CN1294489A - Fungicide mixtures based on triple oxime ether derivatives and rice fungicides - Google Patents
Fungicide mixtures based on triple oxime ether derivatives and rice fungicides Download PDFInfo
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Abstract
Description
本发明涉及防治有害真菌的杀真菌混合物,它包含a)式(Ⅰ)的苯基乙酸衍生物及其盐其中取代基和符号具有下列含意:X 是NOCH3、CHOCH3或CHCH3;Y 是氧或NR;R1、R相互独立地是氢或C1-C4-烷基;R2是氰基、硝基、三氟甲基、卤素、C1-C4-烷基或C1-C4-烷氧基;m 是0、1或2,其中如果m是2,则基团R2可以相同或不同;R3是氢、氰基、C1-C4-烷基、C1-C4-卤代烷基或C3-C6-环烷基;R4、R6相互独立地是氢,The present invention relates to a fungicidal mixture for controlling harmful fungi, which comprises a) phenylacetic acid derivatives of formula (I) and salts thereof Wherein the substituents and symbols have the following meanings: X is NOCH 3 , CHOCH 3 or CHCH 3 ; Y is oxygen or NR; R 1 , R are independently hydrogen or C 1 -C 4 -alkyl; R 2 is cyano , nitro, trifluoromethyl, halogen, C 1 -C 4 -alkyl or C 1 -C 4 -alkoxy; m is 0, 1 or 2, wherein if m is 2, the group R 2 can The same or different; R 3 is hydrogen, cyano, C 1 -C 4 -alkyl, C 1 -C 4 -halogenated alkyl or C 3 -C 6 -cycloalkyl; R 4 , R 6 are independently hydrogen ,
是C1-C10-烷基、C3-C6-环烷基、C2-C10-烯基、C2-C10-炔基、C1-C10-is C 1 -C 10 -alkyl, C 3 -C 6 -cycloalkyl, C 2 -C 10 -alkenyl, C 2 -C 10 -alkynyl, C 1 -C 10 -
烷基羰基、C2-C10-烯基羰基、C3-C10-炔基羰基或C1-C10-烷基磺酰Alkylcarbonyl, C 2 -C 10 -alkenylcarbonyl, C 3 -C 10 -alkynylcarbonyl or C 1 -C 10 -alkylsulfonyl
基,其中这些基团可以被部分或全部卤代,或可以带有一至三个groups, where these groups may be partially or fully halogenated, or may carry one to three
下列基团:氰基、硝基、羟基、巯基、氨基、羧基、氨基羰基、The following groups: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl,
氨基硫代羰基、卤素、C1-C6-烷基、C1-C6-卤代烷基、C1-C6-烷基Aminothiocarbonyl, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -alkyl
磺酰基、C1-C6-烷基磺酰氧基、C1-C6-烷氧基、C1-C6-卤代烷氧基、Sulfonyl, C 1 -C 6 -Alkylsulfonyloxy, C 1 -C 6 -Alkoxy, C 1 -C 6 -Haloalkoxy,
C1-C6-烷氧基羰基、C1-C6-烷硫基、C1-C6-烷基氨基、二-C1-C6-烷C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -alkane
基氨基、C1-C6-烷基氨基羰基、二-C1-C6-烷基氨基羰基、C1-C6-Amino, C 1 -C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -
烷基氨基硫代羰基、二-C1-C6-烷基氨基硫代羰基、C2-C6-烯基、Alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 -alkenyl,
C2-C6-烯氧基、C3-C6-环烷基、C3-C6-环烷基氧基、杂环基、杂环C 2 -C 6 -alkenyloxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, heterocyclyl, heterocycle
基氧基、苄基、苄氧基、芳基、芳氧基、芳硫基、杂芳基、杂芳yloxy, benzyl, benzyloxy, aryl, aryloxy, arylthio, heteroaryl, heteroaryl
氧基和杂芳硫基,其中环状基团部分可以被部分或全部卤代,或Oxy and heteroarylthio, wherein the cyclic group moiety may be partially or fully halogenated, or
可以带有一至三个下列基团:氰基、硝基、羟基、巯基、氨基、Can carry one to three of the following groups: cyano, nitro, hydroxyl, mercapto, amino,
羧基、氨基羰基、氨基硫代羰基、卤素、C1-C6-烷基、C1-C6-卤代Carboxyl, Aminocarbonyl, Aminothiocarbonyl, Halogen, C 1 -C 6 -Alkyl, C 1 -C 6 -Halo
烷基、C1-C6-烷基磺酰基、C1-C6-烷基磺酰氧基、C1-C6-烷氧基、Alkyl, C 1 -C 6 -alkylsulfonyl, C 1 -C 6 -alkylsulfonyloxy, C 1 -C 6 -alkoxy,
C1-C6-卤代烷氧基、C1-C6-烷氧基羰基、C1-C6-烷硫基、C1-C6-烷C 1 -C 6 -haloalkoxy, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alk
基氨基、二-C1-C6-烷基氨基、C1-C6-烷基氨基羰基、二-C1-C6-烷di-C 1 -C 6 -alkylamino, C 1 -C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkane
基氨基羰基、C1-C6-烷基氨基硫代羰基、二-C1-C6-烷基氨基硫代Aminocarbonyl, C 1 -C 6 -Alkylaminothiocarbonyl, Di-C 1 -C 6 -Alkylaminothiocarbonyl
羰基、C2-C6-烯基、C2-C6-烯氧基、C3-C6-环烷基、C3-C6-环烷基Carbonyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyloxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl
氧基、杂环基、杂环基氧基、苄基、苄氧基、芳基、芳氧基、芳Oxy, heterocyclyl, heterocyclyloxy, benzyl, benzyloxy, aryl, aryloxy, aryl
硫基、杂芳基、杂芳氧基、杂芳硫基和C(=NOR7)-An-R8;Thio, heteroaryl, heteroaryloxy, heteroarylthio and C(=NOR 7 )-A n -R 8 ;
是芳基、芳基羰基、芳基磺酰基、杂芳基、杂芳基羰基或杂芳基is aryl, arylcarbonyl, arylsulfonyl, heteroaryl, heteroarylcarbonyl, or heteroaryl
磺酰基,其中这些基团可以被部分或全部卤代,或可以带有一至Sulfonyl, where these groups may be partially or fully halogenated, or may carry from one to
三个下列基团:氰基、硝基、羟基、巯基、氨基、羧基、氨基羰Three of the following groups: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl
基、氨基硫代羰基、卤素、C1-C6-烷基、C1-C6-卤代烷基、C1-C6-radical, aminothiocarbonyl, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -
烷基磺酰基、C1-C6-烷基磺酰氧基、C1-C6-烷氧基、C1-C6-卤代烷Alkylsulfonyl, C 1 -C 6 -alkylsulfonyloxy, C 1 -C 6 -alkoxy, C 1 -C 6 -halogenated alkyl
氧基、C1-C6-烷氧基羰基、C1-C6-烷硫基、C1-C6-烷基氯基、二-C1-C6-Oxygen, C 1 -C 6 -Alkoxycarbonyl, C 1 -C 6 -Alkylthio, C 1 -C 6 -Alkylchloride, Di-C 1 -C 6 -
烷基氨基、C1-C6-烷基氨基羰基、二-C1-C6-烷基氨基羰基、C1-C6-Alkylamino, C 1 -C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -
烷基氨基硫代羰基、二-C1-C6-烷基氨基硫代羰基、C2-C6-烯基、Alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 -alkenyl,
C2-C6-烯氧基、C3-C6-环烷基、C3-C6-环烷基氧基、苄基、苄氧基、C 2 -C 6 -alkenyloxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, benzyl, benzyloxy,
芳基、芳氧基、芳硫基、杂芳基、杂芳氧基、杂芳硫基和Aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy, heteroarylthio and
C(=NOR7)-An-R8;R5是氢,C(=NOR 7 )-A n -R 8 ; R 5 is hydrogen,
是C1-C6-烷基、C2-C6-烯基、C2-C6-炔基,其中这些基团可以被部is C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, wherein these groups may be partially
分或全部卤代,或可以带有一至三个下列基团:氰基、硝基、羟Partly or fully halogenated, or may carry one to three of the following groups: cyano, nitro, hydroxyl
基、巯基、氨基、羧基、氨基羰基、氨基硫代羰基、卤素、C1-C6-Group, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, halogen, C 1 -C 6 -
烷基氨基羰基、二-C1-C6-烷基氨基羰基、C1-C6-烷基氨基硫代羰Alkylaminocarbonyl, Di-C 1 -C 6 -Alkylaminocarbonyl, C 1 -C 6 -Alkylaminothiocarbonyl
基、二-C1-C6-烷基氨基硫代羰基、C1-C6-烷基磺酰基、C1-C6-烷Di-C 1 -C 6 -alkylaminothiocarbonyl, C 1 -C 6 -alkylsulfonyl, C 1 -C 6 -alkane
基磺酰氧基、C1-C6-烷氧基、C1-C6-卤代烷氧基、C1-C6-烷氧基羰Sulfonyloxy, C 1 -C 6 -alkoxy, C 1 -C 6 -haloalkoxy, C 1 -C 6 -alkoxycarbonyl
基、C1-C6-烷硫基、C1-C6-烷基氨基、二-C1-C6-烷基氨基、C2-C6-radical, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -alkylamino, C 2 -C 6 -
烯氧基、C3-C6-环烷基、C3-C6-环烷基氧基、杂环基、杂环基氧基、Alkenyloxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, heterocyclyl, heterocyclyloxy,
