group is substituted with a substituent selected from the group consisting of cyano group, Nitro, hydroxy, C(O)OR 2 , OC(O)R 5 , S(O) p R 6 , Si(R 7a )(R 7b )(R 7c ), or T 1 represents C 2 -C 6 Alkenyl or C 2 -C 6 -alkynyl, wherein the above groups may be independently mono-substituted to trisubstituted or C 1 -C 6 -alkoxy or C 1 -C 6 -haloalkoxy, respectively, as desired. Monosubstituted, or T 1 represents phenylmethyl, phenylethyl, phenylpropyl, bisphenylmethyl, pyridylmethyl, pyrimidinylmethyl, thiazolylmethyl, An azolylmethyl, pyrazolylmethyl, thienylmethyl, furylmethyl or furanosylmethyl group, wherein the above groups may be independently monosubstituted to trisubstituted by the following groups, respectively: halogen, cyano, Nitro, SF 5 , hydroxy, amine, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -cyanoalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 4 -alkylcarbonyl, or T 1 represents C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkenyl, C 4 -C 8 -bicycloalkyl, C 3 -C 8 -cycloalkane -C 1 -C 4 -alkyl, azetidinyl, oxetanyl, oxolane, oxacyclohexane, dioxanyl, thioheterocycle Butanyl, pendant oxythietane, di-side oxirane, thiolanyl, tetrahydrofuranyl, tetrahydrothiofuranyl, pendant oxytetrahydrofuranyl, Bilateral oxytetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiopyranyl, oxytetrahydrothiopyranyl, di-oxytetrahydrothiopyranyl, C 3 -C 6 - Cycloalkylmethyl C 3 -C 6 - cycloalkyl group, azetidinyl group, oxetanyl group, oxolane group, thietanyl group, oxygen-side a thietanemethyl group, a 2-sided oxirane group, a tetrahydrofuranylmethyl group or a tetrahydropyranylmethyl group, wherein the above groups may be independently substituted by the following groups, respectively, as needed To trisubstituted: halogen, cyano, nitro, SF5, hydroxy, amine, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 4 -alkylcarbonyl, T 2 represents benzene Methyl, phenylethyl, phenylpropyl, pyridylmethyl, pyrimidinylmethyl, thiazolylmethyl, An azolylmethyl, pyrazolylmethyl, thienylmethyl, furylmethyl or furanosylmethyl group, wherein the above groups may be independently monosubstituted to trisubstituted by the following groups, respectively: halogen, cyano, Nitro, SF 5 , hydroxy, amine, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy , C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl or C 2 -C 4 -alkylcarbonyl, or T 2 represents C 3 -C 6 -cycloalkane a C 3 -C 6 -cycloalkenyl group or a C 4 -C 8 -bicycloalkyl group, wherein the above groups may be independently monosubstituted to trisubstituted or via cyano, nitro, SF 5 , hydroxy, Amino, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkane a group of -S(O) p -, C 2 -C 6 -alkoxycarbonyl, C 2 -C 4 -alkylcarbonyl, G represents -C(R 9 )(R 10 )-, and U represents a : a ring in the group consisting of U-2, U-4, U-5, U-6, U-9, U-20, U-23, U-24 and U-25, X a represents halogen, nitro , cyano, SF 5, C 1 -C 4 - alkyl, C 1 -C 4 - haloalkyl, C 1 -C 4 - alkoxy , C 1 -C 4 - haloalkoxy, C 1 -C 4 - alkoxy, -C 1 -C 4 - alkyl, cyano, -C 1 -C 4 - alkyl, C 2 -C 4 - alkenyl , C 3 -C 4 -alkynyl, C 1 -C 4 -alkyl-S(O) p -, C 1 -C 4 -alkylcarbonyl, C 1 -C 4 -alkoxycarbonyl, C 1 -C 4 -alkoxyimino-C 1 -C 4 -alkyl or C 1 -C 4 -haloalkylsulfonyl, R 1 represents halogen, nitro, cyano, C 1 -C 4 - Alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkoxy-C 1 -C 4 - Alkyl, cyano-C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 3 -C 4 -alkynyl, C 1 -C 4 -alkyl-S(O) p -, C 1- C 4 -alkylcarbonyl, C 1 -C 4 -alkoxycarbonyl or C 1 -C 4 -alkoxyimino-C 1 -C 4 -alkyl, R 1a represents C 1 -C 4 -alkyl, R 2 represents hydrogen, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, phenyl, pyridyl, phenylmethyl or pyridylmethyl, wherein phenyl, pyridyl, benzene The methyl group and the pyridylmethyl group may be the same as those selected from the group consisting of or Isopropyl substituent group mono- or polysubstituted by: halogen, cyano, nitro, C 1 -C 4 - alkyl, C 1 -C 4 - haloalkyl, C 1 -C 4 - alkoxy with C 1 -C 4 -haloalkoxy, R 5 represents hydrogen, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl -C 1 -C 4 -alkyl, phenyl, pyridyl, phenylmethyl or pyridylmethyl, wherein phenyl, pyridyl, phenylmethyl and pyridylmethyl may optionally consist of the following Single or multiple substitutions of the same or different substituents in the group: halogen, cyano, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy a C 1 -C 4 -haloalkoxy group, a C 1 -C 4 -alkyl-S(O) p - group and a C 1 -C 4 -alkoxycarbonyl group, and R 6 represents a C 1 -C 4 -alkane group a C 1 -C 4 -haloalkyl group, a C 3 -C 6 -cycloalkyl group, a phenyl group or a phenylmethyl group, wherein the phenyl group and the phenylmethyl group may be the same as those selected from the group consisting of the following: Or a monosubstituted or polysubstituted heterocyclic substituent: halogen, cyano, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p And with a C 1 -C 4 -alkoxycarbonyl group, R 7a , R 7b , R 7c each independently represent a C 1 -C 4 -alkyl group, and R 9 represents a hydrogen, fluorine, chlorine or C 1 -C 4 -alkane And R 10 represents hydrogen, fluorine, chlorine or C 1 -C 4 -alkyl, m represents 0, 1, 2 or 3, n represents 0, 1, 2 or 3, and p represents 0, 1 or 2.
進一步較佳(組態3-1)為式(I)化合物中A 代表O， Q 代表基團Q-1、Q-5或Q-6中之一，Y 代表苯基、吡唑基或噻吩基，其中上述基團可視需要經相同或相異取代基單取代至三取代，且取代基係分別獨立選自下列：鹵素、氰基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基與C2-C4-烷基羰基，T 代表T1，T1 代表C1-C4-烷基、C2-C6-烯基或C2-C6-炔基，其中上述基團係經選自下列所組成群中之取代基取代：氰基、硝基、羥基、C(O)OR2、OC(O)R5、S(O)pR6、Si(R7a)(R7b)(R7c)，或T1 代表C2-C6-烯基或C2-C6-炔基，其中上述基團可視需要經鹵素單取代至三取代或經C1-C6-烷氧基或C1-C6-鹵烷氧基單取代，或T1 代表苯基甲基、苯基乙基、苯基丙基、雙苯基甲基、吡啶基甲基、嘧啶基甲基、噻唑基甲基、唑基甲基、吡唑基甲基、噻吩基甲基、呋喃基甲基或呋喃酮基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基、乙氧基羰基，或T1 代表環丙基、環丁基、環己基、環己烯基、雙環庚烷、氮雜環丁烷基、氧雜環丁烷基、氧雜環戊烷基、氧雜環己烷基、二氧雜環己烷基、硫雜環丁烷基、側氧基硫雜環丁烷基、二側氧基硫雜環丁烷基、硫雜環 己烷基、四氫呋喃基、四氫硫呋喃基、側氧基四氫硫呋喃基、二側氧基四氫硫呋喃基、四氫哌喃基、四氫硫哌喃基、環丙基甲基、環丁基甲基、環己基甲基、氮雜環丁烷基甲基、氧雜環丁烷基甲基、四氫呋喃基甲基或四氫哌喃基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫、甲基亞磺醯基、甲基磺醯基、甲氧基羰基與乙氧基羰基，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-9與U-23所組成群中之環，Xa 代表鹵素、氰基、硝基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基、甲基硫、甲基亞磺醯基、甲基磺醯基或甲氧基羰基，R1 代表鹵素、氰基、甲基、乙基、正-、異丙基、正-、異-、第二-、第三丁基、三氟甲基、甲氧基、乙氧基、正-、異丙氧基、三氟甲氧基、甲基硫、乙基硫基、甲基亞磺醯基、乙基亞磺醯基、甲基磺醯基、乙基磺醯基或甲氧基羰基，R1a 代表甲基或乙基，R2 代表氫、甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基、環丙基、環丁基、環戊基、環丙基甲基、環丁基甲基、環戊基甲基或環己基甲基，R5 代表氫、甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基、二氟甲基、三氟甲基、五氟乙基、C3-C6-環烷基、苯基、吡啶基、苯基甲基或吡啶基甲基，其中苯基、吡啶基、苯基甲基與吡啶基甲基可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、 氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基與乙氧基羰基，R6 代表甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基、苯基或苯基甲基，其中苯基與苯基甲基可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基與乙氧基羰基，R7a、R7b、R7c 彼此分別獨立代表甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基，R9 代表氫、氟、甲基或乙基，R10 代表氫、氟或甲基，m 代表0、1、2或3，n 代表0、1、2或3，及p 代表0、1或2。 Further preferably (Configuration 3-1) is a compound of formula (I) wherein A represents O, Q represents one of the groups Q-1, Q-5 or Q-6, and Y represents phenyl, pyrazolyl or thiophene a group wherein the above groups may be mono-substituted to trisubstituted by the same or different substituents, and the substituents are each independently selected from the group consisting of halogen, cyano, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxy a carbonyl group and a C 2 -C 4 -alkylcarbonyl group, T represents T 1 , and T 1 represents a C 1 -C 4 -alkyl group, a C 2 -C 6 -alkenyl group or a C 2 -C 6 -alkynyl group, wherein The group is substituted with a substituent selected from the group consisting of cyano, nitro, hydroxy, C(O)OR 2 , OC(O)R 5 , S(O) p R 6 , Si (R 7a (R 7b )(R7 c ), or T 1 represents C 2 -C 6 -alkenyl or C 2 -C 6 -alkynyl, wherein the above group may be monosubstituted to trisubstituted or via C 1 - as desired. C 6 -alkoxy or C 1 -C 6 -haloalkoxy monosubstituted, or T 1 represents phenylmethyl, phenylethyl, phenylpropyl, bisphenylmethyl, pyridylmethyl, Pyrimidinylmethyl, thiazolylmethyl, An azolylmethyl, pyrazolylmethyl, thienylmethyl, furylmethyl or furanosylmethyl group, wherein the above groups may be mono-substituted to trisubstituted as desired, and the substituents are each independently selected from the following: Fluorine, chlorine, bromine, cyano, nitro, methyl, ethyl, n- or i-propyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy, tri Fluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl, methoxycarbonyl, ethoxycarbonyl, or T 1 represents cyclopropyl, cyclobutyl, cyclohexyl, cyclohexyl Alkenyl, bicycloheptane, azetidinyl, oxetanyl, oxolane, oxacyclohexane, dioxanyl, thietane, Oxyl thietane, dioxiranethiolane, thiacyclohexane, tetrahydrofuranyl, tetrahydrothiofuranyl, pendant oxytetrahydrothiofuranyl, di-oxy Tetrahydrothiofuranyl, tetrahydropyranyl, tetrahydrothiopyranyl, cyclopropylmethyl, cyclobutylmethyl, cyclohexylmethyl, azetidinylmethyl, oxetanyl Tetrahydrofuranyl Or tetrahydropyranylmethyl, wherein the above groups may be mono-substituted to trisubstituted as desired, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine, cyano, nitro, methyl, ethyl, Ortho- or iso-propyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, methyl Sulfhydryl, methoxycarbonyl and ethoxycarbonyl, G represents -C(R 9 )(R 10 )-, and U represents a ring selected from the group consisting of U-2, U-9 and U-23 X a represents halogen, cyano, nitro, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, methyl Sulfhydryl or methoxycarbonyl, R 1 represents halogen, cyano, methyl, ethyl, n-, isopropyl, n-, i-, second-, tert-butyl, trifluoromethyl, Methoxy, ethoxy, n-, isopropoxy, trifluoromethoxy, methylthio, ethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl , ethyl sulfonic acyl group or a methoxycarbonyl, R 1a represents a methyl or ethyl group, R 2 represents hydrogen, methyl, ethyl , n- or iso-propyl, n-, i-, second- or tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentyl Or cyclohexylmethyl, R 5 represents hydrogen, methyl, ethyl, n- or i-propyl, n-, i-, second- or tert-butyl, difluoromethyl, trifluoromethyl , pentafluoroethyl, C 3 -C 6 -cycloalkyl, phenyl, pyridyl, phenylmethyl or pyridylmethyl, wherein phenyl, pyridyl, phenylmethyl and pyridylmethyl are optionally required Monosubstituted to trisubstituted, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine, cyano, nitro, methyl, ethyl, n- or i-propyl, trifluoromethyl, difluoro. Methyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl, methoxycarbonyl and ethoxycarbonyl, R 6 represents a methyl group, an ethyl group, a n- or i-propyl group, a n-, an iso-, a second- or a tert-butyl group, a phenyl group or a phenylmethyl group, wherein a phenyl group and a phenylmethyl group are optionally required Monosubstituted to trisubstituted, and the substituents are each independently selected from the following: fluorine, , bromine, cyano, nitro, methyl, ethyl, n- or i-propyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy a group, a methylthio group, a methylsulfinyl group, a methylsulfonyl group, a methoxycarbonyl group and an ethoxycarbonyl group, and R 7a , R 7b and R 7c each independently represent a methyl group, an ethyl group, a positive group - Or iso-propyl, n-, iso-, second- or tert-butyl, R 9 represents hydrogen, fluorine, methyl or ethyl, R 10 represents hydrogen, fluorine or methyl, m represents 0, 1, 2 or 3, n represents 0, 1, 2 or 3, and p represents 0, 1 or 2.
同樣進一步較佳(組態3-2)為式(I)化合物中A 代表O或S，Q 代表基團Q-1、Q-5或Q-6中之一，Y 代表苯基、吡唑基或噻吩基，其中上述基團可視需要經相同或相異取代基單取代至三取代，且取代基係分別獨立選自下列：鹵素、氰基、硝基、C1-C4-烷基、C1-C4-鹵烷基、C1-C4-烷氧基、C1-C4-鹵烷氧基、C1-C4-烷基-S(O)p-、C2-C6-烷氧基羰基與C2-C4-烷基羰基， T 若A代表O時，則代表T1，或T 若A代表S時，則代表T2，T1 代表C1-C4-烷基、C2-C6-烯基或C2-C6-炔基，其中上述基團係經選自下列所組成群中之取代基取代：氰基、硝基、羥基、C(O)OR2、OC(O)R5、S(O)pR6、Si(R7a)(R7b)(R7c)，或T1 代表C2-C6-烯基或C2-C6-炔基，其中上述基團可視需要經鹵素單取代至三取代或經C1-C6-烷氧基或C1-C6-鹵烷氧基單取代，或T1 代表苯基甲基、苯基乙基、苯基丙基、雙苯基甲基、吡啶基甲基、嘧啶基甲基、噻唑基甲基、唑基甲基、吡唑基甲基、噻吩基甲基、呋喃基甲基或呋喃酮基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、氰基甲基、硝基、甲基、乙基、正-或異-丙基、乙烯基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基、乙氧基羰基，或T1 代表環丙基、環丁基、環己基、環己烯基、雙環庚烷、氮雜環丁烷基、氧雜環丁烷基、氧雜環戊烷基、氧雜環己烷基、二氧雜環己烷基、硫雜環丁烷基、側氧基硫雜環丁烷基、二側氧基硫雜環丁烷基、四氫呋喃基、四氫硫呋喃基、側氧基四氫硫呋喃基、二側氧基四氫硫呋喃基、四氫哌喃基、四氫硫哌喃基、側氧基四氫硫哌喃基、二側氧基四氫硫哌喃基、環丙基甲基、環丁基甲基、環己基甲基、氮雜環丁烷基甲基、氧雜環丁烷基甲基、四氫呋喃基甲基或四氫哌喃基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、 甲基亞磺醯基、甲基磺醯基、甲氧基羰基與乙氧基羰基，T2 代表苯基甲基、苯基乙基或吡啶基甲基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：氟、氯、溴、氰基、硝基、羥基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基或乙氧基羰基，或T2 代表環丙基、環丁基、環戊基、環己基或環己烯基，其中上述基團可視需要分別獨立經下列基團單取代至三取代：氟、氯或溴，或經氰基、硝基、羥基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基或乙氧基羰基單取代，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-4、U-5、U-9、U-23、U-24與U-25所組成群中之環，Xa 代表鹵素、氰基、硝基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基或甲氧基羰基，R1 代表鹵素、氰基、甲基、乙基、正-、異丙基、正-、異-、第二-、第三丁基、三氟甲基、甲氧基、乙氧基、正-、異丙氧基、三氟甲氧基、甲基硫基、乙基硫基、甲基亞磺醯基、乙基亞磺醯基、甲基磺醯基、乙基磺醯基或甲氧基羰基，R1a 代表甲基或乙基，R2 代表氫、甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基、環丙基、環丁基、環戊基、環丙基甲基、環丁基甲基、環戊基甲基或環 己基甲基，R5 代表氫、甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基、二氟甲基、三氟甲基、五氟乙基、C3-C6-環烷基、苯基、吡啶基、苯基甲基或吡啶基甲基，其中苯基、吡啶基、苯基甲基與吡啶基甲基可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基與乙氧基羰基，R6 代表甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基、苯基或苯基甲基，其中苯基與苯基甲基可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、正-或異-丙基、三氟甲基、二氟甲基、五氟乙基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基、甲氧基羰基與乙氧基羰基，R7a、R7b、R7c 彼此分別獨立代表甲基、乙基、正-或異-丙基、正-、異-、第二-或第三丁基，R9 代表氫、氟、甲基或乙基，R10 代表氫、氟或甲基，m 代表0、1、2或3，n 代表0、1、2或3，及p 代表0、1或2。 It is further preferred (configuration 3-2) that in the compound of formula (I), A represents O or S, and Q represents one of the groups Q-1, Q-5 or Q-6, and Y represents phenyl, pyrazole. Or a thiophenyl group, wherein the above groups may be mono-substituted to trisubstituted by the same or different substituents, and the substituents are each independently selected from the group consisting of halogen, cyano, nitro, C 1 -C 4 -alkyl , C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkyl-S(O) p -, C 2 -C 6 -alkoxycarbonyl and C 2 -C 4 -alkylcarbonyl, T If A represents O, it represents T 1 , or T. If A represents S, it represents T 2 and T 1 represents C 1 - a C 4 -alkyl group, a C 2 -C 6 -alkenyl group or a C 2 -C 6 -alkynyl group, wherein the above group is substituted with a substituent selected from the group consisting of a cyano group, a nitro group, a hydroxyl group, C(O)OR 2 , OC(O)R 5 , S(O) p R 6 , Si(R 7a )(R 7b )(R 7c ), or T 1 represents C 2 -C 6 -alkenyl or C a 2- C 6 -alkynyl group, wherein the above group may be mono-substituted to trisubstituted or mono-substituted by C 1 -C 6 -alkoxy or C 1 -C 6 -haloalkoxy, or T 1 may be optionally substituted by halogen. Phenylmethyl, phenylethyl, phenylpropyl Bis phenylmethyl, pyridinylmethyl, pyrimidinylmethyl, thiazolylmethyl, An azolylmethyl, pyrazolylmethyl, thienylmethyl, furylmethyl or furanosylmethyl group, wherein the above groups may be mono-substituted to trisubstituted as desired, and the substituents are each independently selected from the following: Fluorine, chlorine, bromine, cyano, cyanomethyl, nitro, methyl, ethyl, n- or i-propyl, vinyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, A An oxy group, an ethoxy group, a trifluoromethoxy group, a methylthio group, a methylsulfinyl group, a methylsulfonyl group, a methoxycarbonyl group, an ethoxycarbonyl group, or T 1 represents a cyclopropyl group or a ring. Butyl, cyclohexyl, cyclohexenyl, bicycloheptane, azetidinyl, oxetanyl, oxolane, oxacyclohexane, dioxane ,Thetylene,thyleneoxythicyclobutane,dihydrothiazepine,tetrahydrofuranyl, tetrahydrothiofuranyl, oxirane tetrahydrothiofuranyl, two-sided oxygen Tetrahydrothiofuranyl, tetrahydropyranyl, tetrahydrothiopyranyl, iso-oxytetrahydrothiopyranyl, di-oxytetrahydrothiopyranyl, cyclopropylmethyl, cyclobutylmethyl Cyclohexylmethyl, nitrogen a cyclobutanemethyl group, an oxetanylmethyl group, a tetrahydrofuranylmethyl group or a tetrahydrohydropyranylmethyl group, wherein the above groups may be mono-substituted to trisubstituted as desired, and the substituents are each independently selected from the group consisting of The following: fluorine, chlorine, bromine, cyano, nitro, methyl, ethyl, n- or i-propyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy , trifluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl, methoxycarbonyl and ethoxycarbonyl, T 2 represents phenylmethyl, phenylethyl or pyridyl a methyl group, wherein the above groups may be independently monosubstituted to trisubstituted by the following groups, respectively: fluorine, chlorine, bromine, cyano, nitro, hydroxy, methyl, ethyl, n- or i-propyl, three Fluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl, methoxycarbonyl or ethoxycarbonyl, or T 2 represents cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cyclohexenyl, wherein said radicals are optionally independently substituted by oxo, mono- to trisubstituted Fluorine, chlorine or bromine, or via cyano, nitro, hydroxy, methyl, ethyl, n- or i-propyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, B Oxyl, trifluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl, methoxycarbonyl or ethoxycarbonyl monosubstituted, G represents -C(R 9 ) (R 10 ), U represents a ring selected from the group consisting of U-2, U-4, U-5, U-9, U-23, U-24 and U-25, and X a represents halogen, cyano, Nitro, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl or methoxycarbonyl R 1 represents halogen, cyano, methyl, ethyl, n-, isopropyl, n-, i-, di-, t-butyl, trifluoromethyl, methoxy, ethoxy, N-, isopropoxy, trifluoromethoxy, methylthio, ethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl or methoxycarbonyl group, R 1a represents a methyl or ethyl group, R 2 represents hydrogen, methyl, ethyl, n - or iso - propyl, n -, iso -, the second - or tert-butyl, Cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl or cyclohexylmethyl, R 5 represents hydrogen, methyl, ethyl, n - or iso - propyl , n-, iso-, second- or tert-butyl, difluoromethyl, trifluoromethyl, pentafluoroethyl, C 3 -C 6 -cycloalkyl, phenyl, pyridyl, phenyl Or pyridylmethyl, wherein phenyl, pyridyl, phenylmethyl and pyridylmethyl may optionally be mono-substituted to trisubstituted, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine and cyano. , nitro, methyl, ethyl, n- or i-propyl, trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy, methylsulfide Methylsulfinyl, methylsulfonyl, methoxycarbonyl and ethoxycarbonyl, R 6 represents methyl, ethyl, n- or i-propyl, n-, iso-, second Or a tert-butyl, phenyl or phenylmethyl group, wherein the phenyl group and the phenylmethyl group may be mono-substituted to tri-substituted, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine and cyano. , nitro, methyl, ethyl, n- or i-propyl, Trifluoromethyl, difluoromethyl, pentafluoroethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, methylsulfonyl, methoxy a carbonyl group and an ethoxycarbonyl group, R 7a , R 7b , and R 7c each independently represent a methyl group, an ethyl group, a n- or i-propyl group, a n-, an iso-, a second- or a third butyl group, and R 9 Represents hydrogen, fluorine, methyl or ethyl, R 10 represents hydrogen, fluorine or methyl, m represents 0, 1, 2 or 3, n represents 0, 1, 2 or 3, and p represents 0, 1 or 2.
特別佳(組態4-1)為式(I)化合物中A 代表O， Q 代表基團Q-1或Q-6其中之一，Y 代表苯基，其可視需要經相同或相異取代基單取代至三取代，其中取代基係分別獨立選自下列：氟、氯、溴、碘、氰基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基與甲基硫基，T 代表T1，T1 代表苯基甲基、吡啶-2-基甲基、吡啶-3-基甲基或吡啶-4-基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基與甲基磺醯基，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-9與U-23所組成群中之環，Xa 代表氟、氯、溴、氰基、硝基、甲基、乙基、三氟甲基、甲氧基、乙氧基或三氟甲氧基，R1 代表氟、氯、溴、碘、氰基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基或甲基硫基，R1a 代表甲基，R9 為氫或甲基，R10 代表氫，m 代表0、1或2，及n 代表0、1或2。 Particularly preferred (configuration 4-1) is that in the compound of formula (I), A represents O, Q represents one of the groups Q-1 or Q-6, and Y represents a phenyl group which may optionally have the same or different substituents. Monosubstituted to trisubstituted, wherein the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine, iodine, cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, trifluoromethoxy And methylthio, T represents T 1 , T 1 represents phenylmethyl, pyridin-2-ylmethyl, pyridin-3-ylmethyl or pyridin-4-ylmethyl, wherein the above groups may be optionally Monosubstituted to trisubstituted, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine, cyano, nitro, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, trifluoro Methoxy, methylthio, methylsulfinyl and methylsulfonyl, G represents -C(R 9 )(R 10 )-, and U represents a selected from: U-2, U-9 and U a ring in the group consisting of -23, X a represents fluorine, chlorine, bromine, cyano, nitro, methyl, ethyl, trifluoromethyl, methoxy, ethoxy or trifluoromethoxy, R 1 represents fluorine, chlorine, bromine, iodine, cyano, methyl, ethyl, trifluoromethyl, methoxy, Ethoxy, trifluoromethoxy or methylthio, R 1a represents methyl, R 9 is hydrogen or methyl, R 10 represents hydrogen, m represents 0, 1 or 2, and n represents 0, 1 or 2 .
同樣特別佳(組態4-2)為式(I)化合物中A 代表O或S，Q 代表基團Q-1或Q-6其中之一， Y 代表苯基，其可視需要經相同或相異取代基單取代至三取代，其中取代基係分別獨立選自下列：氟、氯、溴、碘、氰基、硝基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基與甲基硫基，T 若A代表O時，則代表T1，或T 若A代表S時，則代表T2，T1 代表苯基甲基、吡啶-2-基甲基、吡啶-3-基甲基或吡啶-4-基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、氰基甲基、硝基、甲基、乙基、乙烯基、三氟甲基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基、甲基磺醯基與乙氧基羰基，或代表苯基乙基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：氟、氯、溴、氰基、硝基、甲基、乙基、乙烯基、三氟甲基、甲氧基、乙氧基、三氟甲氧基、甲基硫基、甲基亞磺醯基與甲基磺醯基，或代表環己基或環丙基，其中上述基團可視需要經單取代或二取代，且取代基係分別獨立選自下列：甲基、乙基與異丙基，或代表環己基甲基或環丙基甲基，其中上述基團可視需要經單取代至三取代，且取代基係分別獨立選自下列：甲基、氯或氟，或代表乙基，其中乙基係經乙氧基羰基或乙氧基羰基甲基單取代或二取代，或代表乙基，其中乙基係經甲基磺醯基或乙醯氧基取代，或代表四氫哌喃-4-基或二側氧基四氫硫哌喃基，T2 代表苯基甲基，其中上述基團可視需要經氟、氯或甲基取代，或代表環己基，其中上述基團可視需要經氟、氯或甲基取代， G 代表-C(R9)(R10)-，U 代表選自：U-2、U-5、U-9、U-23、U-24與U-25所組成群中之環，Xa 代表氟、氯、溴、氰基、硝基、甲基、乙基、三氟甲基、甲氧基、乙氧基或三氟甲氧基，R1 代表氟、氯、溴、碘、氰基、甲基、乙基、三氟甲基、甲氧基、乙氧基、三氟甲氧基或甲基硫基，R1a 代表甲基，R9 代表氫或甲基，R10 代表氫，m 代表0、1或2，及n 代表0、1或2。 Also particularly preferred (configuration 4-2) is that in the compound of formula (I), A represents O or S, Q represents one of the groups Q-1 or Q-6, and Y represents a phenyl group which may be the same or phase as desired The hetero-substitution is mono-substituted to tri-substituted, wherein the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine, iodine, cyano, nitro, methyl, ethyl, trifluoromethyl, methoxy, ethoxy. Base, trifluoromethoxy and methylthio, T, if A represents O, represents T 1 , or T. If A represents S, it represents T 2 , and T 1 represents phenylmethyl, pyridin-2- Methyl, pyridin-3-ylmethyl or pyridin-4-ylmethyl, wherein the above groups may be mono-substituted to trisubstituted, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine and cyanide. Base, cyanomethyl, nitro, methyl, ethyl, vinyl, trifluoromethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl, Methylsulfonyl and ethoxycarbonyl, or phenylethyl, wherein the above groups may be mono-substituted to trisubstituted, and the substituents are each independently selected from the group consisting of fluorine, chlorine, bromine, cyano, Nitro, methyl, Base, vinyl, trifluoromethyl, methoxy, ethoxy, trifluoromethoxy, methylthio, methylsulfinyl and methylsulfonyl, or represents cyclohexyl or cyclopropyl Wherein the above group may be mono- or di-substituted as desired, and the substituents are each independently selected from the group consisting of methyl, ethyl and isopropyl, or a cyclohexylmethyl or cyclopropylmethyl group, wherein the above group The group may be mono-substituted to trisubstituted, and the substituents are each independently selected from the group consisting of methyl, chloro or fluoro, or an ethyl group, wherein the ethyl group is monosubstituted by ethoxycarbonyl or ethoxycarbonylmethyl. Or disubstituted, or represents ethyl, wherein ethyl is substituted with methylsulfonyl or ethoxylated, or represents tetrahydropyran-4-yl or di- oxytetrahydrothiopyranyl, T 2 Represents a phenylmethyl group, wherein the above group may be optionally substituted by fluorine, chlorine or methyl, or represents a cyclohexyl group, wherein the above group may be optionally substituted by fluorine, chlorine or methyl, and G represents -C(R 9 ) ( R 10 )-, U represents a ring selected from the group consisting of U-2, U-5, U-9, U-23, U-24 and U-25, and X a represents fluorine, chlorine, bromine and cyanide. base Nitro, methyl, ethyl, trifluoromethyl, methoxy, ethoxy or trifluoromethoxy group, R 1 represents fluorine, chlorine, bromine, iodine, cyano, methyl, ethyl, trifluoromethyl, Methyl, methoxy, ethoxy, trifluoromethoxy or methylthio, R 1a represents methyl, R 9 represents hydrogen or methyl, R 10 represents hydrogen, m represents 0, 1 or 2, and n stands for 0, 1, or 2.
極特別佳(組態5-1)為式(I)化合物中A 代表O，Q 代表基團Q-1或Q-6其中之一，Y 代表苯基，T 代表T1，T1 代表苯基甲基，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-9與U-23所組成群中之環，Xa 代表氯，R1 代表甲基，R1a 代表甲基，R9 代表氫， R10 代表氫，m 代表0或1，及n 代表0或1。 Very particularly preferred (Configuration 5-1) is a compound of formula (I) wherein A represents O, Q represents one of the groups Q-1 or Q-6, Y represents phenyl, T represents T 1 and T 1 represents benzene Methyl, G represents -C(R 9 )(R 10 )-, U represents a ring selected from the group consisting of U-2, U-9 and U-23, X a represents chlorine, and R 1 represents A And R 1a represents a methyl group, R 9 represents hydrogen, R 10 represents hydrogen, m represents 0 or 1, and n represents 0 or 1.
同樣極特別佳(組態5-2)為式(I)化合物中A 代表O，Q 代表基團Q-1或Q-6其中之一，Y 代表苯基，其中上述基團可視需要經取代，且取代基係分別獨立選自下列：氯、硝基、三氟甲基與甲氧基，T 代表T1，T1 代表苯基甲基，其中苯基可經氯取代，且其中甲基可經甲基、氰基、氰基甲基、乙烯基或乙氧基羰基取代，或代表苯基乙基或吡啶基甲基，其中吡啶基可經氯取代，或代表環己基，其中環己基可經甲基與異丙基取代，或代表環丙基，其中環丙基可經甲基取代，或代表環己基甲基或環丙基甲基，其中環丙基可經單取代至三取代，且取代基係分別獨立選自：甲基與氟，或代表乙基，其中乙基係經乙氧基羰基單取代或二取代，或代表乙基，其中乙基係經乙氧基羰基甲基取代，或代表乙基，其中乙基係經甲基磺醯基取代，或代表乙基，其中乙基係經乙醯氧基取代，或代表四氫哌喃-4-基或二側氧基四氫硫哌喃基，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-5、U-9、U-23、U-24與U-25所組成群中之環， Xa 代表氫或氯，R1 代表甲基，R1a 代表甲基，R9 代表氫，R10 代表氫，m 代表0或1，及n 代表0或1。 Also very particularly preferred (configuration 5-2) is that in the compound of formula (I), A represents O, Q represents one of the groups Q-1 or Q-6, and Y represents a phenyl group, wherein the above groups may be substituted as needed And the substituents are each independently selected from the group consisting of chlorine, nitro, trifluoromethyl and methoxy, T represents T 1 , and T 1 represents a phenylmethyl group, wherein the phenyl group may be substituted by chlorine, and wherein methyl It may be substituted by methyl, cyano, cyanomethyl, vinyl or ethoxycarbonyl, or represents phenylethyl or pyridylmethyl, wherein the pyridyl group may be substituted by chlorine or represent a cyclohexyl group, wherein cyclohexyl It may be substituted by a methyl group and an isopropyl group, or may represent a cyclopropyl group, wherein the cyclopropyl group may be substituted by a methyl group, or may represent a cyclohexylmethyl group or a cyclopropylmethyl group, wherein the cyclopropyl group may be monosubstituted to trisubstituted. And the substituents are each independently selected from: methyl and fluorine, or represent an ethyl group, wherein the ethyl group is mono- or di-substituted with an ethoxycarbonyl group, or represents an ethyl group, wherein the ethyl group is an ethoxycarbonyl group. Substituted, or represents an ethyl group, wherein the ethyl group is substituted with a methylsulfonyl group or represents an ethyl group in which the ethyl group is substituted with an ethoxy group. Or represents tetrahydropyran-4-yl or two sulfur-oxo-tetrahydro-pyran-yl, G Representative -C (R 9) (R 10 ) -, U represents selected from: U-2, U-5 , U -9, a ring in the group consisting of U-23, U-24 and U-25, X a represents hydrogen or chlorine, R 1 represents a methyl group, R 1a represents a methyl group, R 9 represents hydrogen, and R 10 represents hydrogen, m stands for 0 or 1, and n stands for 0 or 1.
同樣極特別佳(組態5-3)為式(I)化合物中A 代表S，Q 代表Q-1，Y 代表苯基，T 代表T2，T2 代表環己基或苯基甲基，G 代表-C(R9)(R10)-，U 代表選自：U-2、U-9與U-23所組成群中之環，Xa 代表氫或氯，R9 代表氫，R10 代表氫，m 代表0，及n 代表0或1。 Also very particularly preferred (configuration 5-3) is that in the compound of formula (I), A represents S, Q represents Q-1, Y represents phenyl, T represents T 2 , T 2 represents cyclohexyl or phenylmethyl, G Represents -C(R 9 )(R 10 )-, U represents a ring selected from the group consisting of U-2, U-9 and U-23, X a represents hydrogen or chlorine, R 9 represents hydrogen, R 10 Represents hydrogen, m stands for 0, and n stands for 0 or 1.
較佳具體實施例中，本發明係有關一種式(I)化合物，其中A代表O。 In a preferred embodiment, the invention relates to a compound of formula (I) wherein A represents O.
進一步較佳具體實施例中，本發明係有關一種式(I)化合物，其中A代表S。 In a further preferred embodiment, the invention relates to a compound of formula (I) wherein A represents S.
下列較佳具體實施例(I-1)與(IA)至(IJ)中，所有結構元素具有如上述組態(1-1)或組態(2-1)或組態(2-2)或組態(3-1)或組態(3-2)或組態(4-1)或組態(4-2)或組態(5-1)或組態(5-2)中之定義，除非另有說明。T1中，若沒有針對T1明確定義，則適用T之定義，此時，例如：則與組態(1-1)相關。若個別具體實施例中，出現仍未定義之結構元素時，其等將於下文中分別針對相關具體實施例說明。 In the following preferred embodiments (I-1) and (IA) to (IJ), all structural elements have the configuration (1-1) or configuration (2-1) or configuration (2-2) as described above. Or configure (3-1) or configure (3-2) or configure (4-1) or configure (4-2) or configure (5-1) or configure (5-2) Definition unless otherwise stated. In T 1 , if it is not clearly defined for T 1 , the definition of T is applied. In this case, for example, it is related to configuration (1-1). If structural elements that are still undefined are present in the particular embodiments, they will be described below with respect to the specific embodiments.
進一步較佳具體實施例中，本發明係有關一種式(I-1)化合物。式(I-1)中之U較佳代表U-2、U-5、U-9、U-23、U-24或U-25。 In a further preferred embodiment, the invention relates to a compound of formula (I-1). U in the formula (I-1) preferably represents U-2, U-5, U-9, U-23, U-24 or U-25.
