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

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

1975-11-28

1978-02-21

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

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

260283S, 260283CN, 260287CF, 260287K, 260288D, 260288CF, C07D47104, A61K 3153

Patent

active

040753417

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 Riuter et al.

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