发明名称 Process for the synthesis of the hydroxyacetyl side-chain of steroids of the pregnane type, novel 21-hydroxy-20-oxo-17 alpha -pregnane compounds and pharmaceutical preparations containing them
摘要 The present invention relates to a novel general process for synthesizing a alpha - or beta -oriented hydroxyacetyl side chain of steroids of the pregnane type, which comprises treating a corresponding steroid carbaldehyde in succession with formaldehyde dimethylmercaptal-S-oxide in the form of an alkali metal salt thereof, and with a strongly acid hydrolysing agent. Preferred final products are compounds of the formula <IMAGE> (IA) wherein n is 1 or 2, R2 represents methyl or difluoromethyl, and R1 represents hydroxymethyl, methoxymethyl, acetoxymethyl or hydrogen, and, if n is 2 and/or R2 is difluoromethyl, R1 also represents methyl. These compounds act as agonists or antagonists of natural steroid hormones. The antigestagenic 19,21-dihydroxy-17 alpha -pregn-4-ene-3,20-dione and its 6,7-dehydro derivatives and diacetates are of particular interest.
申请公布号 US4424159(A) 申请公布日期 1984.01.03
申请号 US19820345309 申请日期 1982.02.03
申请人 CIBA-GEIGY CORPORATION 发明人 BIOLLAZ, MICHEL
分类号 A61K31/565;C07J1/00;C07J5/00;C07J31/00;C07J33/00;C07J41/00;C07J63/00;(IPC1-7):C07J33/00 主分类号 A61K31/565
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