芳基、芳氧基、芳基-C1-C4-烷氧基、芳硫基、芳基-C1-C4-烷硫基、Aryl, aryloxy, aryl-C 1 -C 4 -alkoxy, arylthio, aryl-C 1 -C 4 -alkylthio,
杂芳基、杂芳氧基、杂芳基-C1-C4-烷氧基、杂芳硫基、杂芳基-C1-C4-Heteroaryl, heteroaryloxy, heteroaryl-C 1 -C 4 -alkoxy, heteroarylthio, heteroaryl-C 1 -C 4 -
烷硫基,其中环状基团部分可以被部分或全部卤代,或可以带有Alkylthio, wherein the cyclic group moiety may be partially or fully halogenated, or may carry
一至三个下列基团:氰基、硝基、羟基、巯基、氨基、羧基、氨One to three of the following groups: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, ammonia
基羰基、氨基硫代羰基、C1-C6-烷基、C1-C6-卤代烷基、C1-C6-烷C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -alk
基磺酰基、C1-C6-烷基磺酰氧基、C3-C6-环烷基、C1-C6-烷氧基、Sulfonyl, C 1 -C 6 -alkylsulfonyloxy, C 3 -C 6 -cycloalkyl, C 1 -C 6 -alkoxy,
C1-C6-卤代烷氧基、C1-C6-烷氧基羰基、C1-C6-烷硫基、C1-C6-烷C 1 -C 6 -haloalkoxy, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alk
基氨基、二-C1-C6-烷基氨基、C1-C6-烷基氨基羰基、二-C1-C6-烷di-C 1 -C 6 -alkylamino, C 1 -C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkane
基氨基羰基、C1-C6-烷基氨基硫代羰基、二-C1-C6-烷基氨基硫代Aminocarbonyl, C 1 -C 6 -Alkylaminothiocarbonyl, Di-C 1 -C 6 -Alkylaminothiocarbonyl
羰基、C2-C6-烯基、C2-C6-烯氧基、苄基、苄氧基、芳基、芳氧基、Carbonyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyloxy, benzyl, benzyloxy, aryl, aryloxy,
芳硫基、杂芳基、杂芳氧基、杂芳硫基和C(=NOR7)-An-R8;Arylthio, heteroaryl, heteroaryloxy, heteroarylthio and C(=NOR 7 )-A n -R 8 ;
是C3-C6-环烷基、C3-C6-环烯基、杂环基、芳基、杂芳基,其中is C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkenyl, heterocyclyl, aryl, heteroaryl, wherein
环状基团部分可以被部分或全部卤代,或可以带有一至三个下列The cyclic moiety may be partially or fully halogenated, or may carry one to three of the following
基团:氰基、硝基、羟基、巯基、氨基、羧基、氨基羰基、氨基Groups: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, amino
硫代羰基、C1-C6-烷基、C1-C6-卤代烷基、C1-C6-烷基磺酰基、C1-Thiocarbonyl, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -alkylsulfonyl, C 1 -
C6-烷基磺酰氧基、C3-C6-环烷基、C1-C6-烷氧基、C1-C6-卤代烷氧C 6 -Alkylsulfonyloxy, C 3 -C 6 -Cycloalkyl, C 1 -C 6 -Alkoxy, C 1 -C 6 -Haloalkoxy
基、C1-C6-烷氧基羰基、C1-C6-烷硫基、C1-C6-烷基氨基、二-C1-C6-radical, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -
烷基氨基、C1-C6-烷基氨基羰基、二-C1-C6-烷基氨基羰基、C1-C6-Alkylamino, C 1 -C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -
烷基氨基硫代羰基、二-C1-C6-烷基氨基硫代羰基、C2-C6-烯基、Alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 -alkenyl,
C2-C6-烯氧基、苄基、苄氧基、芳基、芳氧基、芳硫基、杂芳基、C 2 -C 6 -alkenyloxy, benzyl, benzyloxy, aryl, aryloxy, arylthio, heteroaryl,
杂芳氧基、杂芳硫基和C(=NOR7)-An-R8;Heteroaryloxy, heteroarylthio and C(=NOR 7 )-A n -R 8 ;
其中in
A是氧、硫或氮,且其中氮带有氢或C1-C6-烷基;A is oxygen, sulfur or nitrogen, wherein nitrogen carries hydrogen or C 1 -C 6 -alkyl;
n 是0或1;n is 0 or 1;
R7是氢或C1-C6-烷基,和R 7 is hydrogen or C 1 -C 6 -alkyl, and
R8是氢或C1-C6-烷基,和b)至少一种选自下列式Ⅱ至Ⅶ的杀真菌剂 R 8 is hydrogen or C 1 -C 6 -alkyl, and b) at least one fungicide selected from the following formulas II to VII
本发明的目的是提供在特别是防治稻作物真菌病害上具有超越混合物单个组分的良好杀真菌活性的杀真菌混合物。It is an object of the present invention to provide fungicidal mixtures which have a good fungicidal activity over and above the individual components of the mixture, especially against fungal diseases of rice crops.
我们发现,此目的通过权利要求1中要求的混合物实现。We have found that this object is achieved by the mixture claimed in claim 1 .
式Ⅰ化合物及其制备是本身已知的,且描述于文献中(WO 97/15552)。The compounds of formula I and their preparation are known per se and described in the literature (WO 97/15552).
式Ⅱ至Ⅶ的杀虫剂同样是已知的且描述于文献中。另外,它们以下文括号中所提到的商标名出售:Ⅱ:GB 1394373,通用名:咯喹酮(商标名:Coratop,诺华公司生产);Ⅲ:GB 1419121,通用名:三环唑(商标名:Beam,陶氏益农公司生产);Ⅳ:第八届杀虫剂杀菌剂大会议文集(Proc.Insect.Fungic.Conf.8th),2(1975),715,通用名:稻瘟病(商标名:富士一号,日本农药株式会社生产);Ⅴ:DE 1493736,通用名:敌瘟磷(商标名:Hinosan,拜耳公司生产);Ⅵ:GB-A-1312536、US 3755350;通用名:嘧菌腙(商标名:takeda生产);Ⅶ:农药手册第10版,1994,482;通用名:咯菌腈(商标名:Celest,诺华公司生产)。The insecticides of the formulas II to VII are likewise known and described in the literature. In addition, they are sold under the trade names mentioned in the following brackets: Ⅱ: GB 1394373, common name: pyroquinone (trade name: Coratop® , produced by Novartis); Ⅲ: GB 1419121, common name: tricyclazole ( Trademark name: Beam®, produced by Dow AgroSciences); Ⅳ: Proceedings of the Eighth Conference on Insecticides and Fungicides (Proc.Insect.Fungic.Conf.8 th ), 2(1975), 715, common name: Rice blast (trade name: Fuji No. 1, produced by Japan Agricultural Chemical Co., Ltd.); Ⅴ: DE 1493736, common name: difenfos (trade name: Hinosan , produced by Bayer); Ⅵ: GB-A-1312536, US 3755350; common name: pyrizone (trade name: manufactured by Takeda); VII: Pesticide Handbook, 10th edition, 1994, 482; common name: fludioxonil (trade name: Celest®, manufactured by Novartis).
由于C=C和C=N双键,化合物Ⅰ的制备可以产生E/Z异构体混合物,它们可以用常规方式例如结晶法或色谱法分离成单独的化合物。Due to the C=C and C=N double bonds, the preparation of compounds I may result in a mixture of E/Z isomers which can be separated into individual compounds by conventional means such as crystallization or chromatography.
然而,如果合成产生异构体混合物,由于在某些情况下(例如在光或酸或碱作用下)在准备使用或在使用中,单独的异构体可以相互转换,因此通常不需要进行分离。类似的转化还可以在使用中发生,例如在处理植物时或处理过的植物上或在意欲防治的有害真菌或动物害虫上。However, if the synthesis results in a mixture of isomers, separation is usually not required since the individual isomers can be interconverted under certain circumstances (e.g., under the action of light or acids or bases) either ready for use or in use . Similar transformations can also take place in use, for example when or on treated plants or on harmful fungi or animal pests which are to be controlled.
对于其活性而言,由于C=X双键,优选的是化合物Ⅰ的Z异构体(以-OCH3或-CH3基团相对于-CO2R1基团的构型而言)。For its activity, the Z isomer of compound I (in terms of the configuration of the -OCH3 or -CH3 group relative to the -CO2R1 group) is preferred due to the C=X double bond.
对于其活性而言,由于-C(R3)=NOCH2-双键,优选的是化合物Ⅰ的顺式异构体(以R3基团相对于-OCH2-基团的构型而言)。For its activity, due to the -C(R 3 )=NOCH 2 - double bond, the cis isomer of compound I is preferred (in terms of the configuration of the R 3 group relative to the -OCH 2 - group ).
