发明名称 |
PROCESS FOR THE PREPARATION OF 17-ALPHA-ETHYNYL-17-BETA-HYDROXY-18-METHYL-4,15-ESTRADIEN-3-ONE, AND INTERMEDIATES FOR THIS PROCESS |
摘要 |
1. Process for the manufacture of 17 alpha-ethynyl-17 beta-hydroxy-18-methyl-4,15-estradien- 3-one of the formula I see diagramm : EP0285548,P6,F1 characterised in that a 17-enol ester of the general formula II see diagramm : EP0285548,P6,F2 wherein R1 represents an alkyl radical having 1-3 carbon atoms and R2 represents an acyl or a trialkylsilyl group having up to 10 carbon atoms, is reacted with palladium catalysis to form compounds of the general formula III see diagramm : EP0285548,P6,F3 wherein R1 represents an alkyl radical having 1-3 carbon atoms, and, in a manner known per se, the 17-keto group is reduced, the aromatic A-ring is reacted by the Birch reaction with liquid ammonia to form the corresponding 3-alkoxy-2,5(10),15-estratrien-17 beta-ol, the 17-hydroxy group is reoxidised to the 17-keto group, the 17-keto group is ethynylated and the 3-enol ether is cleaved.
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申请公布号 |
EP0285548(B1) |
申请公布日期 |
1990.09.05 |
申请号 |
EP19880730075 |
申请日期 |
1988.03.25 |
申请人 |
SCHERING AKTIENGESELLSCHAFT BERLIN UND BERGKAMEN |
发明人 |
BOHLMANN, ROLF, DR.;LAURENT, HENRY, DR.;HOFMEISTER, HELMUT, DR.;WIECHERT, RUDOLF, PROF. DR. |
分类号 |
A61K31/565;C07J1/00;C07J13/00;C07J75/00 |
主分类号 |
A61K31/565 |
代理机构 |
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代理人 |
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