Process for preparing ergot derivatives

Details Process for preparing ergot derivatives Process for preparing ergot derivatives

C - Chemistry, Metallurgy

07

D

260/206.7

C07D 457/02 (2006.01)

Patent

CA 1128502

ABSTRACT OF THE DISCLOSURE The present invention relates to a process for making compounds having the formula (I): Image (I) wherein R1 represents a methyl, phenyl, piperidino, 1-pyrroli- dinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' repre- sents an alkyl group having from 1 to 4 carbon atoms, a cyclo- alkyl. group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR" R" I (wherein R" and R"' both represent alkyl groups having from 1 to 4 carbon atoms); R2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, or a phenyl group; R3 represents a fluorine atom, a cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl or sulphonamido group, an alkoxy group having from 1 to 4 carbon atoms, an acyl group having from 2 to 4 carbon atoms, or a benzoyl group; R4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R5 represents a hydrogen atom or a methoxy group; R6 represents a hydrogen or halogen atom or a methyl group; and R7 represents a hydrogen atom or a methyl group. The 2-cyano derivatives are especially preferred. The compounds of the general formula (I) as defined hereinbefore are useful as antihypertensive agents and have moderate to good anti- prolactinic activity, while exhibiting fewer and more reduced side effects as compared with prior art preparations. When compared to the prior art preparations, they exhibit a good therapeutic ratio, the same or lower LD50 and reduced variations of heart rate.

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