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6 beta - hydroxy 6 alpha, 17 alpha dimethylpregn - 4 - ene - 3.10 - dion, as inhibitors of the proliferation of smooth muscle cells

机译:6β-羟基6α,17α-二甲基-戊烯-4-烯-3.10-dion,作为平滑肌细胞增殖的抑制剂

摘要

A process for the production of medrogestone, in which, in an intermediate step, the solvate 3 beta ,5 alpha ,6 beta -trihydroxy-6 alpha ,17 alpha -dimethylpregnan-20-one monomethanolate is obtained as a solid, stable compound by displacing the organic solvent from a solution of of 3 beta ,5 alpha ,6 beta -trihydroxy-6 alpha ,17 alpha -dimethylpregnan-20-one with a lower alkanol, and a Diels-Alder adduct of 6-methylene-17 alpha -methylpregn-4-ene-3,20-dione with maleic anhydride is used as an intermediate for production of the corresponding dicarboxylic acid salt for removal of 6-methylene-17 alpha -methylpregn-4-ene-3,20-dione contamination of the desired product. Another intermediate, 6 beta -hydroxy-6 alpha ,17 alpha -dimethylpregn-4-ene-3,20-dione, has been found to prevent smooth muscle proliferation and is useful in the treatment of atherosclerosis and restinosis.
机译:制备甲磺晶的方法,其中在中间步骤中,通过以下方法获得固体,稳定化合物的溶剂化物3β,5α,6β-三羟基-6α,17α-二甲基戊二醇20-一甲酸酯。将3β,5α,6β-三羟基-6α,17α-二甲基pregnan-20-one与低级烷醇和Diels-Alder加成物的6-亚甲基-17α-取代有机溶剂-带有马来酸酐的甲基pregn-4-ene-3,20-二酮用作生产相应二羧酸盐的中间体,用于去除6-亚甲基-17α-甲基pregn-4-ene-3,20-二酮污染所需的产品。已经发现另一种中间体6-β-羟基-6α,17α-二甲基孕烯-4-烯-3,20-二酮可防止平滑肌增殖,并且可用于治疗动脉粥样硬化和再狭窄。

著录项

  • 公开/公告号DE69533178D1

    专利类型

  • 公开/公告日2004-07-22

    原文格式PDF

  • 申请/专利权人 WYETH MADISON;

    申请/专利号DE19956033178T

  • 申请日1995-04-28

  • 分类号A61K31/57;A61P9/10;

  • 国家 DE

  • 入库时间 2022-08-21 22:41:06

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