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    Steroid spirolactonization
    1.
    发明申请
    Steroid spirolactonization 审中-公开
    类固醇spirolactonization

    公开(公告)号：US20050090663A1

    公开(公告)日：2005-04-28

    申请号：US10806081

    申请日：2004-03-22

    申请人： Thaddeus Franczyk ,  Grace Wagner ,  Bruce Pearlman ,  Amphlett Padilla ,  Jeffrey Havens ,  Sonja Mackey ,  Haifeng Wu

    发明人： Thaddeus Franczyk ,  Grace Wagner ,  Bruce Pearlman ,  Amphlett Padilla ,  Jeffrey Havens ,  Sonja Mackey ,  Haifeng Wu

    IPC分类号： C07D307/94 ,  C07J20060101 ,  C07J1/00 ,  C07J9/00 ,  C07J19/00 ,  C07J71/00

    CPC分类号： C07J9/00 ,  C07J71/00

    摘要： A steroid comprising a 17-spirolactone or corresponding open lactone structure is obtained by carbonylation of a 17-alkenyl or 17-alkynyl substrate. A 17-alkenyl intermediate may be prepared by semi-hydrogenation of a 17-alkynyl group. Multiple reaction schemes are disclosed for preparation of a 3-keto-9,11-epoxy-17-spirolactone steroid such as eplerenone. Novel intermediates are also disclosed, as well as steps for forming such novel intermediates, or converting them to further intermediates or products, by semi-hydrogenation, carbonylation, 6,7-dehydrogenation, furylation or other transformations or combinations thereof.

    摘要翻译： 通过羰基化17-烯基或17-炔基底物获得包含17-螺内酯或相应的开放内酯结构的类固醇。 17链烯基中间体可以通过17-炔基的半氢化制备。 公开了多种反应方案用于制备3-酮-9,11-环氧-17-螺内酯类固醇如依普利酮。 还公开了新的中间体，以及通过半氢化，羰基化，6,7-脱氢，呋喃基化或其它转化或其组合形成这种新型中间体或将其转化为其它中间体或产物的步骤。

    Steroid spirolactonization
    2.
    发明申请
    Steroid spirolactonization 审中-公开
    类固醇spirolactonization

    公开(公告)号：US20060264412A1

    公开(公告)日：2006-11-23

    申请号：US10549819

    申请日：2004-03-22

    申请人： Thaddeus Franczyk II ,  Grace Wagner

    发明人： Thaddeus Franczyk II ,  Grace Wagner

    IPC分类号： A61K31/58 ,  C07J71/00

    CPC分类号： C07J9/00 ,  C07J71/00

    摘要： A steroid comprising a 17-spirolactone or corresponding open lactone structure is obtained by carbonylation of a 17-alkenyl or 17-alkynyl substrate. A 17-alkenyl intermediate may be prepared by semi-hydrogenation of a 17-alkynyl group. Multiple reaction schemes are disclosed for preparation of a 3-keto-9,11-epoxy-17-spirolactone steroid such as eplerenone. Novel intermediates are also disclosed, as well as steps for forming such novel intermediates, or converting them to further intermediates or products, by semi-hydrogenation, carbonylation, 6,7-dehydrogenation, furylation or other transformations or combinations thereof.

    摘要翻译： 通过羰基化17-烯基或17-炔基底物获得包含17-螺内酯或相应的开放内酯结构的类固醇。 17链烯基中间体可以通过17-炔基的半氢化制备。 公开了多种反应方案用于制备3-酮-9,11-环氧-17-螺内酯类固醇如依普利酮。 还公开了新的中间体，以及通过半氢化，羰基化，6,7-脱氢，呋喃基化或其它转化或其组合形成这种新型中间体或将其转化为其它中间体或产物的步骤。