在开头给出的化合物Ⅰ的定义中,使用的上位概念通常表示下列基团:卤素:氟、氯、溴和碘;烷基:具有1至4、6或10个碳原子的直链或支链烷基,例如,C1-C6-烷基甲基、乙基、丙基、1-甲基乙基、丁基、1-甲基丙基、2-甲基丙基、1,1-二甲基乙基、戊基、1-甲基丁基、2-甲基丁基、3-甲基丁基、1,1-二甲基丙基、1,2-二甲基丙基、2,2-二甲基丙基、1-乙基丙基、己基、1-甲基戊基、2-甲基戊基、3-甲基戊基、4-甲基戊基、1,1-二甲基丁基、1,2-二甲基丁基、1,3-二甲基丁基、2,2-二甲基丁基、2,3-二甲基丁基、3,3-二甲基丁基、1-乙基丁基、1,1,2-三甲基丙基、1,2,2-三甲基丙基、1-乙基-1-甲基丙基或1-乙基-2-甲基丙基;卤代烷基:具有1至6个碳原子的直链或支链烷基,其部分或全部被上述提到的卤素原子取代,例如C1-C2-卤代烷基,如氯甲基、二氯甲基、三氯甲基、氟甲基、二氟甲基、三氟甲基、氯氟甲基、二氯氟甲基、氯二氟甲基、1-氟乙基、2-氟乙基、2,2-二氟乙基、2,2,2-三氟乙基、2-氯-2-氟乙基、2-氯-2,2-二氟乙基、2,2-二氯-2-氟乙基、2,2,2-三氯乙基和五氟乙基;环烷基:具有3至6个环成员的单环状烷基,例如环丙基、环丁基、环戊基和环己基;烯基:具有2至6或10个碳原子且在任一位置上有一双键的直链或支链烯基,例如,C2-C6-烯基如1-丙烯基、2-丙烯基、1-甲基乙烯基、1-丁烯基、2-丁烯基、3-丁烯基、1-甲基-1-丙烯基、2-甲基-1-丙烯基、1-甲基-2-丙烯基、2-甲基-2-丙烯基、1-戊烯基、2-戊烯基、3-戊烯基、4-戊烯基、1-甲基-1-丁烯基、2-甲基-1-丁烯基、3-甲基-1-丁烯基、1-甲基-2-丁烯基、2-甲基-2-丁烯基、3-甲基-2-丁烯基、1-甲基-3-丁烯基、2-甲基-3-丁烯基、3-甲基-3-丁烯基、1,1-二甲基-2-丙烯基、1,2-二甲基-2-丙烯基、1,2-二甲基-2-丙烯基、1-乙基-1-丙烯基、1-乙基-2-丙烯基、1-己烯基、2-己烯基、3-己烯基、4-己烯基、5-己烯基、1-甲基-1-戊烯基、2-甲基-1-戊烯基、3-甲基-1-戊烯基、4-甲基-1-戊烯基、1-甲基-2-戊烯基、2-甲基-2-戊烯基、3-甲基-2-戊烯基、4-甲基-2-戊烯基、1-甲基-3-戊烯基、2-甲基-3-戊烯基、3-甲基-3-戊烯基、4-甲基-3-戊烯基、1-甲基-4-戊烯基、2-甲基-4-戊烯基、3-甲基-4-戊烯基、4-甲基-4-戊烯基、1,1-二甲基-2-丁烯基、1,1-二甲基-3-丁烯基、1,2-二甲基-1-丁烯基、1,2-二甲基-2-丁烯基、1,2-二甲基-3-丁烯基、1,3-二甲基-1-丁烯基、1,3-二甲基-2-丁烯基、1,3-二甲基-3-丁烯基、2,2-二甲基-3-丁烯基、2,3-二甲基-1-丁烯基、2,3-二甲基-2-丁烯基、2,3-二甲基-3-丁烯基、3,3-二甲基-1-丁烯基、3,3-二甲基-2-丁烯基、1-乙基-1-丁烯基、1-乙基-2-丁烯基、1-乙基-3-丁烯基、2-乙基-1-丁烯基、2-乙基-2-丁烯基、2-乙基-3-丁烯基、1,1,2-三甲基-2-丙烯基、1-乙基-1-甲基-2-丙烯基、1-乙基-2-甲基-1-丙烯基或1-乙基-2-甲基-2-丙烯基,炔基:具有2至10个碳原子和在任一位置上具有叁键的直链或支链炔基,例如C2-C6-炔基,如乙炔基、2-丙炔基、2-丁炔基、3-丁炔基、1-甲基-2-丙炔基、2-戊炔基、3-戊炔基、4-戊炔基、1-甲基-2-丁炔基、1-甲基-3-丁炔基、2-甲基-3-丁炔基、1,1-二甲基-2-丙炔基、1-乙基-2-丙炔基、2-己炔基、3-己炔基、4-己炔基、5-己炔基、1-甲基-2-戊炔基、1-甲基-3-戊炔基、1-甲基-4-戊炔基、2-甲基-3-戊炔基、2-甲基-4-戊炔基、3-甲基-4-戊炔基、4-甲基-2-戊炔基、1,1-二甲基-2-丁炔基、1,1-二甲基-3-丁炔基、1,2-二甲基-3-丁炔基、2,2-二甲基-3-丁炔基、1-乙基-2-丁炔基、1-乙基-3-丁炔基、2-乙基-3-丁炔基和1-乙基-1-甲基-2-丙炔基;杂环基或杂环基氧基、杂环基硫基和杂环基氨基:三至六元饱和或部分不饱和单-或多环状杂环,它们含有一至三个选自氧、硫和氮的杂原子、且它们直接连接于或经氧原子(杂环基氧基)或经硫原子(杂环基硫基)或经氨基(杂环基氨基)连接于主结构,例如2-四氢呋喃基、环乙烷基、3-四氢呋喃基、2-四氢噻吩基、3-四氢噻吩基、2-吡咯烷基、3-吡咯烷基、3-异噁唑烷基、4-异噁唑烷基、5-异噁唑烷基、3-异噻唑烷基、4-异噻唑烷基、5-异噻唑烷基、3-吡唑烷基、4-吡唑烷基、5-吡唑烷基、2-噁唑烷基、4-噁唑烷基、5-噁唑烷基、2-噻唑烷基、4-噻唑烷基、5-噻唑烷基、2-咪唑烷基、4-咪唑烷基、1,2,4-噁二唑烷-3-基、1,2,4-噁二唑烷-5-基、1,2,4-噻二唑烷-3-基、1,2,4-噻二唑烷-5-基、1,2,4-三唑烷-3-基、1,3,4-噁二唑烷-2-基、1,3,4-噻三唑烷-2-基、1,3,4-三唑烷-2-基、2,3-二氢呋喃-2-基、2,3-二氢呋喃-3-基、2,3-二氢呋喃-4-基、2,3-二氢呋喃-5-基、2,5-二氢呋喃-2-基、2,5-二氢呋喃-3-基、2,3-二氢噻吩-2-基、2,3-二氢噻吩-3-基、2,3-二氢噻吩-4-基、2,3-二氢噻吩-5-基、2,5-二氢噻吩-2-基、2,5-二氢噻吩-3-基、2,3-二氢吡咯-2-基、2,3-二氢吡咯-3-基、2,3-二氢吡咯-4-基、2,3-二氢吡咯-5-基、2,5-二氢吡咯-2-基、2,5-二氢吡咯-3-基、2,3-二氢异噁唑-3-基、2,3-二氢异噁唑-4-基、2,3-二氢异噁唑-5-基、4,5-二氢异噁唑-3-基、4,5-二氢异噁唑-4-基、4,5-二氢异噁唑-5-基、2,5-二氢异噻唑-3-基、2,5-二氢异噻唑-4-基、2,5-二氢异噻唑-5-基、2,3-二氢吡唑-3-基、2,3-二氢异噻唑-4-基、2,3-二氢吡唑-5-基、4,5-二氢异吡唑-3-基、4,5-二氢异吡唑-4-基、4,5-二氢异吡唑-5-基、2,5-二氢异吡唑-3-基、2,5-二氢异吡唑-4-基、2,5-二氢异吡唑-5-基、2,3-二氢噁唑-3-基、2,3-二氢噁唑-4-基、2,3-二氢噁唑-5-基、4,5-二氢噁唑-3-基、4,5-二氢噁唑-4-基、4,5-二氢噁唑-5-基、2,5-二氢噁唑-3-基、4,5-二氢噁唑-4-基、4,5-二氢噁唑-5-基、2,3-二氢噻唑-3-基、2,3-二氢噻唑-4-基、2,3-二氢噻唑-5-基、4,5-二氢噻唑-3-基、4,5-二氢噻唑-4-基、4,5-二氢噻唑-5-基、2,5-二氢噻唑-2-基、2,5-二氢噻唑-4-基、2,5-二氢噻唑-5-基、2,3-二氢咪唑-2-基、2,3-二氢咪唑-4-基、2,3-二氢咪唑-5-基、4,5-二氢咪唑-2-基、4,5-二氢咪唑-4-基、4,5-二氢咪唑-5-基、2,5-二氢咪唑-2-基、2,5-二氢咪唑-4-基、2,5-二氢咪唑-5-基、2-吗啉基、3-吗啉基、2-哌啶基、3-哌啶基、4-哌啶基、3-四氢哒嗪基、4-四氢哒嗪基、2-四氢嘧啶基、4-四氢嘧啶基、5-四氢嘧啶基、2-四氢吡嗪基、1,3,5-四氢三嗪-2-基、1,2,4-四氢三嗪-3-基、1,3-二氢噁嗪-2-基、1,3-二噻烷-2-基、2-四氢吡喃基、1,3-二氢戊烷-2-基、3,4,5,6-四氢吡啶-2-基、4H-1,3-噻嗪-2-基、4H-3,1-苯并噻嗪-2-基、1,1-二氧杂-2,3,4,5-四氢噻吩-2-基,2H-1,4-苯并噻嗪-3-基、2H-1,4-苯并噁嗪-3-基、1,3-二氢噁嗪-2-基、1,3-二噻烷-2-基;芳基或芳氧基、芳硫基、芳基羰基和芳基磺酰基:芳族单-或多环状烃基,它们直接连接于或经氧原子(-O-)(芳氧基)或经硫原子(-O-)(芳硫基)或经羰基(-CO-)(芳基羰基)或磺酰基(-SO2-)连接于主结构,例如苯基、萘基和蒽基或苯氧基、萘氧基和蒽氧基和相应的羰基和磺酰基;杂芳基或杂芳氧基、杂芳硫基、杂芳羰基和杂芳基磺酰基:芳族单-或多环状基团,它们除了碳环成员外,可以另外含有一至四个氮原子或一至三个氮原子和一个氧原子或硫原子或一个氧原子或一个硫原子且它们直接或(杂芳氧基)经氧原子(-O-)或(杂硫基)经硫原子(-S-)、(杂芳基羰基)经羰基(-CO-)或(杂芳基磺酰基)经磺酰基(-SO2-),例如-5-元杂芳基,含有一至三个氮原子:5-元杂芳基,它们除了碳原In the definition of compound I given at the outset, the generic terms used usually denote the following groups: Halogen: fluorine, chlorine, bromine and iodine; Alkyl: straight-chain or branched with 1 to 4, 6 or 10 carbon atoms Alkanyl, for example, C 1 -C 6 -alkylmethyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, 1,1 -Dimethylethyl, pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl , 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1, 1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3, 3-Dimethylbutyl, 1-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl Or 1-ethyl-2-methylpropyl; haloalkyl: a straight-chain or branched-chain alkyl group with 1 to 6 carbon atoms, which is partially or fully substituted by the above-mentioned halogen atoms, such as C 1 -C 2 -Haloalkyl, such as chloromethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl, trifluoromethyl, chlorofluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl , 1-fluoroethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, 2-chloro-2-fluoroethyl, 2-chloro-2,2 - difluoroethyl, 2,2-dichloro-2-fluoroethyl, 2,2,2-trichloroethyl and pentafluoroethyl; cycloalkyl: monocyclic with 3 to 6 ring members Alkyl, for example cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; alkenyl: straight-chain or branched alkenyl having 2 to 6 or 10 carbon atoms and having a double bond at any position, for example, C 2 -C 6 -alkenyl such as 1-propenyl, 2-propenyl, 1-methylvinyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-methyl-1 -propenyl, 2-methyl-1-propenyl, 1-methyl-2-propenyl, 2-methyl-2-propenyl, 1-pentenyl, 2-pentenyl, 3-pentene Base, 4-pentenyl, 1-methyl-1-butenyl, 2-methyl-1-butenyl, 3-methyl-1-butenyl, 1-methyl-2-butene Base, 2-methyl-2-butenyl, 3-methyl-2-butenyl, 1-methyl-3-butenyl, 2-methyl-3-butenyl, 3-methyl -3-butenyl, 1,1-dimethyl-2-propenyl, 1,2-dimethyl-2-propenyl, 1,2-dimethyl-2-propenyl, 1-ethyl -1-propenyl, 1-ethyl-2-propenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl -1-pentenyl, 2-methyl-1-pentenyl, 3-methyl-1-pentenyl, 4-methyl-1-pentenyl, 1-methyl-2-pentenyl , 2-methyl-2-pentenyl, 3-methyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl-3-pentenyl, 2-methyl- 3-pentenyl, 