CN1149924C - Fungicidal mixtures based on tris (oxime ether) derivatives and other strobilurins - Google Patents
Fungicidal mixtures based on tris (oxime ether) derivatives and other strobilurins Download PDFInfo
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Abstract
本发明提供了一种杀真菌混合物,其中包含增效有效量的以下物质作为活性组分:a)式I苯乙酸衍生物及其盐,其中各取代基及下标如说明书所定义,和b)至少一种式II-V的化合物。
The present invention provides a fungicidal mixture, which comprises a synergistically effective amount of the following substances as active ingredients: a) a phenylacetic acid derivative of formula I and its salt, wherein each substituent and subscript is as defined in the specification, and b) at least one compound of formula II-V.
Description
本发明涉及用于防治有害真菌的杀真菌混合物,其包括:The present invention relates to a fungicidal mixture for controlling harmful fungi comprising:
a)式I苯乙酸衍生物及其盐A) formula I phenylacetic acid derivative and salt thereof
其中各取代基及下标含义如下:Wherein each substituting group and subscript meaning are as follows:
X为NOCH3,CHOCH3,CHCH3;X is NOCH 3 , CHOCH 3 , CHCH 3 ;
Y为O,NR;Y is O, NR;
R1,R各自彼此独立地为氢或C1-C4-烷基;R 1 , R are each independently of each other hydrogen or C 1 -C 4 -alkyl;
R2为氰基,硝基,三氟甲基,卤素,C1-C4-烷基或C1-C4-烷氧基;R 2 is cyano, nitro, trifluoromethyl, halogen, C 1 -C 4 -alkyl or C 1 -C 4 -alkoxy;
m为0,1或2,当m为2时,基团R2可以是不同的;m is 0, 1 or 2, when m is 2, the group R2 can be different;
R3为氢,氰基,C1-C4-烷基,C1-C4-卤代烷基,C3-C6-环烷基;R 3 is hydrogen, cyano, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl;
R4,R6各自彼此独立地为氢,R 4 and R 6 are each independently hydrogen,
C1-C10-烷基,C3-C6-环烷基,C2-C10-链烯基,C2-C10-炔基,C1-C10-烷基羰基,C2-C10-链烯基羰基,C3-C10-炔基羰基或C1-C10-烷基磺酰基,这些基团可以是部分或全部卤代的,或者连接有1-3个下述基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6-烷基,C1-C6-卤代烷基,C1-C6-烷基磺酰基,C1-C6-烷基亚磺酰基(sulfoxyl),C1-C6-烷氧基,C1-C6-卤代烷氧基,C1-C6-烷氧基羰基,C1-C6-烷硫基,C1-C6-烷基氨基,二-C1-C6-烷基氨基,C1-C6-烷基氨基羰基,二-C1-C6-烷基氨基羰基,C1-C6-烷基氨基硫代羰基,二-C1-C6-烷基氨基硫代羰基,C2-C6-链烯基,C2-C6-链烯氧基,C3-C6-环烷基,C3-C6-环烷基氧基,杂环基,杂环氧基,苄基,苄氧基,芳基,芳氧基,芳硫基,杂芳基,杂芳氧基和杂芳硫基,其中的环状基团本身又可以是部分或全部卤代的,或者连有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6-烷基,C1-C6-卤代烷基,C1-C6-烷基磺酰基,C1-C6-烷基亚磺酰基,C3-C6-环烷基,C1-C6-烷氧基,C1-C6-卤代烷氧基,C1-C6-烷氧基羰基,C1-C6-烷硫基,C1-C6-烷基氨基,二-C1-C6-烷基氨基,C1-C6-烷基氨基羰基,二-C1-C6-烷基氨基羰基,C1-C6-烷基氨基硫代羰基,二-C1-C6-烷基氨基硫代羰基,C2-C6-链烯基,C2-C6-链烯氧基,苄基,苄氧基,芳基,芳氧基,芳硫基,杂芳基,杂芳氧基,杂芳硫基或C(=NOR7)-An-R8;C 1 -C 10 -alkyl, C 3 -C 6 -cycloalkyl, C 2 -C 10 -alkenyl, C 2 -C 10 -alkynyl, C 1 -C 10 -alkylcarbonyl, C 2 -C 10 -alkenylcarbonyl, C 3 -C 10 -alkynylcarbonyl or C 1 -C 10 -alkylsulfonyl, which may be partially or fully halogenated, or have 1-3 attached The above groups: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -Alkylsulfonyl, C 1 -C 6 -alkylsulfinyl (sulfoxyl), C 1 -C 6 -alkoxy, C 1 -C 6 -halogenated alkoxy, C 1 -C 6 -alkoxy C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -alkylamino, C 1 -C 6 -alkylaminocarbonyl , di-C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 -alkenyl, C 2 - C 6 -alkenyloxy, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyloxy, heterocyclyl, heterocyclyloxy, benzyl, benzyloxy, aryl, aryl Oxygen, arylthio, heteroaryl, heteroaryloxy and heteroarylthio, wherein the cyclic group itself can be partially or fully halogenated, or have 1-3 of the following groups attached: cyano radical, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -alkylsulfonyl Acyl, C 1 -C 6 -Alkylsulfinyl, C 3 -C 6 -Cycloalkyl, C 1 -C 6 -Alkoxy, C 1 -C 6 -Haloalkoxy, C 1 -C 6 - Alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -alkylamino, C 1 -C 6 -alkylaminocarbonyl, di- C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyloxy, benzyl, benzyloxy, aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy, heteroarylthio or C(=NOR 7 )-A n -R 8 ;
芳基,芳基羰基,芳基磺酰基,杂芳基,杂芳基羰基或杂芳基磺酰基,这些基团可以是部分或全部卤代的,或者可带有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6-烷基,C1-C6-卤代烷基,C1-C6-烷基羰基,C1-C6-烷基磺酰基,C1-C6-烷基亚磺酰基,C3-C6-环烷基,C1-C6-烷氧基,C1-C6-卤代烷氧基,C1-C6-烷氧基羰基,C1-C6-烷硫基,C1-C6-烷基氨基,二-C1-C6-烷基氨基,C1-C6-烷基氨基羰基,二-C1-C6-烷基氨基羰基,C1-C6-烷基氨基硫代羰基,二-C1-C6-烷基氨基硫代羰基,C2-C6-链烯基,C2-C6-链烯氧基,苄基,苄氧基,芳基,芳氧基,杂芳基,杂芳氧基或C(=NOR7)-An-R8;Aryl, arylcarbonyl, arylsulfonyl, heteroaryl, heteroarylcarbonyl or heteroarylsulfonyl, which may be partially or fully halogenated, or may carry 1-3 of the following groups : cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -alk C 1 -C 6 -Alkylcarbonyl, C 1 -C 6 -Alkylsulfonyl, C 1 -C 6 -Alkylsulfinyl, C 3 -C 6 -Cycloalkyl, C 1 -C 6 -Alkoxy, C 1 -C 6 -haloalkoxy, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -alkylamino, C 1 -C 6 -Alkylaminocarbonyl, Di-C 1 -C 6 -Alkylaminocarbonyl, C 1 -C 6 -Alkylaminothiocarbonyl, Di-C 1 -C 6 -Alkylaminothiocarbonyl , C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyloxy, benzyl, benzyloxy, aryl, aryloxy, heteroaryl, heteroaryloxy or C(=NOR 7 )-A n -R 8 ;
R5为氢; R is hydrogen;