其中特別佳為如下所示之組態：
本發明係有關一種式(IA)化合物，其中U代表U-2、U-5、U-9、U-23、U-24或U-25。 The present invention relates to a compound of formula (IA) wherein U represents U-2, U-5, U-9, U-23, U-24 or U-25.
其中特別佳為如下所示之組態：
進一步較佳具體實施例中，本發明係有關一種式(IB)化合物，其中U代表U-2、U-5、U-9、U-23、U-24或U-25。 In a further preferred embodiment, the invention relates to a compound of formula (IB) wherein U represents U-2, U-5, U-9, U-23, U-24 or U-25.
進一步較佳具體實施例中，本發明係有關一種式(IC)化合物，其中U代表U-2、U-5、U-9、U-23、U-24或U-25。 In a further preferred embodiment, the invention relates to a compound of formula (IC) wherein U represents U-2, U-5, U-9, U-23, U-24 or U-25.
其中特別佳為如下所示之組態：
進一步較佳具體實施例中，本發明係有關一種式(ID)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (ID).
進一步較佳具體實施例中，本發明係有關一種式(IE)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (IE).
進一步較佳具體實施例中，本發明係有關一種式(IF)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (IF).
進一步較佳具體實施例中，本發明係有關一種式(IG)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (IG).
進一步較佳具體實施例中，本發明係有關一種式(IH)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (IH).
進一步較佳具體實施例中，本發明係有關一種式(IJ)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (IJ).
上述具體實施例(IA)至(IJ)中，較佳係指下列：IA、IC、ID、IE、IF。 In the above specific examples (IA) to (IJ), the following are preferred: IA, IC, ID, IE, IF.
上述具體實施例(IA)至(IJ)中，特別佳係指下列：IA、ID、IE、IF。 Among the above specific examples (IA) to (IJ), particularly preferred are the following: IA, ID, IE, IF.
上述具體實施例(IA)至(IJ)中，極特別佳係指下列：ID、IE、IF。 Of the above specific examples (IA) to (IJ), very particularly preferred are the following: ID, IE, IF.
進一步較佳具體實施例中，本發明係有關一種式(I-2)化合物。 In a further preferred embodiment, the invention relates to a compound of formula (I-2).
此具體實施例(I-2)中，結構元素U、G、Q與Y係如上述組態(1-1)或組態(2-1)或組態(2-2)或組態(3-1)或組態(3-2)或組態(4-1)或組態(4-2)或組態(5-1)或組態(5-2)或組態(5-3)中之相同定義，除非另有說明。T2中，適用組態(2-1)中說明之定義，其係與其他結構元素之定義分別獨立。式(I-2)中，U較佳代表U-2、U-5、U-9、U-23、U-24或U-25。 In this embodiment (I-2), the structural elements U, G, Q and Y are as described above (1-1) or configured (2-1) or configured (2-2) or configured ( 3-1) or configuration (3-2) or configuration (4-1) or configuration (4-2) or configuration (5-1) or configuration (5-2) or configuration (5- The same definition in 3) unless otherwise stated. In T 2 , the definitions described in Configuration (2-1) apply, which are independent of the definitions of other structural elements. In the formula (I-2), U preferably represents U-2, U-5, U-9, U-23, U-24 or U-25.
其中特別佳為如下所示之組態：
進一步較佳具體實施例中，本發明係有關一種式(I-2)化合物，其中所有結構元素均如上述組態(1-1)或組態(2-1)或組態(2-2)或組態(3-1)或組態(3-2)或組態(4-1)或組態(4-2)或組態(5-1)或組態(5-3)中之相同定義，除非另有說明。T2中，若T2沒有明確定義時，則適用T之定義，此時例如：與組態(1-1)相關。此等化合物中，式(I-2)中之U較佳代表U-2、U-5、U-9、U-23、U-24或U-25。 In a further preferred embodiment, the invention relates to a compound of formula (I-2) wherein all structural elements are as configured (1-1) or configured (2-1) or configured (2-2) ) or configuration (3-1) or configuration (3-2) or configuration (4-1) or configuration (4-2) or configuration (5-1) or configuration (5-3) The same definition, unless otherwise stated. In T 2 , if T 2 is not clearly defined, the definition of T is applied, for example, related to configuration (1-1). Among these compounds, U in the formula (I-2) preferably represents U-2, U-5, U-9, U-23, U-24 or U-25.
其中特別佳為如下所示之組態：
同樣較佳之根據本發明化合物為表1中所示之通式(I)化合物。 Also preferred are the compounds of the formula (I) shown in Table 1 according to the invention.
上述結構元素之一般或較佳定義適用於所有式(I)化合物及對應之起始物與中間物。此等定義可依需要彼此組合，亦即包括個別較佳範圍之間之組合。 The general or preferred definitions of the above structural elements apply to all compounds of formula (I) and the corresponding starting materials and intermediates. These definitions can be combined with each other as desired, that is, including combinations of individual preferred ranges.
根據本發明較佳為其中組合上述較佳定義之式(I)化合物，且上述每一項較佳具體實施例均構成獨立組合，特定言之如具體實施例2-1或具體實施例2-2中說明之組合。 Preferably, in accordance with the present invention, a compound of formula (I) in combination with the above-described preferred definition is combined, and each of the above preferred embodiments constitutes an independent combination, in particular, as in embodiment 2-1 or embodiment 2 The combination described in 2.
根據本發明進一步較佳為其中組合上述進一步較佳定義之式(I)化合物，且上述每一項進一步較佳具體實施例均構成獨立組合，特定言之如具體實施例3-1或具體實施例3-2中說明之組合。 Further preferred according to the present invention is a compound of the formula (I) in which the above further preferred definitions are combined, and each of the further preferred embodiments described above constitutes an independent combination, in particular as in the specific example 3-1 or in the specific embodiment. The combination illustrated in Example 3-2.
根據本發明特別佳為其中組合上述特別佳定義之式(I)化合物，且上述每一項特別佳具體實施例均構成獨立組合，特定言之如具體實施例4-1或具體實施例4-2中說明之組合。 Particularly preferred according to the invention are the compounds of the formula (I) in which the above-mentioned particularly preferred definitions are combined, and each of the above-mentioned particularly preferred embodiments constitutes an independent combination, in particular as in the specific example 4-1 or in the specific example 4 The combination described in 2.
根據本發明極特別佳為其中組合上述極特別佳定義之式(I)化合物，且上述每一項極特別佳具體實施例均構成獨立組合，特定言之如具體實施例5-1或具體實施例5-2或具體實施例5-3中說明之組合。 Very particularly preferred according to the invention are the compounds of the formula (I) in which the above-mentioned very particularly preferred definitions are combined, and each of the above-mentioned very particularly preferred embodiments constitutes an independent combination, in particular as embodied in specific examples 5-1 or embodied The combination illustrated in Example 5-2 or Specific Example 5-3.
可視需要經取代之基團可經單取代或多取代，其中經多取代時之取代基可相同或相異。 The group which may be optionally substituted may be mono- or poly-substituted, and the substituents upon multi-substitution may be the same or different.
依據取代基之性質，式(I)化合物亦可能呈立體異構型，亦即幾何異構型與/或光學異構型物或不同組成之異構物混合物型式。本發明同時提 供純立體異構物與此等異構物之任何所需混合物，即使本文中通常僅以式(I)化合物討論。 Depending on the nature of the substituents, the compounds of formula (I) may also be in stereoisomeric form, ie geometrically isomeric and/or optically isomeric or isomeric mixtures of different compositions. The invention also mentions Any desired mixture of pure stereoisomers and such isomers, even though generally only discussed herein with a compound of formula (I).
然而，根據本發明較佳係使用式(I)化合物與其鹽類之光學活性立體異構型。 However, it is preferred according to the invention to use optically active stereoisomers of the compounds of formula (I) and their salts.
本發明因此係同時有關純對映異構物與非對映異構物，及其混合物，用於控制動物害蟲，包括節肢動物，特定言之昆蟲。 The invention thus relates to both pure enantiomers and diastereomers, and mixtures thereof, for controlling animal pests, including arthropods, in particular insects.
若適當時，式(I)化合物可呈各種不同多晶型或各種不同多晶型之混合物。本發明同時提供純的多晶型與多晶型混合物，且均可依據本發明使用。 Where appropriate, the compounds of formula (I) may be in a mixture of various polymorphs or of various polymorphs. The present invention provides both a pure polymorphic and polymorphic mixture and can be used in accordance with the present invention.
本發明內容中，除非另有不同定義，否則術語「烷基」不論本身或與其他術語組合，例如：鹵烷基，咸瞭解係指具有1至12個碳原子且可能為分支或未分支之飽和脂系烴基。C1-C12-烷基實例為甲基、乙基、正丙基、異丙基、正丁基、異丁基、第二丁基、第三丁基、正戊基、異戊基、新戊基、第三戊基、1-甲基丁基、2-甲基丁基、1-乙基丙基、1,2-二甲基丙基、己基、正庚基、正辛基、正壬基、正癸基、正十一碳烷基與正十二碳烷基。此等烷基中，特別佳係指C1-C6-烷基。尤其佳係指C1-C4-烷基。 In the context of the present invention, the term " alkyl ", whether by itself or in combination with other terms, such as haloalkyl, is understood to mean having from 1 to 12 carbon atoms and possibly branched or unbranched, unless otherwise defined. Saturated aliphatic hydrocarbon group. Examples of C 1 -C 12 -alkyl are methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, t-butyl, tert-butyl, n-pentyl, isopentyl, Neopentyl, third amyl, 1-methylbutyl, 2-methylbutyl, 1-ethylpropyl, 1,2-dimethylpropyl, hexyl, n-heptyl, n-octyl, N-decyl, n-decyl, n-undecyl and n-dodecyl. Of these alkyl groups, particularly preferred is C 1 -C 6 -alkyl. Particularly preferred is C 1 -C 4 -alkyl.
根據本發明，除非另有不同定義，否則術語「烯基」不論本身或與其他術語組合，咸瞭解係指具有至少一個雙鍵之直鏈或未分支之C2-C12-烯基，例如：乙烯基、烯丙基、1-丙烯基、異丙烯基、1-丁烯基、2-丁烯基、3-丁烯基、1,3-丁二烯基、1-戊烯基、2-戊烯基、3-戊烯基、4-戊烯基、1,3-戊二烯基、1-己烯基、2-己烯基、3-己烯基、4-己烯基、5-己烯基與1,4-己二烯基。其中較佳係指C2-C6-烯基，特別佳為C2-C4-烯基。 According to the present invention, unless otherwise defined differently, the term " alkenyl ", whether by itself or in combination with other terms, means a straight or unbranched C 2 -C 12 -alkenyl group having at least one double bond, for example : vinyl, allyl, 1-propenyl, isopropenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1,3-butadienyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1,3-pentadienyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl , 5-hexenyl and 1,4-hexadienyl. Preferred among these are C 2 -C 6 -alkenyl groups, particularly preferably C 2 -C 4 -alkenyl groups.
根據本發明，除非另有不同定義，否則術語「炔基」不論本身或與其他術語組合，咸瞭解係指具有至少一個參鍵之直鏈或未分支之C2-C12- 炔基，例如：乙炔基、1-丙炔基、與炔丙基。其中較佳係指C3-C6-炔基，特別佳為C3-C4-炔基。炔基亦可包含至少一個雙鍵。 According to the present invention, unless otherwise defined differently, the term " alkynyl ", whether by itself or in combination with other terms, refers to a straight or unbranched C 2 -C 12 -alkynyl group having at least one reference, for example : ethynyl, 1-propynyl, and propargyl. Preferred among them are C 3 -C 6 -alkynyl groups, and particularly preferably C 3 -C 4 -alkynyl groups. An alkynyl group can also contain at least one double bond.
根據本發明，除非另有不同定義，否則術語「環烷基」不論本身或與其他術語組合，咸瞭解係指C3-C8-環烷基，例如：環丙基、環丁基、環戊基、環己基、環庚基與環辛基。其中較佳係指C3-C6-環烷基。 According to the invention, unless otherwise defined differently, the term " cycloalkyl ", whether by itself or in combination with other terms, means C 3 -C 8 -cycloalkyl, for example: cyclopropyl, cyclobutyl, ring. Pentyl, cyclohexyl, cycloheptyl and cyclooctyl. Of these, it preferably means a C 3 -C 6 -cycloalkyl group.
根據本發明，除非另有不同定義，否則術語「芳基」咸瞭解係指具有6至14個碳原子之芳香系基團。較佳為苯基、萘基、蒽基或菲基，更佳為苯基。 According to the present invention, the term " aryl " is understood to mean an aromatic group having 6 to 14 carbon atoms unless otherwise defined. Phenyl, naphthyl, anthracenyl or phenanthryl is preferred, and phenyl is more preferred.
除非另有不同定義，否則術語「芳基烷基」咸瞭解係指根據本發明基團「芳基」與「烷基」定義之組合，其中該基團一般係利用烷基附接。此等實例為苯甲基、苯基乙基或α-甲基苯甲基，以苯甲基特別佳。 Unless otherwise defined differently, the term " arylalkyl " is used in the context of the definition of the group "aryl" and "alkyl" according to the invention, wherein the group is typically attached using an alkyl group. These examples are benzyl, phenylethyl or alpha-methylbenzyl, especially preferably benzyl.
除非另有不同定義，否則術語「雜芳基」係指碳原子與至少一個雜原子之單環、二環或三環雜環基團，其中至少一個環為芳香系。較佳係雜芳基包含3、4、5或6個碳原子，其係選自以下基團：呋喃基、噻吩基、吡咯基、吡唑基、咪唑基、1,2,3-三唑基、1,2,4-三唑基、唑基、異唑基、噻唑基、異噻唑基、1,2,3-二唑基、1,2,4-二唑基、1,3,4-二唑基、1,2,5-二唑基、1,2,3-噻二唑基、1,2,4-噻二唑基、1,3,4-噻二唑基、1,2,5-噻二唑基、吡啶基、嘧啶基、噠嗪基、吡嗪基、1,2,3-三嗪基、1,2,4-三嗪基、1,3,5-三嗪基、苯并呋喃基、苯并異呋喃基、苯并噻吩基、苯并異噻吩基、吲哚基、異吲哚基、吲唑基、苯并噻唑基、苯并異噻唑基、苯并唑基、苯并異唑基、苯并咪唑基、2,1,3-苯并二唑、喹啉基、異喹啉基、噌啉基、酞嗪基、喹唑啉基、喹喔啉基、萘啶基、苯并三嗪基、嘌呤基、蝶啶基與吲哚嗪基。 Unless otherwise defined differently, the term " heteroaryl " refers to a monocyclic, bicyclic or tricyclic heterocyclic group of a carbon atom and at least one heteroatom, at least one of which is aromatic. Preferably, the heteroaryl group contains 3, 4, 5 or 6 carbon atoms selected from the group consisting of furyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, 1,2,3-triazole Base, 1,2,4-triazolyl, Azolyl, different Azyl, thiazolyl, isothiazolyl, 1,2,3- Diazolyl, 1,2,4- Diazolyl, 1,3,4- Diazolyl, 1, 2, 5- Diazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,5-thiadiazolyl, pyridyl , pyrimidinyl, pyridazinyl, pyrazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, benzofuranyl, benziso Furanyl, benzothienyl, benzisothienyl, fluorenyl, isodecyl, oxazolyl, benzothiazolyl, benzisothiazolyl, benzo Azolyl, benzopyrene Azolyl, benzimidazolyl, 2,1,3-benzo Diazole, quinolyl, isoquinolyl, porphyrinyl, pyridazinyl, quinazolinyl, quinoxalinyl, naphthyridinyl, benzotriazinyl, fluorenyl, pteridinyl and pyridazine base.
除非另有不同定義，否則術語「雜環基」係指單環之飽和或部份 飽和4-、5-、6-或7-員環，環中包含碳原子與至少一個雜原子。較佳係該雜環基包含3、4、5或6個碳原子與1或2個選自氧、硫與氮所組成群中之雜原子。雜環基實例為氮雜環丁烷基、唑啶基(azolidinyl)、氮雜環己烷基(azinayl)、氧雜環丁烷基(oxetanyl)、氧雜環戊烷基(oxolanyl)、氧雜環己烷基(oxanyl)、二氧雜環己烷基、硫雜環丁烷(thietanyl)、硫雜環戊烷基(thiolanyl)、硫雜環己烷基(thianyl)與四氫呋喃基。 Unless otherwise defined differently, the term " heterocyclyl " refers to a saturated or partially saturated 4-, 5-, 6- or 7-membered ring of a single ring containing a carbon atom and at least one heteroatom. Preferably, the heterocyclic group contains 3, 4, 5 or 6 carbon atoms and 1 or 2 hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen. Examples of heterocyclic groups are azetidinyl, azolidinyl, azinayl, oxetanyl, oxolanyl, oxygen. Oxanyl, dioxanyl, thietanyl, thiolanyl, thianyl and tetrahydrofuranyl.
除非另有不同定義，否則術語「側氧基雜環基」與「二側氧基雜環基」係指雜環基在環中至少一個位置上包含一個分別經一個與兩個(=O)基團取代之環原子。較佳係雜原子(例如：硫)經一個或兩個(=O)基團取代，分別產生-S(=O)-與-S(=O)2-基團，其中硫原子為環之組成原子。 Unless otherwise defined, the terms " sideoxyheterocyclyl " and " bilateral oxyheterocyclyl " mean that the heterocyclyl contains one or two (=O) at least one position in the ring. A ring atom substituted by a group. Preferably, a hetero atom (eg, sulfur) is substituted with one or two (=O) groups to give -S(=O)- and -S(=O) 2 - groups, respectively, wherein the sulfur atom is a ring Make up the atom.
本發明內容中，經鹵素取代之基團，例如：「鹵烷基」，咸瞭解係指經鹵素單取代或多取代之基團，其最多可達最高取代基數量。若經多鹵化時，該等鹵原子可相同或相異。此時，「鹵素」代表氟、氯、溴或碘，較佳為氟或氯。 In the context of the present invention, a halogen-substituted group, for example, " haloalkyl ", is used to mean a group which is mono- or polysubstituted by halogen, up to the highest number of substituents. If polyhalogenated, the halogen atoms may be the same or different. In this case, "halogen" represents fluorine, chlorine, bromine or iodine, preferably fluorine or chlorine.
術語「烷氧基」不論本身或與其他術語組合，例如：鹵烷氧基，在本例中咸瞭解係指O-烷基，其中術語「烷基」係如上述定義。 The term " alkoxy ", whether by itself or in combination with other terms, such as haloalkoxy, is used in this context to mean O-alkyl, wherein the term "alkyl" is as defined above.
式(I-1)中A代表氧之化合物可採用例如：製程A製備。 A compound of the formula (I-1) wherein A represents oxygen can be produced, for example, by Process A.
步驟a)Step a)
式(IV)化合物可自商品取得或可類似Journal of Organic Chemistry,51(1986),263-265；Organic Synthesis,34(1954),26-29；Tetrahedron,57(2001),2781-2786與Journal of the American Chemical Society,114(1992),3441-3445中說明之製法，由式(II)化合物與合適之醇於酸性或加熱條件下反應或經由形成活性酯中間物來製備。 The compound of formula (IV) is commercially available or can be similar to Journal of Organic Chemistry, 51 (1986), 263-265; Organic Synthesis, 34 (1954), 26-29; Tetrahedron, 57 (2001), 2781-2786 and Journal. The process described in the American Chemical Society, 114 (1992), 3441-3445, is prepared by reacting a compound of formula (II) with a suitable alcohol under acidic or heated conditions or by forming an active ester intermediate.
步驟b)Step b)
式(VI)化合物可類似Angewandte Chemie,International Edition,51(2012),1028-1032；Chemistry-A European Journal,10(2004),5607-5622；US2010/0069440與Journal of Organic Chemistry,67(2002),541-555中說明之製法，由式(IV)化合物與化合物(V)於鹼性銅催化之條件下反應來製備。 The compound of formula (VI) can be similar to Angewandte Chemie, International Edition, 51 (2012), 1028-1032; Chemistry-A European Journal, 10 (2004), 5607-5622; US2010/0069440 and Journal of Organic Chemistry, 67 (2002). The process described in 541-555 is prepared by reacting a compound of the formula (IV) with a compound (V) under the conditions of basic copper catalysis.
步驟c)Step c)
式(VII)化合物可類似WO2008/150487；Tetrahedron Letters,49(2008),4434-4436；Journal of Organic Chemistry,65(2000),5834-5836與US2001/6300499中說明之製法，使用一當量鹼水解式(VI)化合物來製備。 或者，式(VII)化合物可自商品取得，例如：3-苯甲基氧-3-側氧基-2-苯基丙酸、3-(2-乙氧基-1-甲基-2-側氧基乙氧基)-3-側氧基-2-苯基丙酸、3-(環己氧基)-3-側氧基-2-苯基丙酸與3-(2-乙氧基-2-側氧基-1-苯基乙氧基)-3-側氧基-2-苯基丙酸。 The compound of formula (VII) can be similar to the process described in WO 2008/150487; Tetrahedron Letters, 49 (2008), 4434-4436; Journal of Organic Chemistry, 65 (2000), 5834-5836 and US2001/6300499, using one equivalent of base hydrolysis. The compound of formula (VI) is prepared. Alternatively, a compound of formula (VII) can be obtained from the commercial product, for example: 3-benzyloxy-3-oxo-2-phenylpropionic acid, 3-(2-ethoxy-1-methyl-2- Oxyoxyethoxy)-3-oxo-2-phenylpropionic acid, 3-(cyclohexyloxy)-3-oxo-2-phenylpropionic acid and 3-(2-ethoxyl) Keto-2-oxo-1-phenylethoxy)-3-oxo-2-phenylpropionic acid.
步驟d)Step d)
式(VIII)化合物可類似CN2013/103159672；Organic & Biomolecular Chemistry,12(2014),8386-8389；Organic & Biomolecular Chemistry,12(2014),9822-9830與Chemical & Pharmaceutical Bulletin,33(1985),61-66中說明之製法，由式(VII)化合物與氯化劑(如，例如：草醯氯、亞硫醯氯、或磷醯氯)反應來製備。 The compound of formula (VIII) can be similar to CN 2013/103159672; Organic & Biomolecular Chemistry, 12 (2014), 8386-8389; Organic & Biomolecular Chemistry, 12 (2014), 9822-9830 and Chemical & Pharmaceutical Bulletin, 33 (1985), 61 The process described in -66 is prepared by reacting a compound of formula (VII) with a chlorinating agent such as, for example, chloroform, sulfoxide, or phosphonium chloride.
步驟e)Step e)
式(I)化合物可類似Helvetica Chimica Acta,96(2013),2160-2172；Organic Letters,11(2009),2820-2823；WO2011/024872與US2007/0249596中說明之製法，由式(VIII)化合物與式(IX)胺於鹼性或酸性條件下反應來製備。 The compound of formula (I) can be similar to the process described in Helvetica Chimica Acta, 96 (2013), 2160-2172; Organic Letters, 11 (2009), 2820-2823; WO2011/024872 and US2007/0249596, from the compound of formula (VIII) It is prepared by reacting an amine of the formula (IX) under basic or acidic conditions.
式(IX)胺可自商品取得，例如：N-[(6-氯-3-吡啶基)甲基]吡啶-2-胺、N-(嘧啶-5-基甲基)吡啶-2-胺、N-[(2-氯噻唑-5-基)甲基]吡啶-2-胺與N-[(2-氯噻唑-5-基)甲基]-3-甲基吡啶-2-胺，或可類似文獻中已知之製法製備(參見例如：Medicinal Chemistry Research,23(2014),5043-5057；WO2009/099929、WO2011/017351或WO2012/092115)。 The amine of formula (IX) is commercially available, for example: N-[(6-chloro-3-pyridyl)methyl]pyridin-2-amine, N-(pyrimidin-5-ylmethyl)pyridin-2-amine , N-[(2-chlorothiazol-5-yl)methyl]pyridin-2-amine and N-[(2-chlorothiazol-5-yl)methyl]-3-methylpyridin-2-amine, Alternatively, it can be prepared by a method known in the literature (see, for example, Medicinal Chemistry Research, 23 (2014), 5043-5057; WO2009/099929, WO2011/017351 or WO2012/092115).
或者，可能在製程A中成為中間物出現之式(VII)化合物可類似下文中說明之製法製備。 Alternatively, a compound of formula (VII) which may be present as an intermediate in Process A may be prepared analogously to the processes described below.
步驟a)Step a)
式(XI)化合物可類似Angewandte Chemie,International Edition,51(2012),1028-1032；Chemistry-A European Journal,10(2004),5607-5622；US2010/0069440與Journal of Organic Chemistry,67(2002),541-555中說明之製法，由式(X)化合物與化合物(V)於鹼性銅催化之條件下反應來製備。 The compound of formula (XI) can be similar to Angewandte Chemie, International Edition, 51 (2012), 1028-1032; Chemistry-A European Journal, 10 (2004), 5607-5622; US2010/0069440 and Journal of Organic Chemistry, 67 (2002). The process described in 541-555 is prepared by reacting a compound of the formula (X) with a compound (V) under the conditions of basic copper catalysis.
步驟b)Step b)
式(XII)化合物可類似WO2008/150487；Tetrahedron Letters,49(2008),4434-4436；Journal of Organic Chemistry,65(2000),5834-5836與US2001/6300499中說明之製法，由式(XI)化合物於酸性或鹼性條件下水解來製備。 The compound of the formula (XII) can be similar to the process described in WO 2008/150487; Tetrahedron Letters, 49 (2008), 4434-4436; Journal of Organic Chemistry, 65 (2000), 5834-5836 and US2001/6300499, by formula (XI) The compound is prepared by hydrolysis under acidic or basic conditions.
或者，式(XII)化合物可自商品取得，例如：2-(3-甲氧基苯基)丙二酸、2-苯基丙二酸、2-(4-甲氧基苯基)丙二酸、2-[3-(三氟甲基)苯基]丙二酸、2-(4-氯苯基)丙二酸、2-(2-氯苯基)丙二酸與2-[2-硝基-4-(三氟甲基)苯基]丙二酸。 Alternatively, the compound of the formula (XII) can be obtained from a commercial product, for example: 2-(3-methoxyphenyl)malonic acid, 2-phenylmalonic acid, 2-(4-methoxyphenyl)propane Acid, 2-[3-(trifluoromethyl)phenyl]malonic acid, 2-(4-chlorophenyl)malonic acid, 2-(2-chlorophenyl)malonic acid and 2-[2 -Nitro-4-(trifluoromethyl)phenyl]malonic acid.
步驟c)Step c)
式(VII)化合物可類似Organic Letters,4(2002),1415-1418；Journal of Organic Chemistry,54(1989),5395-5397；Bioorganic & Medicinal Chemistry,13(2003),2659-2662與Synthetic Communications,44(2014),275-279中說明之製法，由 式(XII)化合物與約一當量式(T1)-OH適當醇於酸性或加熱條件下反應或經由形成活性酯中間物來製備。 The compound of formula (VII) can be similar to Organic Letters, 4 (2002), 1415-1418; Journal of Organic Chemistry, 54 (1989), 5395-5397; Bioorganic & Medicinal Chemistry, 13 (2003), 2659-2662 and Synthetic Communications, 44 (2014), 275-279 described the production method, a compound of formula (XII) and about one equivalent of formula (T 1) -OH in the reaction of the appropriate alcohol under acidic conditions or by heating or prepared via formation of the active ester intermediate.
或者，式(I-1)中A代表氧之化合物亦可採用製程B製備。 Alternatively, a compound of formula (I-1) wherein A represents oxygen can also be prepared by Process B.
步驟a)Step a)
式(XIV)化合物可類似WO2010/057121；Journal of Medicinal Chemistry,54(2011),3348-3359；Helvetica Chimica Acta,96(2013),2160-2172與Organic Letters,11(2009),2820-2823中說明之製法，由化合物(XIII)與式(IX)胺反應來製備。 The compound of formula (XIV) can be similar to WO 2010/057121; Journal of Medicinal Chemistry, 54 (2011), 3348-3359; Helvetica Chimica Acta, 96 (2013), 2160-2172 and Organic Letters, 11 (2009), 2820-2823 The preparation method is prepared by reacting a compound (XIII) with an amine of the formula (IX).
步驟b)Step b)
式(XV)化合物可類似WO2008/150487；Tetrahedron Letters,49(2008),4434-4436；Journal of Organic Chemistry,65(2000),5834-5836與US2001/6300499中說明之製法，由式(XIV)化合物於酸性或鹼性條件下水解來製備。 The compound of the formula (XV) can be similar to the process described in WO 2008/150487; Tetrahedron Letters, 49 (2008), 4434-4436; Journal of Organic Chemistry, 65 (2000), 5834-5836 and US2001/6300499, by the formula (XIV) The compound is prepared by hydrolysis under acidic or basic conditions.
步驟c)Step c)
式(XVI)化合物可類似Organic Letters,4(2002),1415-1418；Journal of Organic Chemistry,54(1989),5395-5397；Bioorganic & Medicinal Chemistry,13(2003),2659-2662與Synthetic Communications,44(2014),275-279中說明之製法，由式(XV)化合物與式(T1)-OH適當醇於酸性或加熱條件下反應或經由形成活性酯中間物來製備。 The compound of formula (XVI) can be similar to Organic Letters, 4 (2002), 1415-1418; Journal of Organic Chemistry, 54 (1989), 5395-5397; Bioorganic & Medicinal Chemistry, 13 (2003), 2659-2662 and Synthetic Communications, 44 (2014), 275-279 described the preparation method, the formula (XV) with a compound of formula (T 1) -OH in the reaction of the appropriate alcohol under acidic conditions or by heating or prepared via formation of the active ester intermediate.
步驟d)Step d)
式(I-1)化合物可類似Angewandte Chemie,International Edition,51(2012),1028-1032；Chemistry-A European Journal,10(2004),5607-5622；US2010/0069440與Journal of Organic Chemistry,67(2002),541-555中說明之製法，由式(XVI)化合物與一化合物於鹼性銅催化之條件下反應來製備。 The compound of the formula (I-1) can be similar to Angewandte Chemie, International Edition, 51 (2012), 1028-1032; Chemistry-A European Journal, 10 (2004), 5607-5622; US2010/0069440 and Journal of Organic Chemistry, 67 ( 2002), the process described in 541-555, prepared by reacting a compound of formula (XVI) with a compound under basic copper catalysis.
式(I-2)中A代表硫之化合物可採用例如：製程C製備。 The compound of the formula (I-2) wherein A represents sulfur can be produced, for example, by Process C.
步驟a)Step a)
式(XVIII)化合物可類似Chemical Communications,48(2012),142-144；Organic Letters,11(2009),5630-5633與Journal of the American Chemical Society,116(1994),73-81中說明之製法，由式(XVII)經適當取代之芳基乙腈之2-位置使用二氧化碳進行羧酸化來製備。 The compound of formula (XVIII) can be similar to that described in Chemical Communications, 48 (2012), 142-144; Organic Letters, 11 (2009), 5630-5633 and Journal of the American Chemical Society, 116 (1994), 73-81. It is prepared by the carboxylation of carbon dioxide from the 2-position of the appropriately substituted aryl acetonitrile of the formula (XVII).
步驟b)、c)Steps b), c)
式(XIX)化合物可類似CN2013/103159672；Organic & Biomolecular Chemistry,12(2014),8386-8389；Organic & Biomolecular Chemistry,12(2014),9822-9830與Chemical & Pharmaceutical Bulletin,33(1985),61-66；Helvetica Chimica Acta,96(2013),2160-2172；Organic Letters,11(2009),2820-2823；WO2011/024872與US2007/0249596中說明之製法，由式(XVIII)羧酸轉化成相應之醯基鹵化物，然後於鹼(如，例如：三乙基胺或N,N-二甲基胺基吡啶)之存在下，轉化成羧醯胺。 The compound of formula (XIX) can be similar to CN 2013/103159672; Organic & Biomolecular Chemistry, 12 (2014), 8386-8389; Organic & Biomolecular Chemistry, 12 (2014), 9822-9830 and Chemical & Pharmaceutical Bulletin, 33 (1985), 61 -66; Helvetica Chimica Acta, 96 (2013), 2160-2172; Organic Letters, 11 (2009), 2820-2823; WO2011/024872 and US2007/0249596, the conversion of the carboxylic acid of formula (XVIII) to the corresponding The sulfhydryl halide is then converted to the carboxamide in the presence of a base such as, for example, triethylamine or N , N -dimethylaminopyridine.
步驟d)Step d)
式(I-2)化合物可類似Synthesis,10(1993),964與WO2012/137982中說明之製法，由式(XIX)腈類與適當之式(XX)硫醇，於合適之布忍斯特(Brnsted)酸或路易士(Lewis)酸(如，例如：鹽酸或AlCl3)之存在下，於無水條件下反應。 The compound of the formula (I-2) can be similar to the process described in Synthesis, 10 (1993), 964 and WO2012/137982, from the nitrile of the formula (XIX) and the appropriate thiol of the formula (XX), in the suitable Brent ( Br The reaction is carried out under anhydrous conditions in the presence of nsted acid or Lewis acid (for example, hydrochloric acid or AlCl 3 ).
步驟a)Step a)
式(XI)化合物可類似Angewandte Chemie,International Edition,51(2012),1028-1032；Chemistry-A European Journal,10(2004),5607-5622；US2010/0069440與Journal of Organic Chemistry,67(2002),541-555中說明之製法，由式(X)化合物與化合物(V)於鹼性銅催化之條件下反應來製備。 The compound of formula (XI) can be similar to Angewandte Chemie, International Edition, 51 (2012), 1028-1032; Chemistry-A European Journal, 10 (2004), 5607-5622; US2010/0069440 and Journal of Organic Chemistry, 67 (2002). The process described in 541-555 is prepared by reacting a compound of the formula (X) with a compound (V) under the conditions of basic copper catalysis.
步驟b)Step b)
式(XII)化合物可類似WO2008/150487；Tetrahedron Letters,49(2008),4434-4436；Journal of Organic Chemistry,65(2000),5834-5836與US2001/6300499中說明之製法，由式(XI)化合物於酸性或鹼性條件下水解來製備。 The compound of the formula (XII) can be similar to the process described in WO 2008/150487; Tetrahedron Letters, 49 (2008), 4434-4436; Journal of Organic Chemistry, 65 (2000), 5834-5836 and US2001/6300499, by formula (XI) The compound is prepared by hydrolysis under acidic or basic conditions.
步驟c)Step c)
式(XXI)化合物可類似Organic & Biomolecular Chemistry,11(2013),4449-4458；Biochemistry,51(2012),4568-4579；Nature Chemical Biology,10(2014),251-258與Journal of Organic Chemistry,78(2013),6412-6426中說明之製法，由式(XII)化合物與約一當量適當之式(T2)-OH硫醇，於酸性或加熱條件下反應或經由形成活性酯中間物來製備。 The compound of the formula (XXI) can be similar to Organic & Biomolecular Chemistry, 11 (2013), 4449-4458; Biochemistry, 51 (2012), 4568-4579; Nature Chemical Biology, 10 (2014), 251-258 and Journal of Organic Chemistry, 78 (2013), the method described in 6412-6426, by reacting a compound of the formula (XII) with about one equivalent of the appropriate formula (T 2 )-OH thiol under acidic or heated conditions or by forming an active ester intermediate. preparation.
或者，式(I-2)中A代表硫之化合物亦可採用製程B製備。 Alternatively, a compound of the formula (I-2) wherein A represents sulfur can also be produced by Process B.
步驟d)Step d)
式(XXII)化合物可類似CN2013/103159672；Organic & Biomolecular Chemistry,12(2014),8386-8389；Organic & Biomolecular Chemistry,12(2014),9822-9830與Chemical & Pharmaceutical Bulletin,33(1985),61-66中說明之製法，由式(XXI)化合物與氯化劑(如，例如：草醯氯、亞硫醯氯、或磷醯氯)反應來製備。 The compound of formula (XXII) can be similar to CN 2013/103159672; Organic & Biomolecular Chemistry, 12 (2014), 8386-8389; Organic & Biomolecular Chemistry, 12 (2014), 9822-9830 and Chemical & Pharmaceutical Bulletin, 33 (1985), 61 The process described in -66 is prepared by reacting a compound of formula (XXI) with a chlorinating agent such as, for example, chloroform, sulfoxide, or phosphonium chloride.
步驟e)Step e)
式(I-2)化合物可類似Helvetica Chimica Acta,96(2013),2160-2172；Organic Letters,11(2009),2820-2823、WO2011/024872與US2007/0249596中說明之製法，由式(XXII)化合物與式(IX)胺，於鹼性或酸性條件下反應來製備。 The compound of the formula (I-2) can be similar to the method described in Helvetica Chimica Acta, 96 (2013), 2160-2172; Organic Letters, 11 (2009), 2820-2823, WO2011/024872 and US2007/0249596, by the formula (XXII) The compound is prepared by reacting an amine of the formula (IX) under basic or acidic conditions.
