C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
260/602.3
C07C 91/30 (1985.01)
Patent
CA 1207799
- 36 - Abstract of the Disclosure Novel (E)-1-[4'-(2-alkylaminoethoxy)phenyl]-1- (3'-hydroxyphenyl)-2-phenylbut-1-enes of the general formula Image wherein R1 and R2 may be the same or different, provided that, when R1 and R2 are the same, each of them is a methyl or ethyl radical, and when R1 and R2 are different, one of them is hydrogen and the other is a methyl or ethyl radical and the therapeutically compatible salts thereof, have a marked anti-estrogenic effect and are suitable for treating hormone-dependent mammary tumors. The compounds can be prepared by dehydrating carbinols of the general formula Image - 37 - wherein R1 and R2 may be the same or different, provided that, when R1 and R2 are the same, each of them is a methyl or ethyl radical, and when R1 and R2 are different, one of them is a benzyl radical and the other is a methyl or ethyl radical; and wherein R3 is hydrogen or an easily hydrolyzable protecting group, through the action of mineral acid while removing any protecting group present, isolating through crystallization the E-form from the pair of isomers obtained, and removing by hydrogenolysis any benzyl group present. Compositions comprising the subject 1,1,2- triphenylbut-l-ene derivatives are described also. The corresponding novel 1,1,2-triphenylbut-1-ene derivatives having the (Z) configuration are also disclosed.
406804
Grill Helmut
Loser Roland
Schickaneder Helmut
Klinge Pharma G.m.b.h.
Sim & Mcburney
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