C1-C6-烷基,C2-C6-链烯基,C2-C6-炔基,这些烃基可以被部分或全部卤代,或者连有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6-烷基氨基羰基,二-C1-C6-烷基氨基羰基,C1-C6-烷基氨基硫代羰基,二-C1-C6-烷基氨基硫代羰基,C1-C6烷基磺酰基,C1-C6-烷基亚磺酰基,C1-C6-烷氧基,C1-C6-卤代烷氧基,C1-C6-烷氧基羰基,C1-C6-烷硫基,C1-C6-烷基氨基,二-C1-C6-烷基氨基,C2-C6-链烯氧基,C3-C6-环烷基,C3-C6-环烷基氧基,杂环基,杂环氧基,芳基,芳氧基,芳基-C1-C4-烷氧基,芳硫基,芳基-C1-C4-烷硫基,杂芳基,杂芳氧基,杂芳基-C1-C4-烷氧基,杂芳硫基,杂芳基-C1-C4-烷硫基,而其中的环状基团本身又可以是部分或全部卤代的和/或连有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,C1-C6-烷基,C1-C6-卤代烷基,C1-C6-烷基磺酰基,C1-C6-烷基亚磺酰基,C3-C6-环烷基,C1-C6-烷氧基,C1-C6-卤代烷氧基,C1-C6-烷氧基羰基,C1-C6-烷硫基,C1-C6-烷基氨基,二-C1-C6-烷基氨基,C1-C6-烷基氨基羰基,二-C1-C6-烷基氨基羰基,C1-C6-烷基氨基硫代羰基,二-C1-C6-烷基氨基硫代羰基,C2-C6-链烯基,C2-C6-链烯氧基,苄基,苄氧基,芳基,芳氧基,芳硫基,杂芳基,杂芳氧基,杂芳硫基和C(=NOR7)-An-R8;C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, these hydrocarbyl groups may be partially or fully halogenated, or 1-3 of the following groups are attached: cyano radical, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, halogen, C 1 -C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkylaminocarbonyl, C 1 - C 6 -Alkylaminothiocarbonyl, Di-C 1 -C 6 -Alkylaminothiocarbonyl, C 1 -C 6 Alkylsulfonyl, C 1 -C 6 -Alkylsulfinyl, C 1 - C 6 -alkoxy, C 1 -C 6 -haloalkoxy, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di- C 1 -C 6 -Alkylamino, C 2 -C 6 -Alkenyloxy, C 3 -C 6 -Cycloalkyl, C 3 -C 6 -Cycloalkyloxy, Heterocyclyl, Heteroepoxy radical, aryl, aryloxy, aryl-C 1 -C 4 -alkoxy, arylthio, aryl-C 1 -C 4 -alkylthio, heteroaryl, heteroaryloxy, heteroaryl -C 1 -C 4 -alkoxy, heteroarylthio, heteroaryl-C 1 -C 4 -alkylthio, and the cyclic group itself can be partially or fully halogenated and/ Or 1-3 of the following groups are connected: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, C 1 -C 6 -alkyl, C 1 -C 6 -halogenated alkyl , C 1 -C 6 -alkylsulfonyl, C 1 -C 6 -alkylsulfinyl, C 3 -C 6 -cycloalkyl, C 1 -C 6 -alkoxy, C 1 -C 6 - Haloalkoxy, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylthio, C 1 -C 6 -alkylamino, di-C 1 -C 6 -alkylamino, C 1 - C 6 -alkylaminocarbonyl, di-C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyloxy, benzyl, benzyloxy, aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy, heteroarylthio and C(=NOR 7 )-A n -R 8 ;
C3-C6-环烷基,C3-C6-环烯基,杂环基,芳基,杂芳基,这些环状基团可以被部分或全部卤代或连有1-3个下列基团:氰基,硝基,羟基,巯基,氨基,羧基,氨基羰基,氨基硫代羰基,卤素,C1-C6-烷基,C1-C6-卤代烷基,C1-C6-烷基磺酰基,C1-C6-烷基亚磺酰基,C3-C6-环烷基,C1-C6-烷氧基,C1-C6-卤代烷氧基,C1-C6-烷氧基羰基,C1-C6-烷硫基,C1-C6-烷基氨基,二-C1-C6-烷基氨基,C1-C6-烷基氨基羰基,二-C1-C6-烷基氨基羰基,C1-C6-烷基氨基硫代羰基,二-C1-C6-烷基氨基硫代羰基,C2-C6-链烯基,C2-C6-链烯氧基,苄基,苄氧基,芳基,芳氧基,杂芳基和杂芳氧基;C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkenyl, heterocyclyl, aryl, heteroaryl, these cyclic groups can be partially or fully halogenated or linked with 1-3 The following groups: cyano, nitro, hydroxyl, mercapto, amino, carboxyl, aminocarbonyl, aminothiocarbonyl, halogen, C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -Alkylsulfonyl, C 1 -C 6 -Alkylsulfinyl, C 3 -C 6 -Cycloalkyl, C 1 -C 6 -Alkoxy, C 1 -C 6 -Haloalkoxy, C 1 -C 6 -Alkoxycarbonyl, C 1 -C 6 -Alkylthio, C 1 -C 6 -Alkylamino, Di-C 1 -C 6 -Alkylamino, C 1 -C 6 -Alkyl Aminocarbonyl, di-C 1 -C 6 -alkylaminocarbonyl, C 1 -C 6 -alkylaminothiocarbonyl, di-C 1 -C 6 -alkylaminothiocarbonyl, C 2 -C 6 - Alkenyl, C 2 -C 6 -alkenyloxy, benzyl, benzyloxy, aryl, aryloxy, heteroaryl and heteroaryloxy;
其中A为氧,硫或氮,其中氮连有氢或C1-C6烷基;Wherein A is oxygen, sulfur or nitrogen, wherein nitrogen is connected with hydrogen or C 1 -C 6 alkyl;
n为0或1;n is 0 or 1;
R7为氢或C1-C6烷基;和R 7 is hydrogen or C 1 -C 6 alkyl; and
R8为氢或C1-C6烷基,R 8 is hydrogen or C 1 -C 6 alkyl,
和and
b)至少一种选自式II-V的杀真菌剂:b) at least one fungicide selected from formula II-V:
本发明的目的是提供具有良好杀真菌活性(特别是对稻真菌病害)、且其效力超越混合物各组分单独效力的杀真菌混合物。It is an object of the present invention to provide fungicidal mixtures having good fungicidal activity, especially against fungal diseases of rice, and whose efficacy exceeds that of the individual components of the mixture.
我们发现本发明的这一目的可由权利要求1所述的混合物实现。We have found that this object of the invention is achieved by the mixtures described in claim 1 .
式I化合物本身是已知的,并记载于文献(WO 97/15552)内。The compounds of formula I are known per se and are described in the literature (WO 97/15552).
式II-V杀真菌剂也是已知的,并且记载于文献中。另外,如果合适的话,它们能够以下面括号内给出的商品名从市场上购得:The fungicides of the formulas II-V are also known and described in the literature. Alternatively, where appropriate, they are commercially available under the trade names given in parentheses below:
II:通用名:azoxystrobin(商品名:Amistar,Zeneca)II: Generic name: azoxystrobin (trade name: Amistar® , Zeneca)
III:EP-A 253,313,通用名:kresoxim-methyl(商品名:Brio,BASF)III: EP-A 253,313, common name: kresoxim-methyl (trade name: Brio® , BASF)
IV:EP 398,692,推荐通用名:metominostrobin(研制代码:SSF-126,Shionogi);IV: EP 398,692, recommended generic name: metominostrobin (development code: SSF-126, Shionogi);
V:EP 398,692,CAS RN 162535-21-9,SSF 129,Shionogi有限公司的开发产品)。V: EP 398,692, CAS RN 162535-21-9, SSF 129, a development product of Shionogi Co., Ltd.).
鉴于其C=C和C=N双键,制备化合物I时可能产生E/Z异构体混合物,它们随后可用常规方法(例如结晶和色谱法)分离为单一化合物。Due to its C=C and C=N double bonds, the preparation of compound I may result in a mixture of E/Z isomers which can then be separated into individual compounds by conventional methods such as crystallization and chromatography.
