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. |