通常，式(I)化合物可採用上述製程製備。若無法採用上述製程製備個別化合物時，可能由其他式(I)化合物之衍化反應來合成，或個別修正上述製程來合成。可能宜例如：由其他式(I)化合物經過例如：水解、酯化、形成醯胺、還原、醚化、氧化、烯烴化、鹵化、醯化、烷化、與類似反應，製成某些式(I)化合物。 In general, the compound of formula (I) can be prepared by the above process. If it is not possible to prepare individual compounds by the above process, it may be synthesized by the derivatization reaction of other compounds of the formula (I), or may be separately modified to synthesize the above process. It may be desirable, for example, to form certain formulas from other compounds of formula (I) by, for example, hydrolysis, esterification, formation of decylamine, reduction, etherification, oxidation, olefination, halogenation, deuteration, alkylation, and the like. (I) a compound.
根據本發明製備該新穎式(I)化合物之方法較佳係使用稀釋劑進行。適用於進行根據本發明製法之稀釋劑為水及所有惰性溶劑。其等實例包括：鹵化烴類(例如：氫氯碳化物，如：四伸乙基(tetraethylene)、四氯乙烷、二氯丙烷、二氯甲烷、二氯丁烷、氯仿、四氯化碳、三氯乙烷、三氯乙烯、五氯乙烷、二氟苯、1,2-二氯乙烷、氯苯、溴苯、二氯苯、氯甲苯、三氯苯)、醇類(例如：甲醇、乙醇、異丙醇、丁醇)、醚類(例如：乙基丙基醚、甲基第三丁基醚、苯甲醚、苯乙醚、環己基甲基醚、二甲基醚、乙醚、二丙基醚、二異丙基醚、二正丁基醚、二異丁基醚、二異戊基醚、伸乙二醇二甲基醚、四氫呋喃、1,4-二烷、二氯乙醚、及環氧乙烷與/氧化丙烯之聚醚類)、胺類(例如：三甲基-、三乙基-、三丙基-與三丁基胺、N-甲基嗎啉、吡啶與四亞甲基二胺)、硝基烴類(例如：硝基甲烷、硝基乙烷、硝基丙烷、硝基苯、氯硝基苯、鄰硝基甲苯)；腈類(例如：乙腈、丙腈、丁腈、異丁腈、苯甲腈、間氯苯甲腈)、四氫噻吩二氧化物、二甲亞碸、四亞甲基亞碸、二丙基亞碸、苯甲基甲基亞碸、二異丁基亞碸、二丁基亞碸、二異戊基亞碸、碸類(例如：二甲基、二乙基、二丙基、二丁基、二苯基、二己基、甲基乙基、乙基丙基、乙基異丁基與五亞甲基碸)、脂系、環脂系或芳香系烴類(例 如：戊烷、己烷、庚烷、辛烷、壬烷與工業級烴類)、及其中組份之沸點在例如：40℃至250℃之亦稱為「石油精」者、傘花烴、沸點在70℃至190℃範圍內之輕油精餾份、環己烷、甲基環己烷、石油醚、石油英、辛烷、苯、甲苯、氯苯、溴苯、硝基苯、二甲苯、酯類(例如：乙酸甲酯、乙酯、丁酯與異丁酯、碳酸二甲酯、二丁酯與伸乙基酯)；醯胺類(例如：六亞甲基磷醯胺、甲醯胺、N-甲基甲醯胺、N,N-二甲基甲醯胺、N,N-二丙基甲醯胺、N,N-二丁基甲醯胺、N-甲基吡咯啶、N-甲基己內醯胺、1,3-二甲基-3,4,5,6-四氫-2(1H)-嘧啶、辛基吡咯啶酮、辛基己內醯胺、1,3-二甲基-2-咪唑啉二酮、N-甲醯基哌啶、N,N'-二甲醯基哌嗪)與酮類(例如：丙酮、苯乙酮、甲基乙基酮、甲基丁基酮)。 The process for the preparation of the novel compounds of the formula (I) according to the invention is preferably carried out using a diluent. Suitable diluents for carrying out the process according to the invention are water and all inert solvents. Examples thereof include: halogenated hydrocarbons (for example, hydrochlorocarbons such as tetraethylene, tetrachloroethane, dichloropropane, dichloromethane, dichlorobutane, chloroform, carbon tetrachloride) , trichloroethane, trichloroethylene, pentachloroethane, difluorobenzene, 1,2-dichloroethane, chlorobenzene, bromobenzene, dichlorobenzene, chlorotoluene, trichlorobenzene), alcohols (eg : methanol, ethanol, isopropanol, butanol), ethers (eg, ethyl propyl ether, methyl tert-butyl ether, anisole, phenethyl ether, cyclohexyl methyl ether, dimethyl ether, Ether, dipropyl ether, diisopropyl ether, di-n-butyl ether, diisobutyl ether, diisoamyl ether, ethylene glycol dimethyl ether, tetrahydrofuran, 1,4-two Alkane, dichloroethyl ether, and polyethers of ethylene oxide and / propylene oxide, amines (for example: trimethyl-, triethyl-, tripropyl- and tributylamine, N-methyl Morpholine, pyridine and tetramethylenediamine), nitrohydrocarbons (eg nitromethane, nitroethane, nitropropane, nitrobenzene, chloronitrobenzene, o-nitrotoluene); nitriles (eg acetonitrile, propionitrile, butyronitrile, isobutyronitrile, benzonitrile, m-chlorobenzonitrile), tetrahydrothiophene dioxide, dimethyl hydrazine, tetramethylene fluorene, dipropyl fluorene , benzylmethylhydrazine, diisobutyl fluorene, dibutyl fluorene, diisoamyl hydrazine, hydrazine (eg dimethyl, diethyl, dipropyl, dibutyl, Diphenyl, dihexyl, methylethyl, ethylpropyl, ethyl isobutyl and pentamethylene), aliphatic, cycloaliphatic or aromatic hydrocarbons (eg pentane, hexane, Heptan, octane, decane and industrial grade hydrocarbons, and their intermediate components have a boiling point of, for example, 40 ° C to 250 ° C, also known as "petroleum", cymene, boiling point of 70 ° C to 190 ° C Light oil fraction, cyclohexane, methylcyclohexane, petroleum , petroleum, octane, benzene, toluene, chlorobenzene, bromobenzene, nitrobenzene, xylene, esters (eg methyl acetate, ethyl ester, butyl ester and isobutyl ester, dimethyl carbonate, dibutyl Ester and ethyl ester); guanamines (eg hexamethylene phosphoniumamine, formamide, N-methylformamide, N,N-dimethylformamide, N,N-II Propylcarbamide, N,N-dibutylformamide, N-methylpyrrolidine, N-methylcaprolactam, 1,3-dimethyl-3,4,5,6-tetrahydro- 2(1H)-pyrimidine, octylpyrrolidone, octyl caprolactam, 1,3-dimethyl-2-imidazolidinone, N-methylhydrazine piperidine, N,N'-dimethyl Mercaptopiperazine and ketones (for example: acetone, acetophenone, methyl ethyl ketone, methyl butyl ketone).
根據本發明製程當然亦可能在上述溶劑與稀釋劑之混合物中進行。 The process according to the invention may of course also be carried out in a mixture of the abovementioned solvents and diluents.
當進行根據本發明製程時，反應溫度可在相當大範圍內變化。通常，該製程在-30℃至+150℃之溫度間進行，較佳在-10℃至+100℃之間。 When the process according to the invention is carried out, the reaction temperature can be varied within a relatively large range. Typically, the process is carried out at temperatures between -30 ° C and +150 ° C, preferably between -10 ° C and +100 ° C.
根據本發明製程通常在標準壓力下進行。然而，根據本發明製程亦可能在加壓或減壓下進行-通常在0.1巴至15巴之間之絕對壓力下進行。 The process according to the invention is generally carried out under standard pressure. However, the process according to the invention may also be carried out under elevated or reduced pressure - usually at an absolute pressure of between 0.1 and 15 bar.
為了進行根據本發明的製程，通常使用約等莫耳量之起始物。然而，其中一種組份之用量亦可能相當大幅超量。該反應通常在合適稀釋劑中，於反應助劑之存在下，可視需要亦在保護性氣體蒙氣下(例如：氮氣、氬氣或氦氣下)進行，反應混合物通常在所要求溫度下攪拌數小時。採用習知方法進行操作(參見製備實例)。 In order to carry out the process according to the invention, about a molar amount of starting material is usually used. However, the amount of one of the components may also be quite large. The reaction is usually carried out in a suitable diluent in the presence of a reaction auxiliary, optionally under a protective gas atmosphere (for example, under nitrogen, argon or helium), and the reaction mixture is usually stirred at the desired temperature. Hours. The operation is carried out by a conventional method (see Preparation Example).
用於進行根據本發明製程之鹼性反應助劑可為所有合適之酸結合劑。該等實例包括：鹼土金屬或鹼金屬化合物(例如：鋰、鈉、鉀、鎂、 鈣與鋇之氫氧化物、氫化物、氧化物與碳酸鹽)、脒鹼類或胍鹼類(例如：7-甲基-1,5,7-三氮雜雙環[4.4.0]癸-5-烯(MTBD)；二氮雜雙環[4.3.0]壬烯(DBN)、二氮雜雙環[2.2.2]辛烷(DABCO)、1,8-二氮雜雙環[5.4.0]十一碳烯(DBU)、環己基四丁基胍(CyTBG)、環己基四甲基胍(CyTMG)、N,N,N,N-四甲基-1,8-萘二胺、五甲基哌啶)與胺類，尤指三級胺類(例如：三乙基胺、三甲基胺、三苯甲基胺、三異丙基胺、三丁基胺、三環己基胺、三戊基胺、三己基胺、N,N-二甲基苯胺、N,N-二甲基甲苯胺、N,N-二甲基-對-胺基吡啶、N-甲基吡咯啶、N-甲基哌啶、N-甲基咪唑、N-甲基吡唑、N-甲基嗎啉、N-甲基六亞甲基二胺、吡啶、4-吡咯啶并吡啶、4-二甲基胺基吡啶、喹啉、α-甲基吡啶、ß-甲基吡啶、嘧啶、吖啶、N,N,N’,N’-四亞甲基二胺、N,N,N’,N’-四伸乙基二胺、喹喔啉、N-丙基二異丙基胺、N-乙基二異丙基胺、N,N’-二甲基環己基胺、2,6-二甲基吡啶、2,4-二甲基吡啶或三乙基二胺)。 The basic reaction auxiliaries used to carry out the process according to the invention may be all suitable acid binders. Examples include: alkaline earth metals or alkali metal compounds (eg lithium, sodium, potassium, magnesium, Calcium and barium hydroxides, hydrides, oxides and carbonates, sulfonates or sulfonates (eg 7-methyl-1,5,7-triazabicyclo[4.4.0]癸- 5-ene (MTBD); diazabicyclo[4.3.0]nonene (DBN), diazabicyclo[2.2.2]octane (DABCO), 1,8-diazabicyclo[5.4.0] Undecene (DBU), cyclohexyltetrabutylphosphonium (CyTBG), cyclohexyltetramethylguanidine (CyTMG), N,N,N,N-tetramethyl-1,8-naphthalenediamine, Wujia A piperidine) and an amine, especially a tertiary amine (eg triethylamine, trimethylamine, tritylamine, triisopropylamine, tributylamine, tricyclohexylamine, three) Amylamine, trihexylamine, N,N-dimethylaniline, N,N-dimethyltoluidine, N,N-dimethyl-p-aminopyridine, N-methylpyrrolidine, N- Methylpiperidine, N-methylimidazole, N-methylpyrazole, N-methylmorpholine, N-methylhexamethylenediamine, pyridine, 4-pyrrolidinopyridine, 4-dimethyl Aminopyridine, quinoline, α-methylpyridine, ß-methylpyridine, pyrimidine, acridine, N,N,N',N'-tetramethylenediamine, N,N,N',N' - tetraethylamine, quinoxaline, N-propyldiisopropylamine, N-ethyldiisopropylamine , N,N'-dimethylcyclohexylamine, 2,6-lutidine, 2,4-dimethylpyridine or triethyldiamine).
用於進行根據本發明製程之酸性反應助劑包括所有礦物酸類(例如：氫鹵酸類，如：氫氟酸、氫氯酸、氫溴酸、或氫碘酸，亦指硫酸、磷酸、亞磷酸、硝酸)、路易士酸(例如：氯化鋁(III)、三氟化硼或其醚合物、氯化鈦(IV)、氯化錫(IV))與有機酸類(例如：甲酸、乙酸、丙酸、丙二酸、乳酸、草酸、富馬酸、己二酸、硬脂酸、酒石酸、油酸、甲烷磺酸、苯甲酸、苯磺酸或對甲苯磺酸)。 The acidic reaction aids used in the process according to the invention include all mineral acids (for example: hydrohalic acids such as hydrofluoric acid, hydrochloric acid, hydrobromic acid, or hydroiodic acid, also referred to as sulfuric acid, phosphoric acid, phosphorous acid , nitric acid), Lewis acid (for example: aluminum (III) chloride, boron trifluoride or its etherate, titanium (IV) chloride, tin (IV) chloride) and organic acids (for example: formic acid, acetic acid , propionic acid, malonic acid, lactic acid, oxalic acid, fumaric acid, adipic acid, stearic acid, tartaric acid, oleic acid, methanesulfonic acid, benzoic acid, benzenesulfonic acid or p-toluenesulfonic acid).
式(I)化合物可能隨其取代基性質而定，而呈幾何與/或光學活性異構物或不同組成之相應異構物混合物型式。此等立體異構物為例如：對映異構物、非對映異構物、滯轉異構物(atropisomer)或幾何異構物。因此本發明包括純的立體異構物及此等異構物之任何混合物。 The compound of formula (I) may be a geometrically and/or optically active isomer or a corresponding mixture of isomers of different composition depending on the nature of the substituent. Such stereoisomers are, for example, enantiomers, diastereomers, atropisomers or geometric isomers. Thus the invention includes both pure stereoisomers and any 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。較佳係不包括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 surgery or medical treatment of the human or animal body and the diagnostic method performed on the human or animal body are not included.
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，術語「除害劑」亦總是包括術語「作物保護劑」。 In the context of this application, the term "peonicide" 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因子，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，尤指線蟲與軟體動物，可用於保護庫存產品與材料，及用於衛生領域。 The compound of formula (I) has good plant tolerance, favorable toxicity to warm-blooded animals and good environmental compatibility, and is suitable for protecting plants and plant organs against biological and abiotic stress factors, increasing yield and improving The quality of harvested materials and the control of animal pests, especially in the fields of agriculture, horticulture, animal husbandry, aquaculture, forests, gardens and leisure facilities, insects, spiders, worms, especially nematodes and mollusks, can be used to protect stock products and materials. And for the health sector.
本申請案內容中，術語「衛生」咸瞭解係指目的在於預防疾病(尤指感染性疾病)及用於維持人類、動物健康及/或保護環境及/或維持清潔之所有措施、方法與過程。根據本發明，其特別包括例如：紡織品或硬表面(尤指玻璃、木材、水泥、陶、瓷、塑膠或金屬(類))之清潔、消毒與殺菌之措施，以確保沒有有害衛生的生物及/或其分泌物。根據本發明此態樣之保護範圍較佳係不包括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。 In the context of this application, the term "hygienic" refers to all measures, methods and processes aimed at preventing diseases (especially infectious diseases) and for maintaining human, animal health and/or protecting the environment and/or maintaining cleanliness. . According to the invention, it comprises, inter alia, measures for the cleaning, disinfection and sterilization of textiles or hard surfaces (especially glass, wood, cement, ceramic, porcelain, plastic or metal) to ensure that there are no harmful organisms and / or its secretions. The scope of protection according to this aspect of the invention is preferably a method that does not include surgery or medical treatment of a human or animal body, and a diagnostic method performed on a human or animal body.
因此術語「衛生領域」包括以此等衛生措施、方法與過程為重點之所有區域、技術領域與工業應用，例如：廚房、烘焙坊、機場、浴室、游泳池、購物中心、旅館、醫院、畜養棚、動物飼養，等等之衛生。 Therefore, the term “health area” includes all areas, technical fields and industrial applications that focus on such hygiene measures, methods and processes, such as: kitchens, bakeries, airports, bathrooms, swimming pools, shopping centers, hotels, hospitals, livestock sheds. , animal feeding, and so on.
因此術語「衛生害蟲」咸瞭解係指出現在衛生領域中造成問題(尤指造成健康問題)之一或多種動物害蟲。因此其主要目的在於避免衛生領域中衛生害蟲之出現或與其之接觸，或限制到最低程度。尤其可透過使用除害劑達成此點，其中製劑可同時用於預防害蟲入侵及預防現存之害蟲入侵。亦可能使用可防止或減少接觸到害蟲之調配物。衛生害蟲包括例如：下述生物體。 Therefore, the term "sanitary pests" is understood to indicate one or more animal pests that cause problems (especially health problems) in the health sector. Therefore, its main purpose is to avoid the occurrence or contact with sanitary pests in the health sector, or to a minimum. This can be achieved, inter alia, by the use of pesticides, which can be used simultaneously to prevent pest infestation and to prevent the infestation of existing pests. It is also possible to use a formulation that prevents or reduces exposure to pests. Hygienic pests include, for example, the following organisms.
因此術語「衛生保護」包括所有用於維持及/或改善此等衛生措施、方法與製程之作用。 The term "hygiene protection" therefore includes all the functions used to maintain and/or improve such hygiene measures, methods and processes.
式(I)化合物較佳係作為除害劑使用。其有活性對抗正常敏感性與抗性物種，及對抗所有或某些發展階段。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：咖啡小爪蟎(Oligonychus coffee)、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)、姬蜚蠊(Loboptera decipiens)、斑蠊(Neostylopyga rhombifolia)、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))、蔗蠊(Pycnoscelus surinamensis)、長鬚帶蠊(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.)、小蜂窩甲蟲(Aethina tumida)、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.)、芽象甲屬(Epicaerus 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)、莖象甲屬(Listronotus(=Hyperodes)spp.)、黃象甲屬(Lixus spp.)、葉甲屬(Luperodes spp.)、黃胸葉甲(Luperomorpha xanthodera)、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.)、新螢金花蟲屬(Neogalerucella 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))、負泥蟲屬(Oulema spp.)、橙足負泥蟲(Oulema melanopus)、稻負泥蟲(Oulema oryzae)、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)、象鼻蟲屬(Rhynchophorus spp.)、椰子象鼻蟲(Rhynchophorus ferrugineus)、棕櫚象鼻蟲(Rhynchophorus palmarum)、雙棘長蠹蟲(Sinoxylon perforans)、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：黑粉榖盜(Tribolium audax)、擬榖盜(Tribolium castaneum)、扁擬榖盜(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))；革翅目(Dermaptera)，例如：肥螋(Anisolabis maritime)、歐洲球螋(Forficula auricularia)、蠼螋(Labidura riparia)；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.)、芹菜尤列實蠅(Euleia heraclei)、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或Pegomyia 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)、蘆筍實蠅(Platyparea poeciloptera)、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))、彎尾托實蠅(Toxotrypana curvicauda)；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.)、蕙蘭粉虱屬(Aleurocanthus 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(Aulacoithum 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)、絮蚧屬(Capulinia spp.)、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)、褐圓蚧(Chrysomphalus aonidum)、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.)、裸粉虱(Dialeurodes chittendeni)、柑桔裸粉虱(Dialeurodes citri)、柑桔木虱(Diaphorina citri)、盾蚧屬(Diaspis spp.)、麥蚜屬(Diuraphis spp.)、Doralis屬、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.)、檸檬按木虱屬(Eucalyptolyma spp.)、褐木風屬(Euphyllura spp.)、鈍鼻葉蟬(Euscelis bilobatus)、拂粉蚧屬(Ferrisia spp.)、圍盾蚧屬(Fiorinia spp.)、盾蚧屬(Furcaspis oceanica)、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)、日本長片盾蚧(Lopholeucaspis japonica)、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)、粉蝨屬(Neomaskellia spp.)、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(Nettigoniclla spectra)、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)、扁角飛虱屬(Perkinsiella spp.)、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(Pirnnaspis 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.)、棉蚧屬(Pulvinaria 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)、牛鞭草蚜(Sipha flava)、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：麥蝽屬(Aelia spp.)、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))、菜蝽屬(Eurydema spp.)、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)、豆龜蝽(Megacopta cribraria)、盲蝽科(Miridae)、金光綠盲蝽(Monalonion atratum)、綠蝽屬(Nezara spp.)(例如：稻綠蝽象(Nezara viridula))、小長蝽屬(Nysius spp.)、盾蝽屬(Oebalus spp.)、蝽科(Pentomidae)、擬配軍蟲(Piesma qpadrata)、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.)、木螞蟻屬(Camponotus spp.)、長黃胡蜂屬(Dolichovespula 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(Iridiomyrmex)humile)、廚蟻(Monomorium pharaonis)、黃山蟻屬(Paratrechina spp.)、黃蜂屬(Paravespula spp.)、斜結蟻屬(Plagiolepis spp.)、樹蜂屬(Sirex spp.)、入侵紅火蟻(Solenopsis invicta)、酸臭蟻屬((Tapinoma spp.)、白足扁蟻(Technomyrmex albipes)、樹蜂(Urocerus spp.)、胡蜂屬(Vespa spp.)(例如：黃邊胡蜂(Vespa crabro))、小火蟻(Wasmannia auropunctata)、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：台灣家白蟻(Coptotermes formosanus))、白蟻(Cornitermes cumulans)、堆砂白蟻屬(Cryptotermes spp.)、楹白蟻屬(Incisitermes spp.)、木白蟻屬(Kalotermes spp.)、甘蔗白蟻(Microtermes obesi)、象白蟻屬(Nasutitermes spp.)、土白蟻屬(Odontotermes spp.)、按白蟻屬(Porotermes 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.)、丫蚊夜蛾屬(Autographa spp.)、甘藍夜蛾(Barathra brassicae)、蘋髓尖蛾(Blastodacna atra)、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))、蘋果舞蛾(Choreutis pariana)、雲杉卷葉蛾屬(Choristoneura spp.)、金色雙斑蛾(Chrysodeixis chalcites)、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.)、螟蛉屬(Diparopsis 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：煙草粉螟(Ephestia elutella)、地中海斑螟(Ephestia kuehniella))、小卷蛾屬(Epinotia spp.)、蘋果飛蛾(Epiphyas postvittana)、尺蛾屬(Erannis spp.)、皮夜蛾(Erschoviella musculana)、螟蛾屬(Etiella spp.)、木葉蛾屬(Eudocima 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)、灰蝶屬(Lampides spp.)、黏蟲屬(Laphygma spp.)、梨小食心蟲(Laspeyresia molesta)、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 anternnata))、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.)、榖蛾科(Monopis obviella)、東方黏蟲(Mythimna separate)、穀蛾(Nemapogon cloacellus)、水螟屬(Nymphula spp.)、扇頭蜱屬(Oiketicus spp.)、螟蛾屬(Omphisa spp.)、秋尺蛾屬(Operophtera 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))、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)、山植潛葉蛾(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.)、織蛾屬(Stenoma spp.)、潛葉蟲(Stomopteryx subsecivella)、透翅蛾屬 (synanthedon spp.)、馬鈴薯塊莖蛾(Tecia solanivora)、松舟蛾屬(Thaumetopoea spp.)、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：囓蟲屬(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)、中斑圍孔薊馬(Chaetanaphothrips leeuweni)、葡萄德薊馬(Drepanothris reuteri)、黃帶薊馬(Enneothrips flavens)、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))、正皮薊馬屬(Haplothrips spp.)、網薊馬屬(Heliothrips spp.)、溫室條籬薊馬(Hercinothrips femoralis)、卡薊馬屬(Kakothrips spp.)、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.)；來自線蟲動物門(Nematoda)之植物害蟲，亦即植物寄生性線蟲，特別指：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))、穿根線蟲屬(Hirschmaniella spp.)、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.)、殘根線蟲屬(Paralongidorus 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.)。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、抗黴劑、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 compound of formula (I) is preferably used as a pesticide. It is active against normal sensitive and resistant species and against all or some 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. (eg: Hemitarsonemus latus (= Polyphagotarsonemus latus), genus Hyalomama spp. ), hard genus (Ixodes spp. ), the genus Arachnid (Latrodectus spp. ), Loxosceles spp. ), autumn scorpion (Neutrombicula autumnalis), Nuphersa genus, genus Oligonychus spp. (eg: Oligonychus coffee, 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, Loboptera decipiens, Neostyylopyga rhombifolia, Panchlora spp. ), Pacoblatta spp. ), family genus (Periplaneta spp. (eg, Periplaneta americana, Periplaneta australasiae), Pycnoscelus surinamensis, Supella longipalpa, Coleoptera, for example: striped cucumber beetle ( Acalymma vittatum), soy elephant (Acanthoscelides obtectus), genus Aurora (Adoretus spp. ), Aethina tumida, Agelastica alni, Agriotes 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, Coniferous sp. ), 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. ), genus Epicaerus 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, tobacco beetle (Lasioderma serricorne), Latheticus oryzae, Lathridius spp. ) Lema spp. ), potato beetle (Leptinotarsa decemlineata), Lepidoptera spp. (eg: Leucoptera coffeella), Lisorhoptrus oryzophilus, Listronotus (=Hyperodes) spp. ), the yellow genus (Lixus spp. ), Luperodes spp. ), Luperomorpha xanthodera, Lyctus 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. ), Neogolder nectar (Neogalerucella spp. ), Niptus hololeucus, Oryctes rhinoceros, Oryzaephilus surinamensis, Oryzaphagus oryzae, Otiorrhynchus spp. (eg: Otiorhynchus cribricollis, Otiorhynchus ligustici, Otiorhynchus ovatus, Otiorhynchus rugosostriarus, Otiorhynchus sulcatus), Negative worms (Oulema spp. ), Oulema melanopus, Oulema oryzae, 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, Rhynchophorus spp. ), Rhynchophorus ferrugineus, Rhynchophorus palmarum, Sinoxylon perforans, Sitophilus spp. (eg: Sitophilus granarius, Sitophilus linearis, Sitophilus oryzae, Sitophilus zeamais), Sphenophorus spp. ), Stembium paniceum, Stemichus spp. ) (for example: Sternechus paludatus), Lyrics genus (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); Dermaptera, for example: Anisolabis maritime, Forficula auricularia, Labidura riparia; 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 (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. ), genus 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. ), Euleia heraclei, genus 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), Liriomyza (Pegomya or Pegomyia spp. ) (eg: Pegomya betae, spinach migratory fly) (Pegomya hyoscyami), Pegomya rubivora, and Phlebotomus spp. ), the genus Hypora (Phorbia spp. ), the genus Phormia spp. ), Piophila casei, Platyparea poeciloptera, 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. ), the genus Stratus (Tetanops spp. ), the genus of the genus (Tipula spp. (eg: Tipula paludosa, Tipula simplex), Toxotrypana curvicauda, Hemiptera, eg Acizzia acaciaebaileyanae, Acizzia dodonaeae, Acizzia uncatoides, Acrida turrita, Acyrthosipon spp. ) (eg: Acyrthosiphon pisum), Acrogonia spp. ), Aeneolamia genus, Aragonoscena spp. ), Aleurocanthus 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, Aphis spiraecola, Aphis viburniphila, Arboridia apicalis , hibiscus (Arytainilla spp. ), Aspidiella spp. ), the round shield genus (Aspidiotus spp. (eg: Aspidiotus nerii), Atanus genus, Aulacoithum solani, Bemisia tabaci, Blastopsylla occidentalis, Boreioglycaspis melaleucae, light tube Brachycaudus helichrysi, Brachycolus spp. ), Brasserie (Brevicoryne brassicae), Liriodendron (Cacopsylla spp. ) (eg: Cacopsylla pyricola), Calligypona marginata, Capulinia spp. ), Carneocephala fulgida, Ceratovacuna lanigera, Cercopidae, Ceroplastes spp. ), Chaetosiphon fragaefolii, Chionaspis tegalensis, Chlorita onukii, Chondracris rosea, Chromaphis juglandicola, Chrysomphalus aonidum ), 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 chittendeni, Dialeurodes citri, Diaphorina citri, Diaspis spp. ), genus Diuraphis spp. ), Doralis genus, genus Drosicha spp. ), Stem Aphid (Dysaphis spp. ) (for example: Dysaphis apiifolia, Dysaphis plantaginea, Dysaphis tulipae), Dysmicoccus spp. ), small green leaf genus (Empoasca spp. ) (eg: potato leafhopper (Empoasca abrupta), potato leafhopper (Empoasca fabae), apple small green leaf Po(Empoasca maligna), Empoasca solana, Empoasca stevensi, Eriosoma spp. (eg: Eriosoma americanum, Eriosoma lanigerum, Eriosoma pyricola), Erythroneura spp. ), lemon according to the genus Eucalyptolyma spp. ), brown wood (Euphyllura spp. ), Euscelis bilobatus, Ferrisia spp. ), the genus Fiorinia spp. ), Curcaspis oceanica, Geococcus coffeae, Glycaspis spp. ), Heteropsylla cubana, Heteropsylla spinulosa, Homalodisca coagulata, Hyalopterus arundinis, Hyalopterus pruni, blown cotton Genus (Icerya spp. ) (eg, Icerya purchasi), Idiocerus spp. ), green leaf genus (Idioscopus spp. ), Laodelphax striatellus, Lecanium spp. ) (eg Lecanium corni (Parthenolecanium corni), Lepidosaphes spp. (eg: Lepidosaphes ulmi), Lipaphis erysimi, Lopholeucaspis japonica, 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) Myzus nicotianae), Nasonovia ribisnigri, Neomaskellia spp. ), Nephotettix spp. ) (eg: Nephotettix cincticeps, Nephotettix Nigropictus)), Nettigoniclla spectra, 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, Perkinsiella spp. ), white genus (Phenacoccus spp. (eg: Phenacoccus madeirensis), Phloeomyzus passerinii, Phorodon humuli, Phylloxera spp. (eg: Phylloxera devastatrix, Phylloxera notabilis), Pirnnaspis aspidistrae, Planococcus spp. (for example: Planococcus citri), Prosopidopsylla flava, 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. ), Aphis gossypii (Pulvinaria 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, hard ridges) (Saissetia oleae)), Scaphoides titanus, Schizaphis graminum, Selenaspidus articulatus, Sipha flava, Sitobion avenae, genus Sogata 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: Aelia spp. ), 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), Eurydema spp. ), Hedgehog (Eurygaster spp. ), Halyomorpha halys, Heliopeltis spp. ), Horbians nobilellus, Leptocorisa spp. ), Leptocorisa varicornis, Leptoglossus occidentalis, Leptoglossus phyllopus, Lygocoris spp. ) (for example: Lygocoris pabulinus), Lygus (Lygus) Spp. (eg: Lygus elisus, Lygus hesperus, Lygus lineolaris), Macropes excavatus, Megacopta cribraria, blind Miridae, Monalonion atratum, Nezara spp. ) (eg Nezara viridula), Nysius spp. ), Shield genus (Oebalus spp. ), Penentidae, Piesma qpadrata, Piezodorus 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. ), wood ant genus (Camponotus spp. ), the genus Polychaete (Dolichovespula spp. ), Dipterus spp. ) (eg: Diprion similis), Hoplocampa spp. ) (eg: Hoplocampa cookei, Hoplocampa testudinea), genus (Lasius spp. ), Argentine ants (Linepithema (Iridiomyrmex) humile), kitchen ants (Monomorium pharaonis), Yellow Mountain genus (Paratrechina spp. ), wasp genus (Paravespula spp. ), stellate genus (Plagiolepis spp. ), Tree Bee (Sirex spp. ), invasive red fire ant (Solenopsis invicta), acid odorant genus ((Tapinoma spp. ), Whitefoot ant (Technomyrmex albipes), tree bee (Urocerus spp. ), Vespa (Vespa spp. ) (for example: Vespa crabro), Wasmannia auropunctata, and 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 Cryptotermes spp. ), Termite genus (Incisitermes spp. ), wood termite genus (Kalotermes spp. ), sugar termites (Microtermes obesi), like termites (Nasutitermes spp. ), the termite genus (Odontotermes spp. ), according to the termite genus (Porotermes 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. ), Autographa spp. ), Barathra brassicae, Blastodacna atra, Borbo cinnara, Bucculatrix thurberiella, Bupalus piniarius, Busseola Spp. ), Cacoecia spp. ), Caloptilia theivora, Capua reticulana, Carpocapsa pomonella, Carposina niponensis, Cheimatobia brumata, Chilo spp. (eg: Chilo plejadellus, Chilo suppressalis), Choreutis pariana, Choristoneura spp. ), Chrysodeixis chalcites, 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. ), genus Diparopsis 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), genus Erannis spp. ), Erschoviella musculana, Etiella spp. ), Eudocima 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, Lampides spp. ), Lacgaria spp. ), Laspeyresia molesta, Leucinodes orbonalis, Leucoptera spp. ) (eg: Leucoptera coffeella), Lithocolletis spp. ) (eg Lithocolletis blancardella, Lithophetan anternnata), Lobesia spp. ) (for example: Lobesia botrana), Loxaltis albicosta, Lymantria spp. ) (eg Lymantria dispar), Lyonetia spp. ) (for example: Lyyonetia clerkella), golden tortoise (Malacosoma neustria), Maruca testulalis, Mamstra brassicae, Melanitis leda, Mocis spp. ), Monopis obviella, Mythimna separate, Nemapogon cloacellus, Nymphula spp. ), genus Oiketicus spp. ), Ophivia spp. ), the genus Operophtera spp. ), Noctuidae (Oria spp. ), Orthaga spp. ), corn genus (Ostrinia spp. ) (eg: Ostrinia nubilalis), 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. ), Stenoma spp. ), leafy insect (Stomopteryx subsecivella), genus (synanthedon spp. ), potato tuber moth (Tecia solanivora), genus Thaumetopoea spp. ), Thermesia gemmatalis, Tinea cloacella, Tinea pellionella, Tineola bisselliella, 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 (Thysanoptera), for example: Anaphothrips obscurus, Baliothrips biformis, Chaetanaphothrips leeuweni, Drepanothris reuteri, Enneothrips flavens ), flower genus (Frankliniella spp. ) (eg: Frankliniella fusca, western flower scorpion horse) (Frankliniella occidentalis), Frankliniella schultzei, Frankliniella tritici, Frankliniella vaccinii, Frankliniella williamsi, Orthopaedic (Haplothrips spp. ), the net genus (Heliothrips spp. ), Greenhouse fence horse (Hercinothrips femoralis), Karthomas spp. ), Rhipiphorothrips cruentatus, hard hummer (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. a plant pest from the Nematoda, also known as a plant-parasitic nematode, especially: the genus Nelenchus spp. ) (eg: Aglenchus agricola), Anguina spp. ) (eg: Anguina tritici), Aphelenchoides spp. (eg: Aphelenchoides arachidis, Aphelenchoides fragariae), Nematodes (Belonolaimus spp. )(E.g: 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), Creptemoides 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), Hirschmaniella spp. ), the genus Nematode (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. ), Parasiticus genus Paralongidorus spp. Nematode (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, Trichodorus primitivus), Tylenchorhynchus spp. ) (for example: Tylenchorhynchus annulatus), Tylenchulus spp. ). 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。該等施用形式可視需要包含其他除害劑與/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. Such application forms may optionally contain other pesticides and/or improved utilities, such as penetrants, for example: vegetable oils (eg, rapeseed oil, sunflower oil), mineral oils (eg, paraffin oil), botanical Alkyl esters of fatty acids (eg, rapeseed oil methyl ester or soybean oil methyl ester), or alkanol alkoxylates, and/or distribution agents, such as alkyl oxanes, and/or salts , for example: organic or inorganic ammonium or phosphonium salts, for example: ammonium sulphate or diammonium hydrogen phosphate, and / or promote retention agents, such as: dioctyl sulfosuccinate or Hydroxypropyl guanosin polymer, and/or humectants such as glycerin, and/or fertilizers, for example, fertilizers containing ammonium, potassium or phosphorus.
根據本發明調配物可為水性或非水性。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)製作之「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」，ISBN：9251048576。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。 Formulations according to the invention may be aqueous or non-aqueous. 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) "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", ISBN: 9251048576. 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、勻散劑、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 include adjuvants (eg, supplements, solvents, spontaneous accelerators, carriers, emulsifiers, leveling agents, frosting 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 Alcohol (may be substituted, etherified and/or esterified if appropriate), ketones (eg acetone, cyclohexanone), esters (including fats and oils) and (poly)ethers, not Substituted and substituted amines, guanamines, intrinsic amines (such as N-alkylpyrrolidone) and lactones, terpenoids and anthraquinones (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：礦物油分餾物、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: mineral oil fraction, mineral oil and vegetable oil), alcohols (such as: butanol or glycols, and ethers and esters), ketones (eg acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone), strong polar solvents (eg dimethylformamide 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)、氯化芳香烴或脂族烴類(如：氯苯、氯化乙烯或二氯甲烷)、脂族烴類(如：環己烷、鏈烷烴、礦物油分餾物、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 or aliphatic hydrocarbons (eg chlorobenzene, ethylene chloride or dichloromethane), aliphatic hydrocarbons (eg cyclohexane, paraffins, mineral oil 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、礬土、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。同樣可能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, alumina, talc, chalk, quartz, strontium, montmorillonite or diatomaceous earth, and synthetic mineral powders such as: highly dispersed Vermiculite, alumina and natural or synthetic silicates, resins, waxes and/or solid fertilizers. It is also possible to use a mixture of such carriers. 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.
