PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE
    6.
    发明公开
    PROCESS FOR PRODUCTION OF ARALKYLOXYPYRROLIDINE DERIVATIVE 有权
    VERFAHREN ZUR HERSTELLUNG VON ARALKYLOXYPYRROLIDINDERIVATEN

    公开(公告)号:EP1947083A4

    公开(公告)日:2009-05-27

    申请号:EP06796649

    申请日:2006-08-22

    申请人: KANEKA CORP

    IPC分类号: C07D207/12

    CPC分类号: C07D207/12 Y02P20/55

    摘要: Disclosed is a process for production of an aralkyloxypyrrolidine derivative which is important for the production of a pharmaceutical or the like. A 3-aralkyloxypyrrolidine derivative can be produced in the form of a crystal by a process comprising reacting an N-protected-3-hydroxypyrrolidine with a halogenated aralkyl in the presence of a base and a metal halide and/or a phase transfer catalyst to give an N-protected-3-aralkyloxypyrrolidine, performing the deprotection of the N-protecting group in the product to give a 3-aralkyloxypyrrolidine derivative, and treating the product in a solvent containing a polar solvent. The process can produce a highly pure 3-aralkyloxypyrrolidine derivative in a simple manner, with good efficiency, and in an industrial scale.

    摘要翻译: 公开了一种生产药物等重要的芳烷氧基吡咯烷衍生物的方法。 3-芳烷氧基吡咯烷衍生物可以通过包括在碱和金属卤化物和/或相转移催化剂存在下使N-保护的-3-羟基吡咯烷与卤代芳烷基反应得到晶体形式,得到 N-保护的-3-芳烷氧基吡咯烷,对产物中的N-保护基进行脱保护得到3-芳烷氧基吡咯烷衍生物,并在含有极性溶剂的溶剂中处理产物。 该方法可以以简单的方式高效纯化并以工业规模生产高纯度的3-芳烷氧基吡咯烷衍生物。