Process for preparing taxol side chain using heterogeneous trifunctional catalyst
    4.
    发明授权
    Process for preparing taxol side chain using heterogeneous trifunctional catalyst 失效
    使用异构三官能催化剂制备紫杉醇侧链的方法

    公开(公告)号:US06706901B1

    公开(公告)日:2004-03-16

    申请号:US10334119

    申请日:2002-12-31

    IPC分类号: C07D30514

    摘要: The present invention relates to an improved process for the preparation of taxol side chain by synthesizing (2R,3S)-2,3-dihydroxy-3-phenylpropionate with greater than 99% enantioselectivity and devoid of osmium even in crude form in a single pot using a recyclable multifunctional catalysts, conversion of diol obtained without further crystallization into bromoacetate, reaction of bromoacetate with NaN3 in organic solvent followed by deacetylation with to obtain azido alcohol, benzoylation followed by hydrogenation of azido alcohol to obtain the (2R,3S)-(N-)-benzoyl-3-phenylisoserine methyl ester in 67% yield.

    摘要翻译: 本发明涉及一种通过合成(2R,3S)-2,3-二羟基-3-苯基丙酸酯制备紫杉醇侧链的改进方法,其具有大于99%的对映选择性,甚至在单一罐中以粗制形式没有锇 使用可回收的多官能催化剂,将未经进一步结晶获得的二醇转化成溴乙酸酯,将溴乙酸酯与NaN 3在有机溶剂中反应,然后脱乙酰,得到叠氮醇,苯甲酰化,然后氢化叠氮醇,得到(2R,3S) - ( N - ) - 苯甲酰基-3-苯基异丝氨酸甲酯,收率67%。