亦可能使用液化氣體補充劑或溶劑。特別適用之補充劑或載劑係彼等在標準溫度與常壓下呈氣態者，例如：氣霧劑推進劑氣體，如：鹵 化烴類，及丁烷、丙烷、氮氣與二氧化碳。 It is also possible to use liquefied gas supplements or solvents. Particularly suitable supplements or carriers are those which are gaseous at standard temperature and atmospheric pressure, for example: aerosol propellant gases such as: halogen Hydrocarbons, 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、勻散劑或濕化劑、或此等表面活性物質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, leveling agents or wetting agents, or mixtures of such surface active materials 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. Derivatives of the root compound, for example: alkyl aryl polyglycol ethers, alkyl sulfonates, alkyl sulfates, aryl sulfonates, protein hydrolysates, lignin sulfite waste liquids With methyl cellulose. 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為染劑，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 are 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.
可能存在之其他組份為安定劑，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 that may be present are 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 the application form derived therefrom may also contain other adjuvants, adhesives 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.
若適當時，調配物及其所衍生施用型式中亦可能包含其他輔劑。此等添加劑實例為香料、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)化合物可與任何常用於調配目的之固態或液態添加劑組合使用。 If appropriate, other adjuvants may also be included in the formulation and the mode of application from which it is derived. Examples of such additives are perfumes, protective colloids, binders, adhesives, thickeners, shakers, Penetrant, prolonged retention agent, stabilizer, chelating agent, error correcting agent, moisturizing agent, and distributing agent. In general, the compounds of formula (I) can be used in combination with any solid or liquid additive commonly used for formulation purposes.
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 materials which are commonly used to improve the penetration of agrochemically active compounds into plants. 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，更佳係0.01%至95%重量比之式(I)化合物，最佳係0.5%至90%重量比之式(I)化合物。 Preferably, the formulation comprises a compound of formula (I), preferably from 0.01% to 95% by weight, based on the weight of the formulation, of the compound of formula (I), preferably from 0.5% to 90% by weight. % by weight of the compound of formula (I).
由調配物(特定言之除害劑)製成之施用型式中之式(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 made from the formulation (specifically, a pesticide) can vary widely. 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、有利生物體、除草劑、肥料、驅鳥劑、強化植物劑、不孕劑、安全劑、化學傳訊物質及/ 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、對乾旱或對上升之水份或土壤鹽份含量之耐受性。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, advantageous organisms, herbicides, Fertilizers, bird repellents, fortified plant agents, infertility agents, safeners, chemical communication substances and/or Or a plant growth regulator forming mixture is used, for example, to broaden the scope of action, prolong the duration of action, increase the rate of action, prevent rejection or prevent the development of 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 elevated moisture or soil 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 improve processability .
此外，式(I)化合物可與其他活性化合物或化學傳訊物質(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)化合物可用於改善植物性質(例如：生長、產量、及所收成材料之品質)。 Furthermore, the compounds of formula (I) may be admixed with other active compounds or chemical signaling 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 to improve plant properties (eg, growth, yield, and quality of the harvested material).
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彼等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 with the compounds 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。所有述及之混合組份亦可能依據其官能基，可能與合適鹼類或酸類形成鹽類。 If one of the compounds described below may exhibit different tautomeric forms, these forms are included even if not individually presented. All of the mixed components mentioned may also form salts with suitable bases or acids depending on their functional groups.
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：「The Pesticide Manual」，第16版，British Crop Protection Council 2012或可搜尋網際網路(例如：http：//www.alanwood.net/pesticides)。 The active compounds referred to herein by their common names are known and described, for example, in "The Pesticide Manual", 16th Edition, British Crop Protection Council 2012 or searchable internet (eg 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)、穀速松(azinphos)-乙基、穀速松(azinphos)-甲基、卡速松(cadusafos)、氯乙松(chlorethoxyfos)、氯芬松(chlorfenvinphos)、氯滅松(chlormephos)、陶斯松(chlorpyrifos)-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)-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), butacarboxim, buthoxycarboxim, carbaryl, plus Carbofuran, carbosulfan, ethiofencarb, fenobucarb, formetanate, furathiocarb, isoprocarb, extinction Methicarb, methomyl, metolcarb, oxamyl, pirimicarb, propoxur, thiodicarb, thiophene (thiofanox), triazamate, trimethacarb, XMC and xylylcarb; or organophosphates such as acephate, azamethiphos, valley Azinphos-ethyl, azinphos-methyl, cadusafos, chlorethoxyfos, chlorfenvinphos, chlormephos, chlorpyrifos -methyl, coumaphos, cyanophos, demeton-S-methyl, diazinon, dichlorvos/DDVP, dicrotophos ), dimethoate, dimethylvinphos, disulfoton, EPN, ethion, ethoprophos, acesulfame (famphur), fenamiphos, fenitrothion, fenthion, fosthiazate, heptenophos, imcyfax, isofenphos O-(methoxyamine thiophosphonium) isopropyl salicylate, isoxathion, malathion, mecarbam, methamidophos, Methidathion, mevinphos, monocrotophos, naled, omethoate, oxydemeton-methyl, parathion- Methyl, phenthoate, phorate, phosalone, phosmet, phosphamidon, phoxim, pirimiphos -methyl, profenofos, propetamphos, prothiofos, pyraclofos, pyridaphenthion, quinalphos, sulfotep , tebupirimfos, temephos, terfufos, tetrachlorin (tetrachlorvinphos), thiometon, triazophos, triclofen and vamidothion.
(2)GABA-閘控之氯離子通道阻斷劑，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 blockers, such as cyclodiene-organochlorines, such as: chlordane and endosulfan; or phenylpyrazoles (feipulo) (Fiprole)), for example: ethiprole and fipronil.
(3)鈉通道調控劑，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(且uvalinate)、海本斯(halfenprox)、益普靈(imiprothrin)、剋特寧(kadethrin)、滅伏靈(momfluorothrin)、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, for example: pyrethroids, for example: acrinathrin, allethrin, d-cis-trans methrin (allethrin), d-trans Allethrin, bifenthrin, bioallethrin, bioallethrin S-cyclopentenyl isomer, bioresmethrin, cycloprothrin, Cyfluthrin, cyfluthrin, cyhalothrin, cyhalothrin, cyhalothrin, cypermethrin, α- Cypermethrin, cypermethrin, cypermethrin, cypermethrin, cyphenothrin [(1R)-trans isomer ], deltamethrin, emtemphrin [(EZ)-(1R) isomer], esfenvalerate, etofenprox, fenpropathrin, fentanyl Fenvalerate, flucythrinate, flumethrin, τ-fuhuali (and uvalinate), halfenprox, imiprothrin, kadethrin Momfluorothrin, permethrin, phenothrin [(1R)-trans isomer], prallethrin, pyrethrins (pyrethrum), Resmethrin, silafluofen, tefluthrin, tetramethrin, tetramethrin [(1R) isomer), tralomethrin and Transfluthrin; or DDT; or methoxychlor.
(4)菸鹼激導性乙醯基膽鹼受體(nAChR)競爭性調控劑，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)或伏達隆(flupyradifurone)。 (4) Nicotine-induced acetylcholine receptor (nAChR) competitive regulators, such as neonicotinoids, such as acetamiprid, clothianidin, and dinofenol ( Dinotefuran), benefit Imidacloprid, nitenpyram, thiacloprid and thiamethoxam; or nicotine or sulfoxaflor or flupyradifurone.
(5)菸鹼激導性乙醯基膽鹼受體(nAChR)異位性調控劑，例如：賜諾殺類(Spinosyns)，例如：賜諾特(spinetoram)與賜諾殺(spinosad)。 (5) Nicotine-induced acetylcholine receptor (nAChR) atopic modulators, such as spinosyns, such as spinetoram and spinosad.
(6)麩胺酸閘控氯離子通道(GluCl)異位性調控劑，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) GluCl agglutination channel (GluCl) atopic modulator, for example: avermectins / milbemycin, for example: abamectin, inhibition Emamectin benzoate, 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)其他非專一性(多重位點)抑制劑，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；或酒石酸銻鉀鹽；或異氰酸甲酯發生劑，例如：棉隆(diazomet)與威百畝(metam)。 (8) other non-specific (multiple site) inhibitors, such as: alkyl halides, such as: methyl bromide and other alkyl halides; or chloropicrin; or thiopurine; or borax; Or potassium barium tartrate; or methyl isocyanate generators, such as: diazomet and metam.
(9)弦音感覺器官調控劑，例如：必滅辛(pymetrozine)或伏卡滅(flonicamid)。 (9) A string sound sensory organ modulator, 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)昆蟲中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 aizawat)、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、Cry1A.105、Cry2Ab、VIP3A、mCry3A、Cry3Ab、Cry3Bb、Cry34Ab1/35Ab1。 (11) Microbial resolving agents for insect midgut, such as Bacillus thuringiensis subspecies israelensis , Bacillus sphaericus , Bacillus thuringiensis subspecies aizawat , Suyun golden spores Bacillus thuringiensis subspecies kurstaki , Bacillus thuringiensis subspecies tenebrionis and BT plant proteins: Cry1Ab, Cry1Ac, Cry1Fa, Cry1A.105, Cry2Ab, VIP3A, mCry3A, Cry3Ab, Cry3Bb, Cry34Ab1/35Ab1.
(12)粒線體ATP合成酶抑制劑，如：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) mitochondrial ATP synthase inhibitors, such as: ATP disintegrating agents, for example: diafenthiuron; Or organotin compounds, such as: azocyclotin, cyhexatin and fenbutatin oxides; or propargite or tetradifon.
(13)破壞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) An oxidative phosphorylation decoupling agent that destroys a proton gradient, such as chlorfenapyr, DNOC, and sulfluramid.
(14)菸鹼激導性乙醯基膽鹼受體通道阻斷劑，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 channel blockers, such as: 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)蛻變瓦解劑(尤指雙翅目)，例如：賽麻辛(cyromazine)。 (17) Metamorphic disintegrating agents (especially diptera), 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)章魚胺受體促效劑，例如：三亞蟎(amitraz)。 (19) Octopamine receptor agonist, for example: amitraz.
(20)粒線體複合物-III電子轉運抑制劑，例如：海滅能(hydramethylnone)或亞克希(acequinocyl)或伏克靈(fluacrypyrim)。 (20) A mitochondrial complex-III electron transport inhibitor, for example, hydramethylnone or acequinocyl or fluacrypyrim.
(21)粒線體複合物-I電子轉運抑制劑，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) mitochondrial complex-I electron transport inhibitors, for example: METI acaricides, for example: fenazaquin, fenpyroximate, pyrimidifen, pyripaben ), tebufenpyrad and tolfenpyrad; or rotenone (Derris).
(22)依賴電壓之鈉通道阻斷劑，例如：因得克(indoxacarb)或滅伏美松(metaflumizone)。 (22) Voltage-dependent sodium channel blockers, such as indoxacarb or metaflumizone.
(23)乙醯基-CoA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 the ethenyl-CoA carboxylase, for example, quetia acid and pyrrolidone derivatives, for example, spirodiclofen, spiromesifen, and spirotetramat.
(24)粒線體複合物-IV電子轉運抑制劑，例如：膦類，例如：磷化鋁、磷化鈣、膦與磷化鋅；或氰化物、氰化鈣、氰化鉀、與氰化鈉。 (24) mitochondrial complex-IV electron transport inhibitors, such as phosphines, such as: aluminum phosphide, calcium phosphide, phosphine and zinc phosphide; or cyanide, calcium cyanide, potassium cyanide, and cyanide Sodium.
(25)粒線體複合物-II電子轉運抑制劑，例如：β-酮基腈衍生物，例如：氰必吩(cyenopyrafen)與賽芬蟎(cyflumetofen)，與羧基替苯胺類，例如：必伏拜(pyflubumide)。 (25) a mitochondrial complex-II electron transport inhibitor, for example, a β-keto nitrile derivative, for example, cyenopyrafen and cyflumetofen, and a carboxyaniline such as: Pyflubumide.
(28)蘭尼鹼(ryanodine)受體調控劑，例如：二醯胺類，例如：氯蒽吡咯(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)與表氟蟲胺(flubendiamide)，其他活性化合物，例如：艾特本(afidopyropen)、艾伏樂(afoxolaner)、查得定(azadirachtin)、苯克賽(benclothiaz)、苯賽滅(benzoximate)、必芬賽(bifenazate)、布伏利(broflanilide)、新殺蟎(bromopropylate)、蟎離丹(chinomethionat)、氯丙炔菊酯(chloroprallethrin)、克利得(cryolite)、環溴蟲醯胺(cyclaniliprole)、環氧蟲啶(cycloxaprid)、氯氟氰蟲醯胺(cyhalodiamide)、二氯滅嗪(dicloromezotiaz)、大克蟎(dicofol)、ε-美特寧(metofluthrin)、ε-滅伏靈(momfluthrin)、氟喹啉(flometoquin)、氟吲哚辛(fluazaindolizine)、氟速吩(fluensulfone)、伏吩靈(flufenerim)、氟菌蟎酯(flufenoxystrobin)、丁烯氟蟲腈(flufiprole)、氟赫吩(fluhexafon)、氟吡菌醯胺(fluopyram)、氟樂(fluralaner)、氟賽醯胺(fluxametamide)、呋喃蟲醯肼(fufenozide)、戊吡蟲胍(guadipyr)、氯氟醚菊酯(heptafluthrin)、氯噻啉(imidaclothiz)、依普同(iprodione)、κ-畢芬寧(kappa bifenthrin)、κ-特芬寧(kappa tefluthrin)、樂地蘭(lotilaner)、氯氟醚菊酯(meperfluthrin)、哌蟲啶(paichongding)、吡啶蟲丙醚(pyridalyl)、必伏松(pyrifluquinazon)、嘧蟎胺(pyriminostrobin)、賜派芬(spirobudiclofen)、四氟醚菊酯(tetramethylfluthrin)、氟氰蟲醯胺(tetraniliprole)、四氯剋安勃(tetrachlorantraniliprole)、塔賽吩(tioxazafen)、硫氟賜滅(thiofluoximate)、三氟普靈(triflumezopyrim)、與碘甲烷；及其他基於堅強芽孢桿菌(Bacillus firmus)之製劑(I-1582,BioNeem,Votivo)，與下列化合物：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(來自WO2006/043635)(CAS 885026-50-6)、{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(來自WO2003/106457)(CAS 637360-23-7)、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]異菸醯胺(來自WO2006/003494)(CAS 872999-66-1)、3-(4-氯-2,6-二甲基苯基)-4-羥基-8-甲氧基-1,8-二氮雜螺[4.5]癸-3-烯-2-酮(來自WO 2010052161)(CAS 1225292-17-0)、碳酸3-(4-氯-2,6-二甲基苯基)-8-甲氧基-2-側氧基-1,8-二氮雜螺[4.5]癸-3-烯-4-基酯乙酯(來自EP 2647626)(CAS-1440516-42-6)、4-(丁-2-炔-1-基氧)-6-(3,5-二甲基哌啶-1-基)-5-氟嘧啶(來自WO2004/099160)(CAS 792914-58-0)、PF1364(來自JP2010/018586)(CAS Reg.No.1204776-60-2)、N-[(2E)-1-[(6-氯吡啶-3-基)甲基]吡啶-2(1H)-亞基]-2,2,2-三氟乙醯胺(來自WO2012/029672)(CAS 1363400-41-2)、(3E)-3-[1-[(6-氯-3-吡啶基)甲基]-2-吡啶亞基]-1,1,1-三氟丙-2-酮(來自WO2013/144213)(CAS 1461743-15-6)、N-[3-(苯甲基胺甲醯基)-4-氯苯基]-1-甲基-3-(五氟乙基)-4-(三氟甲基)-1H-吡唑-5-羧醯胺(來自WO2010/051926)(CAS 1226889-14-0)、5-溴-4-氯-N-[4-氯-2-甲基-6-(甲基胺甲醯基)苯基]-2-(3-氯-2-吡啶基)吡唑-3-羧醯胺(來自CN103232431)(CAS 1449220-44-3)、4-[5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異唑基]-2-甲基-N-(順式-1-氧離子基-3-硫雜環丁烷基)苯甲醯胺、4-[5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異唑基]-2-甲基-N-(反式-1-氧離子基-3-硫雜環丁烷基)苯甲醯胺與4-[(5S)-5-(3,5-二氯苯基)-4,5-二氫-5-(三氟甲基)-3-異唑基]-2-甲基-N-(順式-1-氧離子基-3-硫雜環丁烷基)苯甲醯胺(來自WO 2013/050317 A1)(CAS 1332628-83-7)、N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙 基)亞磺醯基]丙醯胺、(+)-N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺與(-)-N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)亞磺醯基]丙醯胺(來自WO 2013/162715 A2、WO 2013/162716 A2、US 2014/0213448 A1)(CAS 1477923-37-7)、5-[[(2E)-3-氯-2-丙烯-1-基]胺基]-1-[2,6-二氯-4-(三氟甲基)苯基]-4-[(三氟甲基)亞磺醯基]-1H-吡唑-3-甲腈(來自CN 101337937A)(CAS 1105672-77-2)、3-溴-N-[4-氯-2-甲基-6-[(甲基胺基)硫代甲基]苯基]-1-(3-氯-2-吡啶基)-1H-吡唑-5-羧醯胺(Liudaibenjiaxuanan，來自CN 103109816 A)(CAS 1232543-85-9)；N-[4-氯-2-[[(1,1-二甲基乙基)胺基]羰基]-6-甲基苯基]-1-(3-氯-2-吡啶基)-3-(氟甲氧基)-1H-吡唑-5-羧醯胺(來自WO 2012/034403 A1)(CAS 1268277-22-0)、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-2-吡啶基)-1H-吡唑-5-羧醯胺(來自WO 2011/085575 A1)(CAS 1233882-22-8)、4-[3-[2,6-二氯-4-[(3,3-二氯-2-丙烯-1-基)氧]苯氧基]丙氧基]-2-甲氧基-6-(三氟甲基)嘧啶(來自CN 101337940 A)(CAS 1108184-52-6)；(2E)-與2(Z)-2-[2-(4-氰基苯基)-1-[3-(三氟甲基)苯基]亞乙基]-N-[4-(二氟甲氧基)苯基]肼羧醯胺(來自CN 101715774 A)(CAS 1232543-85-9)；環丙烷羧酸3-(2,2-二氯乙烯基)-2,2-二甲基-4-(1H-苯并咪唑-2-基)苯基酯(來自CN 103524422 A)(CAS 1542271-46-4)；(4aS)-7-氯-2,5-二氫-2-[[(甲氧基羰基)[4-[(三氟甲基)硫]苯基]胺基]羰基]茚并[1,2-e][1,3,4]二嗪-4a(3H)-羧酸甲基酯(來自CN 102391261 A)(CAS 1370358-69-2)；6-去氧-3-O-乙基-2,4-二-O-甲基-1-[N-[4-[1-[4-(1,1,2,2,2-五氟乙氧基)苯基]-1H-1,2,4-三唑-3-基]苯基]胺甲酸酯]-α-L-哌喃甘露糖(來自US 2014/0275503 A1)(CAS 1181213-14-8)；8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基噠嗪-3-基)-3-氮雜雙環[3.2.1]辛烷(CAS 1253850-56-4)、(8-反側)-8-(2-環丙基甲氧 基-4-三氟甲基苯氧基)-3-(6-三氟甲基噠嗪-3-基)-3-氮雜雙環[3.2.1]辛烷(CAS 933798-27-7)、(8-同側)-8-(2-環丙基甲氧基-4-三氟甲基苯氧基)-3-(6-三氟甲基噠嗪-3-基)-3-氮雜雙環[3.2.1]辛烷(來自WO 2007040280 A1、WO 2007040282 A1)(CAS 934001-66-8)與N-[3-氯-1-(3-吡啶基)-1H-吡唑-4-基]-N-乙基-3-[(3,3,3-三氟丙基)硫]丙醯胺(來自WO 2015/058021 A1、WO 2015/058028 A1)(CAS 1477919-27-9)。 (28) Ryanodine receptor modulators, for example, diamines, for example, chlorantraniliprole, cyantraniliprole and flubendiamide, other active compounds, For example: afidopyropen, afoxolaner, azadirachtin, benclothiaz, benzoximate, bifenazate, broflanilide , new bromopropylate, chinomethionat, chloroprallethrin, cryolite, cyclaniliprole, cycloxaprid, chlorofluorocyanide Cyhalodiamide, dicloromezotiaz, difofo, metofluthrin, momfluthrin, flometoquin, fluoroquinone Fluazaindolizine, fluensulfone, flufenerim, flufenoxystrobin, flufiprole, fluhexafon, fluopyram ), fluralaner, fluxametamide, furan mites (fuf) Enozide), guadipyr, heptafluthrin, imidaclothiz, iprodione, kappa bifenthrin, kappa tefluthrin ), lotilaer, meperfluthrin, paichongding, pyridalyl, pyrifluquinazon, pyriminostrobin, schiffen (spirobudiclofen), tetramethylfluthrin, tetraniliprole, tetrachlorantraniliprole, tioxazafen, thiofluoximate, trifluerazine (triflumezopyrim), with methyl iodide; and other Bacillus firmus-based preparations (I-1582, BioNeem, Votivo), with the following compounds: 1-{2-fluoro-4-methyl-5-[( 2,2,2-Trifluoroethyl)sulfinyl]phenyl}-3-(trifluoromethyl)-1H-1,2,4-triazole-5-amine (from WO2006/043635) CAS 885026-50-6), {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 (from WO2003/106457) (CAS 637360-23-7), 2-chloro -N-[2-{1-[(2E)-3-(4-chlorophenyl)prop-2-en-1-yl]piperidin-4-yl}-4-(trifluoromethyl)benzene Isoniazid (from WO2006/003494) (CAS 872999-66-1), 3-(4-chloro-2,6-dimethylphenyl)-4-hydroxy-8-methoxy-1 , 8-diazaspiro[4.5]indole-3-en-2-one (from WO 2010052161) (CAS 1225292-17-0), 3-(4-chloro-2,6-dimethylphenyl carbonate) 8-methoxy-oxo-oxo-1,8-diazaspiro[4.5]dec-3-en-4-yl ester ethyl ester (from EP 2647626) (CAS-1440516-42-6 , 4-(but-2-yn-1-yloxy)-6-(3,5-dimethylpiperidin-1-yl)-5-fluoropyrimidine (from WO2004/099160) (CAS 792914-58) -0), PF1364 (from JP2010/018586) (CAS Reg. No. 1204776-60-2), N-[(2E)-1-[(6-chloropyridin-3-yl)methyl]pyridine-2 (1H)-subunit]-2,2,2-trifluoroacetamide (from WO2012/029672) (CAS 1363400-41-2), (3E)-3-[1-[(6-chloro-3) -pyridyl)methyl]-2-pyridinylene]-1,1,1-trifluoropropan-2-one (from WO 2013/144213) (CAS 1461743-15-6), N-[3-(benzene Methylamine-mercapto)-4-chlorophenyl]-1-methyl-3-(pentafluoroethyl)-4-(trifluoromethyl)-1H-pyrazole-5-carboxamide (from WO2010/051926) (CAS 1226889-14-0), 5-bromo-4-chloro-N-[4-chloro-2-methyl-6-(methylamine A) Mercapto)phenyl]-2-(3-chloro-2-pyridyl)pyrazole-3-carboxamide (from CN103232431) (CAS 1449220-44-3), 4-[5-(3,5- Dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-3-iso Azyl]-2-methyl-N-(cis-1-iodoxy-3-thietyl)benzamide, 4-[5-(3,5-dichlorophenyl) -4,5-dihydro-5-(trifluoromethyl)-3-iso Azyl]-2-methyl-N-(trans-1-oxo-3-thiat-butyl)benzamide with 4-[(5S)-5-(3,5-di Chlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-3-iso Azolyl]-2-methyl-N-(cis-1-iodoxy-3-thietanealkyl)benzamide (from WO 2013/050317 A1) (CAS 1332628-83-7) , N-[3-Chloro-1-(3-pyridyl)-1H-pyrazol-4-yl]-N-ethyl-3-[(3,3,3-trifluoropropyl)sulfinium Propionamide, (+)-N-[3-chloro-1-(3-pyridyl)-1H-pyrazol-4-yl]-N-ethyl-3-[(3,3,3 -trifluoropropyl)sulfinyl]propanamine and (-)-N-[3-chloro-1-(3-pyridyl)-1H-pyrazol-4-yl]-N-ethyl- 3-[(3,3,3-Trifluoropropyl)sulfinyl]propanamine (from WO 2013/162715 A2, WO 2013/162716 A2, US 2014/0213448 A1) (CAS 1477923-37-7 , 5-[[(2E)-3-chloro-2-propen-1-yl]amino]-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4- [(Trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (from CN 101337937A) (CAS 1105672-77-2), 3-bromo-N-[4-chloro-2-methyl -6-[(Methylamino)thiomethyl]phenyl]-1-(3-chloro-2-pyridyl)-1H-pyrazole-5-carboxamide (Liudaibenjiaxuanan from CN 103109816 A (CAS 1232543-85-9); N-[4-chloro-2-[[(1,1-dimethylethyl)amino]carbonyl]-6-methylphenyl]-1-(3) -Chloro-2-pyridyl)-3-(fluoromethoxy)-1H-pyrazole-5-carboxamide (from WO 2012/034403 A1) (CAS 1268277-22-0), N-[2-(5-Amino-1,3,4-thiadiazol-2-yl)-4-chloro-6-methylphenyl]-3-bromo-1 -(3-chloro-2-pyridyl)-1H-pyrazole-5-carboxamide (from WO 2011/085575 A1) (CAS 1233882-22-8), 4-[3-[2,6-two Chloro-4-[(3,3-dichloro-2-propen-1-yl)oxy]phenoxy]propoxy]-2-methoxy-6-(trifluoromethyl)pyrimidine (from CN 101337940 A) (CAS 1108184-52-6); (2E)- and 2(Z)-2-[2-(4-cyanophenyl)-1-[3-(trifluoromethyl)phenyl] Ethylene]-N-[4-(difluoromethoxy)phenyl]indolecarboxamide (from CN 101715774 A) (CAS 1232543-85-9); cyclopropanecarboxylic acid 3-(2,2- Dichlorovinyl)-2,2-dimethyl-4-(1H-benzimidazol-2-yl)phenyl ester (from CN 103524422 A) (CAS 1542271-46-4); (4aS)-7 -Chloro-2,5-dihydro-2-[[(methoxycarbonyl)[4-[(trifluoromethyl)sulfanyl]phenyl]amino]carbonyl]indole[1,2-e][ 1,3,4] Diazine-4a(3H)-carboxylic acid methyl ester (from CN 102391261 A) (CAS 1370358-69-2); 6-deoxy-3-O-ethyl-2,4-di-O-methyl -1-[N-[4-[1-[4-(1,1,2,2,2-pentafluoroethoxy)phenyl]-1H-1,2,4-triazol-3-yl Phenyl]carbamate]-α-L-mannopyrose (from US 2014/0275503 A1) (CAS 1181213-14-8); 8-(2-cyclopropylmethoxy-4-tris) Fluoromethylphenoxy)-3-(6-trifluoromethylpyridazin-3-yl)-3-azabicyclo[3.2.1]octane (CAS 1253850-56-4), (8-reverse Side)-8-(2-cyclopropylmethoxy-4-trifluoromethylphenoxy)-3-(6-trifluoromethylpyridazin-3-yl)-3-azabicyclo[3.2 .1] Octane (CAS 933798-27-7), (8-Ipsilateral)-8-(2-cyclopropylmethoxy-4-trifluoromethylphenoxy)-3-(6-three Fluoromethylpyridazin-3-yl)-3-azabicyclo[3.2.1]octane (from WO 2007040280 A1, WO 2007040282 A1) (CAS 934001-66-8) and N-[3-chloro-1 -(3-pyridyl)-1H-pyrazol-4-yl]-N-ethyl-3-[(3,3,3-trifluoropropyl)thio]propanamide (from WO 2015/058021 A1 WO 2015/058028 A1) (CAS 1477919-27-9).
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：「The Pesticide Manual」(British Crop Protection Council，第16版)或網際網路(例如：http：//www.alanwood.net/pesticides)。 The active compounds referred to herein by their common names are known and described, for example, in "The Pesticide Manual" (British Crop Protection Council, 16th Edition) or the Internet (for example: http://www.alanwood.net/ Pesticides).
(1)至(15)類所列之所有殺真菌混合組份若含有合適官能基時，均可視需要與合適之鹼類或酸類形成鹽類。此外，(1)至(15)類所列之所有殺真菌混合組份若可能出現互變異構性時，亦可包括互變異構型。 All of the fungicidal mixed components listed in categories (1) to (15), if appropriate functional groups, may form salts with suitable bases or acids as needed. Further, all of the fungicidal mixed components listed in the categories (1) to (15) may include tautomeric forms if they are likely to exhibit tautomerism.
1)麥角固醇生合成抑制劑，例如：(1.001)西普康唑(cyproconazole)、(1.002)吩康唑(difenoconazole)、(1.003)環氧克唑(epoxiconazole)、(1.004)吩醯胺(fenhexamide)、(1.005)芬普定(fenpropidin)、(1.006)芬普福(fenpropimorph)、(1.007)胺苯吡菌酮(fenpyrazamine)、(1.008)伏克康唑(fluquinconazole)、(1.009)護汰芬(flutriafol)、(1.010)依滅列(imazalil)、(1.011)依滅列硫酸鹽(imazalil sulphate)、(1.012)抑普康唑(ipconazole)、(1.013)滅康唑(metconazole)、(1.014)麥克坦尼(myclobutanil)、(1.015)巴克素(paclobutrazole)、(1.016)撲克樂(prochloraz)、(1.017)普克利(propiconazole)、(1.018)普賽康唑(prothioconazole)、(1.019)吡啶菌唑(pyrisoxazole)、(1.020)賜必安(spiroxamine)、(1.021)得克利(tebuconazole)、(1.022)特康唑(tetraconazole)、(1.023)三泰隆(triadimenol)、(1.024)賽得莫 (tridemorph)、(1.025)三狄康唑(triticonazole)、(1.026)(1R,2S,5S)-5-(4-氯苯甲基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇、(1.027)(1S,2R,5R)-5-(4-氯苯甲基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇、(1.028)(2R)-2-(1-氯環丙基)-4-[(1R)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.029)(2R)-2-(1-氯環丙基)-4-[(1S)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.030)(2R)-2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.031)(2S)-2-(1-氯環丙基)-4-[(1R)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.032)(2S)-2-(1-氯環丙基)-4-[(1S)-2,2-二氯環丙基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.033)(2S)-2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.034)(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、(1.035)(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、(1.036)[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、(1.037)1-({(2R,4S)-2-[2-氯-4-(4-氯苯氧基)苯基]-4-甲基-1,3-二氧雜環戊烷-2-基}甲基)-1H-1,2,4-三唑、(1.038)1-({(2S,4S)-2-[2-氯-4-(4-氯苯氧基)苯基]-4-甲基-1,3-二氧雜環戊烷-2-基}甲基)-1H-1,2,4-三唑、(1.039)硫氰酸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、(1.040)硫氰酸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、(1.041)硫氰酸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、(1.042)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、(1.043)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、(1.044)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、(1.045)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、(1.046)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、(1.047)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、(1.048)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、(1.049)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、(1.050)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、(1.051)2-[2-氯-4-(2,4-二氯苯氧基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.052)2-[2-氯-4-(4-氯苯氧基)苯基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.053)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丁-2-醇、(1.054)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)戊-2-醇、(1.055)2-[4-(4-氯苯氧基)-2-(三氟甲基)苯基]-1-(1H-1,2,4-三唑-1-基)丙-2-醇、(1.056)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、(1.057)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、(1.058)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、(1.059)5-(4-氯苯甲基)-2-(氯甲基)-2-甲基-1-(1H-1,2,4-三唑-1-基甲基)環戊醇、(1.060)5-(烯丙基硫烷基)-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、(1.061)5-(烯丙基硫烷基)-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、(1.062)5-(烯丙基硫烷基)-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、(1.063)N'-(2,5-二甲基-4-{[3-(1,1,2,2-四氟乙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基甲脒、(1.064)N'-(2,5-二甲基-4-{[3-(2,2,2-三氟乙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基甲脒、(1.065)N'-(2,5-二甲基-4-{[3-(2,2,3,3-四氟丙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基甲脒、(1.066)N'-(2,5-二甲基-4-{[3-(五氟乙氧基)苯基]硫烷基}苯基)-N-乙基-N-甲基甲脒、(1.067)N'-(2,5-二甲基-4-{3-[(1,1,2,2-四氟乙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基甲脒、(1.068)N'-(2,5-二甲基-4-{3-[(2,2,2-三氟乙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基甲脒、(1.069)N'-(2,5-二甲基-4-{3-[(2,2,3,3-四氟丙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基甲脒、(1.070)N'-(2,5-二甲基-4-{3-[(五氟乙基)硫烷基]苯氧基}苯基)-N-乙基-N-甲基甲脒、(1.071)N'-(2,5-二甲基-4-苯氧基苯基)-N-乙基-N-甲基甲脒、(1.072)N'-(4-{[3-(二氟甲氧基)苯基]硫烷基}-2,5-二甲基苯基)-N-乙基-N-甲基甲脒、(1.073)N'-(4-{3-[(二氟甲基)硫烷基]苯氧基}-2,5-二甲基苯基)-N-乙基-N-甲基甲脒、(1.074)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、(1.075)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、(1.076)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、(1.077)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、(1.078)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、(1.079)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、(1.080)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。 1) ergosterol biosynthesis inhibitors, for example: (1.001) cyproconazole, (1.002) difenoconazole, (1.003) epoxiconazole, (1.004) Amine (fenhexamide), (1.005) fenpropidin, (1.006) fenpropimorph, (1.007) fenpyrazamine, (1.008) fluquinconazole, (1.009) ) flutriafol, (1.010) imazalil, (1.011) imazalil sulphate, (1.012) ipconazole, (1.013) thiconazole (metconazole) ), (1.014) myclobutanil, (1.015) paclobutrazole, (1.016) prochloraz, (1.017) propiconazole, (1.018) prothioconazole, (1.019) pyrisoxazole, (1.020) spiroxamine, (1.021) tebuconazole, (1.022) tetraconazole, (1.023) triadimenol, (1.024) ) tridemorph, (1.025) triticonazole, (1.026) (1R, 2S, 5S)-5-(4-chlorobenzyl)-2-(chloromethyl)-2 -methyl-1-(1H-1,2,4-triazol-1-yl-methyl) Cyclopentanol, (1.027) (1S, 2R, 5R)-5-(4-chlorobenzyl)-2-(chloromethyl)-2-methyl-1-(1H-1,2, 4-triazol-1-ylmethyl)cyclopentanol, (1.028)(2R)-2-(1-chlorocyclopropyl)-4-[(1R)-2,2-dichlorocyclopropyl] 1-(1H-1,2,4-triazol-1-yl)butan-2-ol, (1.029)(2R)-2-(1-chlorocyclopropyl)-4-[(1S)- 2,2-Dichlorocyclopropyl]-1-(1H-1,2,4-triazol-1-yl)butan-2-ol, (1.030)(2R)-2-[4-(4- Chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1H-1,2,4-triazol-1-yl)propan-2-ol, (1.031)(2S)-2 -(1-chlorocyclopropyl)-4-[(1R)-2,2-dichlorocyclopropyl]-1-(1H-1,2,4-triazol-1-yl)but-2- Alcohol, (1.032)(2S)-2-(1-chlorocyclopropyl)-4-[(1S)-2,2-dichlorocyclopropyl]-1-(1H-1,2,4-tri Zin-1-yl)butan-2-ol, (1.033)(2S)-2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1H- 1,2,4-triazol-1-yl)propan-2-ol, (1.034)(R)-[3-(4-chloro-2-fluorophenyl)-5-(2,4-difluoro Phenyl)-1,2- Zin-4-yl](pyridin-3-yl)methanol, (1.035)(S)-[3-(4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)- 1,2- Zin-4-yl](pyridin-3-yl)methanol, (1.036)[3-(4-chloro-2-fluorophenyl)-5-(2,4-difluorophenyl)-1,2- Zin-4-yl](pyridin-3-yl)methanol, (1.037) 1-({(2R,4S)-2-[2-chloro-4-(4-chlorophenoxy)phenyl]-4 -methyl-1,3-dioxol-2-yl}methyl)-1H-1,2,4-triazole, (1.038) 1-({(2S,4S)-2-[ 2-Chloro-4-(4-chlorophenoxy)phenyl]-4-methyl-1,3-dioxolan-2-yl}methyl)-1H-1,2,4- Triazole, (1.039) 1-{[3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-thiocyanate 1,2,4-triazol-5-yl ester, (1.040) 1-{[rel(2R,3R)-3-(2-chlorophenyl)-2-(2,4-difluoro) thiocyanate Phenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazol-5-yl ester, (1.041) 1-{[rel(2R,3S)-3 -(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazol-5-yl ester, (1.042) 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, (1.043)2-[(2R,4R,5S)-1-(2,4-dichlorophenyl)-5- Hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.044)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, (1.045)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, (1.046) 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, (1.047)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, (1.048)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, (1.049) 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, (1.050)2-[1-(2,4 -dichlorophenyl)-5-hydroxy-2,6,6-trimethylheptan-4-yl]-2,4-dihydro-3H-1,2,4-triazole-3-thione ,(1.051)2-[2-Chloro-4-(2,4-dichlorophenoxy)phenyl]-1-(1H-1,2,4-triazol-1-yl)propan-2- Alcohol, (1.052) 2-[2-chloro-4-(4-chlorophenoxy)phenyl]-1-(1H-1,2,4-triazol-1-yl)butan-2-ol, (1.053) 2-[4-(4-Chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1H-1,2,4-triazol-1-yl)butene-2 -Alcohol, (1.054) 2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1H-1,2,4-triazole-1- Pentyl-2-ol, (1.055) 2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1H-1,2,4-triazole -1-yl)propan-2-ol, (1.056) 2-{[3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]- -2}-2,4-dihydro-3H-1,2,4-triazole-3-thione, (1.057)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, (1.058 2-{[rel(2R,3S)-3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-2,4 -dihydro-3H-1,2,4-triazole-3-thione, (1.059) 5-(4-chlorobenzyl)-2-(chloromethyl)-2-methyl-1-( 1H-1,2,4-triazol-1-ylmethyl)cyclopentanol, (1.060) 5-(allylsulfanyl)-1-{[3-(2-chlorophenyl)-2 -(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazole, (1.061) 5-(allylsulfanyl)-1 -{[rel(2R,3R)-3-(2-chlorophenyl)-2-(2,4-difluorophenyl)oxiran-2-yl]methyl}-1H-1,2 ,4-triazole, (1.062) 5-(allylsulfanyl)-1-{[rel(2R,3S)-3-(2-chlorophenyl)-2-(2,4-difluoro Phenyl)oxiran-2-yl]methyl}-1H-1,2,4-triazole, (1.063) N'-(2,5-dimethyl-4-{[3-(1 ,1,2,2-tetrafluoroethoxy)phenyl]sulfanyl}benzene )-N-ethyl-N-methylformamidine, (1.064) N'-(2,5-dimethyl-4-{[3-(2,2,2-trifluoroethoxy)phenyl ]sulfanyl}phenyl)-N-ethyl-N-methylformamidine, (1.065) N'-(2,5-dimethyl-4-{[3-(2,2,3,3) -tetrafluoropropoxy)phenyl]sulfanyl}phenyl)-N-ethyl-N-methylformamidine, (1.066) N'-(2,5-dimethyl-4-{[3 -(pentafluoroethoxy)phenyl]sulfanyl}phenyl)-N-ethyl-N-methylformamidine, (1.067) N'-(2,5-dimethyl-4-{3 -[(1,1,2,2-tetrafluoroethyl)sulfanyl]phenoxy}phenyl)-N-ethyl-N-methylformamidine, (1.068) N'-(2,5 -Dimethyl-4-{3-[(2,2,2-trifluoroethyl)sulfanyl]phenoxy}phenyl)-N-ethyl-N-methylformamidine, (1.069) N'-(2,5-Dimethyl-4-{3-[(2,2,3,3-tetrafluoropropyl)sulfanyl]phenoxy}phenyl)-N-ethyl-N -methylformamidine, (1.070) N'-(2,5-dimethyl-4-{3-[(pentafluoroethyl)sulfanyl]phenoxy}phenyl)-N-ethyl- N-methylformamidine, (1.071) N'-(2,5-dimethyl-4-phenoxyphenyl)-N-ethyl-N-methylformamidine, (1.072) N'-( 4-{[3-(Difluoromethoxy)phenyl]sulfanyl}-2,5-dimethylphenyl)-N-ethyl-N-methylformamidine, (1.073) N'- (4-{3-[(Difluoromethyl)sulfanyl]phenoxy}-2,5-dimethylphenyl) -N-ethyl-N-methylformamidine, (1.074) N'-[5-bromo-6-(2,3-dihydro-1H-indol-2-yloxy)-2-methylpyridine- 3-yl]-N-ethyl-N-methylformamidine, (1.075) N'-{4-[(4,5-dichloro-1,3-thiazol-2-yl)oxy]-2, 5-dimethylphenyl}-N-ethyl-N-methylformamidine, (1.076) N'-{5-bromo-6-[(1R)-1-(3,5-difluorophenyl) Ethoxy]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine, (1.077) N'-{5-bromo-6-[(1S)-1-( 3,5-Difluorophenyl)ethoxy]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine, (1.078) N'-{5-bromo-6- [(cis-4-isopropylcyclohexyl)oxy]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine, (1.079) N'-{5-bromo- 6-[(trans-4-isopropylcyclohexyl)oxy]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine, (1.080) N'-{5- Bromo-6-[1-(3,5-difluorophenyl)ethoxy]-2-methylpyridin-3-yl}-N-ethyl-N-methylformamidine.
