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    VERFAHREN ZUR HERSTELLUNG VON DIFLUORMETHYLPYRAZOLYLCARBOXYLATEN
    3.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON DIFLUORMETHYLPYRAZOLYLCARBOXYLATEN 有权
    VERFAHREN ZUR HERSTELLUNG VON二氟甲基吡唑聚氧乙烯醚

    公开(公告)号：EP2086944A1

    公开(公告)日：2009-08-12

    申请号：EP07822162.9

    申请日：2007-11-02

    申请人： BASF SE

    发明人： RACK, Michael ,  SMIDT, Sebastian Peer ,  LÖHR, Sandra ,  KEIL, Michael ,  DIETZ, Jochen ,  RHEINHEIMER, Joachim ,  GROTE, Thomas ,  ZIERKE, Thomas ,  LOHMANN, Jan Klaas ,  SUKOPP, Martin

    IPC分类号： C07D237/04 ,  C07F7/04

    CPC分类号： C07D231/14

    摘要： The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-yl carboxylates of the formula (I) in which R1 is C1-C8-alkyl, C3-C8-cycloalkyl, C1-C4-alkoxy-C1-C4-alkyl, etc.; and R2 is hydrogen, C1-C4-alkyl, benzyl or phenyl, wherein a) a compound of the general formula (II) in which X is fluorine, chlorine, or bromine, R1 has one of the definitions given above, and R4 is C1-C8-alkyl, C3-C8-cycloalkyl, C2-C8-alkenyl, benzyl or phenyl, is reacted with a silane compound of the general formula R3nSiCl(4-n) in which n is 1, 2 or 3 and the substituents R3 are each independently selected from C1-C8-alkyl and phenyl, and with a metal which is selected from the metals of groups 1, 2, 3, 4 and 12 of the periodic table and has a redox potential of less than -0.7 V, based on a standard hydrogen electrode (at 25°C and 101.325 kPa); and b) the reaction mixture from step a) is reacted with a compound of the general formula (III) in which R2 has one of the definitions given above.

    摘要翻译： 本发明涉及制备式（I）的二氟甲基取代的吡唑-4-基羧酸酯的方法，其中R 1是C 1 -C 8烷基，C 3 -C 8环烷基，C 1 -C 4烷氧基-C 1 -C 4烷基， 烷基等; 其中a）通式（II）的化合物，其中X是氟，氯或溴，R1具有上述定义之一，且R4是氢，C1-C4-烷基，苄基或苯基， C1-C8-烷基，C3-C8-环烷基，C2-C8-链烯基，苄基或苯基与通式R3nSiCl（4-n）的硅烷化合物反应，其中n是1,2或3， R3各自独立地选自C1-C8-烷基和苯基，并且与选自元素周期表第1,2,3,4和12族的金属的金属并且具有小于-0.7V的氧化还原电势 ，基于标准氢电极（在25℃和101.325kPa下）; 和b）将来自步骤a）的反应混合物与通式（III）的化合物反应，其中R 2具有上述定义之一。

    PROCESS FOR THE SULFINYLATION OF A PYRAZOLE DERIVATIVE
    4.
    发明公开
    PROCESS FOR THE SULFINYLATION OF A PYRAZOLE DERIVATIVE 有权
    一种吡唑衍生物的硫化方法

    公开(公告)号：EP2084137A1

    公开(公告)日：2009-08-05

    申请号：EP07822223.9

    申请日：2007-11-05

    申请人： BASF SE

    发明人： SUKOPP, Martin ,  KUHN, Oliver ,  GRÖNING, Carsten ,  KEIL, Michael ,  LONGLET, Jon J.

    IPC分类号： C07D231/44 ,  A01N43/56 ,  A01N43/00 ,  A61K31/415 ,  A61P33/00

    CPC分类号： C07D231/44 ,  A01N43/56 ,  A01N47/02

    摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from secondary and/or tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof, wherein the temperature of the reaction mixture at no time exceeds 39°C.

    摘要翻译： 本发明涉及吡唑衍生物的亚磺酰化方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）为 在至少一种胺酸络合物存在下与亚磺酰化剂S反应，其中所述胺选自仲胺和/或叔胺并且所述酸选自氢氟酸，盐酸，氢溴酸和氢碘酸以及磺酸 酸衍生物，并加入卤化剂，其中S是[CF 3 S（O）] 2 O; 或CF 3 S（O）X，其中X表示氟，氯，溴，碘，羟基或羟基的碱金属或碱土金属盐; 或其混合物，其中反应混合物的温度不超过39℃。

    PROCESS FOR THE SULFINYLATION OF A PYRAZOLE DERIVATIVE
    7.
    发明公开
    PROCESS FOR THE SULFINYLATION OF A PYRAZOLE DERIVATIVE 有权
    一种吡唑衍生物的硫化方法

    公开(公告)号：EP2081909A1

    公开(公告)日：2009-07-29

    申请号：EP07822222.1

    申请日：2007-11-05

    申请人： BASF SE

    发明人： SUKOPP, Martin ,  KUHN, Oliver ,  GRÖNING, Carsten ,  KEIL, Michael ,  LONGLET, Jon J.

