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    • 70. 发明申请
    • PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES
    • 制备吡唑羧酸酰胺的方法
    • WO2011131546A1
    • 2011-10-27
    • PCT/EP2011/055872
    • 2011-04-14
    • SYNGENTA PARTICIPATIONS AGGRIBKOV, DenisSTOHLER, RemoVETTIGER, ThomasROMMEL, Michael
    • GRIBKOV, DenisSTOHLER, RemoVETTIGER, ThomasROMMEL, Michael
    • C07D231/14C07C25/24
    • C07D231/14C07C25/24
    • The invention relates to a process for the preparation of formula (I) which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III), wherein X is chloro or bromo; reacting the halobenzyne with a fulvene (IV), to a compound of formula(V) wherein X is chloro or bromo; b) hydrogenating V in the presence of a suitable metal catalyst to a compound of formula (VI) wherein X is chloro or bromo; and either c1) reacting the compound of formula VI with NH3 in the presence of a catalyst comprising palladium and at least one ligand to the compound of formula (VII); and d) reacting the compound of formula VII in the presence of a base with a compound of formula (VIII), to the compound of formula I; or c2 reacting the compound of formula (VI) in the presence of a copper catalyst and a ligand with the compound of formula (VIIIa), to the compound of formula (I).
    • 本发明涉及一种制备式(I)的方法,该方法包括a)将其中X为氯或溴的式(II)化合物与有机金属物质反应为(III),其中X为氯或溴 ; 将卤代苯与富烯(Ⅳ)反应于其中X为氯或溴的式(Ⅴ)化合物; b)在合适的金属催化剂存在下将V氢化为其中X为氯或溴的式(Ⅵ)化合物; 并且c1)在包含钯和至少一种配体的催化剂存在下使式VI的化合物与NH 3反应到式(VII)的化合物; 和d)使式VII化合物在碱存在下与式(VIII)化合物反应,得到式I化合物; 或c2将式(VI)化合物在铜催化剂和配体的存在下与式(VIIIa)化合物反应,得到式(I)化合物。