PROCESS FOR PREPARATION OF CERITINIB
    8.
    发明申请
    PROCESS FOR PREPARATION OF CERITINIB 审中-公开
    制备CERITINIB的方法

    公开(公告)号:WO2016199020A1

    公开(公告)日:2016-12-15

    申请号:PCT/IB2016/053339

    申请日:2016-06-08

    IPC分类号: C07D239/42

    CPC分类号: C07D239/42

    摘要: The present application relates to a process for preparation of ceritinib and intermediates thereof. Specifically, the present application relates to a process for preparation of N-(4-(1-benzyl- 1,2,3,6-tetrahydropyridin-4-yl)-2-isopropoxy-5-methylphenyl)acetamide (VC) comprising treating N-(4-(bromomethyl)-2-isopropoxy-5-methylphenyl)acetamide (IIID) with 1- benzylpiperidin-4-one (IVA). The present application also relates to a process for conversion of N-(4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)-2-isopropoxy-5-methylphenyl)-acetamide (VC) to ceritinib or an acid-addition salt thereof.

    摘要翻译: 本申请涉及制备硫酸尼他菌及其中间体的方法。 具体地说,本申请涉及制备N-(4-(1-苄基-1,2,3,6-四氢吡啶-4-基)-2-异丙氧基-5-甲基苯基)乙酰胺(VC)的方法,包括 用1-苄基哌啶-4-酮(IVA)处理N-(4-(溴甲基)-2-异丙氧基-5-甲基苯基)乙酰胺(IIID)。 本申请还涉及将N-(4-(1-苄基-1,2,3,6-四氢吡啶-4-基)-2-异丙氧基-5-甲基苯基) - 乙酰胺(VC)转化为 塞立替尼或其酸加成盐。