Some 6-substituted 1-[(5R,8S,10R)-8-ergolinyl]-3,3-diethylureas

Abstract

6-Substituted 1-[(5R,8S,10R)-8-ergolinyl]-3,3-diethylureas II-VII were prepared from hydrazides of (5R,8S,10R)-6-alkyl-8-ergolinecarboxylic acids (VIIIa, VIIIb) via the corresponding azides IXa and IXb and isocyanates Xa and Xb, and/or from 1-[(5R,8S,10R)-6-methyl-8-ergolinyl]-3,3-diethylurea (I) via XI and XII. Two of the by-products arising in the latter route have been identified (XIII, XIV). Some of the ureas prepared, especially II and III, had strong inhibitory effects in vivo on the secretion of prolactin in rats.