然而,如果合成产生了异构体混合物,由于在配制使用制剂的过程或使用制剂的过程中,在某些情况下,单一异构体可以相互转化(例如在光、酸或碱作用下),所以通常并不需要一定将它们分离开。类似的转化也可以在使用后发生,例如在处理植物时,发生于受处理的植物体内或者在要防治的有害真菌或动物害虫体内。However, if the synthesis results in a mixture of isomers, since the single isomers may be interconverted under certain circumstances (e.g. under the action of light, acid or base) during the preparation of the preparation for use or during the use of the preparation, So usually it is not necessary to separate them. Similar transformations can also take place after use, for example in the treatment of plants, in the plants to be treated or in the harmful fungi or animal pests to be controlled.
就C=X双键而言,鉴于其活性,化合物I优选E-异构体(基于-OCH3或-CH3基团相对于-CO2R1基团的构型)。In view of the reactivity of the C=X double bond, compound I is preferably the E-isomer (based on the configuration of the -OCH3 or -CH3 group relative to the -CO2R1 group).
对-C(R3)=NOCH2-双键来讲,考虑到它们的活性,优选化合物I的顺式异构体(基于基团R3相对于-OCH2-基团的构型)。With respect to the -C(R 3 )=NOCH 2 - double bond, the cis isomers of compounds I (based on the configuration of the group R 3 relative to the -OCH 2 - group) are preferred in view of their reactivity.
在本文开头给出的化合物I的定义中,使用了一般表示下述基团的集合术语:In the definition of compound I given at the outset, collective terms generally denoting the following groups are used:
卤素:氟,氯,溴和碘;Halogen: fluorine, chlorine, bromine and iodine;
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,如甲基,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,2,2-二甲基丙基,1-乙基丙基,己基,1,1-二甲基丙基,1,2-二甲基丙基,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,2-乙基丁基,1,1,2-三甲基丙基,1,2,2-三甲基丙基,1-乙基-1-甲基丙基和1-乙基-2-甲基丙基;Alkyl: straight-chain or branched-chain alkyl having 1 to 4, 6 or 10 carbon atoms, for example, C 1 -C 6 -alkyl, such as methyl, ethyl, propyl, 1-methylethyl , Butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl Base, 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 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, 2-ethylbutyl, 1,1,2-tri Methylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl and 1-ethyl-2-methylpropyl;
卤代烷基:具有1-6个碳原子的直链或支链烷基,这些基团中的一些或全部氢原子可能被上面所提及的卤原子取代,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;Haloalkyl: straight-chain or branched-chain alkyl groups having 1 to 6 carbon atoms, some or all of the hydrogen atoms in these groups may be replaced by the above-mentioned halogen atoms, e.g. C 1 -C 2 -haloalkyl, Such as chloromethyl, dichloromethyl, trichloromethyl, fluoromethyl, difluoromethyl, trifluoromethyl, chlorofluoromethyl, dichlorofluoromethyl, chlorodifluoromethyl, 1-fluoroethyl Base, 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;
环烷基:具有3-6个碳环原子的单环烷基,例如环丙基、环丁基、环戊基和环己基。Cycloalkyl: monocycloalkyl having 3 to 6 carbon ring atoms, eg cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl.
链烯基:具有2至6或10个碳原子并在任意位置具有一双键的直链或支链烯基,例如C2-C6-链烯基,如乙烯基,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-1-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-丙烯基和1-乙基-2-甲基-2-丙烯基;Alkenyl: Straight-chain or branched alkenyl having 2 to 6 or 10 carbon atoms and having a double bond in any position, for example C 2 -C 6 -alkenyl, such as vinyl, 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-pentenyl, 4-pentenyl, 1-methyl-1- Butenyl, 2-methyl-1-butenyl, 3-methyl-1-butenyl, 1-methyl-2-butenyl, 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-1-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 Alkenyl, 3-methyl-1-pentenyl, 4-methyl-1-pentenyl, 1-methyl-2-pentenyl, 2-methyl-2-pentenyl, 3-methyl Amyl-2-pentenyl, 4-methyl-2-pentenyl, 1-methyl-3-pentenyl, 2-methyl-3-pentenyl, 3-methyl-3-pentenyl Base, 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 Alkenyl, 1-ethyl-1-butenyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 2-ethyl-1-butenyl, 2-ethyl Base-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1-ethyl-1-methyl-2-propenyl, 1 - ethyl-2-methyl-1-propenyl and 1-ethyl-2-methyl-2-propenyl;
炔基:具有2-10个碳原子并在任意位置具有一三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;Alkynyl: Straight-chain or branched alkynyl having 2 to 10 carbon atoms and having a triple bond in any position, for example, C 2 -C 6 -alkynyl, such as ethynyl, 2-propynyl, 2- Butynyl, 3-butynyl, 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-hexyl Alkynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 1-methyl-4- Pentynyl, 2-methyl-3-pentynyl, 2-methyl-4-pentynyl, 3-methyl-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-ethyl-2-butynyl, 1-ethyl-3-butynyl, 2-ethyl-3-butynyl and 1-ethyl-1-methyl-2-prop Alkynyl;
杂环基或杂环氧基、杂环硫基和杂环氨基:含有1-3个选自氧、氮和硫杂原子的三至六元饱和或部分不饱和的单环或多环杂环,所述杂环直接或经氧原子(杂环氧基)或经硫原子(杂环硫基)或经氮原子(杂环氨基)连接在骨架上,例如2-四氢呋喃基,环氧乙烷基,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-噻二唑烷-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,2,3-二氢异吡唑-3-基,2,3-二氢异吡唑-4-基,2,3-二氢异吡唑-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,2,5-二氢噁唑-4-基,2,5-二氢噁唑-5-基,2,3-二氢噻唑-2-基,2,3-二氢噻唑-4-基,2,3-二氢噻唑-5-基,4,5-二氢噻唑-2-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,1,3-二氧戊环-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,1,1-二氧代-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;Heterocyclic group or heterocyclic oxy group, heterocyclic thio group and heterocyclic amino group: three to six membered saturated or partially unsaturated monocyclic or polycyclic heterocyclic rings containing 1-3 heteroatoms selected from oxygen, nitrogen and sulfur , the heterocyclic ring is connected to the skeleton directly or via an oxygen atom (heterocyclic oxy group) or via a sulfur atom (heterocyclic thio group) or via a nitrogen atom (heterocyclic amino group), such as 2-tetrahydrofuranyl, oxirane Base, 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-thiadiazolidin- 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- Base, 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-dihydroisoxazol- 4-yl, 4,5-dihydroisoxazol-5-yl, 2,5-dihydroisothiazol-3-yl, 2,5-dihydroisothiazol-4-yl, 2,5-dihydro Isothiazol-5-yl, 2,3-dihydroisopyrazol-3-yl, 2,3-dihydroisopyrazol-4-yl, 2,3-dihydroisopyrazol-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- Dihydrooxazol-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, 2,5-dihydrooxazol-4-yl, 2,5-dihydrooxazol-5-yl, 2,3-dihydrothiazol-2-yl, 2,3-dihydrothiazol-4-yl, 2,3-dihydrothiazol-5-yl, 4,5-dihydrothiazol-2-yl, 4, 5-dihydrothiazol-4-yl, 4,5-dihydrothiazol-5-yl, 2,5-dihydrothiazol-2-yl, 2,5-dihydrothiazol-4-yl, 2,5- Dihydrothiazol-5-yl, 2,3-dihydroimidazol-2-yl, 2,3-dihydroimidazol-4-yl, 2,3-dihydroimidazol-5-yl, 4,5-dihydro Imidazol-2-yl, 4,5-dihydroimidazol-4-yl, 4,5-dihydroimidazol-5-yl, 2,5-dihydroimidazol-2-yl, 2,5-dihydroimidazol- 4-yl, 2,5-dihydroimidazol-5-yl, 2-morpholinyl, 3-morpholinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 3-tetrahydro Pyridazinyl, 4-tetrahydropyridazinyl, 2-tetrahydropyrimidinyl, 4-tetrahydropyrimidinyl, 5-tetrahydropyrimidinyl, 2-tetrahydropyrazinyl, 1,3,5-tetrahydrotri Oxazin-2-yl, 1,2,4-tetrahydrotriazin-3-yl, 1,3-dihydrooxazin-2-yl, 1,3-dithian-2-yl, 2-tetrahydro Pyranyl, 1,3-dioxolan-2-yl, 3,4,5,6-tetrahydropyridin-2-yl, 4H-1,3-thiazin-2-yl, 4H-3, 1-benzothiazin-2-yl, 1,1-dioxo-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;
