Studies on Condensed Heterocyclic Compounds (XVI)─Synthesis of 1-Aryl-1, 2, 3-triazolo[4,5-e] pyrimidineone and Piperidine or Azacyclooctane [1,2-b] pyrimidineone Compounds
ZHANG Zi-Yi, LIU Ying, CHEN Mao-Qi, YANG Shi-Yan
1994, 15(12):
1787-1791.
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For the purpose of studying the relationship between molecular structures and biological activies of condensed heterocyclic compounds as a part of our recent progress, a series of new heterocyclic derivatives, 5H-1-aryl-1, 2, 3-triazolo[4, 5-e] pyrimidine-4-one(2a-c), 5-N-methyl-1-aryl-1, 2, 3-triazolo[4, 5-e]pyrimidine-4-one(3a-c), 1-aryl-4-ethoxycarbonyl-5-uramine-1, 2, 3-triazole(4(a, b)), 5H-1-aryl-1, 2, 3-triazolo[4, 5-e] pyrimidine-4, 6-dione( 5(a, b)), 1-aryl-1, 2, 3-triazolo[4, 5-e]piperidine[1, 2-b]pyrimidine-4-one(6a)and 1-aryl-1, 2, 3-triazo-lo[4, 5-e] azacyclooctane[1, 2-b] pyrimidine-4-one (7a), were prepared by treating l-aryl-4-ethyloxycarbonyl-5-amino-1, 2, 3-triazoles 1 with formamide, chlorosulphonyl isocyanate, lactin respectively. The structures of all compounds were confirmed by elemental analysis, IR, 1H NMRand MS. Their antibacterial activities against B. Subtilis, E. coli, E. aerogenes; S. aureus were observed.