Process for preparing ergoline derivatives

Details Process for preparing ergoline derivatives Process for preparing ergoline derivatives

C - Chemistry, Metallurgy

07

D

260/206.7

C07D 457/02 (2006.01)

Patent

CA 1101848

ABSTRACT OF THE DISCLOSURE This invention relates to a new process for preparing new ergoline derivatives of the general formula (I) Image (I) wherein R1 is hydrogen or methoxy; R2 is hydrogen or methyl; and X is hydroxy, R3COO, S-R4 or NR5R6 in which R3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle; R4 is phenyl or a heterocycle, and R5 and R6 are alkyl having from 1 to 4 carbon atoms, or together with the n atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH2 and COOH. These compounds possess a strong anti-prolactin activity in rats and a low emetic activity in dogs. Prolactin is considered to be the only hypophysical hormone involved in the maintenance of the first part of pregnancy in rats. They exhibit marked increase in activity over prior art preparation yet exhibit good tolerances.

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