芳基或芳氧基、芳硫基、芳基羰基和芳基磺酰基:直接或经氧原子(-O-)(芳氧基)或经硫原子(-S-)(芳硫基)或经羰基(-CO-)(芳基羰基)或经磺酰基(-SO2-)(芳基磺酰基)键合到骨架上的芳香性单环或多环烃基,例如苯基,萘基或菲基或者苯氧基、萘氧基和菲氧基以及相应的羰基和磺酰基类基团;Aryl or aryloxy, arylthio, arylcarbonyl and arylsulfonyl: directly or via an oxygen atom (-O-) (aryloxy) or via a sulfur atom (-S-) (arylthio) or Aromatic monocyclic or polycyclic hydrocarbon groups bonded to the backbone via carbonyl (-CO-) (arylcarbonyl) or via sulfonyl (-SO 2 -) (arylsulfonyl), such as phenyl, naphthyl or phenanthrenyl or phenoxy, naphthyloxy and phenanthrenyloxy and corresponding carbonyl and sulfonyl groups;
杂芳基或杂芳氧基、杂芳硫基、杂芳基羰基和杂芳基磺酰基:除碳环原子外,另外可以含有1-4个氮原子或含1-3个氮原子和一个氧或一个硫原子或含一个氧或一个硫原子的芳香性单环或多环基团,它们直接或经氧原子(-O-)(杂芳氧基)或经硫原子(-S-)(杂芳硫基)、经羰基(-CO-)(杂芳基羰基)或经磺酰基(-SO2-)(杂芳基磺酰基)与骨架相连,例如Heteroaryl or heteroaryloxy, heteroarylthio, heteroarylcarbonyl and heteroarylsulfonyl: in addition to carbon ring atoms, may contain 1-4 nitrogen atoms or 1-3 nitrogen atoms and one Oxygen or a sulfur atom or an aromatic monocyclic or polycyclic group containing an oxygen or a sulfur atom, directly or via an oxygen atom (-O-) (heteroaryloxy) or via a sulfur atom (-S-) (heteroarylthio), via a carbonyl (-CO-) (heteroarylcarbonyl) or via a sulfonyl (-SO 2 -) (heteroarylsulfonyl) bonded to the backbone, for example
-含有1-3个氮原子的五元杂芳基:除碳原子外,还可以含有1-3个氮原子作为环原子的五元杂芳基,例如2-吡咯基,3-吡咯基,3-吡唑基,4-吡唑基,5-吡唑基,2-咪唑基,4-咪唑基,1,2,4-三唑-3-基和1,3,4-三唑-2-基。- five-membered heteroaryl containing 1-3 nitrogen atoms: five-membered heteroaryl containing 1-3 nitrogen atoms as ring atoms in addition to carbon atoms, such as 2-pyrrolyl, 3-pyrrolyl, 3-pyrazolyl, 4-pyrazolyl, 5-pyrazolyl, 2-imidazolyl, 4-imidazolyl, 1,2,4-triazol-3-yl and 1,3,4-triazole- 2-base.
-含有1-4个氮原子或含有1-3个氮原子和一个硫或氧原子或含有一个氧或一个硫原子的5-元杂芳基:五元杂芳基,除碳原子外,它还可以含有1-4个氮原子或含有1-3个氮原子和一个硫或氧原子或含有一个氧或硫原子作为环原子,例如2-呋喃基,3-呋喃基,2-噻吩基,3-噻吩基,2-吡咯基,3-吡咯基,3-异噁唑基,4-异噁唑基,5-异噁唑基,3-异噻唑基,4-异噻唑基,5-异噻唑基,3-吡唑基,4-吡唑基,5-吡唑基,2-噁唑基,4-噁唑基,5-噁唑基,2-噻唑基,4-噻唑基,5-噻唑基,2-咪唑基,4-咪唑基,1,2,4-噁二唑-3-基,1,2,4-噁二唑-5-基,1,2,4-噻二唑-3-基,1,2,4-噻二唑-5-基,1,2,4-三唑-3-基,1,3,4-噁二唑-2-基,1,3,4-噻二唑-2-基,1,3,4-三唑-2-基;- 5-membered heteroaryl groups containing 1 to 4 nitrogen atoms or containing 1 to 3 nitrogen atoms and a sulfur or oxygen atom or containing one oxygen or one sulfur atom: five-membered heteroaryl groups which, in addition to carbon atoms, It can also contain 1-4 nitrogen atoms or contain 1-3 nitrogen atoms and a sulfur or oxygen atom or contain an oxygen or sulfur atom as a ring atom, such as 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyrrolyl, 3-pyrrolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 3-isothiazolyl, 4-isothiazolyl, 5- Isothiazolyl, 3-pyrazolyl, 4-pyrazolyl, 5-pyrazolyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 2-imidazolyl, 4-imidazolyl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 1,2,4-thiazolyl Oxadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,4-triazol-3-yl, 1,3,4-oxadiazol-2-yl, 1, 3,4-thiadiazol-2-yl, 1,3,4-triazol-2-yl;
-含有1-3个氮原子或含有一个氮原子和/或一个氧或硫原子的苯并稠合五元杂芳基:五元杂芳基,除碳原子外,它还可以含有1-4个氮原子或含有1-3个氮原子和一个硫或氧原子或含有一个氧或一个硫原子作为环原子,并且其中两个相邻碳环原子或一个氮原子和一个相邻碳环原子可经丁-1,3-二烯-1,4-亚基基团桥连;- Benzofused five-membered heteroaryl containing 1-3 nitrogen atoms or containing one nitrogen atom and/or one oxygen or sulfur atom: a five-membered heteroaryl group which, in addition to carbon atoms, may contain 1-4 nitrogen atoms or contain 1-3 nitrogen atoms and a sulfur or oxygen atom or contain an oxygen or a sulfur atom as a ring atom, and wherein two adjacent carbon ring atoms or a nitrogen atom and an adjacent carbon ring atom can be Bridged via a but-1,3-diene-1,4-ylidene group;
-含有1-4个氮原子且经氮键连的五元杂芳基,或含有1-3个氮原子且经氮键连的苯并稠合五元杂芳基:五元杂芳基,除碳原子外,还可以分别含有1-4个氮原子和1-3个氮原子作为环原子,并且其中的两个相邻碳环原子或一个氮和一个相邻碳环原子可经丁-1,3-二烯-1,4-亚基基团桥连成环,这些环经氮环原子中的一个与骨架键连;- a nitrogen-bonded five-membered heteroaryl containing 1-4 nitrogen atoms, or a benzo-fused five-membered heteroaryl containing 1-3 nitrogen atoms bonded through a nitrogen: five-membered heteroaryl, In addition to carbon atoms, it can also contain 1-4 nitrogen atoms and 1-3 nitrogen atoms as ring atoms, and two adjacent carbon ring atoms or one nitrogen and one adjacent carbon ring atom can be butyl- 1,3-diene-1,4-ylidene groups are bridged to form rings, and these rings are bonded to the backbone via one of the nitrogen ring atoms;
-分别含有1-3个或1-4个氮原子的六元杂芳基:六元杂芳基,除碳原子外,还可以分别含有1-3个或1-4个氮原子作为环原子,例如:2-吡啶基,3-吡啶基,4-吡啶基,3-哒嗪基,4-哒嗪基,2-嘧啶基,4-嘧啶基,5-嘧啶基,2-吡嗪基,1,3,5-三嗪-2-基,1,2,4-三嗪-3-基和1,2,4,5-四嗪-3-基;- six-membered heteroaryl groups containing 1-3 or 1-4 nitrogen atoms respectively: six-membered heteroaryl groups which, in addition to carbon atoms, may contain 1-3 or 1-4 nitrogen atoms respectively as ring atoms , for example: 2-pyridyl, 3-pyridyl, 4-pyridyl, 3-pyridazinyl, 4-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 2-pyrazinyl , 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl and 1,2,4,5-tetrazin-3-yl;
-含有1-4个氮原子的苯并稠合六元杂芳基:其中两个相邻碳环原子可经丁-1,3-二烯-1,4-亚基基团桥连成环的六元杂芳基,例如喹啉,异喹啉,喹唑啉和喹喔啉,以及相应的氧基、硫基、羰基或磺酰基基团。杂芳基氨基:除碳环原子外,还可以含有1-4个氮原子或含有1-3个氮原子和一个氧或一个硫原子的芳香性单环或多环基团,它们经由氮原子与骨架相连。- Benzofused six-membered heteroaryl containing 1-4 nitrogen atoms: where two adjacent carbon ring atoms can be bridged by a but-1,3-diene-1,4-ylidene group to form a ring Six-membered heteroaryl groups such as quinoline, isoquinoline, quinazoline and quinoxaline, and the corresponding oxy, thio, carbonyl or sulfonyl groups. Heteroarylamino: Aromatic monocyclic or polycyclic groups that may contain, in addition to carbon ring atoms, 1 to 4 nitrogen atoms or 1 to 3 nitrogen atoms and an oxygen or a sulfur atom, via nitrogen atoms connected to the skeleton.
