Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1984-07-02
1988-08-16
Hines, Robert V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
546236, 546237, 548575, 564354, C07C 9306, A61K 35135
Patent
active
047645334
ABSTRACT:
Erythro-1,2,3-triphenyl-1-pentanones of Formula 1 ##STR1## wherein R.sup.1 may be a dimethylamino, diethylamino, piperidin-1-yl- or pyrrolidin-1-yl group and R.sup.2 represents a hydrogen atom, a methoxy or hydroxy group, and their pharmacologically acceptable salts, have a pronounced antiestrogenic effect and are suitable for the treatment of hormone-dependent tumors.
They may be prepared by reacting 1,2-diphenyl-ethanone of Formula 2 ##STR2## wherein R.sup.1 is as set forth in Formula 1 and R.sup.2 represents a hydrogen atom or a methoxy group, with sodium hydride in anhydrous dimethyl-formamide, isolating after conversion with 1-chloro-1-phenylpropane, the erythro form from the reaction product and possibly releasing the hydroxy group from the methoxy group by selective cleavage with hydrobromic acid.
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Loser Roland
Schickaneder Helmut
Hines Robert V.
Klinge Pharma GmbH
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