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    Process and intermediates for the production of 7-substituted antiestrogens
    1.
    发明公开
    Process and intermediates for the production of 7-substituted antiestrogens 有权
    方法和中间体的7- substitiuerter抗雌激素剂的制备

    公开(公告)号：EP1918295A3

    公开(公告)日：2012-10-17

    申请号：EP08150796.4

    申请日：2001-10-09

    申请人： AstraZeneca AB

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

    IPC分类号： C07J31/00

    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, R 1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl;
    R 2 , R 3 , R 4 and R 5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III)

    where R 1 , R 2 , R 3 , n, X and R 5 are as defined in relation to formula (II) and R 4' is a group R 4 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 R 4 ' to a group R 4 , or where R 4 ' is a group R 4 , converting it to a different such group.
    Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.