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    Process and intermediates for the production of 7-substituted antiestrogens
    6.
    发明授权
    Process and intermediates for the production of 7-substituted antiestrogens 有权
    用于生产7-取代的抗雌激素的方法和中间体

    公开(公告)号：US07947667B2

    公开(公告)日：2011-05-24

    申请号：US10398924

    申请日：2001-10-09

    申请人： Robert Stevenson ,  Fraser Witton Kerr ,  Anthony Raymond Lane ,  Eve Joanne Brazier ,  Phillip John Hogan ,  David Dermot Patrick Laffan

    发明人： Robert Stevenson ,  Fraser Witton Kerr ,  Anthony Raymond Lane ,  Eve Joanne Brazier ,  Phillip John Hogan ,  David Dermot Patrick Laffan

    IPC分类号： A61K31/56 ,  A61K31/00 ,  C07J41/00

    CPC分类号： C07J31/006 ,  C07J31/00 ,  Y02P20/55

    摘要： A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III) where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4′ is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4′ to a group R4, or where R4′ is a group R4, converting it to a different such group. Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.

    摘要翻译： 制备式（II）的中间体化合物的方法，其中X如说明书中所定义，R 1为卤代烷基，烷基，烯基，环烷基，羧基烷基，烷氧基羰基烷基，芳基或芳基烷基; R2，R3，R4和R5是说明书中定义的有机基团，该方法包括式（III）化合物的芳构化，其中R1，R2，R3，n，X和R5如关于式（II）所定义） 并且R4'为基团R4或其前体基团，然后如果需要或需要，进行一个或多个以下步骤：（i）除去任何羟基保护基团R; （ii）将前体基团R4'转化为基团R4，或其中R4'为基团R4，将其转化为不同的这种基团。 获得的化合物是例如制备氟维司群的有用的中间体。 还要求新的中间体。