发明名称 Process for preparing 17beta-(N-tert-butylcarbonyl)-4-aza-5alph-androst-1-en-3-one
摘要 In the present invention there is disclosed a process for preparing 17beta-(N-tert-butylcarbonyl)-4-aza-5alpha-androst-1-en-3-one of the general formula 2. The invented preparation process is characterized in that (1) ester of the general formula 1, in which R represents alkyl with linear, branched or cyclic chain and containing 1 to 10 carbon atoms, being either unsubstituted or substituted with at least one phenyl radical is brought into contact with tert-butylaminomagnesium halide, whereby molar ratio of the tert-butylaminomagnesium halide to said ester is at least 2:1, in an inert organic solvent and in inert atmosphere, (2) the obtained reaction mixture temperature is maintained at a temperature of at least 10 degC and (3) the resulting butylcarbonyl of the general formula 2 is then isolated.
申请公布号 CZ287842(B6) 申请公布日期 2001.02.14
申请号 CZ19950001268 申请日期 1993.11.05
申请人 MERCK AND CO. 发明人 DOLLING ULF H.;MCCAULEY JAMES A.;VARSOLONA RICHARD J.
分类号 A61K31/58;C07F3/00;C07J73/00;C07J75/00;H04N5/74;(IPC1-7):C07J73/00 主分类号 A61K31/58
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