Racemization and enantiomer separation of clopidogrel
    30.
    发明授权
    Racemization and enantiomer separation of clopidogrel 失效
    氯吡格雷的外消旋化和对映异构体分离

    公开(公告)号:US07259261B2

    公开(公告)日:2007-08-21

    申请号:US10958072

    申请日:2004-10-04

    IPC分类号: C07D471/02 A61K31/70

    摘要: Processes for separation of enantiomers of clopidogrel, and converting one enantiomer of clopidogrel to another enantiomer of clopidogrel are provided. The enantiomers are separated by crystallizing the (S) enantiomer as camphor sulfonate salt from a hydrocarbon, or a mixture of a hydrocarbon and a co-solvent, preferably DMF:toluene. The (R) enantiomer is then racemized and recycled by reaction with a catalytic amount of a base, preferably with t-butoxide.

    摘要翻译: 提供氯吡格雷的对映异构体分离方法,将氯吡格雷的一种对映异构体转化为氯吡格雷的另一种对映异构体。 通过从烃或烃和共溶剂,优选DMF:甲苯的混合物中结晶(S)对映异构体作为樟脑磺酸盐分离对映异构体。 然后将(R)对映异构体外消旋化并通过与催化量的碱,优选与叔丁醇反应而再循环。