1-(mono and bis tertiary amino-4-hydroxy-monocarbocyclic aryl)-1-(monocarbocyclic aryl)-2-(monocarbocyclic aryl)-ethanes, ethylenes and ethanols

摘要

Novel compounds of Formula I FORM:1033920/C2/1 where Z is an ethanol radical FORM:1033920/C2/2 X is a Mannich group of formula R3R4N-CN2-wher R3 and R4 are aliphatic radicals containing 1-5 carbon atoms or R3 and R4 together form a heterocyclic ring, Y is hydrogen or X, and R1 and R2 are hydrogen, alkyl, alkoxy, halogen or trifluoromethyl, are prepared (1) by reacting a benzyl magnesium halide with a benzophenone of Formula II FORM:1033920/C2/3 or (2) by reacting a compound of Formula III FORM:1033920/C2/4 with formaldehyde and an amine of formula R3R4NH. Therapeutic compositions which have anti-inflammatory, pituitary gonadotrophin inhibiting, estrogenic and blood cholesterol level decreasing activity, and which may be administered orally, parenterally or topically, contain as active ingredient compounds of Formula I above. The benzophenone starting materials of Formula II may be prepared by reacting a benzophenone of Formula II in which X and Y are hydrogen with the appropriate amine and formaldehyde. The hydroxy group may further be acylated, the acyl group being removed during the reaction of the benzophenone with the Grignard reagent. The triphenylethanol starting materials of Formula III may be prepared by reacting a benzophenone with a benzylmagnesium halide.