METHOD FOR PREPARING β-SUBSTITUTED 4-AZAANDROSTENE Russian patent published in 1998 - IPC

FIELD: chemical industry. SUBSTANCE: present invention describes β-substituted 4-azaandrostene derivatives of general formula I: wherein R is hydrogen or C_1-3 alkyl; R¹ is carboxamide group, mono- or disubstituted by C_1-8 alkyl group(s); or free carboxy group etherified by C_1-15 alcohol; and is single or double bond. Present invention also describes preparation of salts of said compounds. Method comprises reacting 17-halogen-4- azaandrostene of general formula (II): wherein R and are defined as above, and X is chlorine, bromine or iodine, with primary or secondary alkyl amine or with C_1-5 alcohol in dimethylformamide or dimethylsulfoxide in the presence of palladium (II) salt and phosphines or palladium (II)-base complex as tertiary amine under carbon monoxide atmosphere at 35-80 C and, if desired, converting the resulting compound of general formula I into the other compound of general formula I by hydrogenation, hydrolysis or salt-forming reactions. EFFECT: more efficient preparation method.