发明名称 PROCESS FOR THE PREPARATION OF 7A-METHYLSTEROIDS
摘要 The invention relates to a process for the preparation of 7alpha-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C≡CH; R2 is (CH<SUB>2</SUB>)<SUB>n</SUB>OH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Grignard reagent CH<SUB>3</SUB>MgX, X being a halogen, to the 4,6-unsaturated 3-ketosteroid of formula II, wherein R1 and R2 are as previously defined, comprising protecting the hydroxy group of the steroid of formula II with a trialkylsilyl group, followed by treating the hydroxy protected steroid with the Grignard reagent. The process of the invention is useful for the production of pharmacologically interesting steroids.
申请公布号 ZA200405257(B) 申请公布日期 2005.08.31
申请号 ZA20040005257 申请日期 2004.07.01
申请人 MERCK SHARP & DOHME B.V. 发明人 J STOELWINDER;P.A.M. VAN BUGGENUM;M OSTENDORF
分类号 C07J;C07J1/00;C07J5/00;C07J7/00;C07J51/00 主分类号 C07J
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