Process for the preparation of intermediates of perindopril
    2.
    发明申请
    Process for the preparation of intermediates of perindopril 审中-公开
    培哚普利中间体的制备方法

    公开(公告)号:US20070032661A1

    公开(公告)日:2007-02-08

    申请号:US11495102

    申请日:2006-07-28

    IPC分类号: C07D209/42

    CPC分类号: C07D209/42

    摘要: A process for the preparation of (2S, 3aS, 7aS)perhydroindole-2-carboxylic acid is provided comprising (a) esterifying a cis-perhydroindole-2-carboxylic acid with a first alcohol of the formula ROH and a suitable free acid to provide the acid salt (AS) of Formula V: (b) reacting the acid salt of Formula V with a first base to provide a compound of Formula VI: (c) treating the product of step (b) with an L-tartaric containing acid in a second alcohol of the formula ROH to precipitate a compound of Formula VII: (d) reacting the compound of Formula VII with a second base to provide a compound of Formula II (e) hydrolyzing the compound of Formula II to provide the (2S, 3aS, 7aS)perhydroindole-2-carboxylic acid.

    摘要翻译: 提供了制备(2S,3aS,7aS)全氢吲哚-2-羧酸的方法,其包括(a)使顺式 - 全氢吲哚-2-羧酸与式ROH的第一醇和合适的游离酸酯化,以提供 式Ⅴ的酸性盐(AS):(b)使式Ⅴ的酸式盐与第一碱反应以提供式Ⅵ化合物:(ⅲ)用含L-酒石酸的酸处理步骤(b)的产物 在式ROH的第二个醇中,使式VII化合物沉淀:(d)使式VII化合物与第二碱反应,得到式II化合物(e)水解式II化合物,得到(2S ,3aS,7aS)全氢吲哚-2-羧酸。