PROCESS FOR THE SYNTHESIS OF IB-MECA
    1.
    发明申请
    PROCESS FOR THE SYNTHESIS OF IB-MECA 有权
    合成IB-MECA的方法

    公开(公告)号:US20100087636A1

    公开(公告)日:2010-04-08

    申请号:US12450094

    申请日:2008-03-13

    IPC分类号: C07H19/16 C07H1/00

    CPC分类号: C07H19/16 C07H1/00 Y02P20/55

    摘要: The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.

    摘要翻译: 本公开提供了用于合成IB-MECA的方法。 更具体地,本公开提供了IB-MECA的良好制造生产(GMP)的简单且高产率的方法。 该方法涉及6-卤代嘌呤-9-核糖苷与二醇保护试剂的反应; 用二醇保护试剂氧化二醇保护的6-卤嘌呤-9-核糖苷中的伯醇; 二醇中的伯醇的氧化被保护的6-卤代嘌呤; 二醇保护的6-卤代嘌呤与亲核试剂(如甲胺)的反应; 用碘苄胺取代卤素基团并除去二醇保护基团。

    Process for the synthesis of IB-MECA
    2.
    发明授权
    Process for the synthesis of IB-MECA 有权
    合成IB-MECA的方法

    公开(公告)号:US09102698B2

    公开(公告)日:2015-08-11

    申请号:US12450094

    申请日:2008-03-13

    IPC分类号: C07H19/16 C07H1/00

    CPC分类号: C07H19/16 C07H1/00 Y02P20/55

    摘要: The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.

    摘要翻译: 本公开提供了用于合成IB-MECA的方法。 更具体地,本公开提供了IB-MECA的良好制造生产(GMP)的简单且高产率的方法。 该方法涉及6-卤代嘌呤-9-核糖苷与二醇保护试剂的反应; 用二醇保护试剂氧化二醇保护的6-卤嘌呤-9-核糖苷中的伯醇; 二醇中的伯醇的氧化被保护的6-卤代嘌呤; 二醇保护的6-卤代嘌呤与亲核试剂(如甲胺)的反应; 用碘苄胺取代卤素基团并除去二醇保护基团。