PROCESS FOR THE PREPARATION OF GABAPENTIN
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF GABAPENTIN 审中-公开
    制备GABAPENTIN的方法

    公开(公告)号:US20090326266A1

    公开(公告)日:2009-12-31

    申请号:US12400080

    申请日:2009-03-09

    IPC分类号: C07C229/28

    摘要: A process for the preparation of 1,1-cyclohexanediacetic acid monoamide comprising the amination of 1,1-cyclohexanediacetic acid anhydride by reaction with aqueous NH3 at a temperature lower than 30° C. by using a NH3/anhydride molar ratio lower than 3, and the product precipitation through the acidification of the reaction mixture; a precipitation process of 1,1-cyclohexanediacetic acid monoamide; and a process for the synthesis of gabapentin comprising the above preparation of 1,1-cyclohexanediacetic acid monoamide, the Hofmann transposition of the same monoamide, the purification of a gabapentin salt and the crystallization from organic solvent.

    摘要翻译: 一种制备1,1-环己烷二乙酸单酰胺的方法,该方法包括使用低于3的NH 3 /酐摩尔比,通过与NH 3水溶液在低于30℃的温度下反应来胺化1,1-环己烷二乙酸酐, 并通过反应混合物酸化产物沉淀; 1,1-环己烷二乙酸单酰胺的沉淀过程; 以及合成加巴喷丁的方法,其包括上述1,1-环己烷二乙酸单酰胺的制备,相同单酰胺的霍夫曼转位,加巴喷丁盐的纯化和有机溶剂的结晶。