| abstract |
NEW MATERIAL:A compound of formula I [R is H, R 1 CO (R 1 is H, alkyl which may be substituted, aryl which may be substituted), R 2 SO 2 (R 2 is alkyl)]. n EXAMPLE: 12α-Hydroxypregna-1,4-diene-3,20-dione. n USE: Synthetic intermediate of corticoid, an antiinflammatory. n PREPARATION: 12α-Hydroxypregna-1,4-diene-3-one-20-carbaldehyde of formula IIis acylated with a carboxylic acid of formula: R 1 COOH or its reactive derivative to give 12α-acyloxypregna-1,4-diene-3-one-20-carbaldehyde of formula III. The product is allowed to react with a secondary amine such as piperidine to form an enamine of formula IV, which is oxidized with ozone to give a compound of formula I where R is R 1 CO. n COPYRIGHT: (C)1984,JPO&Japio |