术语“部分或全部卤代”是指以此术语修饰的基团中的一些或所有氢原子可被如上所述的相同或不同卤原子取代。The term "partially or fully halogenated" means that some or all of the hydrogen atoms in a group modified by this term may be replaced by the same or different halogen atoms as described above.
考虑到它们的生物活性,优选其中m为0的式I化合物。Compounds of formula I wherein m is 0 are preferred in view of their biological activity.
同样优选其中R1为甲基的式I化合物。Preference is likewise given to compounds of the formula I in which R 1 is methyl.
此外,还优选其中R3为氢、氰基、环丙基、甲基、乙基、1-甲基乙基或CF3的化合物I。Furthermore, preference is also given to compounds I in which R 3 is hydrogen, cyano, cyclopropyl, methyl, ethyl, 1-methylethyl or CF 3 .
此外优选其中R3为甲基的化合物I。Preference is furthermore given to compounds I in which R 3 is methyl.
还优选其中R3为氰基的化合物I。Preference is also given to compounds I in which R3 is cyano.
而且优选其中R3为环丙基的化合物I。Preference is also given to compounds I in which R3 is cyclopropyl.
另外,优选其中R3为CF3的化合物I。In addition, compounds I in which R3 is CF3 are preferred.
另外,优选其中R5为氢,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。Additionally, preference is given to compounds I in which R is hydrogen , cyclopropyl, methyl, ethyl, isopropyl, unsubstituted or substituted aryl or heteroaryl.
此外优选其中R5为甲基的化合物I。Preference is furthermore given to compounds I in which R 5 is methyl.
另外,优选其中R5为乙基的化合物I。Additionally, preference is given to compounds I in which R 5 is ethyl.
此外优选其中R5为异丙基的化合物I。Preference is furthermore given to compounds I in which R 5 is isopropyl.
此外优选其中R5为环丙基的化合物I。Preference is furthermore given to compounds I in which R 5 is cyclopropyl.
此外优选其中R5为CF3的化合物I。Preference is furthermore given to compounds I in which R 5 is CF 3 .
另外,优选其中R5为未取代或取代的芳基或杂芳基的化合物I。In addition, preference is given to compounds I in which R 5 is unsubstituted or substituted aryl or heteroaryl.
另外优选的化合物I为其中R5为未取代或取代的吡啶基、嘧啶基、吡嗪基、哒嗪基或三嗪基的那些。Further preferred compounds I are those in which R 5 is unsubstituted or substituted pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl.
另外,优选其中R5为未取代或取代的呋喃基、噻吩基或吡咯基的化合物I。In addition, preference is given to compounds I in which R 5 is unsubstituted or substituted furyl, thienyl or pyrrolyl.
另外,优选的化合物I是其中R5为未取代或取代的噁唑基、噻唑基、异噁唑基、异噻唑基、吡唑基或咪唑基的那些。Additionally, preferred compounds I are those in which R is unsubstituted or substituted oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, pyrazolyl or imidazolyl.
另外,优选其中R5为未取代或取代的噁二唑基、噻二唑基或三唑基的化合物I。In addition, preference is given to compounds I in which R is unsubstituted or substituted oxadiazolyl, thiadiazolyl or triazolyl.
此外,还优选这些化合物I,其中R5为未取代的或带有一个或两个下述基团的苯基:硝基,氰基,羟基,氨基,氨基羰基,氨基硫代羰基,卤素,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 those compounds I in which R is phenyl which is unsubstituted or carries one or two of the following groups: nitro, cyano, hydroxy, amino, aminocarbonyl, aminothiocarbonyl, halogen, 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.
此外,还优选这些化合物I,其中R4为氢,C1-C6-烷基,C2-C6-链烯基,C2-C6-炔基,烯丙基,芳烷基,杂芳基烷基,芳氧基烷基,杂芳氧基烷基,芳基或杂芳基。Furthermore, preference is also given to those compounds I in which R 4 is hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, allyl, aralkyl, Heteroarylalkyl, aryloxyalkyl, heteroaryloxyalkyl, aryl or heteroaryl.
另外,优选其中R4为C1-C6-烷基的化合物I。In addition, preference is given to compounds I in which R 4 is C 1 -C 6 -alkyl.
更进一步优选的化合物I公开在WO 97/15,552内。Still further preferred compounds I are disclosed in WO 97/15,552.
包含在本发明混合物中的化合物I对多种植物病原菌都具有优越活性,特别是对于子囊菌纲、半知菌纲、藻状菌纲和担子菌纲真菌。Compound I contained in the mixture according to the invention has superior activity against various phytopathogenic bacteria, especially against Ascomycetes, Deuteromycetes, Phycobacteria and Basidiomycetes fungi.
它们对于各种植物,如棉花、蔬菜类(如黄瓜,菜豆,番茄,马铃薯和葫芦科)、大麦、牧草、燕麦、香蕉、咖啡、玉米、水果类、稻、黑麦、大豆、葡萄、小麦、观赏植物、甘蔗以及各类种子上的多种真菌病害的防治都特别重要。They are useful for a variety of plants such as cotton, vegetables (such as cucumbers, beans, tomatoes, potatoes and cucurbits), barley, pastures, oats, bananas, coffee, corn, fruits, rice, rye, soybeans, grapes, wheat The prevention and control of various fungal diseases on , ornamental plants, sugarcane and various seeds are particularly important.
