CHEMICAL SYNTHESIS
    5.
    发明公开
    CHEMICAL SYNTHESIS 审中-公开
    化学合成

    公开(公告)号:EP1451132A1

    公开(公告)日:2004-09-01

    申请号:EP02791102.3

    申请日:2002-11-08

    IPC分类号: C07B41/02 C07J9/00

    摘要: The present invention relates to a method of producing vicinal diols from a compound, the method characterised by the step of reacting the compound with a moderately strong acid in the presence one or more reagents capable of supplying hydroxyl groups wherein the moderately strong acid is a strongly reducing agent, but has a conjugate base that is a weak nucleophile. In preferred embodiments the moderately strong acid is hypophosphorous acid and the reagent(s) capable of supplying hydroxyl groups is 2-propanol in water, where 2-propanol is water soluable and organic. This method is particularly applicable to the production of vicinal diols of steroids, including lanosterol. Once vicinal diols of lanosterol diols are formed they are then capable of being further reacted to produce high purity lanosterol.

    摘要翻译: 本发明涉及一种从化合物中制备连环二醇的方法,该方法的特征在于使化合物与中等强酸在一种或多种能提供羟基的试剂存在下反应的步骤,其中中等强酸是强烈的 还原剂,但具有弱亲核试剂的共轭碱。 在优选的实施方案中,中等强酸是次磷酸,能够提供羟基的试剂是水中的2-丙醇,其中2-丙醇是水溶性的和有机的。 该方法特别适用于类固醇(包括羊毛甾醇)的邻位二醇的生产。 一旦形成了羊脂醇二醇的邻位二醇,则它们能够进一步反应以产生高纯度羊毛甾醇。