    IPC分类号： C07D231/44 ,  A01N43/56 ,  A01N43/00 ,  A61K31/415 ,  A61P33/00

    CPC分类号： C07D231/44 ,  A01N43/56

    摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from cyclic secondary amines and the acid(s) are selected from sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.

    摘要翻译： 本发明涉及吡唑衍生物的亚磺酰化方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）为 在至少一种胺酸络合物存在下与亚磺酰化剂S反应，其中胺（一种或多种）选自环状仲胺，并且酸选自磺酸衍生物，并且通过加入卤化剂， 其中S是[CF 3 S（O）] 2 O; 或CF 3 S（O）X，其中X表示氟，氯，溴，碘，羟基或羟基的碱金属或碱土金属盐; 或其混合物。

    PROCESS FOR THE PREPARATION OF PYRAZOLE DERIVATIVES
    8.
    发明公开
    PROCESS FOR THE PREPARATION OF PYRAZOLE DERIVATIVES 有权
    用于生产吡唑

    公开(公告)号：EP2443093A1

    公开(公告)日：2012-04-25

    申请号：EP10707918.8

    申请日：2010-03-12

    申请人： BASF SE

    发明人： DOCHNAHL, Maximilian ,  SUKOPP, Martin ,  KORTE, Alexander

    IPC分类号： C07D231/38 ,  A61K31/415

    CPC分类号： C07D231/38

    摘要： The present invention refers to a process for the preparation of pyrazole derivatives of formula (I), wherein W is nitrogen or CR
    1 , R
    1 , R
    2 , R
    4 and R
    5 are each independently selected from hydrogen, halogen, C
    1 -C
    6 -alkyl, C
    1 -C
    6 -haloalkyl, C
    1 -C
    6 -alkoxy, C
    1 -C
    6 -haloalkoxy, R
    7 S(O)n, nitro, cyano, and pentafluorothio; R
    3 is hydrogen, halogen, C
    1 -C
    6 -alkyl, C
    1 -C
    6 -haloalkyl, C
    1 -C
    6 -alkoxy, C
    1 -C
    6- haloalkoxy, R
    7 S(O)n, nitro, cyano, pentafluorothio or phenyl which is unsubstituted or substituted by 1 to 5 members of the group consisting of halogen, C
    1 -C
    6 -alkyl, C
    1 -C
    6- haloalkyl, C
    1 -C
    6 -alkoxy, C
    1 -C
    6- haloalkoxy, R
    7 S(O)n, nitro, cyano, and pentafluorothio which are the same or different; R
    7 is C
    1 -C
    6 -alkyl or C
    1 -C
    6 -haloalkyl; and n is 0, 1, or 2; characterized in that hydrazines of formula (II) wherein W, R
    2 , R
    3 , R
    4 , and R
    5 are as defined for pyrazole derivatives of formula (I), are reacted with a compound of formula (III).

    VERFAHREN ZUR HERSTELLUNG VON 1,3,4-SUBSTITUIERTEN PYRAZOLVERBINDUNGEN
    10.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON 1,3,4-SUBSTITUIERTEN PYRAZOLVERBINDUNGEN 有权
    用于生产取代1,3,4-吡唑

    公开(公告)号：EP2288597A2

    公开(公告)日：2011-03-02

    申请号：EP09742026.9

    申请日：2009-05-04

    申请人： BASF SE

    发明人： WOLF, Bernd ,  MAYWALD, Volker ,  KEIL, Michael ,  KORADIN, Christopher ,  RACK, Michael ,  ZIERKE, Thomas ,  SUKOPP, Martin

    IPC分类号： C07D231/14

    CPC分类号： C07D409/12 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07D231/14

    摘要： The present invention relates to a method for preparing 1,3-substituted pyrazol compounds of formula (I), where X stands for a group CX
    1 X
    2 X
    3 , with X
    1 , X
    2 and X
    3 being hydrogen, fluorine or chlorine, independently of one another, R
    1 being an C
    1 -C
    4 alkyl or cyclopropyl, and R
    2 being hydrogen, CN or a group CO
    2 R
    2a , where R
    2a stands for C
    1 -C
    6 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 R
    2 have the same meaning as indicated for formula (I), Y stands for oxygen, a group NR
    y1 or a group [NR
    y2 R
    y3 ]
    + Z
    - , R
    3 stands for OR
    3a or a group NR
    3b R
    3c , and wherein in formula (III) the variable R
    1 has the same meaning as indicated for formula (I), R
    4 and R
    5 stand for hydrogen, C
    1 -C
    6 alkyl, alternatively substituted phenyl, independent of one another, wherein at least one of the radicals R
    4 or R
    5 is different from hydrogen and where R
    4 and R
    5 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.