3-methyl-3-pentenyl, 4-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-4-pentenyl, 3-methyl-4-pentenyl, 4-methyl-4-pentenyl, 1,1-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-Dimethyl-1-butenyl, 1,2-dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1,3-dimethyl- 1-butenyl, 1,3-dimethyl-2-butenyl, 1,3-dimethyl-3-butenyl, 2,2-dimethyl-3-butenyl, 2, 3-Dimethyl-1-butenyl, 2,3-dimethyl-2-butenyl, 2,3-dimethyl-3-butenyl, 3,3-dimethyl-1- Butenyl, 3,3-dimethyl-2-butenyl, 1-ethyl-1-butenyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl , 2-ethyl-1-butenyl, 2-ethyl-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1 -Ethyl-1-methyl-2-propenyl, 1-ethyl-2-methyl-1-propenyl or 1-ethyl-2-methyl-2-propenyl, alkynyl: with 2 to Straight-chain or branched alkynyl with 10 carbon atoms and a triple bond in any position, for example C2 - C6 -alkynyl, such as ethynyl, 2-propynyl, 2-butynyl, 3-but Alkynyl, 1-methyl-2-propynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-methyl-2-butynyl, 1-methyl-3- Butynyl, 2-methyl-3-butynyl, 1,1-dimethyl-2-propynyl, 1-ethyl-2-propynyl, 2-hexynyl, 3-hexynyl Base, 4-hexynyl, 5-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 1-methyl-4-pentynyl, 2-methyl Base-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-4-pentynyl, 4-methyl-2-pentynyl, 1,1-dimethyl-2 -butynyl, 1,1-dimethyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 1-eth Base-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl and 1-ethyl-1-methyl-2-propynyl; heterocyclyl or Heterocyclyloxy, heterocyclylthio and heterocyclylamino: three to six membered saturated or partially unsaturated mono- or polycyclic heterocycles containing one to three heteroatoms selected from oxygen, sulfur and nitrogen , and they are connected directly or via an oxygen atom (heterocyclyloxy) or via a sulfur atom (heterocyclylthio) or via an amino group (heterocyclylamino) to the main structure, such as 2-tetrahydrofuranyl, cycloethyl Alkyl, 3-tetrahydrofuryl, 2-tetrahydrothienyl, 3-tetrahydrothienyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 3-isoxazolidinyl, 4-isoxazolidinyl, 5-isoxazolidinyl, 3-isothiazolidinyl, 4-isothiazolidinyl, 5-isothiazolidinyl, 3-pyrazolidinyl, 4-pyrazolidinyl, 5-pyrazolidinyl, 2-oxazolidinyl, 4-oxazolidinyl, 5-oxazolidinyl, 2-thiazolidinyl, 4-thiazolidinyl, 5-thiazolidinyl, 2-imidazolidinyl, 4-imidazolidinyl , 1,2,4-oxadiazolidin-3-yl, 1,2,4-oxadiazolidin-5-yl, 1,2,4-thiadiazolidin-3-yl, 1,2, 4-thiadiazolidin-5-yl, 1,2,4-triazolidin-3-yl, 1,3,4-oxadiazolidin-2-yl, 1,3,4-thiatriazolidine -2-yl, 1,3,4-triazolidin-2-yl, 2,3-dihydrofuran-2-yl, 2,3-dihydrofuran-3-yl, 2,3-dihydrofuran -4-yl, 2,3-dihydrofuran-5-yl, 2,5-dihydrofuran-2-yl, 2,5-dihydrofuran-3-yl, 2,3-dihydrothiophene-2 -yl, 2,3-dihydrothiophen-3-yl, 2,3-dihydrothiophen-4-yl, 2,3-dihydrothiophen-5-yl, 2,5-dihydrothiophen-2-yl , 2,5-dihydrothiophen-3-yl, 2,3-dihydropyrrol-2-yl, 2,3-dihydropyrrol-3-yl, 2,3-dihydropyrrol-4-yl, 2 , 3-dihydropyrrol-5-yl, 2,5-dihydropyrrol-2-yl, 2,5-dihydropyrrol-3-yl, 2,3-dihydroisoxazol-3-yl, 2 , 3-dihydroisoxazol-4-yl, 2,3-dihydroisoxazol-5-yl, 4,5-dihydroisoxazol-3-yl, 4,5-dihydroisoxazole -4-yl, 4,5-dihydroisoxazol-5-yl, 2,5-dihydroisothiazol-3-yl, 2,5-dihydroisothiazol-4-yl, 2,5-di Hydroisothiazol-5-yl, 2,3-dihydropyrazol-3-yl, 2,3-dihydroisothiazol-4-yl, 2,3-dihydropyrazol-5-yl, 4,5 -Dihydroisopyrazol-3-yl, 4,5-dihydroisopyrazol-4-yl, 4,5-dihydroisopyrazol-5-yl, 2,5-dihydroisopyrazol-3 -yl, 2,5-dihydroisopyrazol-4-yl, 2,5-dihydroisopyrazol-5-yl, 2,3-dihydrooxazol-3-yl, 2,3-dihydro Oxazol-4-yl, 2,3-dihydrooxazol-5-yl, 4,5-dihydrooxazol-3-yl, 4,5-dihydrooxazol-4-yl, 4,5- Dihydrooxazol-5-yl, 2,5-dihydrooxazol-3-yl, 4,5-dihydrooxazol-4-yl, 4,5-dihydrooxazol-5-yl, 2, 3-dihydrothiazol-3-yl, 2,3-dihydrothiazol-4-yl, 2,3-dihydrothiazol-5-yl, 4,5-dihydrothiazol-3-yl, 4,5- Dihydrothiazol-4-yl, 4,5-dihydrothiazol-5-yl, 2,5-dihydrothiazol-2-yl, 2,5-dihydrothiazol-4-yl, 2,5-dihydro Thiazol-5-yl, 2,3-dihydroimidazol-2-yl, 2,3-dihydroimidazol-4-yl, 2,3-dihydroimidazol-5-yl, 4,5-dihydroimidazol- 2-yl, 4,5-dihydroimidazol-4-yl, 4,5-dihydroimidazol-5-yl, 2,5-dihydroimidazol-2-yl, 2,5-dihydroimidazol-4- Base, 2,5-dihydroimidazol-5-yl, 2-morpholinyl, 3-morpholinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 3-tetrahydropyridazine Base, 4-tetrahydropyridazinyl, 2-tetrahydropyrimidinyl, 4-tetrahydropyrimidinyl, 5-tetrahydropyrimidinyl, 2-tetrahydropyrazinyl, 1,3,5-tetrahydrotriazine- 2-yl, 1,2,4-tetrahydrotriazin-3-yl, 1,3-dihydrooxazin-2-yl, 1,3-dithian-2-yl, 2-tetrahydropyran Base, 1,3-dihydropentan-2-yl, 3,4,5,6-tetrahydropyridin-2-yl, 4H-1,3-thiazin-2-yl, 4H-3,1- Benzothiazin-2-yl, 1,1-dioxa-2,3,4,5-tetrahydrothiophen-2-yl, 2H-1,4-benzothiazin-3-yl, 2H- 1,4-benzoxazin-3-yl, 1,3-dihydrooxazin-2-yl, 1,3-dithian-2-yl; aryl or aryloxy, arylthio, aryl Cylcarbonyl and arylsulfonyl: aromatic mono- or polycyclic hydrocarbon radicals attached directly to or via an oxygen atom (-O-) (aryloxy) or via a sulfur atom (-O-) (arylthio) Or through carbonyl (-CO-) (arylcarbonyl) or sulfonyl (-SO 2 -) linked to the main structure, such as phenyl, naphthyl and anthracenyl or phenoxy, naphthyloxy and anthracenyl and the corresponding carbonyl and sulfonyl; heteroaryl or heteroaryloxy, heteroarylthio, heteroarylcarbonyl and heteroarylsulfonyl: aromatic mono- or polycyclic groups which, in addition to carbon ring members, may additionally Containing one to four nitrogen atoms or one to three nitrogen atoms and one oxygen atom or sulfur atom or one oxygen atom or one sulfur atom and they are directly or (heteroaryloxy) via an oxygen atom (-O-) or (heterothio ) via sulfur atom (-S-), (heteroarylcarbonyl) via carbonyl (-CO-) or (heteroarylsulfonyl) via sulfonyl (-SO 2 -), for example -5-membered heteroaryl, Containing one to three nitrogen atoms: 5-membered heteroaryls, which, in addition to carbon atoms
