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. |