Isoxazole derivatives were characterized by broad spectrum of biological activities, but the condensed heterocyclic compounds containing isoxazole were scarcely reported. In this paper, we studied the 1,3-dipolar cycl...Isoxazole derivatives were characterized by broad spectrum of biological activities, but the condensed heterocyclic compounds containing isoxazole were scarcely reported. In this paper, we studied the 1,3-dipolar cycloaddition of p-methoxybenzohydroxamoyl chloride with ethyl sodioacetoacetate to obtain a key intermediate 2. Through compound 2, fifteen novel S-triazolo-1,3,4-thiadiazines(5a-5e), imidazolo-1,3,4-thiadiazoles(9a-9e) and imidazolo-1,3,4-oxadiazoles(10a-10e) containing isoxazole, which have potentially useful biological activities, were synthesized. The structures of the products were confirmed by elemental analyses and spectral analysis. And the characteristic data of IR, 1H NMR and MS were explained reasonably.展开更多
Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested an...Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested and compared. The title compounds Schiff bases, amides,imidazolo[2,1-b]-1,3,4-thiadiazoles and 7H-s-triazolo [3,4-b]-1,3,4-thiadiazines have been confirmedby elemental analyses, ~1H NMR, IR and MS spectra. All the compounds have also been screened fortheir antibacterial activities against B. subtilis, S. aureus and E. coli.展开更多
文摘Isoxazole derivatives were characterized by broad spectrum of biological activities, but the condensed heterocyclic compounds containing isoxazole were scarcely reported. In this paper, we studied the 1,3-dipolar cycloaddition of p-methoxybenzohydroxamoyl chloride with ethyl sodioacetoacetate to obtain a key intermediate 2. Through compound 2, fifteen novel S-triazolo-1,3,4-thiadiazines(5a-5e), imidazolo-1,3,4-thiadiazoles(9a-9e) and imidazolo-1,3,4-oxadiazoles(10a-10e) containing isoxazole, which have potentially useful biological activities, were synthesized. The structures of the products were confirmed by elemental analyses and spectral analysis. And the characteristic data of IR, 1H NMR and MS were explained reasonably.
文摘Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested and compared. The title compounds Schiff bases, amides,imidazolo[2,1-b]-1,3,4-thiadiazoles and 7H-s-triazolo [3,4-b]-1,3,4-thiadiazines have been confirmedby elemental analyses, ~1H NMR, IR and MS spectra. All the compounds have also been screened fortheir antibacterial activities against B. subtilis, S. aureus and E. coli.
