IMPROVED PROCESS FOR PREPARING RIVAROXABAN USING NOVEL INTERMEDIATES

    公开(公告)号:EP2844654A4

    公开(公告)日:2017-12-06

    申请号:EP12876006

    申请日:2012-05-02

    申请人: SYMED LABS LTD

    IPC分类号: C07D409/14

    CPC分类号: C07D413/14 C07D333/38

    摘要: The present inventors have surprisingly found that rivaroxaban of formula I can be prepared in a one-pot process, in high purity and with high yield, by reacting 5-chlorothiophene-2-carboxylic acid or a salt thereof with a sulfonylating agent to produce a sulfonyl ester intermediate, which is then condensed with 4-[4-[(SS)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morpholine-3-one or an acid addition salt thereof to produce rivaroxaban.