2)複合物I或II之呼吸鏈抑制劑，例如：(2.001)苯索伏比(benzovindiflupyr)、(2.002)必賽吩(bixafen)、(2.003)保卡利(boscalid)、(2.004)卡布辛(carboxin)、(2.005)護派楠(fluopyram)、(2.006)護坦尼(flutolanil)、(2.007)護賽保 (fluxapyroxad)、(2.008)福滅普(furametpyr)、(2.009)抑吩滅(isofetamid)、(2.010)抑本散(isopyrazam)(反側-差向對映異構物1R,4S,9S)、(2.011)抑本散(反側-差向對映異構物1S,4R,9R)、(2.012)抑本散(反側-差向異構消旋物1RS,4SR,9SR)、(2.013)抑本散(同側-差向異構消旋物1RS,4SR,9RS與反側-差向異構消旋物1RS,4SR,9SR之混合物)、(2.014)抑本散(同側-差向對映異構物1R,4S,9R)、(2.015)抑本散(同側-差向對映異構物1S,4R,9S)、(2.016)抑本散(同側-差向異構消旋物1RS,4SR,9RS)、(2.017)本福吩(penflufen)、(2.018)本賽能(penthiopyrad)、(2.019)必福吩(pydiflumetofen)、(2.020)必福滅(pyraziflumid)、(2.021)速達散(sedaxane)、(2.022)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、(2.023)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、(2.024)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、(2.025)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、(2.026)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、(2.027)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、(2.028)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、(2.029)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、(2.030)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、(2.031)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、(2.032)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、(2.033)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、(2.034)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、(2.035)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、(2.036)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、(2.037)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、(2.038)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、(2.039)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、(2.040)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、(2.041)N-[1-(2,4-二氯苯基)-1-甲氧基丙-2-基]-3-(二氟甲基)-1-甲基-1H-吡唑-4-羧醯胺、(2.042)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、(2.043)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、(2.044)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、(2.045)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、(2.046)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、(2.047)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、(2.048)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-甲硫醯胺、(2.049)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、(2.050)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、(2.051)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、(2.052)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、(2.053)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、(2.054)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、(2.055)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、(2.056)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。 2) Respiratory chain inhibitors of complex I or II, for example: (2.001) benzovindiflupyr, (2.002) bixafen, (2.003) boscalid, (2.004) card Carboxin, (2.005) flunan (fluopyram), (2.006) flutolanil, (2.007) Guardian (fluxapyroxad), (2.008) furametpyr, (2.009) isofetamid, (2.010) isopyrazam (reverse-diverse enantiomer 1R, 4S, 9S) , (2.011) 本本散 (reverse-diverse enantiomers 1S, 4R, 9R), (2.012) osmoto (negative-episomeric racemates 1RS, 4SR, 9SR), ( 2.013) Suppressol (Isolateral-episomeric racemate 1RS, 4SR, 9RS and reverse-isomeric racemate 1RS, 4SR, 9SR mixture), (2.014) Suppressed (same side) -Differential enantiomers 1R, 4S, 9R), (2.015) Suppresses (ipsilateral-diverse enantiomers 1S, 4R, 9S), (2.016) Suppresses (isolated-difference) To the racemates 1RS, 4SR, 9RS), (2.017) penflufen, (2.018) penthiopyrad, (2.019) pydiflumetofen, (2.020) must be ( Pyraziflumid), (2.021) sedaxane, (2.022) 1,3-dimethyl-N-(1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl -1H-pyrazole-4-carboxamide, (2.023) 1,3-dimethyl-N-[(3R)-1,1,3-trimethyl-2,3-dihydro-1H-茚-4-yl]-1H-pyrazole-4-carboxamide, (2.024) 1,3-dimethyl-N-[(3S)-1,1,3-trimethyl-2,3- Dihydro-1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.025)1- 3-(3-trifluoromethyl)-N-[2'-(trifluoromethyl)biphenyl-2-yl]-1H-pyrazole-4-carboxyguanamine, (2.026) 2-fluoro-6 -(trifluoromethyl)-N-(1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl)benzamide, (2.027)3-(difluoromethyl) -1-methyl-N-(1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl)-1H-pyrazole-4-carboxamide, (2.028 3-(Difluoromethyl)-1-methyl-N-[(3R)-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1H- Pyrazole-4-carboxyguanamine, (2.029) 3-(difluoromethyl)-1-methyl-N-[(3S)-1,1,3-trimethyl-2,3-dihydro- 1H-indol-4-yl]-1H-pyrazole-4-carboxamide, (2.030) 3-(difluoromethyl)-N-(7-fluoro-1,1,3-trimethyl-2 ,3-dihydro-1H-indol-4-yl)-1-methyl-1H-pyrazole-4-carboxamide, (2.031) 3-(difluoromethyl)-N-[(3R)- 7-Fluoro-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1-methyl-1H-pyrazole-4-carboxamide, (2.032)3 -(difluoromethyl)-N-[(3S)-7-fluoro-1,1,3-trimethyl-2,3-dihydro-1H-indol-4-yl]-1-methyl- 1H-pyrazole-4-carboxyguanamine, (2.033) 5,8-difluoro-N-[2-(2-fluoro-4-{[4-(trifluoromethyl)pyridin-2-yl]oxy }phenyl)ethyl]quinazolin-4-amine, (2.034) N-(2-cyclopentyl-5-fluorobenzyl)-N-cyclopropyl-3-(difluoromethyl)- 5-fluoro-1-methyl-1H-pyridyl Oxazole-4-carboxyguanamine, (2.035) N-(2-tert-butyl -5-Methylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.036) N- (2-t-butylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxyguanamine, (2.037) N-(5-Chloro-2-ethylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxyguanamine , (2.038) N-(5-chloro-2-isopropylbenzyl)-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole- 4-carboxyguanamine, (2.039) N-[(1R,4S)-9-(dichloromethylene)-1,2,3,4-tetrahydro-1,4-methylenenaphthalene-5- 3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide, (2.040) N-[(1S,4R)-9-(dichloromethylene)- 1,2,3,4-tetrahydro-1,4-methylenenaphthalen-5-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxyguanamine, (2.041) N-[1-(2,4-Dichlorophenyl)-1-methoxypropan-2-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole- 4-carboxyguanamine, (2.042) N-[2-chloro-6-(trifluoromethyl)benzyl]-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1- Methyl-1H-pyrazole-4-carboxamide, (2.043) N-[3-chloro-2-fluoro-6-(trifluoromethyl)benzyl]-N-cyclopropyl-3-( Difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.044) N-[5-chloro -2-(Trifluoromethyl)benzyl]-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, 2.045) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-N-[5-methyl-2-(trifluoromethyl)benzyl]-1H-pyridyl Oxazole-4-carboxyguanamine, (2.046) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(2-fluoro-6-isopropylbenzyl)-1-methyl -1H-pyrazole-4-carboxamide, (2.047) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(2-isopropyl-5-methylbenzene 1-methyl-1H-pyrazole-4-carboxamide, (2.048) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(2-isopropylbenzene Methyl)-1-methyl-1H-pyrazole-4-methylthioguanamine, (2.049) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(2-isopropyl Benzylmethyl)-1-methyl-1H-pyrazole-4-carboxamide, (2.050) N-cyclopropyl-3-(difluoromethyl)-5-fluoro-N-(5-fluoro 2-isopropylbenzyl)-1-methyl-1H-pyrazole-4-carboxamide, (2.051) N-cyclopropyl-3-(difluoromethyl)-N-(2- Ethyl-4,5-dimethylbenzyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.052) N-cyclopropyl-3-(difluoromethyl) -N-(2-ethyl-5-fluorobenzyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.053) N-cyclopropyl-3- (difluoromethyl)-N-(2-ethyl-5- Benzylmethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.054) N-cyclopropyl-N-(2-cyclopropyl-5-fluorobenzyl )-3-(difluoro Methyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.055) N-cyclopropyl-N-(2-cyclopropyl-5-methylbenzyl) -3-(Difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide, (2.056) N-cyclopropyl-N-(2-cyclopropylbenzyl) --3-(Difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide.
3)複合物III之呼吸鏈抑制劑，例如：(3.001)辛唑嘧菌胺(ametoctradin)、(3.002)安美速(amisulbrom)、(3.003)亞托敏(azoxystrobin)、(3.004)甲香菌酯(coumethoxystrobin)、(3.005)丁香菌酯(coumoxystrobin)、(3.006)賽發滅(cyazofamid)、(3.007)醚菌胺(dimoxystrobin)、(3.008)烯肟菌酯(enoxastrobin)、(3.009)芬色丹(famoxadone)、(3.010)芬滅酮(fenamidone)、(3.011)吩嘧菌酯(flufenoxystrobin)、(3.012)氟嘧菌酯(fluoxastrobin)、(3.013)甲基醚菌酯(kresoxim-methyl)、(3.014)氧菌胺(metominostrobin)、(3.015)肟醚菌胺(orysastrobin)、(3.016)啶氧菌酯(picoxystrobin)、(3.017)唑菌胺酯(pyraclostrobin)、(3.018)唑胺菌酯(pyrametostrobin)、(3.019)唑菌酯(pyraoxystrobin)、(3.020)三氟敏(trifloxystrobin)、(3.021)(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、(3.022)(2E,3Z)-5-{[1-(4-氯苯基)-1H-吡唑-3-基]氧}-2-(甲氧基亞胺基)-N,3-二甲基戊-3-烯醯胺、(3.023)(2R)-2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺、(3.024)(2S)-2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺、(3.025)(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2-甲基丙酸酯、(3.026)2-{2-[(2,5-二甲基苯氧基)甲基]苯基}-2-甲氧基-N-甲基乙醯胺、(3.027)N-(3-乙基-3,5,5-三甲基環己基)-3-甲醯胺基-2-羥基苯甲醯胺、(3.028)(2E,3Z)-5-{[1-(4-氯-2-氟苯基)-1H-吡唑-3-基]氧}-2-(甲氧基亞胺基)-N,3-二甲基戊-3-烯醯胺。 3) Respiratory chain inhibitors of complex III, for example: (3.001) acetoctradin, (3.002) amisulbrom, (3.003) azoxystrobin, (3.004) carbaryl Ester (coumethoxystrobin), (3.005) coumoxystrobin, (3.006) cyazofamid, (3.007) dimoxystrobin, (3.008) enoxastrobin, (3.009) fen Famoxadone, (3.010) fenamidone, (3.011) flufenoxystrobin, (3.012) fluoxastrobin, (3.013) methylsoxim-methyl , (3.014) methotrexate (metominostrobin), (3.015) anthracycline (orysastrobin), (3.016) picoxystrobin, (3.017) pyraclostrobin (pyracostrobin), (3.018) azole Pyromtostrobin, (3.019) pyraoxystrobin, (3.020) trifloxystrobin, (3.021) (2E)-2-{2-[({[(1E)-1-(3-) {[(E)-1-Fluoro-2-phenylvinyl]oxy}phenyl)ethylidene]amino}oxy)methyl]phenyl}-2-(methoxyimino)-N -methylacetamide, (3.022)(2E,3Z)-5-{[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxy}-2-(methoxyimine Base)-N, 3-Dimethylpent-3-enylamine, (3.023)(2R)-2-{2-[(2,5-dimethylphenoxy)methyl]phenyl}-2-methoxy -N-methylacetamide, (3.024) (2S)-2-{2-[(2,5-dimethylphenoxy)methyl]phenyl}-2-methoxy-N-A Ethyl amide, (3.025) (3S, 6S, 7R, 8R)-8-benzyl-3-[({3-[(isobutyl) oxy)methoxy]-4-methoxypyridine-2 -yl}carbonyl)amino]-6-methyl-4,9-di-oxy-1,5-dioxan-7-yl 2-methylpropionate, (3.026)2- {2-[(2,5-Dimethylphenoxy)methyl]phenyl}-2-methoxy-N-methylacetamide, (3.027) N-(3-ethyl-3, 5,5-trimethylcyclohexyl)-3-carboxamido-2-hydroxybenzamide, (3.028)(2E,3Z)-5-{[1-(4-chloro-2-fluorobenzene -1H-pyrazol-3-yl]oxy}-2-(methoxyimino)-N,3-dimethylpent-3-enylamine.
4)有絲分裂與細胞分化之抑制劑，例如：(4.001)卡苯辛(carbendazim)、(4.002)地吩卡(diethofencarb)、(4.003)噻唑菌胺(ethaboxam)、(4.004)氟吡菌胺(fluopicolid)、(4.005)賓克隆(pencycuron)、(4.006)腐絕(thiabendazole)、(4.007)甲基多保淨(thiophanate-methyl)、(4.008)索醯胺(zoxamide)、(4.009)3-氯-4-(2,6-二氟苯基)-6-甲基-5-苯基噠嗪、(4.010)3-氯-5-(4-氯苯基)-4-(2,6-二氟苯基)-6-甲基噠嗪、(4.011)3-氯-5-(6-氯吡啶-3-基)-6-甲基-4-(2,4,6-三氟苯基)噠嗪、(4.012)4-(2-溴-4-氟苯基)-N-(2,6-二氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.013)4-(2-溴-4-氟苯基)-N-(2-溴-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.014)4-(2-溴-4-氟苯基)-N-(2-溴苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.015)4-(2-溴-4-氟苯基)-N-(2-氯-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.016)4-(2-溴-4-氟苯基)-N-(2-氯苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.017)4-(2-溴-4-氟苯基)-N-(2-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.018)4-(2-氯-4-氟苯基)-N-(2,6-二氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.019)4-(2-氯-4-氟苯基)-N-(2-氯-6-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.020)4-(2-氯-4-氟苯基)-N-(2-氯苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.021)4-(2-氯-4-氟苯基)-N-(2-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.022)4-(4-氯苯基)-5-(2,6-二氟苯基)-3,6-二甲基噠嗪、(4.023)N-(2-溴-6-氟苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.024)N-(2-溴苯基)-4-(2-氯-4-氟苯基)-1,3-二甲基-1H-吡唑-5-胺、(4.025)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。 4) Inhibitors of mitosis and cell differentiation, for example: (4.001) carbendazim, (4.002) diehofencarb, (4.003) ethaboxam, (4.004) fluopyram ( Fluopicolid), (4.005) pencycuron, (4.006) thiabendazole, (4.007) thiophanate-methyl, (4.008) zoxamide, (4.009) 3- Chloro-4-(2,6-difluorophenyl)-6-methyl-5-phenylpyridazine, (4.010) 3-chloro-5-(4-chlorophenyl)-4-(2,6 -difluorophenyl)-6-methylpyridazine, (4.011) 3-chloro-5-(6-chloropyridin-3-yl)-6-methyl-4-(2,4,6-trifluoro Phenyl)pyridazine, (4.012) 4-(2-bromo-4-fluorophenyl)-N-(2,6-difluorophenyl)-1,3-dimethyl-1H-pyrazole-5 -amine, (4.013) 4-(2-bromo-4-fluorophenyl)-N-(2-bromo-6-fluorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine (4.014) 4-(2-Bromo-4-fluorophenyl)-N-(2-bromophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.015)4- (2-bromo-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.016) 4-(2 -Bromo-4-fluorophenyl)-N-(2-chlorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.017) 4-(2-bromo-4-fluoro Phenyl)-N-(2-fluorophenyl)-1,3-dimethyl-1H-pyrazole-5- , (4.018) 4-(2-chloro-4-fluorophenyl)-N-(2,6-difluorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.019 4-(2-chloro-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.020)4 -(2-chloro-4-fluorophenyl)-N-(2-chlorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.021) 4-(2-chloro- 4-fluorophenyl)-N-(2-fluorophenyl)-1,3-dimethyl-1H-pyrazole-5-amine, (4.022) 4-(4-chlorophenyl)-5-( 2,6-difluorophenyl)-3,6-dimethylpyridazine, (4.023) N-(2-bromo-6-fluorophenyl)-4-(2-chloro-4-fluorophenyl) -1,3-dimethyl-1H-pyrazole-5-amine, (4.024) N-(2-bromophenyl)-4-(2-chloro-4-fluorophenyl)-1,3-di Methyl-1H-pyrazole-5-amine, (4.025) N-(4-chloro-2,6-difluorophenyl)-4-(2-chloro-4-fluorophenyl)-1,3- Dimethyl-1H-pyrazole-5-amine.
5)具有多重位點活性容量之化合物，例如：(5.001)波爾多(Bordeaux)混合物、(5.002)四氯丹(captafol)、(5.003)蓋普丹(captan)、(5.004)四氯異苯腈(chlorthalonil)、(5.005)氫氧化銅、(5.006)萘甲酸銅、(5.007)氧化銅、(5.008)鹼性氯氧化銅、(5.009)硫酸銅(2+)、(5.010)腈硫醌(dithianon)、(5.011)多 寧(dodin)、(5.012)福爾培(folpet)、(5.013)錳粉克(mancozeb)、(5.014)錳乃浦(maneb)、(5.015)滅得賴(metiram)、(5.016)滅得賴鋅鹽(zinc metiram)、(5.017)快得寧(copper oxine)、(5.018)甲基鋅乃浦(propineb)、(5.019)硫與硫製劑，包括：多硫化鈣、(5.020)得恩地(thiram)、(5.021)鋅乃浦(zineb)、(5.022)益穗(ziram)。 5) Compounds having multiple site activity capacities, for example: (5.001) Bordeaux mixture, (5.002) captafol, (5.003) captan, (5.004) tetrachloroisophthalonitrile (chlorthalonil), (5.005) copper hydroxide, (5.006) copper naphthoate, (5.007) copper oxide, (5.008) alkaline copper oxychloride, (5.009) copper sulfate (2+), (5.010) nitrile sulphide ( Dithianon), (5.011) Dodin, (5.012) folpet, (5.013) manganese powder (mancozeb), (5.014) manganese nap (maneb), (5.015) metiram (metram), (5.016) Zinc metiram, (5.017) copper oxine, (5.018) methyl zinc propofol (propineb), (5.019) sulfur and sulfur preparations, including: calcium polysulfide, (5.020) (thiram), (5.021) Zinnapu (zineb), (5.022) Yisui (ziram).
6)可啟動宿主防衛性之化合物，例如：(6.01)阿拉酸式苯(acibenzolar)-S-甲基、(6.002)異噻菌胺(isotianil)、(6.003)撲殺熱(probenazole)、(6.004)地得尼(tiadinil)。 6) Compounds capable of initiating host defense, such as: (6.01) acibenzolar-S-methyl, (6.002) isotianil, (6.003) probenazole, (6.004) ) tiadinil.
7)胺基酸與/或蛋白質生合成抑制劑，例如：(7.001)嘧菌環胺(cyprodinil)、(7.002)賜黴素(kasugamycin)、(7.003)賜黴素鹽酸鹽水合物(kasugamycin hydrochloride hydrate)、(7.004)土黴素(oxytetracycline)、(7.005)比坦尼(pyrimethanil)、(7.006)3-(5-氟-3,3,4,4-四甲基-3,4-二氫異喹啉-1-基)喹啉。 7) Amino acid and/or protein biosynthesis inhibitors, for example: (7.001) cyprodinil, (7.002) kasugamycin, (7.003) vasomycin hydrochloride hydrate (kasugamycin hydrochloride) Hydrate, (7.004) oxytetracycline, (7.005) pyridone (pyrimethanil), (7.006) 3-(5-fluoro-3,3,4,4-tetramethyl-3,4-di Hydrogen isoquinolin-1-yl)quinoline.
8)ATP生產抑制劑，例如：(8.001)矽硫吩(silthiofam)。 8) ATP production inhibitors, for example: (8.001) silthiofam.
9)細胞壁合成抑制劑，例如：(9.001)苯賽卡(benthiavalicarb)、(9.002)地滅莫(dimethomorph)、(9.003)伏莫(flumorph)、(9.004)抑發利(iprovalicarb)、(9.005)曼普胺(mandipropamid)、(9.006)丁吡嗎啉(pyrimorph)、(9.007)發利列(valifenalate)、(9.008)(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、(9.009)(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。 9) Cell wall synthesis inhibitors, for example: (9.001) benthiavalicarb, (9.002) dimethomorph, (9.003) flumorph, (9.004) iprovalicarb, (9.005) Mandipropamid, (9.006) pyrimorph, (9.007) valifenalate, (9.008) (2E)-3-(4-t-butylphenyl)-3 -(2-chloropyridin-4-yl)-1-(morpholin-4-yl)prop-2-en-1-one, (9.009) (2Z)-3-(4-tert-butylphenyl --3-(2-chloropyridin-4-yl)-1-(morpholin-4-yl)prop-2-en-1-one.
10)脂質與膜合成抑制劑，例如：(10.001)普莫卡(propamocarb)、(10.002)普莫卡鹽酸鹽(propamocarb hydrochloride)、(10.003)特克斯-甲基(tolclofos-methyl)。 10) Lipid and membrane synthesis inhibitors, for example: (10.001) propamocarb, (10.002) propamocarb hydrochloride, (10.003) tolclofos-methyl.
11)黑色素生合成抑制劑，例如：(11.001)三賽唑(tricyclazole)、(11.002){3-甲基-1-[(4-甲基苯甲醯基)胺基]丁-2-基}胺甲酸2,2,2-三氟乙基酯。 11) Melanin synthesis inhibitors, for example: (11.001) tricyclazole, (11.002) {3-methyl-1-[(4-methylbenzylidene)amino]butan-2-yl } 2,2,2-trifluoroethyl carbamate.
12)核酸合成抑制劑，例如：(12.001)本達樂(benalaxyl)、(12.002)本達樂-M(benalaxyl-M)(克拉利(kiralaxyl))、(12.003)滅達樂(metalaxyl)、(12.004)滅達樂-M(metalaxyl-M)(滅芬散(mefenoxam))。 12) Inhibitors of nucleic acid synthesis, for example: (12.001) benalaxyl, (12.002) benalaxyl-M (kiralaxyl), (12.003) metalaxyl, (12.004) Metalaxyl-M (mefenoxam).
13)訊號轉導抑制劑，例如：(13.001)護汰寧(fludioxonil)、(13.002)依普同(iprodione)、(13.003)撲滅寧(procymidone)、(13.004)丙氧喹啉(proquinazid)、(13.005)快諾芬(quinoxyfen)、(13.006)免克寧(vinclozolin)。 13) Signal transduction inhibitors, for example: (13.001) fludioxonil, (13.002) iprodione, (13.003) procymidone, (13.004) propoxyquinoline (proquinazid), (13.005) quinoxyfen, (13.006) vinclozolin.
14)可作為去偶合劑之化合物，例如：(14.001)扶吉胺(fluazinam)、(14.002)敵蟎普(meptyldinocap)。 14) A compound which can be used as a decoupling agent, for example: (14.001) fluazinam, (14.002) meptyldinocap.
15)其他化合物，例如：(15.001)離層酸、(15.002)本噻唑(benthizole)、(15.003)苯井(bethoxazine)、(15.004)卡普黴素(capsimycin)、(15.005)卡吩(carvone)、(15.006)喹啉甲硫胺酸鹽(chinomethionat)、(15.007)庫發尼(cufraneb)、(15.008)賽伏醯胺(cyflufenamid)、(15.009)西莫尼(cymoxanil)、(15.010)環丙磺草胺(cyprosulfamide)、(15.011)噻菌淨(flutianil)、(15.012)福賽得鋁(fosetyl-aluminium)、(15.013)福賽得鈣(fosetyl-calcium)、(15.014)福賽得鈉(fosetyl-sodium)、(15.015)異硫氰酸甲酯、(15.016)滅奇吩(metrafenone)、(15.017)米德黴素(mildiomycin)、(15.018)納坦黴素(natamycin)、(15.019)二甲基二硫代胺甲酸鎳、(15.020)硝基太(nitrothal)-異丙基、(15.021)歐賽保(oxamocarb)、(15.022)氧硫普靈(oxathiapiproline)、(15.023)歐芬汀(oxyfenthiin)、(15.024)五氯酚與鹽類、(15.025)膦酸與其鹽類、(15.026)霜黴威乙膦酸鹽(propamocarb-fosetylate)、(15.027)必伏農(pyriofenone)(克吩農(chlazafenon))、(15.028)特伏克(tebufloquin)、(15.029)特伏爛(tecloftalam)、(15.030)特利吩(tolnifanide)、(15.031)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、(15.032)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、(15.033)2-(6-苯甲基吡啶-2-基)喹唑啉、(15.034)2,6-二甲基-1H,5H-[1,4]二硫雜環己烯并[2,3-c：5,6-c']二吡咯-1,3,5,7(2H,6H)-四酮、(15.035)2-[3,5-雙(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-(丙-2-炔-1-基氧)苯基]-4,5-二氫-1,2-唑-3-基}-1,3-噻唑-2-基)哌啶-1-基]乙酮、(15.036)2-[3,5-雙(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-氯-6-(丙-2-炔-1-基氧)苯基]-4,5-二氫-1,2-唑-3-基}-1,3-噻唑-2-基)哌啶-1-基]乙酮、(15.037)2-[3,5-雙(二氟甲基)-1H-吡唑-1-基]-1-[4-(4-{5-[2-氟-6-(丙-2-炔-1-基氧)苯基]-4,5-二氫-1,2-唑-3-基}-1,3-噻唑-2-基)哌啶-1-基]乙酮、(15.038)2-[6-(3-氟-4-甲氧基苯基)-5-甲基吡啶-2-基]喹唑啉、(15.039)甲磺酸2-{(5R)-3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}-3-氯苯基酯、(15.040)甲磺酸2-{(5S)-3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}-3-氯苯基酯、(15.041)2-{2-[(7,8-二氟-2-甲基喹啉-3-基)氧]-6-氟苯基}丙-2-醇、(15.042)2-{2-氟-6-[(8-氟-2-甲基喹啉-3-基)氧]苯基}丙-2-醇、(15.043)甲磺酸2-{3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}-3-氯苯基酯、(15.044)甲磺酸2-{3-[2-(1-{[3,5-雙(二氟甲基)-1H-吡唑-1-基]乙醯基}哌啶-4-基)-1,3-噻唑-4-基]-4,5-二氫-1,2-唑-5-基}苯基酯、(15.045)2-苯基酚與其鹽類、(15.046)3-(4,4,5-三氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.047)3-(4,4-二氟-3,3-二甲基-3,4-二氫異喹啉-1-基)喹啉、(15.048)4-胺基-5-氟嘧啶-2-醇(互變異構形：4-胺基-5-氟嘧啶-2(1H)-酮)、(15.049)4-側氧基-4-[(2-苯基乙基)胺基]丁酸、(15.050)5-胺基-1,3,4-噻二唑-2-硫醇、(15.051)5-氯-N'-苯基-N'-(丙-2-炔-1-基)噻吩-2-磺醯基醯肼、(15.052)5-氟-2-[(4-氟苯甲基)氧]嘧啶-4-胺、(15.053)5-氟-2-[(4- 甲基苯甲基)氧]嘧啶-4-胺、(15.054)9-氟-2,2-二甲基-5-(喹啉-3-基)-2,3-二氫-1,4-苯并氧氮雜環庚烷、(15.055){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、(15.056)(2Z)-3-胺基-2-氰基-3-苯基丙烯酸乙酯、(15.057)吩嗪-1-羧酸、(15.058)3,4,5-三羥基苯甲酸丙酯、(15.059)喹啉-8-醇、(15.060)喹啉-8-醇硫酸鹽(2：1)、(15.061){6-[({[(1-甲基-1H-四唑-5-基)(苯基)亞甲基]胺基}氧)甲基]吡啶-2-基}胺甲酸第三丁酯。 15) Other compounds, for example: (15.001) lytic acid, (15.002) benzothiazole (benthizole), (15.003) benzene Well (bethoxazine), (15.004) cappmycin (capsimycin), (15.005) carvone, (15.006) quinoline thioacetate (chinomethionat), (15.007) cufraneb, ( 15.008) Cyflufenamid, (15.009) cymoxanil, (15.010) cyprosulfamide, (15.011) flutianil, (15.012) forexine ( Fosetyl-aluminium), (15.013) fosetyl-calcium, (15.014) fosetyl-sodium, (15.015) methyl isothiocyanate, (15.016) metrafenone (15.017) mildiomycin, (15.018) natamycin, (15.019) nickel dimethyldithiocarbamate, (15.020) nitrothal-isopropyl, (15.021) Oxalcarb (oxamocarb), (15.022) oxathiapiproline, (15.023) oxyfenthiin, (15.024) pentachlorophenol and salts, (15.025) phosphonic acid and its salts, (15.026) propamocarb-fosetylate, (15.027) pyrofenone (chlazafenon), (15.028) tebufloquin, (15.029) (tecloftalam), (15.030) Trinity (tolnif Anide), (15.031) 1-(4-{4-[(5R)-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, (15.032) 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 Ethyl ketone, (15.033) 2-(6-benzylpyridin-2-yl)quinazoline, (15.034) 2,6-dimethyl-1H,5H-[1,4]dithiocyclohexane Alkeno[2,3-c:5,6-c']dipyrrole-1,3,5,7(2H,6H)-tetraone, (15.035)2-[3,5-bis(difluoromethyl) -1H-pyrazol-1-yl]-1-[4-(4-{5-[2-(prop-2-yn-1-yloxy)phenyl]-4,5-dihydro- 1,2- Zyrid-3-yl}-1,3-thiazol-2-yl)piperidin-1-yl]ethanone, (15.036) 2-[3,5-bis(difluoromethyl)-1H-pyrazole- 1-yl]-1-[4-(4-{5-[2-chloro-6-(prop-2-yn-1-yloxy)phenyl]-4,5-dihydro-1,2- Zyrid-3-yl}-1,3-thiazol-2-yl)piperidin-1-yl]ethanone, (15.037) 2-[3,5-bis(difluoromethyl)-1H-pyrazole- 1-yl]-1-[4-(4-{5-[2-fluoro-6-(prop-2-yn-1-yloxy)phenyl]-4,5-dihydro-1,2- Zyrid-3-yl}-1,3-thiazol-2-yl)piperidin-1-yl]ethanone, (15.038) 2-[6-(3-fluoro-4-methoxyphenyl)-5 -methylpyridin-2-yl]quinazoline, (15.039) 2-{(5R)-3-[2-(1-{[3,5-bis(difluoromethyl)-1H-) Pyrazol-1-yl]ethenyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2- Zyrid-5-yl}-3-chlorophenyl ester, (15.040) 2-{(5S)-3-[2-(1-{[3,5-bis(difluoromethyl)-1H) methanesulfonate -pyrazol-1-yl]ethenyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2- Zyrid-5-yl}-3-chlorophenyl ester, (15.041) 2-{2-[(7,8-difluoro-2-methylquinolin-3-yl)oxy]-6-fluorophenyl }propan-2-ol, (15.042) 2-{2-fluoro-6-[(8-fluoro-2-methylquinolin-3-yl)oxy]phenyl}propan-2-ol, (15.043) 2-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]ethenyl}piperidin-4-yl)-1 methanesulfonate ,3-thiazol-4-yl]-4,5-dihydro-1,2- Zyrid-5-yl}-3-chlorophenyl ester, (15.044) 2-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazole- 1-yl]ethinyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2- Oxazol-5-yl}phenyl ester, (15.045) 2-phenylphenol and its salts, (15.046) 3-(4,4,5-trifluoro-3,3-dimethyl-3,4-di Hydrogen isoquinolin-1-yl)quinoline, (15.047) 3-(4,4-difluoro-3,3-dimethyl-3,4-dihydroisoquinolin-1-yl)quinoline, (15.048) 4-Amino-5-fluoropyrimidin-2-ol (tautomeric form: 4-amino-5-fluoropyrimidine-2(1H)-one), (15.049) 4-sided oxy-4 -[(2-phenylethyl)amino]butyric acid, (15.050) 5-amino-1,3,4-thiadiazole-2-thiol, (15.051) 5-chloro-N'-benzene -N'-(prop-2-yn-1-yl)thiophene-2-sulfonylhydrazine, (15.052) 5-fluoro-2-[(4-fluorobenzyl)oxy]pyrimidine-4- Amine, (15.053) 5-fluoro-2-[(4-methylbenzyl)oxy]pyrimidine-4-amine, (15.054) 9-fluoro-2,2-dimethyl-5-(quinoline- 3-yl)-2,3-dihydro-1,4-benzoxazepine, (15.055) {6-[({[(Z)-(1-methyl-1H-tetrazole-) 5-yl)(phenyl)methylene]amino}oxy}methyl]pyridin-2-yl}aminecarboxylic acid,but-3-yn-1-yl, (15.056)(2Z)-3-amino Ethyl 2-cyano-3-phenylacrylate, (15.057) phenazine-1-carboxylic acid, (15.058) propyl 3,4,5-trihydroxybenzoate, (15.059) quinoline-8-ol , (15.060) quinoline-8-ol sulfate (2:1), (15.061) {6-[({[(1-methyl-1H-tetrazole-5-) ) (Phenyl) methylene] amino} oxy) methyl] pyridin-2-yl} amine acid tert-butyl ester.