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 graminis)(禾谷白粉病)、葫芦科上的二孢白粉菌(Erysiphe cichoracearum)和苍耳单丝壳菌(Sphaerothecafuliginea)、苹果上的苹果白粉病菌(Podosphaera leucotricha)(苹果白粉病)、葡萄上的葡萄钩丝壳(Uncinula necator)(葡萄白粉病),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(苹果黑星病)(Venturia inaequalis)、禾谷类上的长蠕孢菌(Helminthosporium)、小麦上的颖枯病菌(小麦颍枯病)(Septoria nodorum)、草莓、蔬菜、观赏植物和葡萄上的灰葡萄孢(Botrytis cinera)(灰霉病)、花生上的花生尾孢菌(Cercospora arachidicola)、小麦和大麦上的眼斑病菌(Pseudocercosporella herpotrichoides)、稻上的稻梨孢(Pyricularia oryzae)、马铃薯和蕃茄上的致病疫霉(Phytophthora infestans)、葡萄上的葡萄生单轴霉(Plasmoparaviticola)、啤酒花和黄瓜上的假霜霉菌(Pseudoperonospora)、蔬菜和水果上的链格孢菌(Alternaria),香蕉上的球腔菌(Mycosphaerella),以及镰刀菌(Fusarium)和轮枝孢菌(Verticillium)。They are particularly suitable for controlling the following phytopathogenic fungi: Erysiphe graminis (cereal powdery mildew) on cereals, Erysiphe cichoracearum and Sphaerothecafuliginea on cucurbitaceae , Podosphaera leucotricha (apple powdery mildew) on apples, Uncinula necator (vine powdery mildew) on grapes, Puccinia on cereals, cotton, rice and turf Rhizoctonia on cereals, Ustilago on cereals and sugarcane, Venturia inaequalis on apples, Helminthosporium on cereals ), Septoria nodorum on wheat, Botrytis cinera (Botrytis cinera) on strawberries, vegetables, ornamentals and grapes, Cercospora arachis on peanuts ( Cercospora arachidicola), Pseudocercosporella herpotrichoides on wheat and barley, Pyricularia oryzae on rice, Phytophthora infestans on potatoes and tomatoes, Plasmopara viticola on grapes (Plasmoparaviticola), Pseudoperonospora on hops and cucumbers, Alternaria on vegetables and fruits, Mycosphaerella on bananas, and Fusarium and Verticillium (Verticillium).
化合物II-V为市售杀真菌剂。Compounds II-V are commercially available fungicides.
在制备混合物时,优选采用纯净活性成分I和II-V,其中可以另外混入对有害真菌或其它害虫(如昆虫,蛛形纲动物或线虫)具有活性的其它成份,或具有除草活性或植物生长调节活性的成份或肥料。When preparing mixtures, the pure active ingredients I and II-V are preferably used, which may additionally be mixed with other ingredients which are active against harmful fungi or other pests (such as insects, arachnids or nematodes), or which have herbicidal activity or plant growth Active-modulating ingredients or fertilizers.
化合物I与至少一种化合物II至V的混合物可以同时(即一同或分别)使用,而且显示出对广谱植物病原真菌,特别是属于子囊菌纲、担子菌纲、半知菌纲和藻状菌纲的真菌具有优异的活性。这些化合物中某些可内吸地起作用,因而可用作叶面和土壤杀真菌剂。Mixtures of compound I and at least one compound II to V can be used simultaneously (i.e. together or separately) and are shown to be effective against a broad spectrum of phytopathogenic fungi, especially those belonging to the class Ascomycetes, Basidiomycetes, Deuteromycetes and Phytomycetes. Fungi of the class Mycetes have excellent activity. Some of these compounds act systemically and are therefore useful as foliar and soil fungicides.
它们对于防治各种作物,如棉花、蔬菜类(如黄瓜,菜豆,番茄,马铃薯和葫芦科)、大麦、牧草、燕麦、香蕉、咖啡、玉米、水果类、稻、黑麦、大豆、葡萄、小麦、观赏植物、甘蔗以及各种种子上的许多真菌都特别重要。They are useful for controlling various crops such as cotton, vegetables (such as cucumbers, beans, tomatoes, potatoes and cucurbits), barley, pastures, oats, bananas, coffee, corn, fruits, rice, rye, soybeans, grapes, Many fungi on wheat, ornamentals, sugar cane, and various seeds are of particular importance.
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 graminis)(禾谷白粉病)、葫芦科上的二孢白粉菌(Erysiphe cichoracearum)和苍耳单丝壳菌(Sphaerothecafuliginea)、苹果上的苹果白粉病菌(Podosphaera leucotricha)(苹果白粉病)、葡萄上的葡萄钩丝壳(Uncinula necator)(葡萄白粉病),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(苹果黑星病)(Venturia inaequalis)、禾谷类和稻上的长蠕孢菌(Helminthosporium)、小麦上的颖枯病菌(小麦颍枯病)(Septoria nodorum)、草莓、蔬菜、观赏植物和葡萄上的灰葡萄孢(Botrytis cinera)(灰霉病)、花生上的花生尾孢菌(Cercospora arachidicola)、小麦和大麦上的眼斑病菌(Pseudocercosporella herpotrichoides)、稻和草坪上的稻梨孢(Pyricularia oryzae)、马铃薯和蕃茄上的致病疫霉(Phytophthora infestans)、葡萄上的葡萄生单轴霉(Plasmoparaviticola)、啤酒花和黄瓜上的假霜霉菌(Pseudoperonospora)、蔬菜和水果上的链格孢菌(Alternaria),香蕉上的球腔菌(Mycosphaerella),以及镰刀菌(Fusarium)和轮枝孢菌(Verticillium)。They are particularly suitable for controlling the following phytopathogenic fungi: Erysiphe graminis (cereal powdery mildew) on cereals, Erysiphe cichoracearum and Sphaerothecafuliginea on cucurbitaceae , Podosphaera leucotricha (apple powdery mildew) on apples, Uncinula necator (vine powdery mildew) on grapes, Puccinia on cereals, cotton, rice and turf Rhizoctonia on cereals, Ustilago on cereals and sugarcane, apple scab (Venturia inaequalis) on apples, Helminthes sp. on cereals and rice (Helminthosporium), glume blight (Septoria nodorum) on wheat, Botrytis cinera (Botrytis cinera) (Botrytis cinera) on strawberries, vegetables, ornamentals and grapes, Cercospora arachis on peanuts Cercospora arachidicola, Pseudocercosporella herpotrichoides on wheat and barley, Pyricularia oryzae on rice and lawns, Phytophthora infestans on potatoes and tomatoes, Vitis vinifera on grapes Plasmoparaviticola, Pseudoperonospora on hops and cucumbers, Alternaria on vegetables and fruits, Mycosphaerella on bananas, and Fusarium and Verticillium.
本发明的混合物特别优选用于防治稻瘟病(Pyriculariaoryzae)。The mixtures according to the invention are particularly preferably used for controlling rice blast (Pyricularia eryzae).
化合物I和至少一种化合物II-V可以同时(即一起或分别施用),或先后施用,在分别施用的情形下,其施用次序一般对防治结果没有任何影响。Compound I and at least one compound II-V can be applied simultaneously (ie applied together or separately), or sequentially. In the case of separate application, the order of application generally has no effect on the control results.
本发明混合物的施用量,特别是在大田农作物的情况下,一般为0.01-8kg/ha,优选0.1-5kg/ha,尤为0.5-3.0kg/ha,这取决于所希望的效果。The application rates of the mixtures according to the invention, especially in the case of field crops, are generally 0.01-8 kg/ha, preferably 0.1-5 kg/ha, especially 0.5-3.0 kg/ha, depending on the desired effect.
对化合物I而言,其施用量为0.01-2.5kg/ha,优选0.05-2.5kg/ha,特别是0.1-1.0kg/ha。For compound I, the application rate is 0.01-2.5 kg/ha, preferably 0.05-2.5 kg/ha, especially 0.1-1.0 kg/ha.
相应地,就化合物II-V来说,施用量一般为0.001-5kg/ha,优选0.005-2kg/ha,特别是0.01-1.0kg/ha。Correspondingly, in the case of compounds II-V, the application rates are generally 0.001-5 kg/ha, preferably 0.005-2 kg/ha, in particular 0.01-1.0 kg/ha.
对于种子的处理,该混合物的施用量一般为0.001-250克/kg种子,优选0.01-100克/kg,特别是0.01-50克/kg。For the treatment of seeds, the mixture is generally applied in an amount of 0.001-250 g/kg seed, preferably 0.01-100 g/kg, especially 0.01-50 g/kg.
