PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 有权
    制备吡唑羧酸酰胺的方法

    公开(公告)号:US20130035496A1

    公开(公告)日:2013-02-07

    申请号:US13642406

    申请日:2011-04-14

    Abstract: The invention relates to a process for the preparation of the compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula (X), reacting the halobenzyne of formula X so formed with cyclopentadiene to (III), b) reacting III in the presence of an inert solvent with an oxidant to (IV), c) reacing IV in the presence of a Lewis acid and a hydride source to (V), d) reacting V in the presence of an oxidizing agent, a base and an inert solvent to (VI), e) converting VI in the presence of a phosphane and CCL4 or CHCl3 to (VII), and either f1) reacting VII with NH3 in the presence of a catalyst to the compound of formula (VIII); and g) reacting VIII in the presence of a base with a compound of formula (IX), to the compound of formula (I); or f2) reacting the compound of formula (VII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with the compound of formula (IXa), to the compound of formula (I).

    Abstract translation: 本发明涉及一种制备式(I)化合物的方法,该方法包括:a)使惰性气氛下的有机金属物质使式(II)化合物(其中X为氯或溴)与卤代苯 使式(X)所示的卤代苯与环戊二烯反应,(b)使惰性溶剂与惰性溶剂的存在下的III反应与式(Ⅳ)反应:c)在Lewis 酸和氢化物源至(V),d)使V在氧化剂,碱和惰性溶剂的存在下与(VI)反应,e)将VI在磷烷和CCL 4或CHCl 3存在下转化为(VII ),并且f1)使VII与NH 3在催化剂存在下与式(VIII)化合物反应; 和g)在碱存在下使VIII与式(IX)化合物反应,得到式(I)化合物; 或者f2)使式(Ⅶ)化合物在溶剂存在下,碱,铜催化剂和至少一种配体与式(Ⅸa)化合物反应,得到式(I)化合物。

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