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.
此等已用為或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)，尤指仙人掌桿菌(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)，尤指菌株GB34(登錄號ATCC 700814)與菌株QST2808(登錄號NRRL B-30087)，或枯草桿菌(Bacillus subtilis)，尤指菌株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)，尤指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.aizawai)，尤指菌株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 are available with or examples of bacteria as biological pesticides as: liquefaction of starch Bacillus (Bacillus amyloliquefaciens) strain FZB42 (DSM 231179), or Bacillus cereus (Bacillus cereus), especially Bacillus cereus (B. cereus) Strain CNCM I-1562 or Bacillus firmus strain I-1582 (accession number CNCM I-1582) or Bacillus pumilus , especially strain GB34 (accession number ATCC 700814) and strain QST2808 (accession number) NRRL B-30087), or Bacillus subtilis , especially 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 , especially B. thuringiensis subspecies israelensis (serotype H-14), strain AM65-52 (login No. ATCC 1276), or B. thuringiensis subsp . aizawai , especially strain ABTS-1857 (SD-1372), or Bacillus thuringiensis Kusta subspecies ( B.thuringiensis subsp.kurstaki) strain HD-1, or Bacillus thuringiensis subsp Insecticidal (B.thuringiensis subsp. Tenebrionis) strain NB 176 (SD-5428), Pasteurella puncture (Pasteuria penetrans), Pasteur 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除害劑之真菌及酵母實例為：巴氏蠶白僵菌(Beauveria bassiana)，尤指菌株ATCC 74040；微坦盾殼黴(Coniothyrium minitans)，尤指菌株CON/M/91-8(登錄號DSM-9660)；輪枝菌屬(Lecanicilliumspp.)，尤指菌株HRO LEC 12；蠟蚧輪枝菌(Lecanicillium lecanii)(過去稱為Verticillium lecanii)，尤指菌株KV01；黑殭菌(Metarhizium anisopliae)，尤指菌株F52(DSM3884/ATCC 90448)；核果梅奇酵母(Metschnikowia fructicola)，尤指菌株NRRL Y-30752；玫煙色擬青黴(Paecilomyces fumosoroseus)(新名稱：玫煙色棒束孢(Isaria fumosorosea))，尤指菌株IFPC 200613，或菌株Apopka 97(登錄號ATCC 20874)；淡紫色擬青黴(Paecilomyces lilacinus)，尤指淡紫色擬青黴(P.lilacinus)菌株251(AGAL 89/030550)；大孢籃狀菌(Talaromyces flavus)，尤指菌株V117b；深綠木黴(Trichoderma atroviride)，尤指菌株SC1(登錄號CBS 122089)；哈茨木黴(Trichoderma harzianum)，尤指哈茨木黴(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 pesticides are: Beauveria bassiana , especially strain ATCC 74040; Coniothyrium minitans , especially strains. CON/M/91-8 (accession number DSM-9660); Lecanicilliumspp. , especially strain HRO LEC 12; Lecanicillium lecanii (formerly known as Verticillium lecanii ), especially Strain KV01; Metarhizium anisopliae , especially strain F52 (DSM3884/ATCC 90448); Metschnikowia fructicola , especially strain NRRL Y-30752; Paecilomyces fumosoroseus (new Name: Isaria fumosorosea ), especially strain IFPC 200613, or strain Apopka 97 (accession number ATCC 20874); Paecilomyces lilacinus , especially Paecilomyces lilacinus ( P. lilacinus ) Strain 251 (AGAL 89/030550); Talaromyces flavus , especially strain V117b; Trichoderma atroviride , especially strain SC1 (accession number CBS 122089); Trichoderma Harzianu m ), especially T. harzianum rifai T39 (accession number CNCM I-952).
此等已用為或可用為生物性除害劑之病毒實例為：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 pesticides 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「接種劑(inoculant)」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。可述及之實例為：土壤桿菌屬(Agrobacterium spp.)、甘藍固氮根瘤菌(Azorkizobium 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 "inoculants" to plants or plant parts or plant organs, and uses its special properties to promote plant growth and plant health. Examples which may be mentioned are: Agrobacterium spp. , Azorkizobium caulinodans , Azospirillum spp. , Azotobacter spp. , and slow-growing Rhizobium ( Bradyrhizobium spp. ), Burkholderia spp. (especially Burkholderia cepacia (formerly known as Pseudomonas cepacia )), genus Corydalis ( Gigaspora spp. ) or Gigaspora monosporum , Glomus spp. , Laccaria spp. , Lactobacillus buchneri , Glomus Genus ( 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(rotenone)、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，尤指油菜籽粉或芥末粉。 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, 百里Phenol, Triact 70, TriCon, Tropaeulum majus, Urtica dioica, Veratrin, Viscum album, Cruciferous extract, especially 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、甜椒、胡瓜、甜瓜、胡蘿蔔、西瓜、洋蔥、萵苣、菠菜、大葱、豆類、十字花科蔬菜(例如：大白菜)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，植物意指所有發展階段，如：種子、幼苗、幼株(未成熟)、直到且包括成熟植物。應咸瞭解，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或收成之植株部份，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) , corn, soybeans, potatoes, beets, sugar cane, tomatoes, sweet peppers, courgettes, melons, carrots, watermelons, onions, lettuce, spinach, scallions, beans, cruciferous vegetables (eg, Chinese cabbage) 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 plants mean all stages of development, such as: seeds, seedlings, young plants (immature), up to and including mature plants. It should be understood that the plant part means the plant All aboveground and underground parts and organs, such as buds, leaves, flowers and roots, examples can be described: broadleaf, needles, stems, trunks, flowers, fruit bodies, fruits and seeds, and roots, bulbs, and rhizome. The plant part also includes the harvested plant or harvested plant parts, 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、棲息地或庫存空間，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，尤其處理種子時，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, habitat or stock space, for example: soaking, spraying, evaporating, atomizing, Spreading, painting, injecting, and applying the propagation material, especially when treating the seed, may also apply one or more layers of coating.
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 are treated, or those obtained by conventional biological breeding methods (eg, mating method or protoplast fusion method), and 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(glyphosate)或草銨膦(phosphonotricin)之耐受性(例如：「PAT」基因)。此等賦與所需性質(「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 include all plants that receive genetic material that confers a particularly advantageous property ("trait") through a genetic modification process. 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 special emphasis Examples of such properties are to enhance 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 (eg, gene 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, crickets and snails Further utilizing, for example, acquired plant resistance (SAR), systemin, phytoalexins, elicitors and resistance genes, and corresponding proteins and toxins to enhance plant resistance to plants Resistance to pathogenic fungi, bacteria and/or viruses also increases the resistance of plants to certain herbicidal active compounds such as imidazolinones, sulfonium ureas, glyphosate or phosphonotricin Receptive (eg "PAT" gene). These genes, which confer the desired properties ("traits"), 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. 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時，係採用習知處理法直接處理或作用在其周圍、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，亦可採用乾式種子處理法、濕式種子處理法、漿式處理法、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。 When the plant and plant parts are treated with the compound of formula (I), they are directly treated or applied to the surrounding, habitat or stock space by conventional treatment methods, such as: soaking, spraying, spraying, pouring, evaporating, dusting, fogging. Dispensing, spreading, foaming, painting, spreading, injecting, watering (pouring), drip irrigation, when processing propagation materials, when it is specifically treated with seeds, dry seed treatment, wet seed treatment, Slurry treatment, encapsulation, 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。因此可由式(I)化合物作用在植物所在地來處理植物。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 therefore be treated by the action of a compound of formula (I) at 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，但不讓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 attack by the animal pest, but 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 a method of treating a seed with a compound of formula (I) to protect the seed from the germinating plant 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根據本發明式(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 according to the compound of the formula (I) according to the invention in order 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 also relates 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.
本發明進一步有關一種種子，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。 The invention further 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.
當式(I)化合物具全株作用性時，其優點之一在於經過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。 When the compound of the formula (I) has a whole plant activity, one of the advantages is that the treated seed not only protects the seed itself, but also protects the seed from growing into a plant after the seed is unearthed, and is resistant to animal pests. 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 tomato, hu Seeds of melons, 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。此時涉及之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，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. The plant seeds involved at this point typically comprise 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 organisms, such as: Bacillus (Bacillus), Rhizobium (with Rhizobium), Pseudomonas (of Pseudomonas), Serratia (SERRATIA), Trichoderma ( Trichoderma ), Clavibacter , Glomus or 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：已吸水至稻胚胎特定階段(“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 treating rice seeds, for example, seeds that have been absorbed to a specific stage of the rice embryo ("chicken chest stage") can be used 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 into a common seed dressing formulation, such as: solution, emulsion, suspension Other coating compositions of liquids, powders, foaming agents, slurries 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、勻散劑、乳化劑、消泡劑、防腐劑、二次增稠劑、膠黏劑、赤黴素，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。其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。 The dyes which may be included in the seed dressing formulations which can be used in accordance with the invention are all dyes commonly 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 thereof 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勻散劑與/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勻散劑。較佳為使用非離子性或陰離子性勻散劑或非離子性或陰離子性勻散劑之混合物。合適之非離子性勻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。合適之陰離子性勻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 nonionic or anionic dispersing agent or a mixture of nonionic or anionic dispersing agents. Suitable nonionic dispersing agents include, in particular, ethylene oxide/propylene oxide block polymers, alkylphenol polyglycol ethers and tristyrylphenol polyglycol ethers, and phosphorylated or sulfated derivatives thereof. Suitable anionic dispersing agents especially refer to 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黴素較佳為赤黴素A1、A3(=赤黴酸)、A4與A7；以使用赤黴酸特別佳。該赤黴素係已知者(參見R.Wegler之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. The gibberellin is known (see Chemie der Pflanzenschutz-und Schädlingsbekämpfungsmittel, Vol. 2, Springer Verlag, 1970, pp. 401-412 by R. Wegler).
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, Seeds of sunflower, soybeans and beets, or seeds of various 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加水製成之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 formulation or the water-added application form which can be used according to the invention is used for the treatment of seeds, all suitable mixing devices which are commonly used 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 0.01 per kg of seed. Between 15 grams.
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；或禽類，如：火雞、鴨、鵝，及尤指雞；或魚類或甲殼類，例如：水產養殖，或可能為昆蟲，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; or poultry such as turkeys, ducks, geese, and especially Chicken; or fish or crustaceans, for example: aquaculture, or possibly 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, caged birds, reptiles, amphibians, or fish in aquaria.
明確具體實施例中，式(I)化合物係投與哺乳動物。 In a specific embodiment, the compound of formula (I) is administered to a mammal.
另一項明確具體實施例中，式(I)化合物係投與鳥類，亦即籠內的鳥，或尤指禽類。 In another specific embodiment, the compound of formula (I) is administered to a bird, that is, a bird in a cage, or especially a bird.
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, The parasites are reduced to harmlessness. More specifically, "control" as used herein refers to a compound of formula (I) that kills, inhibits, or inhibits the growth of various parasites.
節肢動物包括(但不限於)：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.)與管蝨屬(Solenopotes spp.)；食毛目(Mallophagida)及鈍角亞目(Amblycerina)與細角亞目(Ischnocerina)，例如：羽蝨屬(Bovicola spp.)、食蟲虻屬(Damalina spp.)、貓羽蝨屬(Felicola spp.)、毛虱屬(Lepikentron spp.)、雞蝨屬(Menopon spp.)、獸鳥蝨屬(Trichodectes spp.)、毛鳥蝨屬(Trimenopon spp.)、巨毛蝨屬(Trinoton spp.)、嚼蝨屬(Werneckiella 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.)、黃虻屬(Atylotus spp.)、蜂虱屬(Braula spp.)、麗蠅屬(Calliphora spp.)、金蠅屬(Chrysomyia spp.)、(Chrysops spp.)、庫蚊屬(Culex spp.)、蚊屬(Culicoides spp.)、真蚋屬(Eusimulium spp.)、廄蠅屬(Fannia spp.)、胃蠅屬(Gasterophilus spp.)、舌蠅屬(Glossina spp.)、血蠅屬(Haematobia spp.)、麻翅虻屬(Haematopota spp.)、蝨蠅屬(Hippobosca spp.)、皮蠅屬(Hypoderma spp.)、齒股蠅屬(Hydrotaea spp.)、瘤虻屬(Hybomitra spp.)、蝨蠅屬(Lipoptena spp.)、綠蠅屬(Lucilia spp.)、沙蠅屬(Lutzomyia spp.)、羊蝨蠅屬(Melophagus spp.)、莫蠅屬(Morellia spp.)、家蠅屬(Musca spp.)、斑虻屬蚋屬(Odagmia spp.)、狂蠅屬(Oestrus spp.)、Philipomyia屬、白蛉屬(Phlebotomus spp.)、鼻狂蠅屬(Rhinoestrus spp.)、麻蠅屬(Sarcophaga spp.)、蚋蚊屬(Simulium spp.)、螫蠅屬(Stomoxys spp.)、虻屬(Tabanus spp.)、大蚊屬(Tipula spp.)、維蚋屬(Wilhelmia spp.)、肉蠅屬(Wohlfahrtia spp.)； 蚤目(Siphonapterida)，例如：角葉蚤屬(Ceratophyllus spp.)、櫛頭蚤屬(Ctenocephalides spp.)、蚤屬(Pulex spp.)、潛蚤屬(Tunga spp.)、鼠蚤屬(Xenopsylla spp.)；異翅目(Heteropterida)，例如：臭蟲屬(Cimex spp.)、金圓蝽屬(Panstrongylus spp.)、紅腹獵蝽屬(Rhodnius spp.)、錐蝽屬(Triatoma spp.)；及蜚蠊目(Blattaria)之擾人及衛生害蟲。 Arthropods include (but are not limited to): Anoplurida, for example: Haematopinus spp., Linognathus spp., Pediculus spp., Phyrrus Spp.) and Solenopotes spp.; Mallophagida and Amblycerina and Ischnocerina, for example: Bovicola spp., Carnivora (Damalina spp.), Felicola spp., Lepikentron spp., Menopon spp., Trichodectes spp., Trimenopon spp .), Trinoton spp., Werneckiella spp.; Diptera and Nematocerina and Brachycerina, eg Aedes (Aedes spp.), Anopheles spp., Atylotus spp., Braula spp., Calliphora spp., Chrysomyia spp. (Chrysops spp.), Culex spp., Culicoides spp., Eusimulium spp., Fannia spp., Gasterophilus spp. Glossina sp. p.), Haematobia spp., Haematopota spp., Hippotosca spp., Hypoderma spp., Hydrotaea spp. , Hybomitra spp., Lipoptena spp., Lucilia spp., Lutzomyia spp., Melophagus spp., Mosquito (Morellia spp.), Musca spp., Odagmia spp., Oestrus spp., Philipomyia, Phlebotomus spp., nose flies Genus (Rhinoestrus spp.), Sarcophaga spp., Simulium spp., Stomoxys spp., Tabanus spp., Tipula spp. Wilhelmia spp., Wohlfahrtia spp.; From the order of Siphonapterida, for example: Ceratophyllus spp., Ctenocephalides spp., Pulex spp., Tunga spp., Xenopsylla Spp.); Heteropterida, for example: Cimex spp., Panstrongylus spp., Rhodnius spp., Triatoma spp. And the eyewitness (Blattaria) disturbing people and sanitary pests.
此外，可述及之節肢動物實例為下列蜱蟲(Acari)：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：花蜱屬(Amblyomma spp.)、革蜱屬(Dermacentor spp.)、血蜱屬(Haemophysalis spp.)、璃眼蜱屬(Hyalomma spp.)、硬蜱屬(Ixodes spp.)、扇頭蜱(Rhipicephalus(牛蜱(Boophilus))屬、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.)、禽剌蟎屬(Ornithonyssus spp.)、肺刺蟎屬(Pneumonyssus spp.)、耳蟎屬(Raillietia spp.)、胸孔蟎屬(Sternostoma spp.)、Tropilaelaps spp.，、瓦蟎屬(Varroa spp.)；光芒蟲亞目(Actinedida)(前氣亞目(Prostigmata))，例如：蜂蟎屬(Acarapis spp.)、姬墊蟎屬(Cheyletiella spp.)、脂蟎屬(Demodex spp.)、螫蟎屬(Listrophorus spp.)、肉蟎屬(Myobia spp.)、新恙蟎屬(Neotrombicula spp.)、禽螫蟎屬(Ornithocheyletia spp.)、綿羊疥蟎屬(Psorergates spp.)、恙蟎屬(Trombicula spp.)；及粉蟎亞目(Acaridida)(無氣亞目(Astigmata))，例如：粉蟎屬(Acarus spp.)、嗜木蟎屬(Caloglyphus spp.)、皮蟎屬(Chorioptes spp.)、雞蟎屬(Cytodites spp.)、皮頸下蟎屬(Hypodectes spp.)、鳥疥蟎屬(Knemidocoptes spp.)、雞雛蟎屬(Laminosioptes spp.)、耳蟎屬(Notoedres spp.)、耳蟎屬(Otodectes spp.)、癢蟎屬(Psoroptes spp.)、翼蟎屬 (Pterolichus spp.)、疥蟎屬(Sarcoptes spp.)、疥癬恙蟲屬(Trixacarus spp.)、食酪蟎屬(Tyrophagus spp.)。 Further, examples of arthropods that may be mentioned are the following aphids: Acari (Acarina) and Metastigmata, for example: Argasidae ), such as: Argas spp., Ornithodorus spp., Otobius spp.; Ixodidae, such as: Amblyomma spp. ), Dermacentor spp., Haemophysalis spp., Hyalomma spp., Ixodes spp., Rhipicephalus (Boophilus) ) genus, Rhipicephalus spp. (the original genus of multiple hosts); Mesostigmata, such as Dermanyssus spp., Ornithonyssus spp. ), Pneumonyssus spp., Raillietia spp., Sternostoma spp., Tropilaelaps spp., Varroa spp.; Actinedida) (Prostigmata), for example: Acarapis spp., Cheyletiella spp., Demodex spp., Listrophorus spp. Genus Obia spp.), Neotrombicula spp., Ornithocheyletia spp., Psorergates spp., Trombula spp.; and whitefly ( Acaridida) (Astigmata), for example: Acarus spp., Caloglyphus spp., Chorioptes spp., Cytodites spp. , Hypodectes spp., Knemidocoptes spp., Laminosioptes spp., Notoedres spp., Otodectes spp., itching Genus (Psoroptes spp.), genus (Pterolichus spp.), genus Sarcoptes spp., Trixacarus spp., Tyrophagus spp.
寄生性原蟲實例包括(但不限於)：鞭毛門(Mastigophora)(鞭毛動物綱(Flagellata))，如：後滴門(Metamonada)：雙滴蟲目(Diplomonadida)，例如：賈第氏滴蟲屬(Giardia spp.)、旋核蟲屬(Spironucleus spp.)副基體綱(Parabasala)：毛滴蟲目(Trichomonadida)，例如：組織鞭毛蟲屬(Histomonas spp.)、五毛滴蟲屬(Pentatrichomonas spp.)、四毛滴蟲屬(Tetratrichomonas spp.)、毛滴蟲屬(Trichomonas spp.)、三毛滴蟲屬(Tritrichomonas spp.)眼蟲門(Euglenozoa)：錐蟲科(Trypanosomatida)，例如：利什曼原蟲屬(Leishmania spp.)、錐蟲屬(Trypanosoma spp.)肉質鞭毛蟲門(Sarcomastigophora)((根足蟲綱(Rhizopoda))，如：內阿米巴科(Entamoebidae)(例如：阿米巴蟲屬(Entamoeba spp.))、阿米巴目(Centramoebidae)(例如：棘阿米巴屬(Acanthamoeba sp.))、真變形目(Euamoebidae)(例如：哈曼原蟲屬(Harmanella sp.))。囊泡蟲總門(Alveolata)，如：頂複合器門(Apicomplexa)(孢子蟲綱(Sporozoa))，例如：隱孢子蟲屬(Cryptosporidium spp.)；艾美球蟲目(Eimeriida)，例如：貝斯諾孢子蟲屬(Besnoitia spp.)、囊等孢子球蟲屬(Cystoisospora spp.)、艾美球蟲屬(Eimeria spp.)、哈芒球蟲屬(Hammondia spp.)、等孢球蟲屬(Isospora spp.)、新孢子蟲屬(Neospora spp.)、肉孢子蟲屬(Sarcocystis spp.)、弓形蟲屬(Toxoplasma spp.)；住血胞子蟲目(Adeleida)，例如：肝簇蟲屬(Hepatozoon spp.)、球蟲屬(Klossiella spp.)；血孢子蟲目(Haemosporida)，例如：住白細胞原蟲屬(Leucocytozoon spp.)、鼠瘧原蟲屬(Plasmodium spp.)；梨形蟲目 (Piroplasmida)，例如：焦蟲屬(Babesia spp.)、纖毛蟲屬(Ciliophora spp.)、Echinozoon屬、泰勒蟲屬(Theileria spp.)；Vesibuliferida目，例如：腸袋蟲屬(Balantidium spp.)、布克斯頓纖毛蟲屬(Buxtonella spp.)微孢子亞門(Microspora)，如：微孢子蟲屬(Encephalitozoon spp.)、腸胞蟲屬(Enterocytozoon spp.)、球蟲屬(Globidium spp.)、微孢子蟲屬(Nosema spp.)、與例如：黏體動物門(Myxozoa spp.) Examples of parasitic protozoa include, but are not limited to, Mastigophora (Flagellata), such as: Metamonada: Diplomonadida, for example: Trichomonas sinensis Genusia spp., Parasala of the genus Spironcleus spp.: Trichomonadida, for example: Histomonas spp., Pentatricomonas spp .), Tetratrichomonas spp., Trichomonas spp., Tritrichomonas spp. Euglenozoa: Trypanosomatida, for example: Leishmania spp., Trypanosoma spp. Sarcomastigophora (Rhizopoda), such as Entamoebidae (eg : Entamoeba spp.), Centramoebidae (eg Acanthamoeba sp.), Euamoebidae (eg Harmania) Harmanella sp.)) Alveolata, such as the Apicomplexa (Sporozoa), Such as: Cryptosporidium spp.; Eimeriida, for example: Besnoitia spp., Cystoisospora spp., Eimeria Genus (Eimeria spp.), Hammondia spp., Isospora spp., Neospora spp., Sarcocystis spp., arch Toxoplasma spp.; Adeleida, for example: Hepatozoon spp., Klossiella spp.; Haemosporida, for example: living leukocytes Leucocytozoon spp., Plasmodium spp.; Pear-like (Piroplasmida), for example: Babesia spp., Ciliophora spp., Echinozoon genus, Theileria spp.; Vesibuliferida, for example: Balantidium spp. , Buxtonella spp. Microspora, such as: Encephalitozoon spp., Enterocytozoon spp., Globidium spp. ), Nosema spp., and, for example, Myxozoa spp.
成為人類或動物之病原菌之蠕蟲包括例如：棘頭動物(Acanthocephala)、線蟲動物門(Nematoden)、舌形動物門(Pentastoma)與扁形動物門(Platyhelminthes)(例如：單殖吸蟲亞綱(Monogenea)、絛蟲(cestodes)與複殖吸蟲(trematodes))。 Worm that becomes a pathogen of human or animal species includes, for example, Acanthocephala, Nematoden, Pentastoma, and Platyhelminthes (eg, Monogonella) Monogenea), cestodes and trematodes.
蠕蟲實例包括(但不限於)：單殖吸蟲亞綱(Monogenea)：例如：指標蟲屬(Dactylogyrus spp.)、三代蟲屬(Gyrodactylus spp.)、小盤吸蟲屬(Microbothrium spp.)、多盤吸蟲屬(Polystoma spp.)、Troglecephalus屬；絛蟲：擬葉目(Pseudophyllidea)，例如：吸葉絛蟲屬(Bothridium spp.)、廣節裂頭絛蟲屬(Diphyllobothrium spp.)、大複殖門絛蟲屬(Diplogonoporus spp.)、Ichthyobothrium屬、舌狀絛蟲屬(Ligula spp.)、裂頭絛蟲屬(Schistocephalus spp.)、裂頭蟲屬(Schistocephalus spp).、螺旋體蟲屬(Spirometra spp.)；圓葉目(Cyclophyllida)，例如：安迪亞絛蟲屬(Andyra spp.)、裸頭絛蟲屬(Anoplocephala spp.)、無卵黃腺絛蟲(Avitellina spp.)、伯特絛蟲屬(Bertiella spp.)、錫帶絛蟲屬(Cittotaenia spp.)、戴文絛蟲屬(Davainea spp.)、迪克氏絛蟲屬(Diochis spp.)、雙孔絛蟲屬(Diplopylidium spp.)、瓜實絛蟲屬(Dipylidium spp.)、棘球絛蟲屬(Echinococcus spp.)、棘葉絛蟲屬(Echinocotyle spp.)、瘍棘殼絛蟲屬(Echinolepis spp.)、泡尾絛蟲屬(Hydatigera spp.)、包膜絛蟲屬 (Hymenolepis spp.)、約優克斯絛蟲屬(Joyeuxiella spp.)、中殖孔屬絛蟲屬(Mesocestoides spp.)、莫尼茨絛蟲屬(Moniezia spp.)、副裸頭絛蟲屬(Paranoplocephala spp.)、雷氏絛蟲屬(Raillietina spp.)、史提拉絛蟲屬(Stilesia spp.)、絛蟲屬(Taenia spp.)、曲子官絛蟲屬(Thysaniezia spp.)、隧體絛蟲屬(Thysanosoma spp.)複殖吸蟲：複殖綱(Digenea)，例如：澳畢吸蟲屬(Austrobilharzia spp.)、短咽吸蟲屬(Brachylaima spp.)、杯殖吸蟲屬(Calicophoron spp.)、下彎吸蟲屬(Catatropis spp.)、支睪吸蟲屬(Clonorchis spp.)、肛瘤吸蟲屬(Collyriclum spp.)、盤吸蟲屬(Cotylophoron spp.)、環腸吸蟲屬(Cyclocoelum spp.)、雙腔吸蟲屬(Dicrocoelium spp.)複口吸蟲屬(Diplostomum spp.)、棘隙吸蟲屬(Echinochasmus spp.)、棘緣吸蟲屬(Echinoparyphium spp.)、棘口吸蟲屬(Echinostoma spp.)、闊盤吸蟲屬(Eurytrema spp.)、肝吸蟲屬(Fasciola spp.)、擬片形吸蟲屬(Fasciolides spp.)、薑片蟲屬(Fasciolopsis spp.)、菲策吸蟲屬(Fischoederius spp.)、腹袋吸蟲屬(Gastrothylacus spp.)、巨畢吸蟲屬(Gigantobilharzia spp.)、巨盤吸蟲屬(Gigantocotyle spp.)、異形吸蟲屬(Heterophyes spp.)、低頸吸蟲屬(Hypoderaeum spp.)、彩蚴吸蟲屬(Leucochloridium spp.)、後殖吸蟲屬(Metagonimus spp.)、次睾吸蟲屬(Metorchis spp.)、隱孔吸蟲屬(Nanophyetus spp.)、背孔吸蟲屬(Notocotylus spp.)、後睾吸蟲屬(Opisthorchis spp.)、毛樣線蟲屬(Ornithobilharzia spp.)、並殖吸蟲屬(Paragonimus spp.)、雙口吸蟲屬(Paramphistomum spp.)、斜睾吸蟲屬(Plagiorchis spp.)、莖雙穴吸蟲屬(Posthodiplostomum spp.)、前殖吸蟲屬(Prosthogonimus spp.)、血吸蟲屬(Schistosoma spp.)、毛畢屬(Trichobilharzia spp.)、鮭吸蟲屬(Troglotrema spp.)、盲腔屬(Typhlocoelum spp.)線蟲：毛形亞目(Trichinellida)，例如：毛細線蟲屬(Capillaria spp.)、旋毛蟲 屬(Trichinella spp.)、線蟲屬(Trichomosoides spp.)、毛首線蟲屬(Trichuris spp.)墊刃目(Tylenchida)，例如：細頸線蟲屬(Micronema spp.)、副糞桿線蟲屬(Parastrangyloides spp.)、糞桿線蟲屬(Strongyloides spp.)小桿亞目(Rhabditina)，例如：住血線蟲屬(Angiostrongylus spp.)、裂口線蟲屬(Amidostomum spp.)、鉤蟲屬(Ancylostoma spp.)、住血線蟲屬(Angiostrongylus spp.)、Bronchonema屬、仰口線蟲屬(Bunostomum spp.)、腸線蟲屬(Chabertia spp.)、古柏線蟲屬(Cooperia spp.)、Cooperioides spp.、環體線蟲屬(Crenosoma spp.)、節蟲屬(Cyathostomum spp.)、線蟲屬(Cyclococercus spp.)、環齒口鉤蟲屬(Cyclodontostomum spp.)、杯環線蟲屬(Cylicocyclus spp.)、杯冠線蟲屬(Cylicostephanus spp.)、柱咽線蟲屬(Cylindropharynx spp.)、囊尾線蟲屬(Cystocaulus spp.)、網尾線蟲屬(Dictyocaulus spp.)、鹿圓線蟲屬(Elaphostrongylus spp.)、類絲線蟲屬(Filaroides spp.)、球首線蟲屬(Globocephalus spp.)、毛樣線蟲屬(Graphidium spp.)、輻首線蟲屬(Gyalocephalus spp.)、血矛線蟲屬(Haemonchus spp.)、螺旋線蟲屬(Heligmosomoides spp.)、胃圓線蟲屬(Hyostrongylus spp.)、馬歇爾線蟲屬(Marshallagia spp.)、後圓線蟲屬(Metastrongylus spp.)、繆勒線蟲屬(Muellerius spp.)、鉤蟲屬(Necator spp.)、細頸線蟲屬(Nematodirus spp.)、新圓線蟲屬(Neostrongylus spp.)、日圓線蟲屬(Nippostrongylus spp.)、尖頭胃線蟲屬(Obeliscoides spp.)、食道齒線蟲屬(Oesophagodontus spp.)、結線蟲屬(Oesophagostomum spp.)、壺肛線蟲屬(Ollulanus spp.)、圓蟲屬(Ornithostrongylus spp.)、奧斯勒絲蟲屬(Oslerus spp.)、胃絲蟲屬(Ostertagia spp.)、副古柏線蟲屬(Paracooperia spp.)、副環體線蟲屬(Paracrenosoma spp.)、副類絲線蟲屬(Parafilaroides spp.)、副麂圓線蟲屬(Parelaphostrongylus spp.)、肺尾屬(Pneumocaulus spp.)、肺圓線蟲屬(Pneumostrongylus spp.)、盆口線蟲 屬(Poteriostomum spp.)、原圓線蟲屬(Protostrongylus spp.)、指尾線蟲屬(Spicocaulus spp.)、冠尾線蟲屬(Stephanurus spp.)、圓線蟲屬(Strongylus spp.)、比翼線蟲屬(Syngamus spp.)、牛胃絲蟲屬(Teladorsagia spp.)、毛線線蟲屬(Trichonema spp.)、毛圓線蟲屬(Trichostrongylus spp.)、三齒線蟲屬(Triodontophorus spp.)、隱圓屬(Troglostrongylus spp.)、彎口線蟲屬(Uncinaria spp.)旋尾目(Spirurida)，例如：棘唇蟲屬(Acanthocheilonema spp.)、海獸胃線蟲屬(Anisakis spp.)、禽蛔屬(Ascaridia spp.)、蛔蟲屬(Ascaris spp.)、螺咽屬(Ascarops spp.)、無刺蟯蟲屬(Aspiculuris spp.)、貝利蛔蟲屬(Baylisascaris spp.)、布魯線蟲屬(Brugia spp.)、Cercopithifilaria屬、寄生線蟲(Crassicauda spp.)、雙瓣線蟲屬(Dipetalonema spp.)、血直絲蟲屬(Dirofilaria spp.)、龍線蟲屬(Dracunculus spp.)、德拉西線蟲屬(Draschia spp.)、蟯蟲屬(Enterobius spp.)、絲蟲屬(Filaria spp.)、棘口線蟲屬(Gnathostoma spp.)、筒線蟲屬(Gongylonema spp.)、馬胃線蟲屬(Habronema spp.)、異刺線蟲屬(Heterakis spp.)、光絲蟲屬(Litomosoides spp.)、羅阿絲蟲屬(Loa spp.)、蟠尾絲蟲屬(Onchocerca spp.)、尖尾線蟲屬(Oxyuris spp.)、副柔絲線蟲屬(Parabronema spp.)、類絲蟲屬(Parafilaria spp.)、副蛔屬(Parascaris spp.)、栓尾線蟲屬(Passalurus spp.)、泡翼線蟲屬(Physaloptera spp.)、普氏線蟲屬(Probstmayria spp.)、假絲蟲屬(Pseudofilaria spp.)、絲狀線蟲屬(Setaria spp.)、Skjrabinema屬、旋尾線蟲屬(Spirocerca spp.)、冠絲蟲屬(Stephanofilaria spp.)、圓蟲屬(Strongyluris spp.)、管狀線蟲屬(Syphacia spp.)、吸吮線蟲屬(Thelazia spp.)、弓蛔屬(Toxascaris spp.)、弓首線蟲屬(Toxocara spp.)、吳策線蟲屬(Wuchereria spp.)棘頭動物(Acanthocephala)：少棘目(Oligacanthorhynchida)，例如：巨吻棘頭 蟲屬(Macracanthorhynchus spp.)、前睾棘頭蟲屬(Prosthenorchis spp.)；念珠目(Moniliformida)，例如：聯珠狀棘頭蟲屬(Moniliformis spp.)多形目(Polymorphida)，例如：細頸棘頭蟲屬(Filicollis 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.) Examples of worms include, but are not limited to, Monoogenea: for example, Dactylogyrus spp., Gyrodactylus spp., Microbothrium spp. , Polystoma spp., Troglecephalus; Aphid: Pseudophyllidea, for example: Bothridium spp., Diphyllobothrium spp., Da Fu Diplogonoporus spp., Ichthyobothrium, Ligula spp., Schistocephalus spp., Schistocephalus spp., Spirometra spp. ); Cyclophyllida, for example: Andyra spp., Anoplocephala spp., Avitellina spp., Bertiella spp. ), Cittotaenia spp., Davainea spp., Diochis spp., Diplopylidium spp., Dipylidium spp. ), Echinococcus spp., Echinocotyle spp .), Echinolepis spp., Hydatigera spp., Aphis (Hymenolepis spp.), Joyeuxiella spp., Mesocestoides spp., Moniezia spp., Paranoplocephala spp. ), Raillietina spp., Stilesia spp., Taenia spp., Thysaniezia spp., Thysanosoma spp. Recombinant trematode: Digenea, for example: Austrobilharzia spp., Brachylaima spp., Calicophoron spp., lower bend Catatropis spp., Clonorchis spp., Collyriclum spp., Cotylophoron spp., Cyclocoelum spp. Dicrocoelium spp., Diclostomum spp., Echinochasmus spp., Echinoparyphium spp., R. genus Echinostoma spp.), Eurytrema spp., Fasciola spp., Fasciolides spp., Fasciolops Is spp.), Fischoederius spp., Gastrothylacus spp., Gigantobilharzia spp., Gigantocotyle spp., Alien Heterophyes spp., Hypoderaeum spp., Leucochloridium spp., Metatagonimus spp., Metalschis spp .), Nanophyetus spp., Notocotylus spp., Opisthorchis spp., Ornithobilharzia spp., Paragonimus Genus (Paragonimus spp.), Paramphistomum spp., Plagiorchis spp., Posthodiplostomum spp., Prosthogonimus spp. ), Schistosoma spp., Trichobilharzia spp., Troglotrema spp., Typhlocoelum spp. nematode: Trichinellida, for example: capillary Nematode (Capillaria spp.), Trichinella Trichinella spp., Trichomosoides spp., Trichuris spp., Tylenchida, for example: Micronema spp., Parastrangyloides Spp.), Strongiaides spp. Rhabditina, for example: Angiostrongylus spp., Amidostomum spp., Ancylostoma spp. Angiostrongylus spp., Bronchonema, Bunostomum spp., Chabertia spp., Cooperia spp., Cooperioides spp., Nematode (Crenosoma spp.), Cyathostomum spp., Cyclococercus spp., Cyclodontostomum spp., Cylicocyclus spp., Cylicostephanus Spp.), Cylindropharynx spp., Cystocaulus spp., Dictyocaulus spp., Elaphostrongylus spp., Filaroides Spp.), Globocephalus spp., Graphidium spp., Gyalocephalus spp., Haemonchus spp., Heligmosomoides spp., Hyostrongylus spp., Marshall nematode Genus (Marshallagia spp.), Metastrongylus spp., Muellerius spp., Necator spp., Nematodirus spp., Neospora Neostrongylus spp.), Nippostrongylus spp., Obeliscoides spp., Oesophagodontus spp., Oesophagostomum spp., Ollulanus Spp.), Ornithostrongylus spp., Oslerus spp., Ostertagia spp., Paracooperia spp., Parasitic nematode Genus (Paracrenosoma spp.), Parafilaroides spp., Parelaphostrongylus spp., Pneumocaulus spp., Pneumostrongylus spp., basin mouth Nematode Genus (Poteriostomum spp.), Protostrongylus spp., Spicocaulus spp., Stephanurus spp., Strongylus spp., Helicobacter spp. Syngamus spp.), Teladorsagia spp., Trichonema spp., Trichostrongylus spp., Triodontophorus spp., Troglostrongylus Spp.), Uncinaria spp., Spirurida, for example: Acanthocheilonema spp., Anisakis spp., Ascaridia spp. Ascaris spp., Ascarops spp., Aspiculuris spp., Baylisascaris spp., Brugia spp., Cercopithifilaria , Parasitic nematode (Crassicauda spp.), Dipetalonema spp., Dirofilaria spp., Dracunculus spp., Draschia spp. Enterobius spp., Filaria spp., Gnathostoma spp. ), Gangylonema spp., Habronema spp., Heterakis spp., Litomosoides spp., Loa spp. ), Onchocerca spp., Oxyuris spp., Parabronema spp., Parafilaria spp., Parascaris spp .), Passarus spp., Physaloptera spp., Probstmayria spp., Pseudofilaria spp., Setaria spp .), Skjrabinema genus, Spirocerca spp., Stephanofilaria spp., Strongyluris spp., Syphacia spp., Thelazia spp .), Toxascaris spp., Toxocara spp., Wuchereria spp. Acanthocephala: Oligacanthorhynchida, for example: giant kiss spines head Genus (Macracanthorhynchus spp.), Prosthenorchis spp.; Moniliformida, for example: Moniliformis spp. Polymorphida, for example: fine Filicollis 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、補救性預防(metaphylactic)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, metaphylactic or medical.
