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    • 3. 发明授权
    • Process for the preparation of pyrazole carboxylic acid amides
    • 制备吡唑羧酸酰胺的方法
    • US08450499B2
    • 2013-05-28
    • US13642512
    • 2011-04-14
    • Raphael DumeunierHans Tobler
    • Raphael DumeunierHans Tobler
    • C07D231/10C07D303/02C07C211/43
    • C07D231/14C07D303/08C07D303/36
    • The invention relates to a process for the preparation of formula (I), which process comprises a) reacting the compound (II), with cyclopentadiene to (III); b) reacting this compound in the presence of an oxidant to the compound of formula (IV); c) hydrogenating this compound in the presence of a metal catalyst and an inert solvent under hydrogen atmosphere to the compound of formula (V); d) reacting this compound in the presence of a Brönsted acid followed by a reducing agent to the compound of formula (VI); e) reacting VI with a compound (VII), in the presence of a base to a compound of formula (VIII); f) converting the compound of formula VIII in the presence of an oxidizing agent to the compound of formula (IX); and g) reacting the compound of formula IX in the presence of triphenylphosphane/carbon tetrachloride or riphenylphosphane/bromotrichloromethane to the compound of formula I.
    • 本发明涉及制备式(I)的方法,该方法包括:a)使化合物(II)与环戊二烯反应至(III); b)在氧化剂存在下使该化合物与式(Ⅳ)化合物反应; c)在金属催化剂和惰性溶剂的存在下,在氢气氛下将该化合物氢化成式(V)化合物; d)在布朗斯台德酸的存在下将该化合物与式(VI)化合物的还原剂反应; e)使VI与化合物(VII)在碱的存在下与式(VIII)的化合物反应; f)将式VIII化合物在氧化剂存在下转化为式(Ⅸ)化合物; 和g)在三苯基膦/四氯化碳或联苯基膦/溴三氯甲烷存在下将式IX化合物与式I化合物反应。