83647-28-3Relevant articles and documents
1,1,2-TRIPHENYLBUT-1-ENE DERIVATIVES
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, (2008/06/13)
Novel (E)-1-[4'-(2-alkylaminoethoxy)phenyl]-1-(3'-hydroxyphenyl)-2-phenylbut-1-enes of the general formula STR1 wherein R 1 and R. sup.2 may be the same or different, provided that, when R 1 and R 2 are the same, each of them is a methyl or ethyl radical, and when R 1 and R 2 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 STR2 wherein R 1 and R 2 may be the same or different, provided that, when R. sup.1 and R 2 are the same, each of them is a methyl or ethyl radical, and when R 1 and R 2 are different, one of them is a benzyl radical and the other is a methyl or ethyl radical; and wherein R 3 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-1-ene derivatives are described also. The corresponding novel 1,1,2-triphenylbut-1-ene derivatives having the (Z) configuration are also disclosed.