因此，本發明一項具體實施例係使用式(I)化合物作為醫藥。 Thus, a particular embodiment of the invention uses a compound of formula (I) as a medicament.
本發明另一態樣係有關使用式(I)化合物作為抗體內寄生蟲劑。 Another aspect of the invention pertains to the use of a compound of formula (I) as an antibody endoparasite.
本發明另一態樣係有關使用式(I)化合物作為抗蠕蟲劑，尤指作為殺線蟲劑、殺扁平蠕蟲劑、殺棘頭蟲劑或殺舌形動物劑。 Another aspect of the invention relates to the use of a compound of formula (I) as an anthelmintic, especially as a nematicide, a flattening worm, a echinoderma or a morphogen.
本發明另一態樣係有關使用式(I)化合物作為抗原蟲劑。 Another aspect of the invention relates to the use of a compound of formula (I) as an anti-protozoal agent.
本發明另一態樣係有關使用式(I)化合物作為抗體外寄生蟲劑，尤指殺節肢動物劑，極特定言之為殺昆蟲劑或殺蜱蟎劑。 Another aspect of the invention relates to the use of a compound of formula (I) as an antibody ectoparasite, especially an arthropodicide, in particular an insecticide or an acaricide.
本發明另一態樣係有關一種獸醫學調配物，其包含有效量之至少一種式(I)化合物與至少一種下列製劑：醫藥上可接受之賦形劑(例如：固態或液態稀釋劑)、醫藥上可接受之輔劑(例如：界面活性劑)，尤指常用於獸醫學調配物中之醫藥上可接受之賦形劑與/或常用於獸醫學調配物中之醫藥上可接受之輔劑。 Another aspect of the invention relates to a veterinary formulation comprising an effective amount of at least one compound of formula (I) and at least one of the following: a pharmaceutically acceptable excipient (eg, a solid or liquid diluent), Pharmaceutically acceptable adjuvants (eg, surfactants), especially pharmaceutically acceptable excipients commonly used in veterinary formulations and/or pharmaceutically acceptable supplements commonly used in veterinary formulations Agent.
本發明一相關態樣係一種製造本文所說明獸醫學調配物之方法，其包括混合至少一種式(I)化合物與醫藥上可接受之賦形劑與/或輔劑，尤指 常用於獸醫學調配物中之醫藥上可接受之賦形劑與/或常用於獸醫學調配物中之輔劑之步驟。 A related aspect of the invention is a method of making a veterinary formulation as described herein, comprising mixing at least one compound of formula (I) with a pharmaceutically acceptable excipient and/or adjuvant, especially A step commonly used in veterinary formulations for pharmaceutically acceptable excipients and/or adjuvants commonly used in veterinary formulations.
本發明另一明確態樣係一種選自殺體外寄生蟲與殺體內寄生蟲調配物之群中之獸醫學調配物，尤指選自殺蠕蟲、抗原蟲與殺節肢動物調配物之群中，極特定言之係選自根據上述態樣之殺線蟲、殺扁平蠕蟲、殺棘頭蟲、殺舌形動物、殺昆蟲與殺蜱蟎調配物之群，及其製造方法。 Another clarified aspect of the invention is a veterinary formulation selected from the group consisting of an ectoparasite and an in vivo parasite formulation, particularly selected from the group consisting of helminth, antigenic and arthropod formulations, Specifically, the system is selected from the group consisting of nematicidal, flattened worm, echinoderma, morphogen, insecticidal and acaricidal formulations according to the above aspects, and a method for producing the same.
另一態樣係有關一種使用有效量之式(I)化合物，為有需要之動物(尤指非人類動物)治療寄生蟲感染，尤指因選自本文所述體外寄生蟲與體內寄生蟲之群組中之寄生蟲所引起之感染之方法。 Another aspect relates to the use of an effective amount of a compound of formula (I) for the treatment of a parasitic infection in an animal in need thereof, especially a non-human animal, especially as selected from the ectoparasites and endoparasites described herein. A method of infection caused by parasites in a group.
另一態樣係有關一種使用本文所定義之獸醫學調配物，為有需要之動物(尤指非人類動物)治療寄生蟲感染，尤指因選自本文所述體外寄生蟲與體內寄生蟲之群組中之寄生蟲所引起之感染之方法。 Another aspect relates to the use of a veterinary formulation as defined herein for the treatment of a parasitic infection in an animal in need thereof, particularly a non-human animal, especially as selected from the ectoparasites and endoparasites described herein. A method of infection caused by parasites in a group.
另一態樣係有關一種以式(I)化合物於治療動物(尤指非人類動物)之寄生蟲感染上之用途，尤指因選自本文所述體外寄生蟲與體內寄生蟲之群組中之寄生蟲所引起之感染。 Another aspect relates to the use of a compound of formula (I) for the treatment of a parasitic infection in an animal, in particular a non-human animal, in particular in a group selected from the group consisting of ectoparasites and endoparasites described herein. An infection caused by parasites.
本發明動物健康或獸醫學內容中，術語「治療」包括預防性、補救性預防(metaphylactic)與醫療性處理。 In the animal health or veterinary content of the present invention, the term "treatment" includes prophylactic, metaphylactic and medical treatment.
依此方式，在特定具體實施例中，為獸醫學領域提供至少一種式(I)化合物與活性化合物(尤指殺體內與體外寄生蟲藥)之混合物。 In this manner, in a particular embodiment, a mixture of at least one compound of formula (I) and an active compound (especially a bactericidal and ectoparasite) is provided for the field of veterinary medicine.
在動物健康領域中，「混合物」不僅指兩種(或更多種)不同活性化合物調配成同一調配物中，因此係共同使用，而且係有關一種包含各活性化合物之分開調配物之產品。因此，當使用兩種以上活性化合物時，所有活性化合物均調配成同一調配物或所有活性化合物可調配成分開調配物；同樣可理解之混合型式為其中有些活性化合物係共同調配，及有些活性化 合物係分開調配。分開調配物可以分開或連續施用該相關活性化合物。 In the field of animal health, "mixture" means not only that two (or more) different active compounds are formulated into the same formulation, and therefore are used together, and are related to a product comprising separate formulations of the active compounds. Therefore, when two or more active compounds are used, all active compounds are formulated into the same formulation or all active compound-adjustable ingredients. It is also understood that the mixed form is that some of the active compounds are co-formulated, and some are activated. The compounds are formulated separately. The relevant active compound can be administered separately or sequentially from separate formulations.
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：「The Pesticide Manual」(如上述)，或可搜尋網際網路(例如：http：//www.alanwood.net/pesticides)。 The active compounds referred to herein by their common names are known and described, for example, in "The Pesticide Manual" (as described above), or may be searched the Internet (eg, http://www.alanwood.net/pesticides).
選自殺體外寄生蟲劑群組中作為混合組份之活性化合物實例包括(但不限於)上文詳細列出之殺昆蟲劑與殺蜱蟎劑。其他可使用之活性化合物係依據上文中根據最新IRAC作用分類圖(IRAC Mode of Action Classification Scheme)列於下文中：(1)乙醯基膽鹼酯酶(AChE)抑制劑；(2)GABA-閘控之氯離子通道阻斷劑；(3)鈉通道調控劑；(4)菸鹼激導性乙醯基膽鹼受體(nAChR)競爭性調控劑；(5)菸鹼激導性乙醯基膽鹼受體(nAChR)異位性調控劑；(6)麩胺酸閘控氯離子通道(GluCl)異位性調控劑；(7)幼保激素擬似物；(8)其他非特異性(多重位點)抑制劑；(9)弦音感覺器官調控劑；(10)蟎生長抑制劑；(12)粒線體ATP合成酶抑制劑，如：ATP瓦解劑；(13)破壞質子梯度之氧化性磷酸化反應去偶合劑；(14)菸鹼激導性乙醯基膽鹼受體通道阻斷劑；(15))幾丁質生合成抑制劑，第0型；(16)幾丁質生合成抑制劑，第I型；(17)蛻變瓦解劑(尤指雙翅目(Diptera))；(18)脫皮激素受體促效劑；(19)章魚胺受體促效劑；(21)粒線體複合物I電子轉運抑制劑；(25)粒線體複合物II電子轉運抑制劑；(20)粒線體複合物III電子轉運抑制劑；(22)電壓閘控之鈉通道阻斷劑；(23)乙醯基CoA羧酸酶之抑制劑；(28)蘭尼鹼(ryanodine)受體調控劑；作用機轉未知或非專一性之活性化合物，例如：吡氟草胺(fentrifanil)、抗蟎唑(fenoxacrim)、環普靈(cycloprene)、殺蟎酯(chlorobenzilate)、殺蟲脒(chlordimeform)、氟苯滅(flubenzimin)、地昔尼爾(dicyclanil)、艾滅得(amidoflumet)、滅蟎猛(quinomethionat)、苯蟎噻(triarathene)、氯噻苯 (clothiazoben)、殺蟎好(tetrasul)、油酸鉀、石油、噁蟲酮(metoxadiazone)、葛昔普(gossyplur)、氟蟎嗪(flutenzine)、溴蟎酯(brompropylate)、克利得(cryolite)；其他類別化合物，例如：畜蟲威(butacarb)、地麥威(dimetilan)、除線威(cloethocarb)、磷光威(phosphocarb)、亞特松(pirimiphos)(-乙基)、巴拉松(parathion)(-乙基)、蟲蟎畏(methacrifos)、鄰水酸異丙基酯、三氯松(trichlorfon)、硫丙磷(sulprofos)、丙蟲磷(propaphos)、硫線磷(sebufos)、吡硫磷(pyridathion)、發硫磷(prothoate)、除線磷(dichlofenthion)、滅賜松(demeton)-S-甲基碸、依殺松(isazofos)、苯腈磷(cyanofenphos)、氯亞胺硫磷(dialifos)、三硫磷(carbophenothion)、特硫磷(autathiofos)、愛吩磷(aromfenvinfos)(-甲基)、穀速松(azinphos)(-乙基)、陶斯松(chlorpyrifos)(-乙基)、丁苯硫磷(fosmethilan)、丙胺磷(iodofenphos)、蔬果磷(dioxabenzofos)、福木松(formothion)、地蟲磷(fonofos)、吡氟硫磷(flupyrazofos)、繁福松(fensulfothion)、乙嘧硫磷(etrimfos)；有機氯化合物，例如：毒殺芬(camphechlor)、林丹(lindane)、飛布達(heptachlor)；或苯基吡唑類，例如：乙醯蟲腈(acetoprole)、吡蟲腈(pyrafluprole)、吡啶氟蟲腈(pyriprole)、氟吡唑蟲(vaniliprole)、維吉黴素(sisapronil)；或異唑啉類，例如：賽蘭(sarolaner)、艾伏樂(afoxolaner)、樂地蘭(lotilaner)、氟樂(fluralaner)；擬除蟲菊酯類，例如：(順式-、反式-)美特寧(metofluthrin)、丙氟菊酯(profluthrin)、三氟醚菊酯(flufenprox)、溴氟菊酯(flubrocythrinate)、苄蟎醚(fubfenprox)、五氟菊酯(fenfluthrin)、普賽吩布(protrifenbut)、二氯苯醚菊酯(pyresmethrin)、RU15525、環戊烯丙菊酯(terallethrin)、順式-利滅靈(resmethrin)、氯氟醚菊酯(heptafluthrin)、生物乙醚菊酯(bioethanomethrin)、 生物氯菊酯(biopermethrin)、芬普寧(fenpyrithrin)、順式-賽滅寧(cis-cypermethrin)、順式-百滅寧(cis-permethrin)、功夫菊酯(clocythrin)、賽洛寧(cyhalothrin)(λ-)、氯波寧(chlovaporthrin)、或鹵化烴化合物(HCH)，類新菸鹼，例如：硝蟲噻嗪(nithiazine)二氯滅嗪(dicloromezotiaz)、三氟普靈(triflumezopyrim)大環內酯類，例如：尼美克定(nemadectin)、抑伏克定(ivermectin)、拉替菌素(latidectin)、莫西克定(moxidectin)、希樂克定(selamectin)、普滅克定(eprinomectin)、得滅克定(doramectin)、抑滅克定(emamectin)苯甲酸鹽；美保黴素肟(milbemycin oxime)硫烯酸酯(triprene)、保幼醚(epofenonane)、二苯丙醚(diofenolan)；生物物質、激素、或費洛蒙類，例如：天然產物，例如：蘇力菌素(thuringiensin)、十二碳二烯醇(codlemone)或印楝組份二硝基酚，例如：敵蟎普(dinocap)、敵蟎通(dinobuton)、樂殺蟎(binapacryl)；苯甲醯基脲類，例如：氟佐隆(fluazuron)、氟幼脲(penfluron)，脒衍生物，例如：氯甲脒(chlormebuform)、蟎蜱胺(cymiazole)、得米地曲(demiditraz)瓦蟎窩殺蜱蟎劑，例如：有機酸類，例如：甲酸、草酸。 Examples of active compounds as a mixed component in the suicide ectoparasite group include, but are not limited to, the insecticides and acaricides detailed above. Other active compounds which can be used are listed below according to the latest IRAC Mode of Action Classification Scheme: (1) acetylcholinesterase (AChE) inhibitor; (2) GABA- Chloride channel blocker for gate control; (3) sodium channel modulator; (4) nicotine-induced acetylcholine receptor (nAChR) competitive regulator; (5) nicotine-induced B醯-choline receptor (nAChR) atopic modulator; (6) glutamate gated chloride channel (GluCl) atopic modulator; (7) juvenile hormone mimics; (8) other non-specific (multiple site) inhibitors; (9) stringy sensory organ modulators; (10) sputum growth inhibitors; (12) mitochondrial ATP synthase inhibitors, such as: ATP disintegrator; (13) disruption of proton gradients Oxidative phosphorylation decoupling agent; (14) nicotine-induced acetylcholine receptor channel blocker; (15)) chitinogenic synthesis inhibitor, type 0; (16) chitin synthesis Inhibitor, type I; (17) phlegm-removing agent (especially Diptera); (18) ecdysone receptor agonist; (19) octopamine receptor agonist; (21) Linear complex I electron transport Formulation; (25) mitochondrial complex II electron transport inhibitor; (20) mitochondrial complex III electron transport inhibitor; (22) voltage-gated sodium channel blocker; (23) acetylated CoA An inhibitor of a carboxylase; (28) a ryanodine receptor modulator; an active compound that acts on an unknown or non-specificity, for example, fentrifanil, fenoxacrim, Cycloprene, chlorobenzilate, chlordimeform, flubenzimin, dicyclanil, amidoflumet, quinomethionat, Triarathene, clothiazoben, tetrasul, potassium oleate, petroleum, metoxadiazone, gossyplur, flutenzine, bromine Brompropylate, cryolite; other classes of compounds, for example: butacarb, dimetilaan, cloethocarb, phosphocarb, pirimiphos (-ethyl), parathion (-ethyl), methacrifos, isopropyl ortho-acid, triclosan (tri Chlorfon), sulprofos, propaphos, sebufos, pyridathion, prothoate, deichlofenthion, demeton )-S-methyl hydrazine, isazofos, cyanofenphos, dialifos, carbophenothion, autathiofos, aromfenvinfos ) (-methyl), azinphos (-ethyl), chlorpyrifos (-ethyl), fosmethilan, iodofenphos, dioxabenzofos, blessing Formothion, fonofos, flupyrazofos, fensulfothion, etrimfos; organochlorine compounds such as camphechlor, lindane ), heptachlor; or phenylpyrazoles, for example: acetoprole, pyrafluprole, pyriprol, pyriliprole, vitamin Gismycin (sisapronil); or different Oxazolines, for example: sarolaner, afoxolaner, lotilaner, fluraraner; pyrethroids, for example: (cis-, trans-) Metofluthrin, profluthrin, flufenprox, flubrocythrinate, fubfenprox, fenfluthrin, prasin Protrifenbut, pyresmethrin, RU15525, terallethrin, resmethrin, heptafluthrin, bioethermethrin (bioethanomethrin), biopermethrin, fenpyrithrin, cis-cypermethrin, cis-permethrin, clocythrin, race Cyhalothrin (λ-), chlovaporthrin, or halogenated hydrocarbon compound (HCH), neonicotinoids, for example: nithiazine dicloromezotiaz, trifluoroprop Triflumezopyrim macrolides such as nemadectin, ivermectin, and latiectin Moxidectin, selamectin, eprinomectin, doramectin, emamectin benzoate; milbemycin Oxime) triprene, epofenonane, diofenolan; biological substances, hormones, or pheromones, eg natural products, eg: thuringiensin , dodecadienyl (codlemone) or neem composition of dinitrophenol, for example: dinocap, dinobuton, binapacryl; benzhydrazide, For example: fluzuron, penfluron, anthraquinone derivatives, such as: chlormebuform, cymiazole, demiditraz, corrugated acaricide For example, organic acids such as formic acid and oxalic acid.
選自殺體內寄生蟲劑群組作為混合組份之活性化合物實例包括(但不限於)：殺蠕蟲活性化合物與抗原蟲活性化合物。 Examples of active compounds selected as a mixed component of the suicide internal parasiticidal group include, but are not limited to, an anthelmintic active compound and an antiprotozoal active compound.
殺蠕蟲活性化合物包括(但不限於)：下列殺線蟲、殺白蟻與/或殺絛蟲活性化合物：大環內酯類，例如：普滅克定(eprinomectin)、艾滅克定(abamectin)、尼美克定(nemadectin)、莫西克定(moxidectin)、得滅克定(doramectin)、希樂克定 (selamectin)、利滅克定(lepimectin)、拉替菌素(latidectin)、美保克定(milbemectin)、抑伏克定(ivermectin)、抑滅克定(emamectin)、美保黴素(milbemycin)；苯并咪唑類與苯硫胍類(probenzimidazoles)，例如：歐苯達唑(oxibendazole)、美苯達唑(mebendazole)、三氯苯咪唑(triclabendazole)、多保淨(thiophanate)、帕苯達唑(parbendazole)、歐菲達唑(oxfendazole)、奈托比胺(netobimin)、菲苯達唑(fenbendazole)、非班太(febantel)、腐絕(thiabendazole)、環苯達唑(cyclobendazole)、卡苯達唑(cambendazole)、阿苯達唑(albendazole)-亞碸、阿苯達唑(albendazole)、伏苯達唑(flubendazole)；縮酸肽類(depsipeptides)，較佳為環狀縮酸肽類，尤指例如：24-員環狀縮酸肽類，例如：恩得肽(emodepside)、PF1022A；四氫嘧啶類，例如：摩朗得(morantel)、哌喃噻(pyrantel)、間酚嘧啶(oxantel)；咪唑并噻唑類，例如：丁咪唑(butamisole)、左旋咪唑(levamisole)、四咪唑(tetramisole)；胺基苯基脒類，例如：阿米登太(amidantel)、脫醯基阿米登太(deacylated amidantel)(dAMD)、三苯雙脒(tribendimidine)；胺基乙腈類，例如：莫米松(monepantel)；派拉荷醯胺類(paraherquamides)，例如：派拉荷醯胺(paraherquamide)、得曲恩特(derquantel)；水楊醯基替苯胺類，例如：三溴柳苯胺(tribromsalan)、溴氟硝柳胺(bromoxanide)、溴硫醯胺(brotianide)、氯碘柳苯胺(clioxanide)、氯氰碘柳胺(closantel)、耐克螺(niclosamide)、氯羥柳胺(oxyclozanide)、碘醚柳胺(rafoxanide)；經取代之苯酚類，例如：硝羥碘芐腈(nitroxynil)、硫雙二氯酚(bithionol)、二 碘硝酚(disophenol)、六氯酚(hexachlorophene)、聯硝氯酚(niclofolan)、甲聯硝氯酚(meniclopholan)；有機磷酸酯類，例如：三氯松(trichlorfon)、萘樂弗斯(naphthalofos)、二氯松(dichlorvos)/DDVP、育畜磷(crufomate)、庫伏斯(coumaphos)、納洛酮(haloxone)；哌嗪酮/喹啉類，例如：吡喹酮(praziquantel)，依西太爾(epsiprantel)；哌嗪類，例如：哌嗪、羥基嗪(hydroxyzine)；四環素類，例如：四環素、氯四環素、去氧羥四環素(doxycycline)、氧四環素(oxycycline)、羅利環素(rolitetracycline)；各種不同其他類別，例如：丁萘脒(bunamidine)、硝唑咪(niridazole)、雷瑣侖太(resorantel)、臍菇亭(omphalotin)、奧替普拉(oltipraz)、硝硫氰酯(nitroscanate)、硝羥碘芣腈(nitroxynil)、奥沙尼喹(oxamniquin)、滅樂散(mirasan)、盧甘宋(miracil)、魯坎松(lucanthon)、海恩酮(hycanthon)、海妥林(hetolin)、吐根鹼(emetin)、二乙基卡馬西平(diethylcarbamazine)、二氯芬(dichlorophen)、地芬尼泰(diamfenetide)、可那氮平(clonazepam)、芐芬寧(bephenium)、硝硫氰胺(amoscanate)、氯舒隆(clorsulon)。抗原蟲活性化合物包括(但不限於)下列活性化合物：三嗪類，例如：地卡珠利(diclazuril)、泊那珠利(ponazuril)、來曲珠利(letrazuril)、托曲珠利(toltrazuril)；聚醚離子載體(ionophores)，例如：莫能菌素(monensin)、鹽黴素(salinomycin)、馬杜黴素(maduramicin)、甲基鹽黴素(narasin)；大環內酯類，例如：美保黴素(milbemycin)、紅黴素(erythromycin)；喹諾酮類，例如：恩諾沙星(enrofloxacin)、普朵沙星(pradofloxacin)；奎寧類，例如：氯奎寧(chloroquin)； 嘧啶類，例如：嘧啶甲胺(pyrimethamine)；磺胺類，例如：磺胺喹啉(sulfaquinoxaline)、甲氧苄啶(trimethoprim)、磺胺氯吡嗪(sulfaclozin)；硫胺素類，例如：胺丙嘧吡啶(amprolium)；林可醯胺類(lincosamide)，例如：克林黴素(clindamycin)；碳醯替苯胺類，例如：雙咪苯脲(imidocarb)；硝基呋喃類，例如：硝呋莫司(nifurtimox)；喹唑啉酮生物鹼類，例如：鹵夫酮(halofuginone)；各種不同其他類別，例如：奥沙尼喹(oxamniquin)、巴龍黴素(paromomycin)；來自微生物之疫苗或抗原類，例如：犬焦蟲(Babesia canis rossi)、盲腸型球蟲(Eimeria tenella)、早熟艾美球蟲(Eimeria praecox)、毒害艾美球蟲(Eimeria necatrix)、和緩艾美球蟲(Eimeria mitis)、巨型艾美球蟲(Eimeria maxima)、布氏艾美球蟲(Eimeria brunetti)、堆型艾美球蟲(Eimeria acervulina)、焦蟲(Babesia canis vogeli)、嬰兒利什曼蟲(Leishmania infantum)、焦蟲(Babesia canis canis)、牛肺蟲(Dictyocaulus viviparus)。 The helminthically active compounds include, but are not limited to, the following nematicidal, termite-killing and/or acaricidal active compounds: macrolides, for example: eprinomectin, abamectin, Nemadectin, moxidectin, doramectin, selamectin, lepimectin, latidectin, melbourne Milbemectin, ivermectin, emamectin, milbemycin; benzimidazoles and probenzimidazoles, eg oxibendazole , mebendazole, triclabendazole, thiophanate, parbendazole, oxfendazole, netobimin, phenanthrene Fenbendazole, febantel, thiabendazole, cyclobendazole, cambendazole, albendazole-arylene, albendazole (albendazole), flubendazole; depsipeptides, preferably cyclic acid Classes, especially for example: 24-membered cyclic acid-reducing peptides, for example: emodepside, PF 1022A; tetrahydropyrimidines, for example: morantel, pyrantel, meta-phenol Anoxantel; imidazothiazoles, for example: butamisole, levamisole, tetramisole; aminophenyl hydrazines, for example: amidantel, deamination Deacylated amidantel (dAMD), tribendimidine; aminoacetonitriles such as: monepantel; paraherquamides, eg, palladium amide (paraherquamide), derquantel; salicyl anilide, such as: tribromsalan, bromoxanide, brotianide, chloroiodaniline ( Clioxanide), closantel, niclosamide, oxyclozanide, rafoxanide; substituted phenols such as nitroxynil , bis-dichlorophenol (bithionol), diisophenol (disophenol), hexachlorophenol (hexachlorophe Ne), niclofolan, meniclopholan; organophosphates such as trichlorfon, naphthalofos, dichlorvos/DDVP , crufomate, coumaphos, haloxone; piperazinone/quinoline, for example: praziquantel, epsiprantel; piperazine For example: piperazine, hydroxyzine; tetracyclines, for example: tetracycline, chlorotetracycline, doxycycline, oxycycline, rolitetracycline; various other categories, such as: Bunamidine, niridazole, resorantel, omphalotin, oltipraz, nitroscanate, nitrosine Nitroxynil), oxamniquin, mirasan, miracil, lucanhon, hycanthon, hetolin, ipecaine Emetin), diethylcarbamazine, dichlorophen, difenfeet De), clonazepam, bephenium, amoxinate, clorsulon. Antiprotozoal active compounds include, but are not limited to, the following active compounds: triazines such as: diclazuril, ponazuril, letrazuril, toltrazuril Polyether ionophores, for example: monensin, salinomycin, maduramicin, narasin; macrolides, For example: milbemycin, erythromycin; quinolones, for example: enrofloxacin, pradofloxacin; quinines, for example: chloroquin; Pyrimidines, for example: pyrimimethamine; sulfonamides, for example, sulfaquinidine Sulfaquinoxaline, trimethoprim, sulfaclozin; thiamines, for example: amprolium; lincosamide, for example, clindamycin Clindamycin; carboquine, for example: imidocarb; nitrofurans, such as nifurtimox; quinazolinone alkaloids, for example: halofuginone ( Halofuginone); various other categories, such as: oxamniquin, paromomycin; vaccines or antigens from microorganisms, such as Babesia canis rossi, cecal coccidia ( Eimeria tenella), Eimeria praecox, Eimeria necatrix, Eimeria mitis, Eimeria maxima, Eimeria maxima (Eimeria brunetti), Eimeria acervulina, Babesia canis vogeli, Leishmania infantum, Babesia canis canis, Dictyocaulus viviparus.
上述所有混合組份若可能時，亦可依據其官能基，與合適鹼類或酸類形成鹽類。 All of the above mixed components may form salts with suitable bases or acids depending on their functional groups, if possible.
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、其他蠕蟲之傳播；- 伊蚊(Aedes)：黃熱病、登革熱、其他病毒疾病、絲蟲病；- 蚋科(Simuliidae)：傳播蠕蟲，特定言之，盤尾線蟲(Onchocerca volvulus)；- 蛾蚋科(Psychodidae)：傳播利什曼原蟲症；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、絛蟲；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(Crimean-Congo haematologic fever)、疏螺旋體病；6)蜱：疏螺旋體病(borelliosis)，如：伯氏疏螺旋體(Borrelia bungdorferi sensu lato)、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))、艾利希氏體症。 Examples of vectors and diseases or pathogens that they transmit are: 1) Mosquito - Anopheles: malaria, filariasis; - Culex: Japanese encephalitis, filariasis, other viral diseases, spread of other worms; - Aedes: yellow fever , dengue fever, other viral diseases, filariasis; - Simuliidae: transmission of worms, specifically, Onchocerca volvulus; - Psychodidae: spread of Leishmaniasis; 2) 虱: skin infectious diseases, epidemic typhus; 3) fleas: blight, rat typhus, aphids; 4) flies: sleeping sickness (trypanosomiasis); cholera, other bacterial diseases; 5) : Liver rickets, epidemic typhus, rickettsialpox, tularamia, Saint-Louis encephalitis, tick-borne encephalitis (TBE), Crimea Crimean-Congo haematologic fever, Borrelia; 6) 蜱: Borelliosis, such as Borrelia bungdorferi sensu lato, Borrelia duttoni , sputum-transmitted encephalitis, Q-heat (Coxiella burnetii), coke Insects (Babesia canis canis), Ehrlich's disease.
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。 Examples of vectors in the context of the present invention are insects, such as aphids, flies, spider mites or thrips that transmit plant viruses to 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)、蛾蚋科(Psychodidae)，如：白蛉(Phlebotomus)、羅蛉(Lutzomyia)、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, Psychodidae, such as: Phlebotomus, Lutzomyia, cockroach, flea, fly, cockroach, and cockroach .
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、森林、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, forest, 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、木材、加工木製品與塗料組成物。本發明用途特別適合保護木材。 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 coating compositions. 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)化合物係呈即用型殺害蟲劑，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 insecticide, 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) are useful for protecting articles in contact with salt water or salt water, in particular hulls, partitions, nets, buildings, moorings and signalling 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，尤其控制出現在例如：住家、廠房、辦公室、車廂、動物畜養設備等封閉空間之昆蟲、蜘蛛、蜱與蟎類。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 stockpile products, especially insects, spiders, mites and mites that appear in closed spaces such as homes, factories, offices, cars, animal husbandry equipment, and the like. . 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.
下列製法與用法實例說明本發明，但未加以限制。 The following preparations and usage examples illustrate the invention, but are not limited.
合成實例No.1 Synthesis example No.1
3-[(2-氯噻唑-5-基)甲基-(2-吡啶基)胺基]-3-側氧基-2-苯基丙酸苯甲基酯(化合物No.I-1-01) 3-[(2-Chlorothothazole-5-yl)methyl-(2-pyridyl)amino]-3-oxo-2-phenylpropionic acid benzyl ester (Compound No. I-1- 01)
步驟1：3-氯-3-側氧基-2-苯基丙酸苯甲基酯
依序添加一滴N,N-二甲基甲醯胺與草醯氯(98%純度，1.34g,10.4mmol)至含3-苯甲基氧-3-側氧基-2-苯基丙酸(2.00g,7.40mmol)之二氯甲烷(20ml)溶液中。攪拌反應混合物1h，小心地濃縮。產生3.75g(92%理論值)粗產物，其未進一步純化即使用。 Add a drop of N , N -dimethylformamide and oxalic acid chloride (98% purity, 1.34g, 10.4mmol) to 3-benzyloxy-3-oxo-2-phenylpropionic acid (2.00 g, 7.40 mmol) in dichloromethane (20 mL). The reaction mixture was stirred for 1 h and concentrated carefully. 3.75 g (92% of theory) of crude product was obtained which was used without further purification.
步驟2：3-[(2-氯噻唑-5-基)甲基-(2-吡啶基)胺基]-3-側氧基-2-苯基丙酸苯甲基酯
取碳酸鉀(184mg,1.33mmol)添加至含3-氯-3-側氧基-2-苯基丙酸苯甲基酯(VIII-1)(307mg,1.06mmol)之乙腈(7.80ml)溶液中，攪拌混合物30min。隨後添加胺(IX-01)(200mg,0.886mmol)，反應混合物於40℃下攪拌16h。冷卻至室溫後，混合物攪拌加至檸檬酸水溶液(1.0M)中。使用二氯甲烷萃取混合物，分離有機相，使用飽和NaCl溶液洗滌，與濃縮。粗產物吸附在矽膠上，經層析法，使用二氯甲烷/甲醇(10/1)純化，產生130mg(29%理論值)標題化合物。 Potassium carbonate (184 mg, 1.33 mmol) was added to a solution of 3-chloro-3-oxo-2-phenylpropanoic acid benzyl ester (VIII-1) (307 mg, 1.06 mmol) in acetonitrile (7.80 ml) The mixture was stirred for 30 min. Then the amine (IX-01) (200 mg, 0.886 mmol) was added and the mixture was stirred at 40 ° C for 16 h. After cooling to room temperature, the mixture was stirred and added to aqueous citric acid (1.0 M). The mixture was extracted with dichloromethane, the organic phase was separated, washed with saturated NaCI and concentrated. The crude product was taken up in EtOAc (EtOAc) elute
HPLC-MS：logP(HCOOH)=3.76；1HNMR-數據：參見波峰列表。 HPLC-MS: log P (HCOOH) = 3.76; 1 H NMR - data: see the peak list.
合成實例No.2 Synthesis example No. 2
3-側氧基-3-[2-吡啶基(嘧啶-5-基甲基)胺基]-2-[3-(三氟甲基)苯基]丙酸苯甲基酯(化合物No.I-1-76) 3-Phenoxy-3-[2-pyridyl(pyrimidin-5-ylmethyl)amino]-2-[3-(trifluoromethyl)phenyl]propanoic acid benzyl ester (Compound No.) I-1-76)
步驟1：3-苯甲基氧-3-側氧基-2-[3-(三氟甲基)苯基]丙酸(化合物No.VII-28)
取亞硫醯氯(0.37ml,5.03mmol)與1滴N,N-二甲基甲醯胺添加至含2-[3-(三氟甲基)苯基]丙二酸(1.25g,5.03mmol)之乙醚(10.0ml)溶液中。反應混合物隨後於40℃下攪拌3h。冷卻至RT後，混合物於旋轉蒸發器上濃縮，與石油醚攪拌後，再濃縮一次。所得油狀物溶於乙醚(10.0ml)中，添加苯甲基醇(0.59mg,5.39mmol)。混合物再於40℃下攪拌2h後，濃縮。粗產物溶於石油醚，及再濃縮一次。所得粗產物未進一步純化即繼續轉化。 Add sulfite chlorine (0.37 ml, 5.03 mmol) and 1 drop of N,N-dimethylformamide to 2-[3-(trifluoromethyl)phenyl]malonic acid (1.25 g, 5.03) Methyl) in diethyl ether (10.0 ml). The reaction mixture was then stirred at 40 ° C for 3 h. After cooling to RT, the mixture was concentrated on a rotary evaporator and stirred with petroleum ether and then concentrated. The obtained oil was dissolved in diethyl ether (10.0 mL). The mixture was further stirred at 40 ° C for 2 h and then concentrated. The crude product was dissolved in petroleum ether and concentrated again. The crude product obtained was further converted without further purification.
HPLC-MS：logP(HCOOH)=2.97。 HPLC-MS: log P (HCOOH) = 2.97.
步驟2：3-氯-3-側氧基-2-[3-(三氟甲基)苯基]丙酸苯甲基酯
取3-苯甲基氧-3-側氧基-2-[3-(三氟甲基)苯基]丙酸(750mg,1.10mmol,50%純度)溶於二氯甲烷(14.3ml)，然後添加1滴N,N-二甲基甲醯胺與草醯氯(0.24ml,1.46mmol)至所得溶液中。混合物於室溫下攪拌2h，及濃縮。粗產物立即繼續與式(IX)胺反應，產生相應之醯胺。 3-Benzyloxy-3-oxo-2-[3-(trifluoromethyl)phenyl]propanoic acid (750 mg, 1.10 mmol, 50% purity) was dissolved in dichloromethane (14.3 ml). Then, 1 drop of N,N-dimethylformamide and oxalic acid chloride (0.24 ml, 1.46 mmol) were added to the resulting solution. The mixture was stirred at room temperature for 2 h and concentrated. The crude product is immediately reacted with the amine of formula (IX) to yield the corresponding guanamine.
