MANUFACTURE OF PREDNISONE DERIVATIVE AND INTERMEDIATE PRODUCT THEREFOR

Japanese Patent JPS60237096

A

A novel process for the preparation of prednisone derivatives of the formula I wherein R1 is alkyl of 1 to 4 carbon atoms and R2 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 8 carbon atoms comprising reacting a compound of the formula II with a reducing agent to obtain a compound of the formula III reacting the latter with a strong base in the presence of copper ions and oxygen to obtain a compound of the formula IV reacting the latter with hydroxylamine to obtain a compound of the formula V in its syn or anti isomeric form or a mixture thereof, reacting the latter with an acylating agent derived from a radical of the formula and with a reducing agent to obtain a compound of the formula VI in its Z or E isomeric form or a mixture thereof, subjecting the latter to treatment with an epoxidizing agent and then a dehydrating agent to obtain a compound of the formula VII reacting the latter with a halogenation agent and subjecting the resulting product to hydrolysis to obtain a compound of the formula VIII wherein Hal is a halogen and reacting the latter with a derivative of an acyl of the formula R1CO- to obtain the compound of formula I which are known compounds.

JIYAN BIYUANDEIA
MISHIERU BIBA

JP1671185A

November 25, 1985

February 01, 1985

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ROUSSEL UCLAF

C07J5/00; C07J7/00; C07J9/00; C07J41/00; C07J43/00; (IPC1-7): C07J7/00; C07J43/00

Motohiro Kurauchi

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