Process for the production of prednisone 17.21-diacylates

Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal

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2603973, C07J 2100

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active

046018549

ABSTRACT:
A novel process for the preparation of prednisone derivatives of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of hydrogen and hydrocarbon of 1 to 8 carbon atoms comprising reacting a compound of the formula ##STR2## with a reducing agent to obtain a compound of the formula ##STR3## reacting the latter with a strong base in the presence of copper ions and oxygen to obtain a compound of the formula ##STR4## reacting the latter with hydroxylamine to obtain a compound of the formula ##STR5## 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 ##STR6## and with a reducing agent to obtain a compound of the formula ##STR7## 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 ##STR8## reacting the latter with a halogenation agent and subjecting the resulting product to hydrolysis to obtain a compound of the formula ##STR9## wherein Hal is a halogen and reacting the latter with a derivative of an acyl of the formula R.sub.1 CO-- to obtain the compound of formula I which are known compounds.

REFERENCES:
patent: 4267106 (1981-05-01), Marx et al.
patent: 4328221 (1982-05-01), Farago et al.

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