如果要防治植物病原有害真菌,化合物I与至少一种化合物II-V的分别或联合施用可在植物播种之前或之后,或者在植物出芽之前或之后,通过对种子、植物或土壤喷雾或撒粉来进行。If phytopathogenic harmful fungi are to be controlled, the compound I and at least one compound II-V can be applied separately or in combination either before or after sowing the plants, or before or after emergence of the plants, by spraying or dusting the seeds, the plants or the soil to proceed.
本发明的杀真菌增效混合物可以配制成,例如即可喷雾的溶液、粉剂和悬浮液形式,或高浓度的水性、油性或其它悬浮液、分散液、乳液,油分散体、糊剂、喷粉剂、撒播剂或颗粒剂的形式,并通过喷雾、弥雾、撒粉、撒播或浇泼施用。施用形式主要取决于预定用途;在任何情况下,应确保本发明混合物尽可能细微和均匀地分散。The fungicidally synergistic mixtures according to the invention can be formulated, for example, in the form of sprayable solutions, powders and suspensions, or in highly concentrated aqueous, oily or other suspensions, dispersions, emulsions, oil dispersions, pastes, sprays, etc. in the form of powders, spreaders or granules and to be applied by spraying, misting, dusting, broadcasting or pouring. The application form depends essentially on the intended use; in any case, it should ensure that the mixture according to the invention is dispersed as finely and homogeneously as possible.
这些制剂以本身已知的方式,例如通过活性成分与溶剂和/或载体混合,如果需要,通过使用乳化剂和分散剂来制备。如果所使用的稀释剂是水,也可以用其它的有机溶剂作助溶剂。对此适合的辅助剂主要是溶剂,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(例如细分散的硅酸、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)和分散剂如木质素亚硫酸盐废液或甲基纤维素。These formulations are prepared in a manner known per se, for example by mixing the active ingredient with solvents and/or carriers, if desired, by using emulsifiers and dispersants. If the diluent used is water, other organic solvents can also be used as auxiliary solvents. Suitable auxiliaries for this are primarily 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 ( such as finely divided silicic acid, silicates); emulsifiers such as nonionic and anionic emulsifiers (e.g. polyoxyethylene fatty alcohol ethers, alkylsulfonates and arylsulfonates) and dispersants such as lignosulfurous acid Salt waste or methylcellulose.
合适的表面活性物质为下列酸的碱金属盐、碱土金属盐和铵盐:芳族磺酸,如木质素磺酸、苯酚磺酸、萘磺酸和二丁基萘磺酸,和脂肪酸、烷基-和烷芳基磺酸,烷基-、月桂基醚-和脂肪醇硫酸;以及硫酸化十六烷基醇、十七烷基醇和十八烷基醇或脂肪醇乙二醇醚的盐,磺化萘及其衍生物与甲醛的缩合产物,萘或萘磺酸与苯酚和甲醛的缩合产物,聚氧乙烯辛基苯酚醚,乙氧基化异辛基苯酚、辛基苯酚或壬基苯酚,烷基苯酚聚乙二醇醚或三丁基苯基聚乙二醇醚,烷芳基聚醚醇,异十三烷基醇、脂肪醇氧化乙烯缩合物,乙氧基化蓖麻油,聚氧乙烯烷基醚或聚氧丙烯,十二烷基醇聚乙二醇醚乙酸盐,山梨醇酯,木素亚硫酸盐废液或甲基纤维素。Suitable surface-active substances are the alkali metal, alkaline earth metal and ammonium salts of the following acids: aromatic sulfonic acids, such as lignosulfonic acid, phenolsulfonic acid, naphthalenesulfonic acid and dibutylnaphthalenesulfonic acid, and fatty acids, alkanes Alkyl- and alkaryl sulfonic acids, alkyl-, lauryl ether- and fatty alcohol sulfuric acids; and sulfated salts of cetyl, heptadecanyl and stearyl alcohol or fatty alcohol glycol ethers , condensation products of sulfonated naphthalene and its derivatives with formaldehyde, condensation products of naphthalene or naphthalenesulfonic acid with phenol and formaldehyde, polyoxyethylene octylphenol ether, ethoxylated isooctylphenol, octylphenol or nonyl Phenol, alkylphenol polyglycol ether or tributylphenyl polyglycol ether, alkylaryl polyether alcohol, isotridecyl alcohol, fatty alcohol ethylene oxide condensate, ethoxylated castor oil, Polyoxyethylene alkyl ethers or polyoxypropylenes, lauryl alcohol polyglycol ether acetates, sorbitol esters, lignosulfite waste or methylcellulose.
粉剂、撒播剂和喷粉剂可通过混合或一同研磨化合物I和至少一种化合物II-V或化合物I及至少一种化合物II-V的混合物与固体载体来制备。Dusts, spreads and dusters can be prepared by mixing or grinding together compound I and at least one compound II-V or a mixture of compound I and at least one compound II-V with a solid carrier.
颗粒剂(例如,包衣颗粒,浸渍颗粒和均质颗粒)通常通过将活性成分粘合到固体载体上来制备。Granules (for example, coated granules, impregnated granules and homogeneous granules) are usually prepared by binding the active ingredients to solid carriers.
填料或固体载体是,例如矿质土类,如硅胶、硅酸、硅石、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、硫酸镁、氧化镁、研碎的合成物质、和肥料,如硫酸铵、磷酸铵、硝酸铵、尿素,以及植物源产物,如谷类作物粉末、树皮粉末、木材粉末和坚果壳粉,纤维素粉末或其它固体载体。Fillers or solid carriers are, for example, mineral earths such as silica gel, silicic acid, silica, silicates, talc, kaolin, limestone, lime, chalk, basalt, loess, clay, dolomite, diatomaceous earth, calcium sulfate , magnesium sulfate, magnesium oxide, ground synthetic substances, and fertilizers such as ammonium sulfate, ammonium phosphate, ammonium nitrate, urea, and products of plant origin such as cereal crop powder, bark powder, wood powder and nut shell powder, fibers plain powder or other solid carrier.
制剂通常包含0.1-95%重量,优选0.5-90%重量的化合物I和至少一种化合物II-V之一或化合物I与至少一种化合物II-V的混合物。所用活性成分的纯度为90%-100%,优选95%-100%(根据NMR谱或HPLC测定)。The formulations generally comprise 0.1-95% by weight, preferably 0.5-90% by weight, of compound I and at least one of the compounds II-V or a mixture of compound I and at least one compound II-V. The purity of the active ingredients used is from 90% to 100%, preferably from 95% to 100% (determined by NMR spectrum or HPLC).
其相应制剂通过用杀真菌有效量的混合物,或(在分别施用情形下)化合物I与至少一种化合物II-IV处理有害真菌、其聚集地、或欲免受它们侵染的植物、种子、土壤、表面,材料或空间的方式施用。The corresponding preparations are prepared by treating harmful fungi, their colonies, or plants, seeds, Application by way of soil, surface, material or space.
施用可在有害真菌侵染前或侵染后进行。Application can be carried out before or after infestation by the harmful fungi.
含有活性成分的这类制剂的实例是:Examples of such formulations containing active ingredients are:
I.90重量份的活性成分与10重量份的N-甲基吡咯烷酮组成的溶液,该溶液适合以微小雾滴的形式使用。The active component of 1.90 weight parts and the solution that the N-methylpyrrolidone of 10 weight parts forms, and this solution is suitable for using in the form of tiny mist.
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组成的混合物;将该溶液细分散在水中获得分散液。II.20 parts by weight of active ingredients, 80 parts by weight of xylene, 10 parts by weight of 8 to 10 moles of ethylene oxide and 1 mole of oleic acid-N-monoethanolamide adduct, 5 parts by weight of dodecane A mixture consisting of calcium salt of alkylbenzenesulfonate and 5 parts by weight of an adduct of 40 moles of ethylene oxide and 1 mole of castor oil; finely dispersing this solution in water to obtain a dispersion.
