ABSTRACT
The potential for compounds with antifertility activity from the reactions of diphenylcyclopropernone (1) and 2, 3-diphenylthiirene 1, 1-dioxide (2) with enamines is described. In certain instances, a marked dissociation of antifertility from estrogenic activity was possible. Two series were studied extensively, one was stilbene amides (7) and the other stilbene amino ketones (8). The latter series (8) afforded several materials from which, on further biological work-up, was singled out compound 21 as a potent antifertility agent in rats and hamsters.
PIP: The antifertility activity from the reactions of diphenylcyclopropene (1) and 2,3-diphenylthiirene 1,1 dioxide (2) with enamines was investigated in laboratory rodents. A considerable dissociation of antifertility from estrogenic activity was observed in certain instances. Stilbene amides (7) and stilbene aminoketones (8) we re extensively studied. The stilbene aminoketone group provided several materials of which compound 21 was found to be a highly potent antifertility agent. The preparation of the materials is described.
