首页> 外国专利> PROCESS FOR THE PRODUCTION OF 17.alpha.-ETHINYL-17.beta.-HYDROXY-18-METHYL-4,15-ESTRADIEN-3-ONE AND NEW INTERMEDIATE PRODUCTS FOR THIS PROCESS

PROCESS FOR THE PRODUCTION OF 17.alpha.-ETHINYL-17.beta.-HYDROXY-18-METHYL-4,15-ESTRADIEN-3-ONE AND NEW INTERMEDIATE PRODUCTS FOR THIS PROCESS

机译:生产17.alpha.-亚乙基-17.beta.-羟基-18-甲基-4,15-estradiien-3-one的方法和新的中间产品

摘要

ABSTRACT OF THE DISCLOSUREA process for the production of 17?-ethinyl-17?-hydroxy-18-methyl-4,15-estradien-3-one is describedcomprising reacting a 17-enolester of formula II II.whereinR1 represents an alkyl radical with 1-3 carbon atoms andR2 represents an acyl or a trialkylsilyl group with 1-10carbon atomsunder palladium catalysis, with compounds of formula III III,whereinR1 represents an alkyl radical with 1-3 carbons atoms,reducing the 17-keto group to the 17-hydroxy group in amanner known in the art, reducing the aromatic A-ringaccording to Birch, with liquid ammonia, to 3-methoxy-2,5(10),15-estratrien-17.beta.;-ol, reoxidizing the 17-hydroxygroup to the 17-keto group, ethinylating the 17-ketogroup and splitting off the 3-enolether to form 17?-ethinyl-17.beta.-hydroxy-18-methyl-4,15-estradiene-3-one.
机译:披露摘要生产17′-乙炔基17′-的方法描述了羟基-18-甲基-4,15-雌二醇-3-一个包括使式II的17-烯酸酯反应 二。其中R 1表示具有1-3个碳原子的烷基R 2代表具有1-10的酰基或三烷基甲硅烷基碳原子在钯催化下,与式Ⅲ化合物 III,其中R1代表具有1-3个碳原子的烷基将17-酮基还原为17-羟基本领域已知的方式,减少芳族A环根据伯奇(Birch)的说法,是用液态氨将水转化为3-甲氧基2,5(10),15-雌三烯-17.-ol,重新氧化17-羟基组到17-酮基团,将17-酮基乙炔化组并分裂3-烯键形成17?-乙炔基17β-羟基-18-甲基-4,15-雌二醇-3-一个。

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