| 摘要 |
There are prepared compounds having good adrenolytic, hypotonic, analgesic, central-sedative and antiserotoninic activity of the formula III <IMAGE> in which R denotes hydrogen or methyl; R1 and R2 in each case denote hydrogen, alkyl having 1 to 3 carbon atoms, methoxy or phenyl; R3 denotes hydrogen, halogen, alkyl or alkoxy having 1 to 3 carbon atoms, phenyl, cyano, nitro, amino, acylamino having 1 to 3 carbon atoms, carboxamido or carbalkoxy having 1 to 3 carbon atoms in the alkoxy group, trifluoromethyl or SO2-Y, where Y is hydroxyl, amino or methyl; and R4 denotes hydrogen or methoxy. These compounds are obtained by reaction of an appropriate 2-aminopyrimidine anion with an appropriate 8- beta -chloro-, bromo-, mesyl- or tosyl-methylergoline derivative. The reaction is carried out in an aprotic solvent, dimethylformamide or dimethyl sulphoxide is preferred. The reaction temperature is preferably 50-110 DEG C. Significantly improved reaction yields are obtained. |
