Collect. Czech. Chem. Commun. 1979, 44, 3385-3390

Some 6-alkyl derivatives of D-8-ergolin-I-ylacetamide

Miloš Beran, Jiří Křepelka and Miroslav Semonský

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


D-6-Alkyl-8-cyanomethylergolines-I were converted either by known procedures via the corresponding methyl esters I-III and hydrazides IV-VI to amides VII-IX, or by hydration of the nitrile group under the conditions of ionic pair extraction to amides VIII and X-XIII. In the same system D-6-methyl-8-ergolin-I-ylacetamide (DeprenonR) was prepared from D-6-methyl-8-cyanomethylergoline-I. Amides VII, VIII and XI had a considerably higher prolactin inhibiting activity than Deprenon.