METHOD FOR PRODUCING DIFLUOROMETHYL-SUBSTITUTED PYRAZOLE COMPOUNDS
    8.
    发明申请
    METHOD FOR PRODUCING DIFLUOROMETHYL-SUBSTITUTED PYRAZOLE COMPOUNDS 审中-公开
    用于生产二氟吡唑

    公开(公告)号:WO2008152138A3

    公开(公告)日:2009-05-28

    申请号:PCT/EP2008057506

    申请日:2008-06-13

    CPC classification number: C07D231/12 C07D231/14

    Abstract: The invention relates to a method for producing 3-difluoromethyl-substituted pyrazole compounds of formula (I), wherein R1 represents H, halogen, nitro, C1-C8 alkyl, C1-C8 haloalkyl, C3-C8 cycloalkyl, phenyl, naphthyl, hetaryl, cyano, -C(=O)-OR1a, -C(=O)-NR1bR1c, -C(=O)-SR1d or -C(=S)-SR1 e; R2 represents H, C1-C4 alkyl, benzyl or phenyl; R3 represents H, halogen, C1-C8 alkoxy, C1-C8 haloalkoxy, C3-C8 cycloalkoxy, C2-C8 alkenyloxy, C1-C8 alkylthio, C1-C8 haloalkylthio, C3-C8 cycloalkylthio or C2-C8 alkenylthio; to compounds of formula (II.a) or (II.b), wherein R1 and R3 have one of the above definitions; R4 represents halogen, -OR4a, -SR4a , -O-SO2-R4a or a group -NR4bR4c; R5 and R6 represent C1-C8 alkyl, C1-C8 haloalkyl, C3-C8 cycloalkyl, benzyl or phenyl or together with the nitrogen atom to which they are bound represent a 3- to 8-membered heterocycle; to Lewis acid adducts of compounds of formula (II.b); to the use of compounds of formula (II.a) or (II.b) and of the Lewis acid adducts thereof for producing compounds of formula (I) or (VI); and to a method for converting said compounds to the corresponding 3-difluoromethylpyrazole-4-yl carboxylic acids.

    Abstract translation: 本发明涉及一种用于制备式-3-二氟甲基吡唑(I)化合物其中R1是H,卤素,硝基,C1-C8烷基,C1-C8卤代烷基,C3-C8环烷基,苯基,萘基,杂芳基, 氰基,-C(= O)-OR1a,-C(= O)-NR1bR1c,-C(= O)-SR1d或-C(= S)-SR1e基; R2是H,C1-C4烷基,苄基或苯基; R 3为H,卤素,C1-C8烷氧基,C1-C8卤代烷氧基,C3-C8环烷氧基,C2-C8链烯氧基,C1-C8烷硫基,C1-C8卤代烷硫基,C3-C8-环烷硫基或C 2 -C C8-烯硫基;式(二.a)或(二.b)的化合物,其中R 1和R 3具有以上给出的含义之一; R 4是卤素,-OR4a,-SR4a,-O-SO2-R4A或一组-NR4bR4c基; R5和R6是C1-C8烷基,C1-C8卤代烷基,C3-C8环烷基,苄基或苯基或一起与氮原子到它们所键合的,代表3-至8-元杂环; 式(二.b)化合物的路易斯酸加合物;使用(二.a)或(二.b)和路易斯酸加合物,式I化合物的对式(I)或(VI)的化合物的制备方法; 并且这些化合物转变成相应的3-二氟甲基吡唑-4-基甲磺酸的方法。

    SUBSTITUTED 5-HETARYL-4-AMINOPYRIMIDINES
    9.
    发明申请
    SUBSTITUTED 5-HETARYL-4-AMINOPYRIMIDINES 审中-公开
    取代的5-杂芳基-4-氨基嘧啶