子外,可以含有一至三个氮原子作为环成员,例如,2-吡咯基、3-In addition, can contain one to three nitrogen atoms as ring members, for example, 2-pyrrolyl, 3-
吡咯基、3-吡唑基、4-吡唑基、5-吡唑基、2-咪唑基、4-咪唑基、Pyrrolyl, 3-pyrazolyl, 4-pyrazolyl, 5-pyrazolyl, 2-imidazolyl, 4-imidazolyl,
1,2,4-三唑-3-基和1,3,4-三唑-2-基;-5-元杂芳基,含有一至四个氮原子或一至三个氮原子和一个硫或1,2,4-triazol-3-yl and 1,3,4-triazol-2-yl; -5-membered heteroaryl containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or
氧原子或一个氧原子或一个硫原子:5-元杂芳基,它们除了碳原Oxygen atom or an oxygen atom or a sulfur atom: 5-membered heteroaryl, which except carbon atoms
子外,可以含有一至四个氮原子或一至三氮原子或一个硫原子或may contain one to four nitrogen atoms or one to three nitrogen atoms or one sulfur atom or
氧原子作为环成员,例如,2-呋喃基、3-呋喃基、2-噻吩基、3-Oxygen atoms as ring members, for example, 2-furyl, 3-furyl, 2-thienyl, 3-
噻吩基、2-吡咯基、3-吡咯基、3-异噁唑基、4-异噁唑基、5-异Thienyl, 2-pyrrolyl, 3-pyrrolyl, 3-isoxazolyl, 4-isoxazolyl, 5-iso
噁唑基、3-异噻唑基、4-异噻唑基、5-异噻唑基、3-吡唑基、4-Oxazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 3-pyrazolyl, 4-
吡唑基、5-吡唑基、2-噁唑基、4-噁唑基、5-噁唑基、2-噻唑基、Pyrazolyl, 5-pyrazolyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 2-thiazolyl,
4-噻唑基、5-噻唑基、2-咪唑基、4-咪唑基、1,2,4-噁二唑-3-基、4-thiazolyl, 5-thiazolyl, 2-imidazolyl, 4-imidazolyl, 1,2,4-oxadiazol-3-yl,
1,2,4-噁二唑-5-基、1,2,4-噻二唑-3-基、1,2,4-噻二唑-3-基、1,2,4-oxadiazol-5-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-3-yl,
1,2,4-三唑-3-基、1,3,4-三唑-2-基、1,3,4-噻二唑-2-基、1,3,4-1,2,4-triazol-3-yl, 1,3,4-triazol-2-yl, 1,3,4-thiadiazol-2-yl, 1,3,4-
三唑-2-基;-苯并稠合的5-元杂芳基,含有一至三个氮原子或一个氮原子和/Triazol-2-yl; -benzo-fused 5-membered heteroaryl containing one to three nitrogen atoms or one nitrogen atom and/or
或氧或硫原子:5-元杂芳基,它们除了碳原子外,可以含有一至or oxygen or sulfur atoms: 5-membered heteroaryl groups which, in addition to carbon atoms, may contain from one to
四个氮原子或一至三个氮原子和一个硫或氧原子或一个氧或硫原Four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom or one oxygen or sulfogen
子作为环成员,且其中二个相邻的碳原子或一个氮原子和一个相As a ring member, and two adjacent carbon atoms or a nitrogen atom and a phase
邻的碳环成员可以通过丁-1,3-二烯-1,4-二基桥接;-5-元杂芳基,经氮原子键合且含有一至四个氮原子,或苯并稠合Adjacent carbon ring members may be bridged by but-1,3-diene-1,4-diyl; -5-membered heteroaryl, bonded through nitrogen and containing one to four nitrogen atoms, or benzofused
的5-元杂芳基,经氮原子键合且含有一至三个氮原子:5-元杂芳5-membered heteroaryl, bonded via a nitrogen atom and containing one to three nitrogen atoms: 5-membered heteroaryl
基,它们除了碳原子外,可以分别含有一至四个氮原子和一至三groups, which, in addition to carbon atoms, may contain, respectively, one to four nitrogen atoms and one to three
个氮原子,作为环成员,且相邻的二个碳环成员或一个氮原子和nitrogen atoms, as ring members, and adjacent two carbon ring members or a nitrogen atom and
一个相邻的碳环成员可以通过丁-1,3-二烯-1,4-二基桥接,这An adjacent carbon ring member can be bridged by a but-1,3-diene-1,4-diyl, which
些基团以氮环成员连接于主结构;-6-元杂芳基,分别含有一至三个氮原子和一至四个氮原子:6-元These groups are connected to the main structure by a nitrogen ring member; -6-membered heteroaryl, containing one to three nitrogen atoms and one to four nitrogen atoms respectively: 6-membered
杂芳基,它们除了碳原子外,可以分别含有一至三个氮原子或一Heteroaryl groups which may respectively contain, in addition to carbon atoms, one to three nitrogen atoms or one
至四个氮原子作为环成员,例如,2-吡啶基、3-吡啶基、4-吡啶Up to four nitrogen atoms as ring members, e.g., 2-pyridyl, 3-pyridyl, 4-pyridine
基、3-哒嗪基、4-哒嗪基、2-嘧啶基、4-嘧啶基、5-嘧啶基、2-Base, 3-pyridazinyl, 4-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 2-
吡嗪基、1,3,4-三嗪-2-基、1,2,4-三嗪-3-基和1,2,4,5-四Pyrazinyl, 1,3,4-triazin-2-yl, 1,2,4-triazin-3-yl and 1,2,4,5-tetra
嗪-3-基;-苯并稠合的6-元杂芳基,含有一至四个氮原子:6-元杂芳基,其Azin-3-yl; -benzo-fused 6-membered heteroaryl containing from one to four nitrogen atoms: 6-membered heteroaryl whose
中二个相邻的碳环成员可以通过丁-1,3-二烯-1,4-二基桥接,Two adjacent carbon ring members in can be bridged by buta-1,3-diene-1,4-diyl,
例如喹啉、异喹啉、喹唑啉和喹喔啉,和相应的氧、硫、羰基或磺酰基。杂芳基氨基:芳族单-或多环状基团,它们除了碳环成员外,还可以含有一至四个氮原子或一至三个氮原子和一个氧或硫原子且它们经氮原子连接于主结构。For example quinoline, isoquinoline, quinazoline and quinoxaline, and the corresponding oxygen, sulfur, carbonyl or sulfonyl groups. Heteroarylamino: Aromatic mono- or polycyclic radicals which, in addition to carbon ring members, may contain from one to four nitrogen atoms or from one to three nitrogen atoms and an oxygen or sulfur atom and which are bonded via the nitrogen atom to main structure.
“被部分或全部卤代“的定义意在表达在所指的基团上的部分或全部的氢原子均可能被相同或不同的如上提到的卤原子替代。The definition of "partially or fully halogenated" means that some or all of the hydrogen atoms on the indicated group may be replaced by the same or different halogen atoms as mentioned above.
对于其活性而言,优选的是其中m是0的式Ⅰ化合物。Compounds of formula I wherein m is zero are preferred for their activity.
同样,优选的是其中R1是甲基的式Ⅰ化合物。Likewise, preference is given to compounds of formula I wherein R 1 is methyl.
此外,优选的是其中R3是氢、氰基、环丙基、甲基、乙基、1-甲基乙基或三氟甲基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R3 is hydrogen, cyano, cyclopropyl, methyl, ethyl, 1-methylethyl or trifluoromethyl.
而且,优选的是其中R3是甲基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R3 is methyl.
此外,优选的是其中R3是氰基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R3 is cyano.
还有,优选的是其中R3是环丙基的化合物Ⅰ。Also, preference is given to compounds I in which R3 is cyclopropyl.
此外,优选的是其中R3是三氟甲基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R3 is trifluoromethyl.
此外,优选的是其中R5是氢、环丙基、甲基、乙基、异丙基、未取代或取代的芳基或杂芳基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is hydrogen, cyclopropyl, methyl, ethyl, isopropyl, unsubstituted or substituted aryl or heteroaryl.
而且,优选的是其中R5是甲基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R5 is methyl.
此外,优选的是其中R5是乙基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is ethyl.
此外,优选的是其中R5是异丙基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is isopropyl.
还有,优选的是其中R5是环丙基的化合物Ⅰ。Also, preference is given to compounds I in which R5 is cyclopropyl.
而且,优选的是其中R5是三氟甲基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R5 is trifluoromethyl.
