Pyridyl substituted ergoline derivatives

Details Pyridyl substituted ergoline derivatives Pyridyl substituted ergoline derivatives

1977-01-04

1978-05-16

Daus, Donald G.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424261, C07D45702

Patent

active

040898628

ABSTRACT:
A process is disclosed for the preparation of a compound of the formula I ##STR1## where R is hydrogen or methyl, X is sulphur or the NH group, Y is selected from the class consisting of methyl, methoxy, chlorine, bromine, iodine, nitro or cyano, m is 0, 1 or 2, and n is 1 or 2, characterized in that a compound of the formula II: ##STR2## where R and n have the above-mentioned meanings, is reacted in a suitable polar aprotic solvent, such as dimethylforamide or dimethylsulphoxide, under a nitrogen atmosphere and at a temperature between 50.degree. and 100.degree. C, with the sodium salt of an appropriate 2-aminopyridine or 2-mercaptopyridine to give, after evaporation of the solvent in vacuo, the desired compound of formula I which is then purified by methods known "per se".
The invention also includes the compounds of general formula I, where R, X, Y, m and n have the same meanings, and their pharmaceutically acceptable salts. These compounds have good alpha-adrenoyltic activity, and especially a very high and unexpected platelets aggregating inhibiting activity compared to e.g. nicergoline.

REFERENCES:
patent: 3014909 (1961-12-01), Rutschmann et al.
patent: 3833585 (1974-09-01), Stadler et al.
patent: 3901891 (1975-08-01), Kornfeld et al.
patent: 3996228 (1976-12-01), Arcari et al.
patent: 4004011 (1977-01-01), Hauth et al.

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