发明名称 PROCESS FOR THE PRODUCTION OF 17ALPHA-ETHINYL-17BETA-HYDROXY-18-METHYL-4,15-ESTRADIEN-3-ONE AND NEW INTERMEDIATE PRODUCTS FOR THIS PROCESS
摘要 A process for the production of 17?-ethinyl-17?-hydroxy-18-methyl-4,15-estradien-3-one is described comprising reacting a 17-enolester of formula II II. wherein R1 represents an alkyl radical with 1-3 carbon atoms and R2 represents an acyl or a trialkylsilyl group with 1-10 carbon atoms under palladium catalysis, with compounds of formula III III, wherein R1 represents an alkyl radical with 1-3 carbons atoms, reducing the 17-keto group to the 17-hydroxy group in a manner known in the art, reducing the aromatic A-ring according to Birch, with liquid ammonia, to 3-methoxy-2,5(10),15-estratrien-17.beta.;-ol, reoxidizing the 17-hydroxy group to the 17-keto group, ethinylating the 17-keto group and splitting off the 3-enolether to form 17?ethinyl-17.beta.-hydroxy-18-methyl-4,15-estradiene-3-one.
申请公布号 CA1306993(C) 申请公布日期 1992.09.01
申请号 CA19880562962 申请日期 1988.03.30
申请人 BOHLMANN, ROLF 发明人 BOHLMANN, ROLF;LAURENT, HENRY;HOFMEISTER, HELMUT;WIECHERT, RUDOLF
分类号 A61K31/565;C07J1/00;C07J13/00;C07J75/00 主分类号 A61K31/565
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