此外,优选的是其中R5是未取代或取代的芳基或杂芳基的化合物。Furthermore, preference is given to compounds in which R is unsubstituted or substituted aryl or heteroaryl.
此外,优选的是其中R5是未取代或取代的吡啶基、嘧啶基、吡嗪基、哒嗪基或三嗪基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is unsubstituted or substituted pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl.
此外,优选的是其中R5是未取代或取代的呋喃基、噻吩基或吡咯基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is unsubstituted or substituted furyl, thienyl or pyrrolyl.
此外,优选的是其中R5是未取代或取代的噁唑基、噻唑基、异噁唑基、异噻唑基、吡唑基或咪唑基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is unsubstituted or substituted oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, pyrazolyl or imidazolyl.
此外,优选的是其中R5是未取代或取代的噁二唑基、噻二唑基或三唑基化合物Ⅰ。Furthermore, preference is given to compounds I in which R 5 is unsubstituted or substituted oxadiazolyl, thiadiazolyl or triazolyl.
而且,优选的还有这样的化合物Ⅰ,其中R5是未取代或带有一或二个下列基团的苯基:硝基、氰基、羟基、氨基、C1-C4-烷基、C1-C4-卤代烷基、C1-C4-烷氧基、C1-C4-卤代烷氧基、C1-C4-烷基氨基、二-C1-C4-烷基氨基、C1-C4-烷基磺酰基、C1-C4-烷氧基羰基、C1-C4-烷基氨基羰基或二-C1-C4-烷基氨基羰基。Furthermore, preference is also given to compounds I in which R 5 is phenyl which is unsubstituted or carries one or two of the following groups: nitro, cyano, hydroxyl, 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 -alkylamino, di-C 1 -C 4 -alkylamino, C 1 -C 4 -alkylsulfonyl, C 1 -C 4 -alkoxycarbonyl, C 1 -C 4 -alkylaminocarbonyl or di-C 1 -C 4 -alkylaminocarbonyl.
而且,优选的还有这样的化合物Ⅰ,其中R4是氢、C1-C6-烷基、C2-C6-烯基、C1-C6-炔基、烯丙基、芳烷基、杂芳烷基、芳氧基烷基、杂芳氧基烷基、芳基或杂芳基。Furthermore, preference is also given to compounds I in which R 4 is hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 1 -C 6 -alkynyl, allyl, arane radical, heteroaralkyl, aryloxyalkyl, heteroaryloxyalkyl, aryl or heteroaryl.
此外,优选的是其中R4是C1-C6-烷基的化合物Ⅰ。Furthermore, preference is given to compounds I in which R 4 is C 1 -C 6 -alkyl.
还优选的化合物Ⅰ公开于WO 97/15,552中。Also preferred compounds I are disclosed in WO 97/15,552.
含在本发明混合物中的化合物Ⅱ对广谱的植物病原真菌、特别是对子囊菌纲、半知菌类、藻菌纲和担子菌纲的真菌有优异的活性。Compound II contained in the mixture according to the invention has excellent activity against a broad spectrum of phytopathogenic fungi, especially against fungi of the classes Ascomycetes, Deuteromycetes, Phycomycetes and Basidiomycetes.
它们在防治各种作物如棉花、蔬菜(例如,黄瓜、豆类、蕃茄、马铃薯和胡瓜)、大麦、禾草、燕麦、香蕉、咖啡、玉米、水果、稻、黑麦、大豆、葡萄、小麦、观赏植物、甘蔗和许多的种子上的许多植物病原真菌方面特别重要。They are effective in controlling various crops such as cotton, vegetables (e.g., cucumbers, beans, tomatoes, potatoes and courgettes), barley, grasses, oats, bananas, coffee, corn, fruit, rice, rye, soybeans, grapes, wheat , ornamental plants, sugarcane and many phytopathogenic fungi on the seeds of many species.
它们特别适合于防治下列植物病原真菌:禾谷类上的禾白粉菌(Erysiphe graminia)、胡瓜上的二孢白粉菌(Erysiphe cichoracearum)和苍耳单丝壳菌(Sphaerotheca fuliginea)、苹果上的苹果白粉病柄球菌(Podosphaera leucotricha)、葡萄上的葡萄白粉病钩丝壳霉(Uncinula necator)、禾谷类上的柄锈菌(Puccinia)、棉花、稻和草坪上的丝核菌(Rhizoctonia)、禾谷类和甘蔗上的黑粉菌(Ustilago)、苹果上的苹果黑星菌(Venturia Inaequalis)、禾谷类上的长蠕孢菌(Helminthosporium)、小麦上的颖枯病菌(Septoria nodorum)、草莓、蔬菜、观赏植物和葡萄上的灰霉菌(Botrytis cinera)、花生上的花生尾孢菌(Cercospora arachidicola)、小麦和大麦上的眼斑病菌(Pseudocercospora herpotophthora)、稻和草坪上的稻梨孢(Pyricularia oryzae)、马铃薯和蕃茄上的蔓延疫霉(Phytophthorainfestans)、葡萄上的葡萄生单轴霉(Plasmopara viticola)、蔬菜和水果上的链格孢菌(Alternaria),以香蕉上的球腔菌(Mycosphaerella)及镰刀菌(Fusarium)和轮枝孢菌(Verticillium)。They are particularly suitable for the control of the following phytopathogenic fungi: Erysiphe graminia on cereals, Erysiphe cichoracearum and Sphaerotheca fuliginea on cucumbers, Erysiphe graminia on apples Podosphaera leucotricha, Uncinula necator on grapes, Puccinia on cereals, Rhizoctonia on cotton, rice and turf, cereals and Ustilago on sugarcane, Venturia Inaequalis on apples, Helminthosporium on cereals, Septoria nodorum on wheat, strawberries, vegetables, Botrytis cinera on ornamentals and grapes, Cercospora arachidicola on peanuts, Pseudocercospora herpotophthora on wheat and barley, Pyricularia oryzae on rice and turf , Phytophthorainfestans on potatoes and tomatoes, Plasmopara viticola on grapes, Alternaria on vegetables and fruits, Mycosphaerella on bananas and Fusarium and Verticillium.
化合物Ⅱ至Ⅶ是市售的杀真菌剂。Compounds II to VII are commercially available fungicides.
当制备混合物时,优选的是采用纯的活性成分Ⅰ和Ⅱ至Ⅶ,它们可以与其它的对有害真菌或其它害虫如昆虫、蜱螨或线虫的活性成分,或是与除草的或生长调节的活性成分或化肥混合。When preparing mixtures, it is preferred to use the pure active ingredients I and II to VII, which may be combined with other active ingredients against harmful fungi or other pests such as insects, acarids or nematodes, or with herbicidal or growth-regulating Active ingredients or fertilizer blends.
化合物Ⅰ与至少一种Ⅱ至Ⅶ的混合物同时、一起或分别使用,对广谱的植物病原真菌、特别是对子囊菌、担子菌、藻菌和半知菌有突出的作用。它们中的一些有内吸作用,因此可以用来作为叶面和土壤作用杀真菌剂。Compound I and at least one mixture of II to VII are used simultaneously, together or separately, and have outstanding effects on broad-spectrum plant pathogenic fungi, especially on Ascomycetes, Basidiomycetes, Algae and Deuteromycetes. Some of them are systemic and can therefore be used as foliar and soil-acting fungicides.
它们在防治各种作物如棉花、蔬菜(例如,黄瓜、豆类、蕃茄、马铃薯和胡瓜)、大麦、禾草、燕麦、香蕉、咖啡、玉米、水果、稻、黑麦、大豆、葡萄、小麦、观赏植物、甘蔗和许多的种子上的许多植物病原真菌方面特别重要。They are effective in controlling various crops such as cotton, vegetables (e.g., cucumbers, beans, tomatoes, potatoes and courgettes), barley, grasses, oats, bananas, coffee, corn, fruit, rice, rye, soybeans, grapes, wheat , ornamental plants, sugarcane and many phytopathogenic fungi on the seeds of many species.
它们特别适合于防治下列植物病原真菌:禾谷类上的禾白粉菌(Erysiphe graminia)、胡瓜上的二孢白粉菌(Erysiphe cichoracearum)和苍耳单丝壳菌(Sphaerotheca fuliginea)、苹果上的苹果白粉病柄球菌(Podosphaera leucotricha)、葡萄上的葡萄白粉病钩丝壳霉菌(Uncinula necator)、禾谷类上的柄锈菌(Puccinia)、棉花、稻和草坪上的丝核菌(Rhizoctonia)、禾谷类和甘蔗上的黑粉菌(Ustilago)、苹果上的苹果黑星菌(Venturia Inaequalis)、禾谷类上的长蠕孢菌(Helminthosporium)、小麦上的颖枯病菌(Septoria nodorum)、草莓、蔬菜、观赏植物和葡萄上的灰霉菌(Botrytis cinera)、花生上的花生尾孢菌(Cercospora arachidicola)、小麦和大麦上的眼斑病菌(Pseudocercospora herpotophthora)、稻和草坪上的稻梨孢(Pyricularia oryzae)、马铃薯和蕃茄上的蔓延疫霉(Phytophthorainfestans)、葡萄上的葡萄生单轴霉(Plasmopara viticola)、蔬菜和水果上的链格孢菌(Alternaria),以香蕉上的球腔菌(Mycosphaerella)及镰刀菌(Fusarium)和轮枝孢菌(Verticillium)。They are particularly suitable for the control of the following phytopathogenic fungi: Erysiphe graminia on cereals, Erysiphe cichoracearum and Sphaerotheca fuliginea on cucumbers, Erysiphe graminia on apples Podosphaera leucotricha, Uncinula necator on grapes, Puccinia on cereals, Rhizoctonia on cotton, rice and turf, cereals and Ustilago on sugarcane, Venturia Inaequalis on apples, Helminthosporium on cereals, Septoria nodorum on wheat, strawberries, vegetables, Botrytis cinera on ornamentals and grapes, Cercospora arachidicola on peanuts, Pseudocercospora herpotophthora on wheat and barley, Pyricularia oryzae on rice and turf , Phytophthorainfestans on potatoes and tomatoes, Plasmopara viticola on grapes, Alternaria on vegetables and fruits, Mycosphaerella on bananas and Fusarium and Verticillium.
