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    • 31. 发明申请
    • PROCESS FOR THE PREPARATION OF CITALOPRAM
    • 制备CITALOPRAM的方法
    • WO2002066453A1
    • 2002-08-29
    • PCT/IN2002/000023
    • 2002-02-11
    • NATCO PHARMA LIMITEDPULLA, Reddy, MuddasaniVENKAIAH, Chowdary, Nannapaneni
    • PULLA, Reddy, MuddasaniVENKAIAH, Chowdary, Nannapaneni
    • C07D307/87
    • C07D307/87
    • This invention discloses an improved process for the preparation of citalopram of the formula III which comprises (i) preparing the compound of the formula VIII by reducing an unisolable magnesium salt of a benzophenone derivative of the formula V using sodium borohydride in the presence of a protic solvent, (ii) reacting the compound of the formula VIII obtained in step (i) with an acid catalyst in a non-polar solvent to obtain a compound of the formula I, (iii) reacting the compound of the formula I obtained in step (ii) with copper (I) cyanide in a polar solvent medium and isolating the resulting cyano compound, by recrystallization by using polar and/or alcoholic solvents to obtain the compound of the formula II and (III) reacting the resulting compound of the formula II by conventional methods to form citalopram of the formula III. Citalopram is widely used as an antidepressant.
    • 本发明公开了一种制备式III西酞普兰的改进方法,其包括(i)通过在质子存在下使用硼氢化钠还原式V的二苯甲酮衍生物的单不溶性镁盐来制备式VIII化合物 溶剂,(ⅱ)使步骤(ⅰ)中获得的式Ⅷ的化合物与酸催化剂在非极性溶剂中反应,得到式Ⅰ化合物,(ⅲ)使步骤 (ii)在极性溶剂介质中加入氰化铜(I),并通过使用极性和/或醇溶剂重结晶分离得到的氰基化合物,得到式II和(III)的化合物,使所得式 II通过常规方法形成式III的西酞普兰。 西酞普兰被广泛用作抗抑郁药。