Inventors:
Mark D. Hylarides - Albuquerque NM
Fred A. Mettler - Albuquerque NM
Assignee:
The University of New Mexico - Albuquerque NM
International Classification:
C07J 100
Abstract:
Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-position. Preferred starting materials include estrones or derivatives thereof. The estrones are preferably reduced after masking and amination to form the corresponding estradiols, which are then halogenated, deaminated and deprotected to provide the novel 1-haloestradiols.