Process for the preparation of delta(15-16)-17-ketosteroids and use thereof in the synthesis of pharmacologically active compounds
    1.
    发明公开
    Process for the preparation of delta(15-16)-17-ketosteroids and use thereof in the synthesis of pharmacologically active compounds 有权
    一种生产德尔塔(15,16)-17-酮基类固醇以及它们在药理学活性的化合物的合成过程中使用

    公开(公告)号:EP1586579A1

    公开(公告)日:2005-10-19

    申请号:EP05101435.5

    申请日:2005-02-25

    IPC分类号: C07J1/00 C07J21/00 C07J31/00

    CPC分类号: C07J21/00 C07J1/00 C07J31/00

    摘要: A process is described for the preparation of Δ 15-16 -17-ketosteroids of the formula
    in which the substituents have the meaning stated in the description, which process comprises a) the reaction of a 17-ketosteroid of the formula
    with diphenyl disulfide in the presence of a strong base, b) the subsequent oxidation reaction of the intermediate 16-phenyl sulfide to the sulfoxide and c) the sulfoxide elimination reaction to yield the Δ 15-16 ―17-ketosteroid compound of the formula (6). Said process is preferably applied to the synthesis of gestodene.

    摘要翻译: 方法描述用于制备DELTA式在其中取代基具有的含义在说明书陈述的<15-16> -17酮基类固醇的方法,其包括A)的一个17-酮类固醇的反应 式在强碱的存在下使用二苯基二硫化物,b)将中间体16 - 苯基硫醚的后续氧化反应成亚砜和c)亚砜消除反应,得到DELTA <15-16> -17- 式酮类固醇化合物(6)。 所述方法优选应用于孕激素的合成。