申请人:Gruppo Lepetit S.p.A.
公开号:US04075341A1
公开(公告)日:1978-02-21
A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.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.sub.1 and R.sub.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. New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl. The new compounds and some of the intermediates of the process are active as antiinflammatories, CNS depressants and anti-fertility agents.
一种制备公式为##STR1##的s-三唑并[5,1-a]-异喹啉衍生物的新工艺,其中A代表基团--CH.sub.2 --CH.sub.2 --或--CH.dbd.CH--; R从氢、氨基、低烷基氨基、双低烷基氨基、酰胺基、二酰胺基、脲基、硫脲基、羰基甲氧基硫脲基、苯甲酰硫脲基、巯基、低烷基、三氟甲基、苯基、取代苯基、吡啶基、甲基吡啶基和二甲基吡啶基中选择;R.sub.1和R.sub.2各自独立地代表氢或低烷氧基;通过将2-氨基-3,4-二氢-1(2H)-异喹啉酮与咪唑基、氰胺、氰酸或硫氰酸衍生物缩合而得。公式I中的新化合物,其中A代表基团--CH.sub.2 --CH.sub.2 --或--CH.dbd.CH--,R的含义与上述相同,但不包括氢、甲基、苯基和三氟甲基,R.sub.1和R.sub.2的含义与上述相同,但当A代表基团--CH.dbd.CH--时,R不能是甲苯基或吡啶基。该新化合物和一些工艺中间体具有抗炎、中枢神经系统抑制剂和抗生育活性。