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、20重量份的40摩尔环氧乙烷与1摩尔蓖麻油的加合物组成的水分散液。III.20 parts by weight of active ingredient, 40 parts by weight of cyclohexanone, 30 parts by weight of isobutanol, 20 parts by weight of the adduct of 40 moles of ethylene oxide and 1 mole of castor oil.
IV.20重量份的活性成分、25重量份的环己醇、65重量份沸点是210至280℃的石油馏份和10重量份40摩尔环氧乙烷与1摩尔蓖麻油的加合物组成的水分散液。IV.20 parts by weight of the active ingredient, 25 parts by weight of cyclohexanol, 65 parts by weight of the boiling point of 210 to 280 ℃ of petroleum fractions and 10 parts by weight of 40 moles of ethylene oxide and 1 mole of castor oil adduct composition of aqueous dispersions.
V.将80重量份的活性成分与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盐废液的木素磺酸钠盐和7重量份粉状硅胶混合,且在锤磨中磨碎混合物,通过将该混合物细分散在水中获得喷雾混合物;V. The active ingredient of 80 parts by weight and the sodium salt of diisobutylnaphthalene-1-sulfonic acid of 3 parts by weight, the sodium lignosulfonate salt and 7 parts by weight of powder derived from sulfite waste liquid of 10 parts by weight Silica gel is mixed and the mixture is ground in a hammer mill to obtain a spray mixture by finely dispersing the mixture in water;
VI.将3重量份的活性成分与97重量份的细粉碎的高岭土均匀混合,由此获得喷粉剂,它包含3重量%的活性成分。VI. 3 parts by weight of the active ingredient are homogeneously mixed with 97 parts by weight of finely divided kaolin, whereby a dusting agent is obtained, which contains 3% by weight of the active ingredient.
VII.30重量份的活性成分、92重量份的粉状硅胶和8重量份预先喷涂到硅胶表面上的石蜡油组成的均匀混合物;得到具有良好粘性的活性成分的制剂。VII. A homogeneous mixture of 30 parts by weight of active ingredient, 92 parts by weight of powdered silica gel and 8 parts by weight of paraffin oil previously sprayed onto the surface of the silica gel; yields a formulation of active ingredient with good viscosity.
VIII.40重量份的活性成分、10重量份的苯酚磺酸/脲/甲醛缩合物的钠盐、2重量份硅胶和48重量份水组成的稳定的水分散液,该分散液可以进一步稀释;VIII.40 parts by weight of the active ingredient, 10 parts by weight of the sodium salt of phenolsulfonic acid/urea/formaldehyde condensate, 2 parts by weight of silica gel and a stable aqueous dispersion of 48 parts by weight of water, which can be further diluted;
IX.20重量份的活性成分、2重量份的十二烷基苯磺酸钙、8重量份的脂肪醇聚乙二醇醚、20重量份的苯酚磺酸/脲/甲醛缩合物的钠盐和88重量份的石蜡矿物油组成的稳定油性分散液。IX.20 parts by weight of the active ingredient, 2 parts by weight of calcium dodecylbenzenesulfonate, 8 parts by weight of fatty alcohol polyglycol ether, 20 parts by weight of the sodium salt of phenolsulfonic acid/urea/formaldehyde condensate A stable oily dispersion composed of 88 parts by weight of paraffinic mineral oil.
本发明混合物的增效活性可以通过下面的试验来证明:The synergistic activity of the mixtures of the invention can be demonstrated by the following tests:
将活性成分(单独或一起)配制成在63%重量环己酮与27%重量乳化剂组成的混合物中的10%乳液,然后用水稀释至所需浓度。The active ingredients (alone or together) were formulated as a 10% emulsion in a mixture of 63% by weight cyclohexanone and 27% by weight of emulsifier and then diluted with water to the desired concentration.
通过测定感染叶面面积的百分数进行评价。将这些百分数换算成作用效力。作用效力(W)采用下述Abbot公式计算:Evaluation is carried out by measuring the percentage of infected leaf area. These percentages were converted to efficacy. The potency (W) was calculated using the following Abbot formula:
W=(1-α/β)·100W=(1-α/β)·100
α对应于处理植物的真菌感染,以%计,和α corresponds to the fungal infection of the treated plants, in %, and
β对应于未处理(对照组)植物的真菌感染,以%计β corresponds to fungal infection of untreated (control) plants in %
效力0表示处理植物的感染程度与未处理对照植物感染程度相当;效力100表示处理植物未被感染。An efficacy of 0 indicates that the treated plants are infected to a degree comparable to that of the untreated control plants; an efficacy of 100 indicates that the treated plants are not infected.
采用Colby公式[R.S.Colby,杂草(Weeds), 15,20-22(1967)]计算活性成分混合物的预期作用效力并与观测到的作用效力加以比较。The expected potency of the active ingredient mixture was calculated using Colby's formula [RS Colby, Weeds, 15 , 20-22 (1967)] and compared to the observed potency.
Colby公式:E=x+y-x·y/100Colby's formula: E=x+y-x y/100
E表示使用浓度分别为a和b的活性成分A和B的混合物的情况下的预期作用效力,以未处理对照组的%表示E represents the expected potency of action in the case of using a mixture of active ingredients A and B at concentrations a and b respectively, expressed as % of the untreated control
X表示使用浓度为a的活性成分A的情况下的作用效力,以未处理对照组的%表示X represents the potency of action in the case of active ingredient A at concentration a, expressed as % of the untreated control
Y表示使用浓度为b的活性成分B的情况下的作用效力,以未处理对照组的%表示。Y indicates the potency of action in the case of active ingredient B at concentration b, expressed in % of the untreated control.
应用实施例1-抗稻梨孢(Pyricularia oryzae)活性(保护作用)Application example 1-anti-rice pear spore (Pyricularia oryzae) activity (protection)
使用由10%的活性成分、63%的环己酮和27%的乳化剂组成的原液制备的含水制剂喷洒盆栽“TaiNong 67”品种稻秧苗叶面至滴流。第二天,用稻梨孢孢子水悬浮液浸染这些植物。然后将试验植物在22-24℃和95-99%相对大气湿度的气候室内放置6天,然后目测叶面病害发展程度。The leaves of potted "TaiNong 67" rice seedlings were sprayed to drip with an aqueous formulation prepared from a stock solution consisting of 10% active ingredient, 63% cyclohexanone, and 27% emulsifier. The next day, the plants were infested with an aqueous suspension of Pyrium oryzae spores. The test plants were then placed in a climate chamber at 22-24° C. and 95-99% relative atmospheric humidity for 6 days, and the degree of development of foliar diseases was then visually assessed.
将目测感染叶面积%值转化为以未处理对照组的%表示的效力。效力0表示与未处理对照组具有相同的感染程度,效力100表示0%感染。活性成分组合的预期效力采用Colby公式计算(Colby,S.R.“除草剂组合的协同和拮抗效应的计算”,《(杂草》(Weeds),第15卷,20-22页;1967),并与所观测到的效力加以比较。The visual % infected leaf area values were converted to efficacy expressed as % of the untreated control. A potency of 0 means the same degree of infection as the untreated control, a potency of 100 means 0% infection. The expected potency of combinations of active ingredients was calculated using Colby's formula (Colby, S.R. "Calculation of the Synergistic and Antagonistic Effects of Herbicide Combinations", (Weeds, Vol. 15, pp. 20-22; 1967) and compared with The observed efficacy was compared.
采用下列化合物I′作为组分a):The following compounds I' are used as component a):
试验结果示于表1和2内:The test results are shown in Tables 1 and 2:
表1:
表2:
*采用Colby公式计算*Calculated using Colby's formula
试验结果表明,对于所有的混合比例,所观察的效力值均高于采用Colby公式计算得到效力值。The test results showed that, for all mixing ratios, the observed potency values were higher than those calculated using Colby's formula.
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