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medrogestone

机译:麦斯通

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的二羧酸盐的中间体,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。

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