Process

Details Process Process

1984-05-21

1986-01-21

Brust, Joseph Paul

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

260464, C07D20956

Patent

active

045658765

ABSTRACT:
A novel process for the preparation of a 16-imino-17-aza-steroid of the formula ##STR1## wherein A is selected from the group consisting of hydrogen and tritium comprising reacting a compound of the formula ##STR2## wherein A has the above definition and R is an acyl of an organic carboxylic acid of 1 to 8 carbon atoms with an oximation agent to obtain a compound of the formula ##STR3## reacting the latter with an agent to form an acid chloride to obtain a compound of the formula ##STR4## reacting the latter with ammonia to obtain a compound of the formula ##STR5## reacting the latter with an alkali metal hypohalite in the presence of a base to obtain a compound of the formula ##STR6## wherein X is a halogen and reacting the latter with a base to obtain the desired compound and the novel compound of formula I wherein A is tritium and the novel intermediates of formulae III, IV, V and VI.

REFERENCES:
patent: 3257412 (1966-06-01), Baran
patent: 3317557 (1967-05-01), Kierstead
patent: 3539588 (1970-11-01), Sallay
patent: 3634419 (1972-01-01), Nelson
patent: 3658880 (1972-04-01), Nelson
Hunt, et al.; Neuropharmacology, 20, pp. 357-361, (1981).

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