2-Substituted phenyl-s-triazolo[5,1-a] isoquinoline compounds

Details 2-Substituted phenyl-s-triazolo[5,1-a] isoquinoline compounds 2-Substituted phenyl-s-triazolo[5,1-a] isoquinoline compounds

1979-04-23

1980-12-23

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

546 82, C01D47104, A61K 3153

Patent

active

RE0304565

ABSTRACT:
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.

REFERENCES:
patent: 2976146 (1961-03-01), Salminen et al.
patent: 3652570 (1972-03-01), Gittos et al.
patent: 3758480 (1973-09-01), Reimlinger et al.
patent: 3775417 (1973-11-01), de Ruiter et al.

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