Process for the preparation of ergoline derivatives

US4748248A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Gerhard Sauer · Berlin, DE
• Gregor Haffer · Berlin, DE

Key dates

• Filing date: Dec 13, 1985
• Grant date: May 31, 1988
• Expiry date: Dec 13, 2005

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D457/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A process for preparing an ergoline of the formula ##STR1## wherein C.sub.9 ----C.sub.10 is a CC single or double bond, PA1 R.sup.1 is hydrogen or CONR.sub.2, R being hydrogen, methyl, or ethyl, and wherein NR' is in the .alpha.- or .beta.- position, PA1 R.sup.2 is lower alkyl of up to 3 carbon atoms, and the salts thereof, comprises treating the corresponding ergolinyl carboxylic acid amide with lead(IV) acetate in an aprotic polar solvent; reacting the intermediarily formed corresponding isocyanate with water or with a reactive amine of up to 4 carbon atoms, (e.g. a mono- or dialkylamine of up to 4-C atoms); and, optionally, treating the resultant product with an acid to form the corresponding salt.