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    Process for preparing zanamivir and intermediates for use in the process
    141.
    发明授权
    Process for preparing zanamivir and intermediates for use in the process 有权
    制备用于该过程的扎那米韦和中间体的制备方法

    公开(公告)号：US08993789B2

    公开(公告)日：2015-03-31

    申请号：US13130692

    申请日：2009-11-24

    申请人： Manjinder Singh Phull ,  Rajendra Narayanrao Kankan ,  Dharmaraj Ramachandra Rao ,  Ashwini Amol Sawant ,  Sanoj Thoppil

    发明人： Manjinder Singh Phull ,  Rajendra Narayanrao Kankan ,  Dharmaraj Ramachandra Rao ,  Ashwini Amol Sawant ,  Sanoj Thoppil

    IPC分类号： C07D309/14 ,  C07D309/28

    CPC分类号： C07D309/28

    摘要： The present invention provides a process for preparing methyl 5-acetamido-4-amino-6-(1,2,3-triacetoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylate (V), which process comprises reducing methyl 5-acetamido-4-azido-6-(1,2,3-triacetoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylate (IV) in the presence of a reducing agent selected from the group consisting of lithium aluminum hydride, sodium borohydride, zinc/ammonium chloride, zinc-ferric chloride and ferric chloride/sodium iodide. The present invention also provides compounds of formula (VIII) and (IX) which may be used in the synthesis of zanamivir. The present invention also provides processes for preparing compounds (VIII) and (IX) and processes involving their use, including in the synthesis of zanamivir.

    摘要翻译： 本发明提供了制备5-乙酰氨基-4-氨基-6-（1,2,3-三
    乙酰氧基丙基）-5,6-二氢-4H-吡喃-2-羧酸甲酯（V）的方法，该方法包括将 5-乙酰氨基-4-叠氮基-6-（1,2,3-三
    乙酰氧基丙基）-5,6-二氢-4H-吡喃-2-羧酸甲酯（Ⅳ）在还原剂存在下，选自 氢化铝锂，硼氢化钠，氯化锌/氯化铵，氯化锌 - 氯化铁和氯化铁/碘化钠。 本发明还提供了可用于合成扎那米韦的式（Ⅷ）和（Ⅸ）化合物。 本发明还提供了制备化合物（VIII）和（IX）的方法和涉及其用途的方法，包括在合并的扎那米韦。