本发明混合物特别适合于采用来防治稻梨孢菌。The mixtures according to the invention are particularly suitable for use against Pyricularia oryzae.
化合物Ⅰ与至少一种化合物Ⅱ至Ⅶ可以同时、或者一起或分别、或依次施用,在分别施用时,顺序通常不影响防治措施的效果。Compound I and at least one compound II to VII can be applied simultaneously, together or separately, or sequentially. In the case of separate application, the order usually does not affect the effect of the control measures.
依据所需效果种类的不同,本发明混合物的使用剂量通常为0.01至8千克/公顷,优选0.01至5千克/公顷,特别是0.5至3.0千克/公顷。Depending on the type of effect desired, the mixtures according to the invention are generally used at a dosage of 0.01 to 8 kg/ha, preferably 0.01 to 5 kg/ha, especially 0.5 to 3.0 kg/ha.
化合物Ⅰ的施用剂量一般是0.01至2.5千克/公顷,优选是0.05至2.5千克/公顷,特别是0.1至1.0千克/公顷。The application rate of compound I is generally 0.01 to 2.5 kg/ha, preferably 0.05 to 2.5 kg/ha, especially 0.1 to 1.0 kg/ha.
相应地,对化合物Ⅱ至Ⅶ而言,施用剂量是0.0015千克/公顷,优选0.005至2千克/公顷,特别是0.01至1.0千克/公顷。Correspondingly, for compounds II to VII, the application rate is 0.0015 kg/ha, preferably 0.005 to 2 kg/ha, especially 0.01 to 1.0 kg/ha.
处理种子时,混合物的施用量通常是0.001至250克/千克种子,优选0.01至100克/千克种子,特别是0.01至50克/千克。When treating seeds, the mixtures are generally applied at rates of 0.001 to 250 g/kg of seed, preferably 0.01 to 100 g/kg of seed, especially 0.01 to 50 g/kg.
如果意欲防治的是植物病原真菌,则通过向种子、植物或播种前或后或植物出芽前或后的土壤喷雾或喷粉,分别或一起施用化合物Ⅰ和化合物Ⅱ至Ⅶ。If phytopathogenic fungi are to be controlled, the compounds I and the compounds II to VII are applied separately or together by spraying or dusting the seeds, the plants or the soil before or after sowing or before or after emergence of the plants.
本发明混合物可以加工成例如可直接喷雾溶液、粉末和悬浮液或高浓度水性、油性或其它悬浮液、分散液、乳剂、油分散液、膏剂、粉剂、撒施组合物或颗粒剂的形式,且通过喷雾、弥雾、喷粉、撒施或浇泼使用。施用形式取决于使用的目的;在每一种情况下,应确保本发明混合物的分散尽可能细微和均匀。The mixtures according to the invention can be processed, for example, in the form of direct sprayable solutions, powders and suspensions or high-concentration aqueous, oily or other suspensions, dispersions, emulsions, oil dispersions, ointments, powders, spray compositions or granules, And it is used by spraying, misting, dusting, spreading or pouring. The application form depends on the purpose of use; in each case, it should ensure as fine and uniform a dispersion of the mixture according to the invention as possible.
这些制剂可以用已知的方式制备,例如通过将活性化合物用溶剂和/或载体,如果需要,采用乳化剂和分散剂,如果用水作稀释剂,也可以用其它的有机溶剂作助溶剂。适合用于此目的的助溶剂主要是:溶剂如芳族化合物(例如二甲苯)、氯代芳族化合物(例如氯苯)、石蜡(例如石油馏份)、醇类(例如甲醇、丁醇)、酮类(例如环己酮)、胺类(例如乙醇胺、二甲基甲酰胺)和水;载体如研碎的天然矿物质(例如高岭土、矾土、滑石、白垩)和研碎的合成矿物质(例如高分散的硅酸、硅酸盐);乳化剂如非离子和阴离子乳化剂(例如聚氧乙烯脂肪醇醚、烷基磺酸盐和芳基磺酸盐)和分散剂如木素亚硫酸盐废液或甲基纤维素。These formulations can be prepared in a known manner, for example by using the active compounds as solvents and/or carriers and, if desired, emulsifiers and dispersants and, if water is used as diluent, also other organic solvents as cosolvents. Co-solvents suitable for this purpose are mainly: solvents such as aromatics (e.g. xylene), chlorinated aromatics (e.g. chlorobenzene), paraffins (e.g. petroleum fractions), alcohols (e.g. methanol, butanol) , ketones (e.g. cyclohexanone), amines (e.g. ethanolamine, dimethylformamide) and water; carriers such as ground natural minerals (e.g. kaolin, alumina, talc, chalk) and ground synthetic minerals Substances (such as highly dispersed silicic acid, silicates); emulsifiers such as nonionic and anionic emulsifiers (such as polyoxyethylene fatty alcohol ethers, alkylsulfonates and arylsulfonates) and dispersants such as lignin Sulphite waste or methylcellulose.
适合的表面活性剂是芳族磺酸例如木素磺酸、苯酚磺酸、萘磺酸和二丁基萘磺酸的碱金属、-碱土金属盐,和脂肪酸、烷基磺酸和烷基芳基磺酸、烷基硫酸、月桂基醚硫酸和脂肪醇硫酸的碱金属、-碱土金属盐,以及硫酸化的十六-、十七-和十八醇或脂肪醇醚的盐,磺化萘和其与甲醛的衍生物的缩合产物,萘或萘磺酸与苯酚和甲醛的缩合产物,聚氧乙烯辛基酚醚、乙氧基化的异辛基-、辛基-或壬基酚、烷基苯酚或三丁基苯基聚乙二醇醚,烷基芳基聚醚醇、异三癸基醇、脂肪醇环氧乙烷缩合物,乙氧基化蓖麻油,聚氧乙烯烷基醚或聚氧丙烯,月桂醇聚乙二醇醚乙酸酯、失水山梨醇酯,木素亚硫酸盐废液或甲基纤维素。Suitable surfactants are alkali metal, -alkaline earth metal salts of aromatic sulfonic acids such as ligninsulfonic acid, phenolsulfonic acid, naphthalenesulfonic acid and dibutylnaphthalenesulfonic acid, and fatty acids, alkylsulfonic acids and alkylarylsulfonic acids. Alkali metal, -alkaline earth metal salts of sulfonic acids, alkylsulfuric acids, lauryl ether sulfates and fatty alcohol sulfates, and sulfated salts of cetyl-, heptadecan- and stearyl alcohols or fatty alcohol ethers, sulfonated naphthalene Condensation products of naphthalene or naphthalenesulfonic acid with phenol and formaldehyde, polyoxyethylene octylphenol ethers, ethoxylated isooctyl-, octyl- or nonylphenols, Alkylphenol or tributylphenyl polyglycol ether, alkyl aryl polyether alcohol, isotridecyl alcohol, fatty alcohol ethylene oxide condensate, ethoxylated castor oil, polyoxyethylene alkyl ether or polyoxypropylene, laureth polyglycol ether acetate, sorbitan ester, lignosulfite waste liquor or methylcellulose.
粉末、撒施材料和粉剂可以通过将化合物Ⅰ与至少一种化合物Ⅱ至Ⅶ或化合物Ⅰ与至少一种化合物Ⅱ至Ⅶ的混合物与固体载体混合或一起研磨而生产。Powders, spreading materials and dusts can be produced by mixing or grinding the compound I with at least one of the compounds II to VII or a mixture of the compound I with at least one of the compounds II to VII with a solid carrier.
颗粒剂(例如,涂敷、浸渍或均质颗粒剂)可以通过将一种或多种活性化合物粘合到固体载体上而制备。Granules (for example, coated, impregnated or homogeneous granules) can be prepared by binding one or more active compounds to solid carriers.
固体载体是矿石土如硅胶、硅酸、硅酸盐、滑石、高岭土、石灰石、石灰、白垩、红玄武土、黄土、陶土、白云石、硅藻土、硫酸钙和硫酸镁、氧化镁,研碎的合成材料、化肥,如硫酸铵、磷酸铵、硝酸铵、尿素和植物产物如面粉、树皮粉、木粉和坚果壳粉、纤维素粉和其它固体载体。在直接可用制剂中的活性化合物浓度可以在相对宽的范围内变化。The solid carrier is ore soil such as silica gel, silicic acid, silicate, talc, kaolin, limestone, lime, chalk, red basalt, loess, clay, dolomite, diatomaceous earth, calcium sulfate and magnesium sulfate, magnesium oxide, research Crushed synthetic materials, fertilizers such as ammonium sulphate, ammonium phosphate, ammonium nitrate, urea and plant products such as flour, bark meal, wood and nut shell meal, cellulose meal and other solid carriers. The active compound concentration in the ready-to-use preparations can be varied within relatively wide ranges.
通常,制剂含有按重量计0.1至95%,优选按重量计0.5至90%的一种化合物Ⅰ和至少一种化合物Ⅱ至Ⅶ或化合物Ⅰ与至少一种化合物Ⅱ至Ⅶ的混合物。活性化合物一般采用90至100%,优选95至100%的纯度(根据NMR或HPLC谱)。In general, the preparations contain 0.1 to 95% by weight, preferably 0.5 to 90% by weight, of one compound I and at least one compound II to VII or a mixture of compound I and at least one compound II to VII . The active compounds are generally employed in a purity of from 90 to 100%, preferably from 95 to 100% (according to NMR or HPLC spectrum).
