abstract |
A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH 2 --CH 2 -- or --CH═CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R 1 and R 2 each independently represents hydrogen or lower alkoxy, by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative. n New compounds of the formula I wherein A represents the group --CH 2 --CH 2 -- or --CH═CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R 1 and R 2 have the same meaning as above, with the proviso that when A represents the group --CH═CH--, R cannot be tolyl or pyridyl. n The new compounds and some of the intermediates of the process are active as antiinflammatories, CNS depressants and anti-fertility agents. |