Triazolo isoquinoline derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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260/271.3

C07D 471/04 (2006.01) C07D 209/46 (2006.01) C07D 217/24 (2006.01)

Patent

CA 1044237

Abstract of the Disclosure A new process for preparing s-triazolo[5,1-a]isoquinoline derivatives of the formula Image wherein A represents the group -CH2-CH2- or -CH=CH-; R is selected from hydrogen, amino, lower alkyl amino, di-lower alkyl amino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl pyridyl, methylpyridyl and dimethylpyridyl; R1 and R2 each independently represent hydrogen or lower alkoxy by condensation of 2-amino-3,4-dihydro-1(2H)-isoquinolinones with imidalyl, cyanamide, cyanic and thiocyanic derivatives. New compounds of the formula I wherein A represents the group -CH2-CH2- or -CH=CH-, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R1 and R2 have the same meaning as above, with the proviso that when A represents the group -CH=CH- R cannot be tolyl or pyridyl. The new compounds and some of the intermediates of the process are active as antinflammatories, CNS depressants and anti-fertility agents.

200726

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