化合物Ⅰ和至少一种化合物Ⅱ至Ⅶ、其混合物或相应的制剂通过用杀真菌有效量的混合物,或在分别施用的情况下,施用化合物Ⅰ和至少一种化合物Ⅱ至Ⅶ,来处理有害真菌、其栖生地或待使之免受感染的植物、种子、土壤、区域、材料或空间。Compound I and at least one compound II to VII, mixtures thereof or corresponding preparations for the treatment of harmful fungi by applying the compound I and at least one compound II to VII in a mixture in a fungicidally effective amount or in the case of separate application , its habitat or a plant, seed, soil, area, material or space to be protected from infection.
施用可以在有害真菌侵染前或后进行。Application can be carried out before or after infestation by the harmful fungi.
这些包含活性成分的制剂的实例有:Ⅰ.90重量份的活性成分和10重量份N-甲基吡咯烷酮的溶液。此溶液适合于以微滴的形式施用。Ⅱ.20重量份的活性成分、80重量份的二甲苯、10重量份的8至10摩尔环氧乙烷与1摩尔油酸N-单乙醇酰胺的加合物、5重量份的十二烷基苯磺酸钙盐和5重量份的40摩尔环氧乙烷与1摩尔蓖麻油的加合物的混合物。将此溶液细分散水中,获得分散液。Ⅲ.20重量份的活性成分、40重量份的环己酮、30重量份的异丁醇和10重量份的40摩尔环氧乙烷与1摩尔蓖麻油的加合物的水分散液。Ⅳ.20重量份的活性成分、25重量份的环己醇、65重量份沸点为210至280℃的矿物油馏份和10重量份的40摩尔环氧乙烷与1摩尔蓖麻油的加成物的水分散液。Ⅴ.80重量份的活性成分、3重量份的二异丁基萘-1-磺酸钠盐、10重量份的来源于亚硫酸废液的木素硫酸钠盐和7重量份的粉状硅胶在锤磨中磨碎的混合物。将此混合物细分散水中,获得喷雾液。Ⅵ.3重量份的活性成分与97重量份细分散的高岭土的密切混合物。此喷粉剂含有按重量计3%(重量)活性化合物。Ⅶ.30重量份的活性成分、92重量份的粉状硅胶和8重量份已喷雾到硅胶表面的石蜡之密切混合物。此制剂赋予活性化合物以良好的粘性。Ⅷ.40重量份的活性成分、10重量份的苯酚磺酸/尿素/甲醛缩合物的钠盐、2重量份的硅胶和48重量份水的稳定水分散液。此分散液可以进一步稀释。Ⅸ.20重量份的活性成分、2重量份的十二烷基苯磺酸钙盐、8重量份的脂肪醇乙二醇醚、2重量份的酚/脲/甲醛缩合物的钠盐和68重量份的石蜡样矿物油的稳定油分散剂。Examples of such formulations containing active ingredients are: Ⅰ. A solution of 90 parts by weight of active ingredient and 10 parts by weight of N-methylpyrrolidone. This solution is suitable for administration in the form of microdroplets. Ⅱ. 20 parts by weight of active ingredients, 80 parts by weight of xylene, 10 parts by weight of an adduct of 8 to 10 moles of ethylene oxide and 1 mole of oleic acid N-monoethanolamide, 5 parts by weight of dodecylbenzene A mixture of calcium sulfonate and 5 parts by weight of an adduct of 40 moles of ethylene oxide and 1 mole of castor oil. This solution was finely dispersed in water to obtain a dispersion. Ⅲ. An aqueous dispersion of 20 parts by weight of active ingredients, 40 parts by weight of cyclohexanone, 30 parts by weight of isobutanol and 10 parts by weight of an adduct of 40 moles of ethylene oxide and 1 mole of castor oil. IV. 20 parts by weight of active ingredients, 25 parts by weight of cyclohexanol, 65 parts by weight of mineral oil fractions with a boiling point of 210 to 280° C., and 10 parts by weight of an adduct of 40 moles of ethylene oxide and 1 mole of castor oil water dispersion. V. 80 parts by weight of the active ingredient, 3 parts by weight of diisobutylnaphthalene-1-sulfonic acid sodium salt, 10 parts by weight of lignosulfate sodium salt derived from sulfurous acid waste liquid and 7 parts by weight of powdered silica gel in the hammer Grind the mixture in a mill. This mixture is finely dispersed in water to obtain a spray liquid. VI. Intimate mixture of 3 parts by weight of active ingredient with 97 parts by weight of finely divided kaolin. The dusting formulation contains 3% by weight of active compound. VII. An intimate mixture of 30 parts by weight of active ingredient, 92 parts by weight of powdered silica gel and 8 parts by weight of paraffin wax sprayed onto the surface of the silica gel. This formulation imparts good viscosity to the active compound. VIII. A stable aqueous dispersion of 40 parts by weight of active ingredient, 10 parts by weight of sodium salt of phenolsulfonic acid/urea/formaldehyde condensate, 2 parts by weight of silica gel and 48 parts by weight of water. This dispersion can be further diluted. Ⅸ. 20 parts by weight of active ingredients, 2 parts by weight of dodecylbenzenesulfonate calcium salt, 8 parts by weight of fatty alcohol glycol ether, 2 parts by weight of sodium salt of phenol/urea/formaldehyde condensate and 68 parts by weight Stabilized oil dispersion of paraffinic mineral oils.
本发明混合物的增效活性可以通过下列实验来证实:The synergistic activity of the mixtures of the invention can be confirmed by the following experiments:
活性成分分别或一起加工成于按重量计含63%环己酮和27%乳化剂的混合物中的、浓度为10%的乳剂,并用水稀释至所需浓度。The active ingredients are processed separately or together to a 10% strength emulsion in a mixture containing 63% by weight cyclohexanone and 27% emulsifier and diluted with water to the desired concentration.
通过确定感病的叶面积百分率进行评价,并将这些百分率值转化成效力。效力(W)使用Abbot公式计算Evaluation was performed by determining the percentage of leaf area susceptible to the disease and converting these percentage values into potency. Potency (W) calculated using Abbot's formula
W=(1-α)100/βW=(1-α)100/β
α 经处理的植物真菌感染%α % fungal infection of treated plants
β 是未处理(对照样)植物的真菌感染%β is the % fungal infection of untreated (control) plants
效力为0时,指感染程度与未处理对照样相当;效力为100,指经处理的植物未感染。When the potency is 0, it means that the degree of infection is equivalent to that of the untreated control; when the potency is 100, it means that the treated plants are not infected.
活性成分混合物的预期效力是用Colby公式来计算[R.S.Colby,《杂草》[Weeds]15,20-22(1967)],并与实测效力作比较。The expected potency of a mixture of active ingredients is calculated using the Colby formula [R. S. Colby, "Weeds" [Weeds] 15, 20-22 (1967)], and compared with the measured efficacy.
Colby公式:Colby's formula:
E=x+y-xy/100E=x+y-xy/100
E 以浓度a与b使用活性成分A与B的混合物时的预期值,以相E Expected value when using a mixture of active ingredients A and B at concentrations a and b, compared to
对于未处理的对照样的%表示Expressed in % for untreated control
x 以浓度a使用活性成分A时的效力,以相对于未处理的对照样x Potency when active ingredient A is used at concentration a, relative to untreated control
的%表示% means
y 以浓度b使用活性成分B时的效力,以相对于未处理的对照样y Potency when active ingredient B is used at concentration b, relative to untreated control
的%表示。Expressed in %.
应用实施例1-对稻瘟病(Pyricularia oryzae)的活性Application Example 1 - Activity against rice blast (Pyricularia oryzae)
将稻秧(品种:Tai Nong 67)用由包含10%活性成分、63%环己酮和27%乳化剂中母液制备的活性成分的含水制剂喷雾,直至向下滴流。第二天,将植物用真菌稻梨孢的孢子水悬浮液喷雾,并在22-24℃、相对湿度95-99%下保持6天。之后目测评价叶片上的病害发展程度。Rice seedlings (variety: Tai Nong 67) were sprayed with an aqueous formulation of the active ingredient prepared from a mother liquor comprising 10% of the active ingredient, 63% of cyclohexanone and 27% of the active ingredient in an emulsifier until it trickled down. The next day, the plants were sprayed with an aqueous spore suspension of the fungus Pyrosporium oryzae and kept for 6 days at 22-24° C. and a relative humidity of 95-99%. The degree of disease development on the leaves was then assessed visually.
将目测确定的发病叶片区域百分率转化成相对于未处理对照的效力。效力0是指与未处理对照样的发病程度相同,效力100%指发病为0%。活性成分组合的预期效力是用Colby公式来计算[R.S.Colby,“计算除草组合的增效与拮抗反应“,《杂草》[Weeds]15,20-22(1967)],并与实测效力作比较。The percentage of diseased leaf area determined visually was converted into efficacy relative to the untreated control. Efficacy 0 means the same degree of disease as the untreated control, and efficacy 100% means 0% disease. The expected potency of a combination of active ingredients is calculated using the Colby formula [R. S. Colby, "Calculation of synergistic and antagonistic responses of herbicidal combinations", Weeds 15, 20-22 (1967)] and comparison with measured efficacy.
作为组分a),使用下列化合物Ⅰ’: As component a), the following compounds I' are used:
试验结果列于下文表1和2中:The test results are listed in Tables 1 and 2 below:
表1
表2
*)用Colby公式计算*) Calculated using Colby's formula
试验结果显示,观察效力超过使用事先用Colby公式计算的效力。The results of the test showed that the observed potency exceeded that calculated using the Colby formula in advance.
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