发明名称 Process For The Preparation of 7 alpha-Methylsteroids
摘要 The invention relates to a process for the preparation of 7α-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C≡CH; R2 is (CH2)nOH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Grignard reagent CH3MgX, 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 US2010204497(A1) 申请公布日期 2010.08.12
申请号 US20100765629 申请日期 2010.04.22
申请人 N.V. ORGANON 发明人 VAN BUGGENUM PATRICK ARNOLDUS MARIA;STOELWINDER JOHANNES;OSTENDORF MARTIN
分类号 C07J7/00;C07J1/00;C07J5/00;C07J51/00 主分类号 C07J7/00
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