1,1,2-triphenylbut-1-ene derivatives

Details 1,1,2-triphenylbut-1-ene derivatives 1,1,2-triphenylbut-1-ene derivatives

1990-05-14

1991-09-10

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514874, 564324, A61K 31135, C07C21720

Patent

active

050474316

ABSTRACT:
Novel (E)-1-[4'-(2-alkylaminoethoxy)phenyl]-1- (3'-hydroxyphenyl)-2-phenylbut-1-enes of the general formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different, provided that, when R.sup.1 and R.sup.2 are the same, each of them is a methyl or ethyl radical, and when R.sup.1 and R.sup.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.sup.1 and R.sup.2 may be the same or different, provided that, when R.sup.1 and R.sup.2 are the same, each of them is a methyl or ethyl radical, and when R.sup.1 and R.sup.2 are different, one of them is a benzyl radical and the other is a methyl or ethyl radical; and wherein R.sup.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.

REFERENCES:
patent: 3288806 (1966-11-01), De Wald
patent: 3341537 (1967-09-01), Richardson
patent: 4198435 (1980-04-01), Richardson
patent: 4206234 (1980-06-01), Richardson
patent: 4536516 (1985-08-01), Harper et al.
patent: 4623660 (1986-11-01), Richardson
March, Advanced Organic Chemistry, 2nd Ed., McGraw-Hill Book Company, (1977), pp. 99-101 and 113 to 115.
Wagner et al., "Synthetic Organic Chemistry", pp. 171-172 (1963).

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