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    • 6. 发明申请
    • METHOD FOR PREPARING 1,3,4-SUBSTITUTED PYRAZOL COMPOUNDS
    • 用于生产取代1,3,4-吡唑
    • WO2009135808A2
    • 2009-11-12
    • PCT/EP2009055328
    • 2009-05-04
    • BASF SEWOLF BERNDMAYWALD VOLKERKEIL MICHAELKORADIN CHRISTOPHERRACK MICHAELZIERKE THOMASSUKOPP MARTIN
    • WOLF BERNDMAYWALD VOLKERKEIL MICHAELKORADIN CHRISTOPHERRACK MICHAELZIERKE THOMASSUKOPP MARTIN
    • C07D231/14
    • C07D409/12C07C251/76C07C251/84C07C251/86C07D231/14
    • The present invention relates to a method for preparing 1,3-substituted pyrazol compounds of formula (I), where X stands for a group CX1X2X3, with X1, X2 and X3 being hydrogen, fluorine or chlorine, independently of one another, R1 being an C1-C4 alkyl or cyclopropyl, and R2 being hydrogen, CN or a group CO2R2a, where R2a stands for C1-C6 alkyl in particular, comprising the following steps: i) reacting a compound of formula II with a hydrazone of formula (III), wherein in formula (II) the variables X and R2 have the same meaning as indicated for formula (I), Y stands for oxygen, a group NRy1 or a group [NRy2Ry3]+Z- , R3 stands for OR3a or a group NR3bR3c, and wherein in formula (III) the variable R1 has the same meaning as indicated for formula (I), R4 and R5 stand for hydrogen, C1-C6 alkyl, alternatively substituted phenyl, independent of one another, wherein at least one of the radicals R4 or R5 is different from hydrogen and where R4 and R5 can also stand for a 5 to 10-membered saturated carbocycle together with the carbon atom connected thereto; treatment of the reaction product obtained thereby with an acid in the presence of water.
    • 本发明涉及一种方法,用于制备1,3-取代的式(I),其中X是特别的一组CX1X2X3,其中X1,X2和X3独立地为特别是氢,氟或氯的吡唑化合物中,R1是C1 〜C 4烷基或环丙基,和R 2是氢,CN或基团CO2R2a,其中R 2a是特别C1-C6烷基,所述方法包括以下步骤:i)将式II的化合物与下式的腙反应 (III)其中在式(II)中,变量,X和R 2具有对式(I)所给出的含义,Y是氧,一组或一组NRy1 [NRy2Ry3] + Z-,R 3表示OR3a或一组NR3bR3c ,并且其中,在式(III)中,变量R1具有式(I)中给出的含义,R4和R5独立地是氢,C1-C6烷基,其任选被取代的苯基,其中至少一个基团 ëR4或R5是不同于氢,并且其中可以与它们所连接为一个5至10元饱和碳环,R4和R5的碳原子一起; 在水存在下用酸处理所得到的反应产物。
    • 7. 发明申请
    • METHOD FOR PRODUCING DIFLUOROMETHYL-SUBSTITUTED PYRAZOLE COMPOUNDS
    • 用于生产二氟吡唑
    • WO2008152138A3
    • 2009-05-28
    • PCT/EP2008057506
    • 2008-06-13
    • BASF SENETT MARKUSGROTE THOMASLOHMANN JAN KLAASDIETZ JOCHENSMIDT SEBASTIAN PEERRACK MICHAELZIERKE THOMAS
    • NETT MARKUSGROTE THOMASLOHMANN JAN KLAASDIETZ JOCHENSMIDT SEBASTIAN PEERRACK MICHAELZIERKE THOMAS
    • C07D231/12C07D231/14
    • C07D231/12C07D231/14
    • 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.
    • 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。