PROCESS FOR THE PREPARATION OF ESTERS OF 1-SUBSTITUTED-3-FLUOROALKYL-PYRAZOLE-4-CARBOXYLIC ACIDS

    公开(公告)号:EP2595962B1

    公开(公告)日:2018-07-11

    申请号:EP11737935.4

    申请日:2011-07-22

    申请人: SOLVAY SA

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: A process for the manufacture of an ester or the respective free acid of a 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acid of formula (I), wherein in such formula (I), Y is H, F or an alkyl group having from 1 to 12 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group or an aryl group; R1 is H or an organic residue; R2 is H or an organic residue. Such process comprises submitting a compound of formula (II) to a reduction reaction, wherein in such formula (II), Y is the same as defined for formula (I); X is Cl, Br or I; R1′ is H or an organic residue; and R2′ is H or an organic residue.

    PROCESS FOR THE PREPARATION OF PYRAZOLE-4-CARBOXAMIDES
    2.
    发明公开
    PROCESS FOR THE PREPARATION OF PYRAZOLE-4-CARBOXAMIDES 审中-公开
    制备吡唑-4-羧酰胺的方法

    公开(公告)号:EP3174857A1

    公开(公告)日:2017-06-07

    申请号:EP15745446.3

    申请日:2015-07-29

    申请人: Solvay SA

    发明人: BRAUN, Max Josef

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: The invention concerns a process for the manufacture of pyrazole-4-carboxamides, in particular, of 3-difluoromethyl-1-methyl-1 H-pyrazole-4-carboxamides which are useful as pharmaceuticals and agrochemicals. The carboxamides are prepared from the corresponding pyzole-4-carboxylic acid esters and appropriate amine in the presence of a Lewis acid. Alternatively, the reaction is performed in the presence of a Lewis acid and a base.

    摘要翻译: 本发明涉及制备可用作药物和农业化学品的吡唑-4-甲酰胺,特别是3-二氟甲基-1-甲基-1H-吡唑-4-甲酰胺的方法。 该酰胺由路易斯酸存在下由相应的吡唑-4-羧酸酯和适当的胺制备。 或者,该反应在路易斯酸和碱存在下进行。

    PROCESS FOR THE MANUFACTURE OF FLUOROMETHOXYMALONIC ACID DERIVATIVES
    4.
    发明公开
    PROCESS FOR THE MANUFACTURE OF FLUOROMETHOXYMALONIC ACID DERIVATIVES 有权
    用于制造氟代甲氧基丙二酸衍生物的方法

    公开(公告)号:EP2673256A1

    公开(公告)日:2013-12-18

    申请号:EP12702050.1

    申请日:2012-02-07

    申请人: Solvay SA

    摘要: Process for the manufacture of a compound of formula R1OOC-CH(OCH2F)-COOR, (I) or R3HNOC-CH(OCH2F)-CONHR4(II) wherein R1, R2, R3, R4 are equal or different from each other and are independently selected from H; an alkyl group having from 1 to 10 carbon atoms which is optionally substituted by at least one halogen atom; an aralkyl group; or an aryl group, comprising reacting a compound of formula R1OOC-CH(OCH2X)-COOR2 (III) or R3HNOC-CH(OCH2X)-CONHR4(IV) wherein X is a leaving group that can be substituted by nucleophilic substitution, and wherein R1, R2, R3, R4 have the same meaning as above, with at least one source of nucleophilic fluorine.

    摘要翻译: 制备式R1OOC-CH(OCH2F)-COOR,(I)或R3HNOC-CH(OCH2F)-CONHR4(II)的化合物的方法,其中R1,R2,R3,R4彼此相同或不同且为 独立地选自H; 具有1至10个碳原子的烷基,其任选被至少一个卤素原子取代; 芳烷基; (OCH 2 X)-COOR 2(III)或R 3 HNOC-CH(OCH 2 X)-CONHR 4(IV)的化合物进行反应,其中X是可以被亲核取代取代的离去基团,并且其中 R1,R2,R3,R4具有与上述相同的含义,与至少一种亲核性氟来源。

    PROCESS FOR THE PREPARATION OF ESTERS OF 1-SUBSTITUTED-3-FLUOROALKYL-PYRAZOLE-4-CARBOXYLIC ACIDS
    5.
    发明公开
    PROCESS FOR THE PREPARATION OF ESTERS OF 1-SUBSTITUTED-3-FLUOROALKYL-PYRAZOLE-4-CARBOXYLIC ACIDS 有权
    用于生产选自酯1-取代-3-氟代烷基吡唑-4-羧酸

    公开(公告)号:EP2595962A1

    公开(公告)日:2013-05-29

    申请号:EP11737935.4

    申请日:2011-07-22

    申请人: SOLVAY SA

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: A process for the manufacture of an ester or the respective free acid of a 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acid of formula (I), wherein in such formula (I), Y is H, F or an alkyl group having from 1 to 12 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group or an aryl group; R1 is H or an organic residue; R2 is H or an organic residue. Such process comprises submitting a compound of formula (II) to a reduction reaction, wherein in such formula (II), Y is the same as defined for formula (I); X is Cl, Br or I; R1′ is H or an organic residue; and R2′ is H or an organic residue.