发明名称 2-Oxa-5beta-cyanpregnane,Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneipraeparaten
摘要 1277754 5-Cyano-2-oxa- and -A-nor-steroids E R SQUIBB & SONS Inc 2 June 1969 [19 June 1968] 27732/69 Heading C2C The invention comprises compounds of Formulae I and II wherein R is H, R<SP>1</SP> is OH, OCOCF 3 or C 1-12 hydrocarbon carboxylic acyloxy, or R and R<SP>1</SP> together represent oxo, and R<SP>11</SP> is OH, OCOCF 3 or C 1-12 hydrocarbon carboxylic acyloxy. Compounds I (R<SP>1</SP> = OCOCF 3 or acyloxy) are prepared from compounds II by reaction with a peracid (e.g. peroxytrifluoroacetic acid) and are convertible by hydrolysis and oxidation into other compounds I. Compound II (R<SP>11</SP> = OH) is prepared by reacting 20#-hydroxy-A-norpregn- 3-en-2-one with KCN and is convertible by esterification into other compounds II. 20#-Hydroxy-A -norpregn-3-en-2-one is prepared by reduction of A-norprogesterone with NaBH 4 or KBH 4 . Compounds I are said to possess antiandro. genie activity and may be made up into pharmaceutical compositions for oral and parenteral administration.
申请公布号 DE1929220(A1) 申请公布日期 1970.01.08
申请号 DE19691929220 申请日期 1969.06.10
申请人 E.R. SQUIBB & SONS INC. 发明人 D. LEVINE,SEYMOUR
分类号 C07J61/00;C07J73/00 主分类号 C07J61/00
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