    公开(公告)号:WO2007110418A3

    公开(公告)日:2008-11-20

    申请号:PCT/EP2007052888

    申请日:2007-03-26

    CPC classification number: A01N43/54

    Abstract: The present invention relates to the use of 5-hetaryl-4-aminopyrimidines of the formula I and of their salts for controlling phytopathogenic fungi. The invention also relates to novel 5-hetaryl-4-aminopyrimidines and to plant protection compositions which contain at least one such compound as active component. Het represents an optionally substituted 5- or 6-membered aromatic heterocycle which has 1, 2, 3 or 4 hetero atoms as ring members which are selected among nitrogen, oxygen and sulphur, where the 5- or 6-membered heteroaromatic radical can have 1, 2, 3 or 4 identical or different substituents L; R 1 , R 2 represent inter alia hydrogen, C 1 -C 8 -alkyl, C 3 -C 8 -cycloalkyl, C 5 -C 10 -bicycloalkyl, C 2 -C 8 -alkenyl, C 4 -C 10 -alkadienyl, C 3 -C 6 -cycloalkenyl, C 2 -C 8 -alkynyl, phenyl, naphthyl or a five- or six-membered saturated, partially unsaturated or aromatic heterocycle which has one, two, three or four hetero atoms from the series O, N or S as ring members; or together form a ring; R 3 represents, inter alia, hydrogen, OH, halogen, cyano, NR 31 R 32 , C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, C 1 -C 8 -alkylsulphinyl, C 1 -C 8 -alkyl-sulphonyl, C 2 -C 8 -alkenyl or C 2 -C 8 -alkynyl; and R 4 represents halogen, cyano, hydroxy, mercapto, N 3 , C 1 -C 6 -alkyl, C 2 -C 8 -alkenyl, C 2 -C 8 -alkynyl, C 1 -C 6 -haloalkyl, C 1 -C 6 -alkoxy, C 3 -C 8 -alkenyloxy, C 3 -C 8 -alkynyloxy, C 1 -C 6 -haloalkoxy, C 1 -C 6 -alkylthio, C 3 -C 8 -alkenylthio, C 3 -C 8 -alkynylthio, C 1 -C 6 -haloalkylthio, or represents a radical of the formulae C(=Z)OR 41 , C(=Z)NR 42 R 43 , C(=Z)NR 44 -NR 42 R 43 , C(=Z)R 45 , CR 46 R 47 -OR 48 , CR 46 R 47 -NR 42 R 43 , ON(=CR 49 R 50 ), O-C(=Z)R 45 , NR 42 R 43a , NR 51 (C(=Z)R 45 ), NR 51 (C(=Z)OR 41 ), NR 51 (C(=Z)-NR 42 R 43 ), NR 52a (N=CR 49 R 50 ), NR 52 NR 42 R 43 , NR 52 OR 41 , or C(=N-X-R 45 )SR 41 .

    Abstract translation: 本发明涉及使用5-杂芳基-4-氨基嘧啶式I及其盐用于防治植物破坏性真菌。 本发明还涉及新的5-杂芳基-4-氨基嘧啶和含有至少一个这样的化合物作为有效成分的杀虫剂。 Het代表任选substituerten 5-或6-元芳族杂环,其具有1,2,3或4个氮,氧和选定的作为环成员的硫杂原子,其中所述5元或6元杂芳族残基1,2,3 可以包括或4个相同或不同的取代基L,R 1 ,R 2 除其他外,氢,C 1 -C 8 < / SUB>烷基,C 3 -C 8 环烷基,C 5 -C 10 二环烷基, ç 2 -C 8 烯基,C 4 -C 10 链二烯基,C 3 < / SUB> -C 6 环烯基,C 2 -C 8 炔基,苯基,萘基或五 - 或六元饱和的,部分 含有一个,具有从所述组的两个,三个或四个杂原子的不饱和或芳族杂环O,N或S作为环成员; 或一起形成一个环; [R 3 除其他外,氢,OH,卤素,氰基,NR 31 - [R 32 ,C 1 -C < SUB> 8 烷基,C 1 -C 8 烷氧基,C 1 -C 8 烷硫基,C 1 -C 8 烷基亚磺酰基,C 1 -C 8 烷基磺酰基,C < SUB> 2 -C 8 链烯基或C 2 -C 8 装置-Alkiny,且R 4 < / SUP>表示卤素,氰基,羟基,巯基,N 3 ,C 1 -C 6 烷基,C 2 < / SUB> -C 8 烯基,C 2 -C 8 炔基,C 1 -C < SUB> 6 卤代烷基,C 1 -C 6 烷氧基,C 3 -C 8 烯,C 3 -C 8 炔氧基,C 1 -C 6 卤代烷氧基,C < SUB> 1 -C 6 烷硫基,C 3 -C 8 烯,C 3 -C 8 炔硫基,C 1 -C 6 卤代烷硫基,或一个基团,式C(= Z)或 41 ,C(= Z)NR 42 ř 43 ,C(= Z)NR 44 -NR 42 - [R 43 ,C(= Z)R < SUP> 45 ,CR 46 - [R 47 为-OR 48 ,CR 46 - [R 47 -NR 42 - [R 43 ,ON(= CR 49 - [R 50 ),OC( = Z)R 45 ,NR 42 - [R 43A ,NR 51 (C(= Z)R 45 ),NR 51 (C(= Z)OR 41 ),NR 51 (C(= Z) - NR 42 - [R 43 ),NR 52A (N = CR 49 - [R 50 ),NR 52 NR 42 - [R 43 ,NR 52 41 ,或 C(= NXR 45 )SR 41 是。

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