- Cu(II)-Catalyzed C-H Amidation/Cyclization of Azomethine Imines with Dioxazolones via Acyl Nitrenes: A Direct Access to Diverse 1,2,4-Triazole Derivatives
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We report a Cu(II)-catalyzed C-H amidation/cyclization of azomethine imines with dioxazolones as acyl nitrene transfer reagents under additive-and ligand-free conditions. An array of 1,2,4-triazolo[1,5-a]pyridine derivatives were afforded in moderate to good yields with excellent functional group tolerance. In addition, scale-up reaction and photoluminescence properties were discussed.
- Liu, Xiang,Li, Wen,Jiang, Wenxuan,Lu, Hao,Liu, Jiali,Lin, Yijun,Cao, Hua
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p. 613 - 618
(2022/01/20)
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- 2-Substituted phenyl-s-triazolo[5,1-a] isoquinoline compounds
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A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula STR1 wherein A represents the group --CH2 --CH2 -- 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 R1 and R2 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 --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 antiinflammatories, CNS depressants and anti-fertility agents.
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- 2-Substituted phenyl-5-triazols [5,1-a] isoquinoline compounds
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A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula STR1 wherein A represents the group --CH2 --CH2 -- 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 R1 and R2 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 --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 antiinflammatories, CNS depressants and anti-fertility agents.
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