Process for the synthesis of CMHTP and intermediates thereof
    18.
    发明申请
    Process for the synthesis of CMHTP and intermediates thereof 失效
    合成CMHTP的方法及其中间体

    公开(公告)号:US20080200676A1

    公开(公告)日:2008-08-21

    申请号:US11892532

    申请日:2007-08-23

    IPC分类号: C07D471/04 C07D213/72

    CPC分类号: C07D213/73 C07D471/04

    摘要: The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.

    摘要翻译: 本发明提供3-苄氧基-2-氨基吡啶(BOPA),3-(2-羟乙基)-2-甲基-9-羟基-4H-吡啶并[1,2-a]嘧啶-4-酮(HMBP) 3-(2-氯乙基)-2-甲基-9-羟基-4H-吡啶并[1,2-a]嘧啶-4-酮(CMHP)和3-(2-氯乙基)-6,7,8,9 - 四氢-9-羟基-2-甲基-4H-吡啶并[1,2-a] - 嘧啶-4-酮(CMHTP),其用作制备帕培培酮的中间体。 本发明还提供了制备这些中间体和制备利培酮的方法。