步驟3：3-側氧基-3-[2-吡啶基(嘧啶-5-基甲基)胺基]-2-[3-(三氟甲基)苯基]丙
酸苯甲基酯
於0℃下，取含3-氯-3-側氧基-2-[3-(三氟甲基)苯基]丙酸苯甲基酯(250mg,0.35mmol)之二氯甲烷(2.0ml)溶液添加至含N-(嘧啶-5-基甲基)吡啶-2-胺(65mg,0.35mmol)與三乙基胺(0.15ml,1.05mmol)之二氯甲烷(3.75ml)溶液中。讓混合物回升至RT，於此溫度下攪拌2h。隨後添加飽和NH4Cl水溶液，使用二氯甲烷萃取混合物。取有機相濃縮，粗產物經HPLC，使用乙腈/水梯度純化。 Dichloromethane (2.0 ml) containing 3-chloro-3-oxo-2-[3-(trifluoromethyl)phenyl]propanoic acid benzyl ester (250 mg, 0.35 mmol) at 0 °C The solution was added to a solution of N-(pyrimidin-5-ylmethyl)pyridin-2-amine (65 mg, 0.35 mmol) and triethylamine (0.15 ml, 1.05 mmol) in dichloromethane (3.75 ml). The mixture was allowed to warm to RT and stirred at this temperature for 2 h. Followed by the addition of saturated aqueous NH 4 Cl, the mixture was extracted with dichloromethane. The organic phase was concentrated and the crude was purified using EtOAc EtOAc.
HPLC-MS：logP(HCOOH)=3.21；1H-NMR(400.0MHz,d6-DMSO)δ=9.05(s,1H,8.66(s,2H),8.40(dd,1H),7.86(dt,1H),7.64(d,1H),7.53(t,1H),7.47(br,1H),7.38-7.26(m,8H),5.29(br,1H),5.16-4.92(m,2H),5.12(s,2H)。 HPLC-MS: logP (HCOOH) = 3.21; 1 H-NMR (400.0MHz, d 6 -DMSO) δ = 9.05 (s, 1H, 8.66 (s, 2H), 8.40 (dd, 1H), 7.86 (dt, 1H), 7.64 (d, 1H), 7.53 (t, 1H), 7.47 (br, 1H), 7.38-7.26 (m, 8H), 5.29 (br, 1H), 5.16-4.92 (m, 2H), 5.12 (s, 2H).
合成式(VII)之其他中間物：
a)由酸性範圍內之LC-MS測定M+之方法係在pH 2.7下，使用乙腈(含0.1%甲酸)與水作為移動相；依10%乙腈至95%乙腈之線性梯度進行，儀器：Agilent 1100 LC系統、Agilent MSD系統、HTS PAL，氣體溫度至高200℃下進行。 a) The method for the determination of M + by LC-MS in the acidic range is carried out at pH 2.7 using acetonitrile (containing 0.1% formic acid) and water as the mobile phase; according to a linear gradient of 10% acetonitrile to 95% acetonitrile, instrument: Agilent 1100 LC system, Agilent MSD system, HTS PAL, gas temperature up to 200 °C.
上述表中及製備實例中之logP值係依據EEC指令79/831 Annex V.A8，採用HPLC(高效液相層析法)，使用逆相管柱(C18)測定。溫度43℃。 The logP values in the above tables and in the preparation examples were determined by HPLC (High Performance Liquid Chromatography) using a reverse phase column (C18) according to EEC Directive 79/831 Annex V.A8. Temperature 43 ° C.
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。 Calibration was carried out using unbranched alkan-2-ones (having from 3 to 16 carbon atoms) with known logP-values.
合成實例No.3 Synthesis example No. 3
N-[(5-氯-1,3-噻唑-2-基)甲基]吡啶-2-胺(化合物No.IX-1) N-[(5-chloro-1,3-thiazol-2-yl)methyl]pyridin-2-amine (Compound No. IX-1)
步驟1：1-(5-氯-1,3-噻唑-2-基)-N-(吡啶-2-基)甲烷亞胺
取含2-胺基吡啶(3.00g,31.9mmol)與5-氯-1,3-噻唑-2-甲醛(5.06g,34.3mmol)之三氯甲烷(500ml)溶液於室溫下攪拌15分鐘。減壓排除溶劑(75℃下1h)。黃色殘質溶於150ml三氯甲烷中，攪拌15min。減壓排除溶劑(75℃下1h)。殘質再次溶於150ml三氯甲烷中，並攪拌15min，隨後減壓排除溶劑(85℃下1h)。殘質於6mbar與50℃之旋轉蒸發器中乾燥1h。產生7.40g(104%理論值)粗產物，其未進一步純化即使用。 A solution of 2-aminopyridine (3.00 g, 31.9 mmol) and 5-chloro-1,3-thiazole-2-carbaldehyde (5.06 g, 34.3 mmol) in chloroform (500 ml) was stirred at room temperature for 15 min. . The solvent was removed under reduced pressure (1 h at 75 ° C). The yellow residue was dissolved in 150 ml of chloroform and stirred for 15 min. The solvent was removed under reduced pressure (1 h at 75 ° C). The residue was redissolved in 150 ml of chloroform and stirred for 15 min, then solvent was removed under reduced pressure (1 h at 85 ° C). The residue was dried in a rotary evaporator at 6 mbar and 50 ° C for 1 h. Yield 7.40 g (104% of theory) of crude material which was used without further purification.
HPLC-MS：logP(中性)=2.64。 HPLC-MS: log P (neutral) = 2.64.
階段2：N-[(5-氯-1,3-噻唑-2-基)甲基]吡啶-2-胺
取氫硼化鈉(1.26g,33.3mmol)加至含甲醇(47ml)與四氫呋喃(118ml)之混合物中，懸浮液於室溫下攪拌5min。慢慢滴加含1-(5-氯-1,3-噻唑-2-基)-N-(吡啶-2-基)甲烷亞胺(7.40g,33.3mmol)之四氫呋喃(350ml)溶液。反應混合物於室溫下攪拌4h，然後添加乙酸(5ml)。攪拌5min後，添加乙酸(1.5ml)與水(20ml)，短暫激烈攪拌溶液。添加乙酸乙酯(400ml)與1.5%強度氫氧化鈉水溶液(400ml)後，分相，有機相經硫酸鈉脫水，及過濾，減壓排除溶劑。粗產物懸浮於二氯甲烷中，使用5%強度氫氧化鈉水溶液萃取。分離有機相，使用水洗滌2次，使用飽和氯化鈉水溶液洗滌一次，經硫酸鈉脫水，及過濾，減壓排除溶劑。產生7.00g(88%理論值，依據HPLC之純度為95%)標題化合物。 Sodium borohydride (1.26 g, 33.3 mmol) was added to a mixture of methanol (47 ml) and tetrahydrofuran (118 ml), and the mixture was stirred at room temperature for 5 min. A solution of 1-(5-chloro-1,3-thiazol-2-yl)-N-(pyridin-2-yl)methaneimine (7.40 g, 33.3 mmol) in tetrahydrofurane (350 ml) was slowly added dropwise. The reaction mixture was stirred at room temperature for 4 h then EtOAc (5 mL). After stirring for 5 min, acetic acid (1.5 ml) and water (20 ml) were added and the solution was stirred briefly. After addition of ethyl acetate (400 ml) and a 1.5% strength aqueous sodium hydroxide solution (400 ml), the phases were separated, and the organic phase was dried over sodium sulfate and filtered, The crude product was suspended in dichloromethane and extracted with 5% aq. The organic phase was separated, washed twice with water, washed with a saturated aqueous solution of sodium chloride, dried over sodium sulfate and filtered and evaporated. Yield 7.00 g (88% of theory, 95% purity according to HPLC) title compound.
HPLC-MS：logP(HCOOH)=0.46；logP(中性)=1.99；1H-NMR(400.0MHz,d6-DMSO)δ=8.00(d,1H),7.70(s,1H),7.46-7.42(m,2H),6.60-6.57(m,2H),4.66(d,2H)。 HPLC-MS: log P (HCOOH) = 0.46; mp (N.) = 1.99; 1 H-NMR (400.0 MHz, d 6 - DMSO) δ = 8.00 (d, 1H), 7.70 (s, 1H), 7.46- 7.42 (m, 2H), 6.60-6.57 (m, 2H), 4.66 (d, 2H).
類似上述方法製備下列通式(IX)化合物：N-[(5-氯-1,3-噻唑-2-基)甲基]吡啶-2-胺(化合物No.IX-2)
HPLC-MS：logP(HCOOH)=0.18；logP(中性)=1.81；1H-NMR(400.0MHz,d6-DMSO)δ=7.96(d,1H),7.40-7.34(m,2H),7.03(t,1H),6.55-6.48(m,2H),4.50(d,2H)。 HPLC-MS: log P (HCOOH) = 0.18; mp (N.) = 1.81; 1 H-NMR (400.0 MHz, d 6 - DMSO) δ = 7.96 (d, 1H), 7.40 - 7.34 (m, 2H), 7.03 (t, 1H), 6.55-6.48 (m, 2H), 4.50 (d, 2H).
N-[(6-氯吡啶-3-基)甲基]-1-甲基-1H-咪唑-2-胺(化合物No.IX-3)
HPLC-MS：logP(HCOOH)=0.18；logP(中性)=1.15；1H-NMR(400.0MHz,d6-DMSO)δ=8.39(d,1H),7.84(dd,1H),7.44(d,1H),6.59(d,1H),6.37(d,1H),6.26(t,1H),4.36(d,2H),3H在DMSO波峰下。 HPLC-MS: logP (HCOOH) = 0.18; logP ( neutral) = 1.15; 1 H-NMR (400.0MHz, d 6 -DMSO) δ = 8.39 (d, 1H), 7.84 (dd, 1H), 7.44 ( d, 1H), 6.59 (d, 1H), 6.37 (d, 1H), 6.26 (t, 1H), 4.36 (d, 2H), 3H.
N-[(2-氯-4-吡啶基)甲基]吡啶2-胺(化合物No.IX-4)
HPLC-MS：logP(中性)=1.66。 HPLC-MS: log P (neutral) = 1.66.
下表1所述根據本發明式(I-1)化合物係同樣較佳之根據本發明式(I)化合物，其等係依據或類似上述合成實例之方法製備。 The compounds of the formula (I-1) according to the invention are also preferably the compounds of the formula (I) according to the invention, which are prepared according to or analogously to the synthesis examples described above.
1H NMR數據1H NMR data b)b)
所選定實例之NMR數據：NMR波峰列表方法 NMR data for selected examples: 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 (ppm), and then the signal strength is listed in parentheses. Each pair of different signal peaks listed has a semicolon as a separator between the δ values and the signal strengths.
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(其同樣為本發明主題之一部份)訊號及/或雜質之波峰。 In addition, as shown in the typical 1H NMR image, 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波峰列表會出示常用溶劑波峰(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 common solvent peaks (eg DMSO peaks in DMSO-D 6 ) and water peaks, which are 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 means of "by-product fingerprints."
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。有關1H NMR波峰列表之進一步詳細內容可參見：Research Disclosure Database Number 564025。 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 detachment method is similar to the relevant peak selection method in a typical 1 H NMR interpretation. Further details regarding the 1H NMR peak list can be found in Research Disclosure Database Number 564025.
a)由酸性範圍內之LC-MS測定[M+H]+之方法係在pH 2.7下，使用乙腈(含0.1%甲酸)與水作為移動相；依10%乙腈至95%乙腈之線性梯度進行，儀器：Agilent 1100 LC系統、Agilent MSD系統、HTS PAL進行。 a) Determination of [M+H] + by LC-MS in the acidic range at pH 2.7 using acetonitrile (containing 0.1% formic acid) with water as the mobile phase; linear gradient from 10% acetonitrile to 95% acetonitrile Performed, instrumentation: Agilent 1100 LC system, Agilent MSD system, HTS PAL.
上述表中及製備實例中之logP值係依據EEC指令79/831 Annex V.A8，採用HPLC(高效液相層析法)，使用逆相管柱(C18)測定。溫度43℃。 The logP values in the above tables and in the preparation examples were determined by HPLC (High Performance Liquid Chromatography) using a reverse phase column (C18) according to EEC Directive 79/831 Annex V.A8. Temperature 43 ° C.
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。 Calibration was carried out using unbranched alkan-2-ones (having from 3 to 16 carbon atoms) with known logP-values.
b)1H NMR數據之測定法係採用Bruker Avance 400與III 600，裝備有樣本流量探頭(sample flow head)(容量60μl)，使用四甲基矽烷(0.0)與溶劑CD3CN、CDCl3或D6-DMSO作為參考物進行。 b) 1 H NMR data was determined using Bruker Avance 400 and III 600 equipped with a sample flow head (capacity 60 μl) using tetramethyl decane (0.0) with solvent CD 3 CN, CDCl 3 or D 6 -DMSO was carried out as a reference.
所選定實例之NMR數據係依傳統方式(δ值、多裂峰、氫原子數)或NMR波峰列表出示。 The NMR data for the selected examples are presented in a conventional manner (δ values, multiple peaks, number of hydrogen atoms) or NMR peaks.
下列實例說明根據本發明化合物之殺昆蟲與殺蜱蟎作用。此等實例中，所採用之根據本發明化合物係與表1所列之以對應參考編號(No.)表示之化合物相關：貓櫛頭蚤(Ctenocephalides felis)-使用貓蚤成蟲之活體外接觸試驗 The following examples illustrate the insecticidal and acaricidal effects of the compounds according to the invention. In these examples, the compounds according to the invention are used in connection with the compounds listed in Table 1 in the corresponding reference number (No.): Ctenocephalides felis - in vitro contact test using adult cat mites
塗佈試管時，先取9mg活性化合物溶於1ml丙酮p.a.中，然後使用丙酮p.a.稀釋至所需濃度。取250μl溶液加至25ml試管中，藉由於環繞式振盪器上旋轉振盪而均勻分佈在內壁與底部(於30rpm下振盪旋轉2h)。在900ppm活性化合物溶液與內表面積44.7cm2下，均勻分佈後可達到單位面積劑量為5μg/cm2。 When the test tube was coated, 9 mg of the active compound was first dissolved in 1 ml of acetone pa, and then diluted to the desired concentration with acetone pa. 250 μl of the solution was added to a 25 ml tube and evenly distributed on the inner wall and the bottom (rotational rotation at 30 rpm for 2 h) due to rotational oscillation on the wraparound oscillator. 900ppm of the active compound in the solution and the surface area of 44.7cm 2, uniformly distributed can reach the area of the dosage unit of 5μg / cm 2.
蒸發排除溶劑後，在試管中接種5-10隻貓蚤成蟲(貓櫛頭蚤(Ctenocephalides felis))，使用多孔之塑膠蓋封口，呈水平位置於室溫及環境濕度下培養。48h後，測定效力。最後試管直立，被擊倒的貓蚤落在試管底部。留在底部不動或以不協調方式移動的貓蚤則視為死亡或垂死。 After evaporating to remove the solvent, 5-10 cat mites ( Ctenocephalides felis ) were inoculated in a test tube, sealed with a porous plastic cap, and cultured at a horizontal position at room temperature and ambient humidity. After 48 h, the potency was determined. Finally, the test tube was erect, and the knocked down cat fell to the bottom of the test tube. Meerkats that remain at the bottom or move in an uncoordinated manner are considered dead or dying.
本試驗中，在5μg/cm2施用率下，對貓櫛頭蚤(Ctenocephalides felis)若達到至少80%效力時，則該物質顯示良好效力。100%效力意指所有跳蚤均已死 亡或垂死。0%效力意指沒有任何跳蚤受到傷害。 In this test, the substance showed good efficacy against Ctenocephalides felis at a rate of 5 μg/cm 2 if it reached at least 80% efficacy. 100% effectiveness means that all fleas are dead or dying. 0% effectiveness means no fleas are hurt.
本試驗中，例如：下列來自製備實例之化合物在5μg/cm2施用率下顯示100%效力：I-1-07、I-1-08、I-1-15、I-1-34 In this test, for example, the following compounds from the preparation examples showed 100% potency at an application rate of 5 μg/cm 2 : I-1-07, I-1-08, I-1-15, I-1-34
貓櫛頭蚤(Ctenocephalides felis)-口服試驗Ctenocephalides felis - oral test
溶劑：二甲亞碸 Solvent: dimethyl hydrazine
製備合適之活性化合物調配物時，取10mg活性化合物與0.5ml二甲亞碸混合。使用經過檸檬酸鹽處理之牛血稀釋至所需濃度。 When a suitable active compound formulation is prepared, 10 mg of the active compound is mixed with 0.5 ml of dimethyl hydrazine. Dilute to the desired concentration using citrated bovine blood.
取約20隻未餵食之貓蚤成蟲(貓櫛頭蚤(Ctenocephalides felis))置入上下均用紗布封口之小箱中。將一個底部已使用石蠟膜封口之金屬量筒置於箱子上。量筒中包含血液/活性化合物調配物，可讓跳蚤透過石蠟膜吸血。 About 20 unfed cat cockroaches ( Ctenocephalides felis ) were placed in a small box sealed with gauze. A metal measuring cylinder with a parafilm seal on the bottom is placed on the box. The cylinder contains a blood/active compound formulation that allows the flea to breathe through the parafilm.
兩天後，測定死亡率%。100%表示已殺死所有跳蚤；0%表示沒有殺死任何跳蚤。 Two days later, the % mortality was determined. 100% means that all fleas have been killed; 0% means that no fleas have been killed.
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示100%效力：I-1-07 In this test, for example, the following compounds from the preparation examples show 100% efficacy at 100 ppm application rate: I-1-07
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示90%效力：I-1-08 In this test, for example, the following compounds from the preparation examples show 90% efficacy at 100 ppm application rate: I-1-08
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示80%效力：I-1-06 In this test, for example, the following compounds from the preparation examples show 80% efficacy at 100 ppm application rate: I-1-06
綿羊赤銅綠蠅(Lucilia cuprina)試驗Sheep Lucilia cuprina test
溶劑：二甲亞碸 Solvent: dimethyl hydrazine
製備合適之活性化合物調配物時，取10mg活性化合物與0.5ml二甲亞碸混合，使用水稀釋該濃縮液至所需濃度。 When preparing a suitable active compound formulation, 10 mg of the active compound is mixed with 0.5 ml of dimethyl hydrazine and the concentrate is diluted with water to the desired concentration.
取約20隻澳洲綿羊赤銅綠蠅(Lucilia cuprina)L1幼蟲移至包含碎馬肉與所需濃度之活性化合物調配物之試驗容器中。 About 20 Australian sheep Lucilia cuprina L1 larvae were transferred to a test vessel containing the ground horse meat and the active compound formulation at the desired concentration.
2天後，測定死亡率%。100%表示已殺死所有幼蟲；0%表示沒有殺死任何幼蟲。 After 2 days, the % mortality was determined. 100% means that all larvae have been killed; 0% means that no larvae have been killed.
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示100%效力：I-1-07 In this test, for example, the following compounds from the preparation examples show 100% efficacy at 100 ppm application rate: I-1-07
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示95%效力：I-1-13 In this test, for example, the following compounds from the preparation examples show 95% potency at 100 ppm application rate: I-1-13
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示80%效力：I-1-06、I-1-08 In this test, for example, the following compounds from the preparation examples show 80% efficacy at 100 ppm application rate: I-1-06, I-1-08
家蠅(Musca domestica)試驗Musca domestica test
溶劑：二甲亞碸 Solvent: dimethyl hydrazine
製備合適之活性化合物調配物時，取10mg活性化合物與0.5ml二甲亞碸混合。加水稀釋該濃縮液至所需濃度。 When a suitable active compound formulation is prepared, 10 mg of the active compound is mixed with 0.5 ml of dimethyl hydrazine. The concentrate was diluted with water to the desired concentration.
取10隻家蠅(Musca domestica)成蟲接種至包含已經過糖溶液與所需濃度之活性化合物調配物處理之海綿之容器中。 Ten adult Musca domestica adults were inoculated into a container containing a sponge that had been treated with the sugar solution and the active compound formulation at the desired concentration.
2天後，測定死亡率%。100%表示已殺死所有蠅；0%表示沒有殺死任何蠅。 After 2 days, the % mortality was determined. 100% means that all flies have been killed; 0% means that no flies have been killed.
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示85%效力：I-1-06、I-1-08 In this test, for example, the following compounds from the preparation examples show 85% potency at 100 ppm application rate: I-1-06, I-1-08
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示80%效力：I-1-07、I-1-15、I-1-36 In this test, for example, the following compounds from the preparation examples show 80% potency at 100 ppm application rate: I-1-07, I-1-15, I-1-36
巴西玉米根蟲(Diabrotica balteata)-噴灑試驗Brazilian corn rootworm (Diabrotica balteata) - spray test
溶劑：78份重量比丙酮 Solvent: 78 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調配物時，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 formulation, dissolve 1 part by weight using a specified portion by weight of the solvent. The active compound is dosed and 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.
取預先膨脹之小麥種子(Triticum aestivum)於已填充洋菜及少量水之多孔盤中培養一天(每個洞5粒種子)。使用所需濃度之活性化合物調配物噴灑發芽之小麥種子。隨後，在每個洞中感染10-20隻玉米根蟲(Diabrotica balteata)之幼蟲。 The pre-expanded wheat seeds ( Triticum aestivum ) were cultured for one day (5 seeds per well) in a porous dish filled with amaranth and a small amount of water. The germinated wheat seeds are sprayed with the active compound formulation at the desired concentration. Subsequently, 10-20 larvae of Diabrotica balteata were infected in each well.
7天後，測定效力%。100%表示所有玉米植株之生長如同未處理、未感染之對照組；0%表示沒有任何玉米植株生長。 After 7 days, the potency % was determined. 100% means that all corn plants grow like untreated, uninfected controls; 0% means that there is no growth of any corn plants.
本試驗中，例如：下列來自製備實例之化合物在160μg/孔施用率下顯示100%效力：I-1-01、I-1-03、I-1-07、I-1-08、I-1-13、I-1-14、I-1-23、I-1-37 In this test, for example, the following compounds from the preparation examples showed 100% potency at 160 μg/well application rate: I-1-01, I-1-03, I-1-07, I-1-08, I- 1-13, I-1-14, I-1-23, I-1-37
本試驗中，例如：下列來自製備實例之化合物在160μg/孔施用率下顯示80%效力：I-1-12、I-1-42、I-1-51 In this test, for example, the following compounds from the preparation examples showed 80% potency at 160 μg/well application rate: I-1-12, I-1-42, I-1-51
南方根瘤線蟲(Meloidogyne incognita)試驗Meloidogyne incognita test
溶劑：125.0份重量比之丙酮 Solvent: 125.0 parts by weight of acetone
製備合適之活性化合物調配物時，由1份重量比之活性化合物與指定量溶劑混合，並加水稀釋該濃縮液至所需濃度。 When preparing a suitable active compound formulation, the active compound is mixed with a specified amount of the solvent in an amount by weight, 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、包含南方根瘤線蟲(Meloidogyne incognita)之卵/幼蟲之懸浮液、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, a solution of the active compound, a suspension of eggs/larvae containing Meloidogyne incognita , and lettuce seeds. Let the lettuce seeds germinate and grow into plants. Forming insects at the roots.
14天後，依據蟲癭之形成百分比決定殺線蟲效力%。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之對照組植物。 After 14 days, the nematicidal efficacy % was determined based on the percentage of formation of the worm. 100% means that no insects appeared; 0% means that the number of insects in the treated group was equivalent to the untreated control plants.
本試驗中，例如：下列來自製備實例之化合物在20ppm施用率下顯示100%效力：I-1-01、I-1-25 In this test, for example, the following compounds from the preparation examples show 100% efficacy at an application rate of 20 ppm: I-1-01, I-1-25
本試驗中，例如：下列來自製備實例之化合物在20ppm施用率下顯示90% 效力：I-1-07、I-1-37、I-1-51、I-1-60、I-1-72 In this test, for example, the following compounds from the preparation examples show 90% at an application rate of 20 ppm. Efficacy: I-1-07, I-1-37, I-1-51, I-1-60, I-1-72
桃赤蚜(Myzus persicae)-口服試驗Myzus persicae - oral test
溶劑：100份重量比丙酮 Solvent: 100 parts by weight of acetone
製備合適之活性化合物調配物時，由1份重量比之活性化合物溶於指定量溶劑中，並加水稀釋該濃縮液至所需濃度。 When preparing a suitable active compound formulation, the active compound is dissolved in a specified amount of the solvent in a weight ratio, and the concentrate is diluted with water to the desired concentration.
在填充活性化合物調配物之容器上蓋上一層薄膜，讓桃赤蚜(Myzus persicae)之混齡族群可以吸取溶液。 A container is placed over the container filled with the active compound formulation to allow the mixed population of Myzus persicae to absorb the solution.
5天後，測定效力%。100%表示已殺死所有蚜蟲；0%表示沒有殺死任何蚜蟲。 After 5 days, the potency was determined. 100% means that all aphids have been killed; 0% means that no aphids have been killed.
本試驗中，例如：下列來自製備實例之化合物在20ppm施用率下顯示100%效力：I-1-01、I-1-02、I-1-05、I-1-06、I-1-07、I-1-08、I-1-09、I-1-10、I-1-11、I-1-12、I-1-13、I-1-14、I-1-15、I-1-16、I-1-17、I-1-18、I-1-19、I-1-20、I-1-22、I-1-23、I-1-24、I-1-25、I-1-26、I-1-27、I-1-28、I-1-29、I-1-30、I-1-31、I-1-32,I-1-33、I-1-34、I-1-35、I-1-36、I-1-37、I-1-38、I-1-39、I-1-40、I-1-41、I-1-42、I-1-43、I-1-44、I-1-45、I-1-47、I-1-48、I-1-49、I-1-50、I-1-51、I-1-52、I-1-53、I-1-54、I-1-55、I-1-56、I-1-57、I-1-61、I-1-62、I-1-63、I-1-64、I-1-65、I-1-66、I-1-67、I-1-68、I-1-69、I-1-70、I-1-71、I-1-72、I-1-75、I-1-76、I-1-77、I-1-79、I-1-80、I-1-81、I-1-82、I-1-84 In this test, for example, the following compounds from the preparation examples show 100% potency at an application rate of 20 ppm: I-1-01, I-1-02, I-1-05, I-1-06, I-1- 07, I-1-08, I-1-09, I-1-10, I-1-11, I-1-12, I-1-13, I-1-14, I-1-15, I-1-16, I-1-17, I-1-18, I-1-19, I-1-20, I-1-22, I-1-23, I-1-24, I- 1-25, I-1-26, I-1-27, I-1-28, I-1-29, I-1-30, I-1-31, I-1-32, I-1- 33, I-1-34, I-1-35, I-1-36, I-1-37, I-1-38, I-1-39, I-1-40, I-1-41, I-1-42, I-1-43, I-1-44, I-1-45, I-1-47, I-1-48, I-1-49, I-1-50, I- 1-51, I-1-52, I-1-53, I-1-54, I-1-55, I-1-56, I-1-57, I-1-61, I-1- 62, I-1-63, I-1-64, I-1-65, I-1-66, I-1-67, I-1-68, I-1-69, I-1-70, I-1-71, I-1-72, I-1-75, I-1-76, I-1-77, I-1-79, I-1-80, I-1-81, I- 1-82, I-1-84
本試驗中，例如：下列來自製備實例之化合物在20ppm施用率下顯示90%效力：I-1-03、I-1-83 In this test, for example, the following compounds from the preparation examples show 90% potency at an application rate of 20 ppm: I-1-03, I-1-83
桃赤蚜(Myzus persicae)-噴灑試驗Myzus persicae - spray test
溶劑：78份重量比丙酮 Solvent: 78 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調配物時，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 formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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. .
在感染所有蟲齡之桃赤蚜(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調配物。 The active compound formulation of the desired concentration is sprayed onto leaf discs of Brassica pekinensis infected with all of the larvae of Myzus persicae .
6天後，測定效力%。100%表示已殺死所有蚜蟲；0%表示沒有殺死任何蚜蟲。 After 6 days, the potency was determined. 100% means that all aphids have been killed; 0% means that no aphids have been killed.
本試驗中，例如：下列來自製備實例之化合物在500g/ha施用率下顯示100%效力：I-1-06、I-1-11、I-1-14、I-1-15、I-1-16、I-1-18、I-1-19、I-1-25、I-1-26、I-1-32、I-1-34、I-1-35、I-1-36、I-1-37、I-1-38、I-1-39、I-1-42、I-1-43、I-1-44、I-1-45、I-1-46、I-1-47、I-1-52、I-1-53、I-1-61、I-1-64,I-1-65、I-1-66、I-1-67、I-1-69、I-1-70、I-1-71、I-1-72、I-1-76、I-1-80、I-1-81 In this test, for example, the following compounds from the preparation examples show 100% potency at an application rate of 500 g/ha: I-1-06, I-1-11, I-1-14, I-1-15, I- 1-16, I-1-18, I-1-19, I-1-25, I-1-26, I-1-32, I-1-34, I-1-35, I-1- 36, I-1-37, I-1-38, I-1-39, I-1-42, I-1-43, I-1-44, I-1-45, I-1-46, I-1-47, I-1-52, I-1-53, I-1-61, I-1-64, I-1-65, I-1-66, I-1-67, I- 1-69, I-1-70, I-1-71, I-1-72, I-1-76, I-1-80, I-1-81
本試驗中，例如：下列來自製備實例之化合物在500g/ha施用率下顯示90%效力：I-1-01、I-1-02、I-1-05、I-1-07、I-1-08、I-1-09、I-1-10、I-1-12、I-1-13、I-1-17、I-1-20、I-1-21、I-1-22、I-1-23、I-1-24、I-1-28、I-1-29、I-1-30、I-1-31、I-1-33、I-1-40、I-1-41、I-1-48、I-1-50、I-1-59、I-1-62、I-1-63、I-1-68、I-1-75、I-1-77、I-1-79、I-1-83 In this test, for example, the following compounds from the preparation examples showed 90% potency at an application rate of 500 g/ha: I-1-01, I-1-02, I-1-05, I-1-07, I- 1-08, I-1-09, I-1-10, I-1-12, I-1-13, I-1-17, I-1-20, I-1-21, I-1- 22. I-1-23, I-1-24, I-1-28, I-1-29, I-1-30, I-1-31, I-1-33, I-1-40, I-1-41, I-1-48, I-1-50, I-1-59, I-1-62, I-1-63, I-1-68, I-1-75, I- 1-77, I-1-79, I-1-83
桃赤蚜(Myzus persicae)-噴灑試驗Myzus persicae - spray test
溶劑：14份重量比二甲基甲醯胺 Solvent: 14 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調配物時，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。若需要添加銨鹽或/與滲透劑時，可分別添加1000ppm濃度至調配溶液中。 When preparing a suitable active compound formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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. If it is necessary to add an ammonium salt or/and a penetrating agent, a concentration of 1000 ppm may be separately added to the formulation solution.
在嚴重感染桃赤蚜(Myzus persicae)之青椒植物(Capsicum annuum)上噴灑所需濃度之活性化合物調配物處理。 The active compound formulation of the desired concentration is sprayed on a green pepper plant ( Capsicum annuum ) that is heavily infected with Myzus persicae .
6天後，測定死亡率%。100%意指已殺死所有蚜蟲；0%意指沒有殺死任何蚜蟲。 After 6 days, the % mortality was determined. 100% means that all aphids have been killed; 0% means that no aphids have been killed.
本試驗中，例如：下列來自製備實例之化合物在100ppm施用率下顯示99%效力：I-1-27 In this test, for example, the following compounds from the preparation examples show 99% potency at 100 ppm application rate: I-1-27
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調配物時，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 formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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調配物噴灑捲心白菜(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 formulation at the desired concentration, dried and inoculated with larvae of Phaedon cochleariae .
7天後，測定效力%。100%意指已殺死所有猿葉蟲幼蟲；0%意指沒有殺死任何猿葉蟲幼蟲。 After 7 days, the potency % was determined. 100% means that all locust larvae have been killed; 0% means that no locust larvae have been killed.
本試驗中，例如：下列來自製備實例之化合物在500g/ha施用率下顯示100%效力：I-1-03、I-1-07 In this test, for example, the following compounds from the preparation examples show 100% efficacy at an application rate of 500 g/ha: I-1-03, I-1-07
本試驗中，例如：下列來自製備實例之化合物在500g/ha施用率下顯示83%效力：I-1-65、I-1-68 In this test, for example, the following compounds from the preparation examples showed 83% potency at an application rate of 500 g/ha: I-1-65, I-1-68
草地斜紋夜蛾(Spodoptera frugiperda)-噴灑試驗Spodoptera frugiperda - 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調配物時，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 formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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.
在玉米(Zea mays)葉圓片上噴灑所需濃度之活性化合物調配物，乾燥後，即接種草地斜紋夜蛾(Spodoptera frugiperda)幼蟲。 The active compound formulation of the desired concentration is sprayed on the corn leaf (Zea mays) leaves, and after drying, the larvae of Spodoptera frugiperda are inoculated.
7天後，測定效力%。100%表示已殺死所有幼蟲；0%表示沒有殺死任何幼蟲。 After 7 days, the potency % was determined. 100% means that all larvae have been killed; 0% means that no larvae have been killed.
本試驗中，例如：下列來自製備實例之化合物在500g/ha施用率下顯示100%效力：I-1-06、I-1-07 In this test, for example, the following compounds from the preparation examples show 100% efficacy at an application rate of 500 g/ha: I-1-06, I-1-07
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調配物時，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 formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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.
在感染所有蟲齡溫室紅葉蟎(Tetranychus urticae)之菜豆(Phaseolus vulgaris)葉圓片上噴灑所需濃度之活性化合物調配物。 The active compound formulation of the desired concentration is sprayed onto leaf disks of Phaseolus vulgaris infected with all of the insect-aged greenhouses of Tetranychus urticae .
6天後，測定效力%。100%表示已殺死所有蜘蛛蟎；0%表示沒有殺死任何蜘蛛蟎。 After 6 days, the potency was determined. 100% means that all spider mites have been killed; 0% means that no spider mites have been killed.
本試驗中，例如：下列來自製備實例之化合物在500g/ha施用率下顯示90%效力：I-1-41 In this test, for example, the following compounds from the preparation examples show 90% efficacy at an application rate of 500 g/ha: I-1-41
棉蚜(Aphis gossypii)-噴灑試驗(APHIGO)Aphis gossypii - Spray Test (APHIGO)
溶劑：14份重量比二甲基甲醯胺 Solvent: 14 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調配物時，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。若需要添加銨鹽或/與滲透劑時，可分別添加1000ppm濃度至調配溶液中。 When preparing a suitable active compound formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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. If it is necessary to add an ammonium salt or/and a penetrating agent, a concentration of 1000 ppm may be separately added to the formulation solution.
使用所需濃度之活性化合物調配物噴灑嚴重感染棉蚜(Aphis gossypii)之棉花植株(Gossypium hirsutum)。 A cotton plant ( Gossypium hirsutum ) that is heavily infected with cotton aphid ( Aphis gossypii ) is sprayed with the active compound formulation at the desired concentration.
經過所需時間後，測定消滅%。100%表示已殺死所有蚜蟲；0%表示沒有殺死任何蚜蟲。 After the required time, the % elimination was determined. 100% means that all aphids have been killed; 0% means that no aphids have been killed.
本試驗中，例如：下列來自製備實例之化合物顯示優於先前技藝之效力：參見表2。 In this test, for example, the following compounds from the preparation examples show superior efficacy to the prior art: see Table 2.
褐飛虱(Nilaparvata lugens)噴灑試驗(NILALU)Nilaparvata lugens spray test (NILALU)
溶劑：14份重量比二甲基甲醯胺 Solvent: 14 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調配物時，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。若需要添加銨鹽或/與滲透劑時，可分別添加1000ppm濃度至調配溶液中。 When preparing a suitable active compound formulation, the active compound is dissolved in a ratio of parts by weight of the solvent, and water containing 1000 ppm of 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. If it is necessary to add an ammonium salt or/and a penetrating agent, a concentration of 1000 ppm may be separately added to the formulation solution.
使用所需濃度之活性化合物調配物噴灑稻植株(Oryza sativa)後，接種褐飛虱(Nilaparvata lugens)幼蟲。 After spraying the rice plants (Oryza sativa) with the active compound formulation of the desired concentration, the larvae of Nilaparvata lugens were inoculated.
經過所需時間後，測定消滅%。100%表示已殺死所有褐飛虱；0%表示沒有殺死任何褐飛虱。 After the required time, the % elimination was determined. 100% means that all brown planthoppers have been killed; 0% means that no brown planthoppers have been killed.
本試驗中，例如：下列來自製備實例之化合物顯示優於先前技藝之效力：參見表2。 In this test, for example, the following compounds from the preparation examples show superior efficacy to the prior art: see Table 2.
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| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| BR112018075734A2 (en) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | compound, pharmaceutical composition, method of treating a patient with a disease or condition mediated at least in part by fxr, and use of a compound. |
| PL3600309T3 (en) | 2017-03-28 | 2022-11-07 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
| JP7265635B2 (en) | 2019-01-15 | 2023-04-26 | ギリアード サイエンシーズ， インコーポレイテッド | FXR (NR1H4) modulating compounds |
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| SK11422003A3 (en) * | 2001-03-15 | 2004-04-06 | Basf Aktiengesellschaft | 5-Phenylpyrimidine, methods and intermediate products for production thereof and use of same for controlling pathogenic fungi |
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| JP2013241403A (en) * | 2012-04-24 | 2013-12-05 | Nissan Chem Ind Ltd | Malonic acid amide compound and pest control agent |
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