Erythro-1,2-1-pentanones

US4764533A · kind A · utility

Assignee

• Klinge Pharma GmbH · DE

Inventors

• Helmut Schickaneder · Eckental, DE
• Roland Loser · Feldafing, DE

Key dates

• Filing date: Jul 2, 1984
• Grant date: Aug 16, 1988
• Expiry date: Jul 2, 2004

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P35/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

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.