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
bis(phenylsulfonyl)-1,2,5-oxadiazole-2-oxide,the NO donor,was synthesized by etherealization of thiophenol,oxidation,and then cyclization with an overall yield of 70%. This process is simpler and the yield of product ...bis(phenylsulfonyl)-1,2,5-oxadiazole-2-oxide,the NO donor,was synthesized by etherealization of thiophenol,oxidation,and then cyclization with an overall yield of 70%. This process is simpler and the yield of product is higher than that previously reported.展开更多
Eight 5-substituted-1,3,4-oxadiazole-2-ones were synthesized using substituted benzoic hydrazides as starting materials and triphosgene as cyclization reagent at ambient temperature with high purity and good yields.Th...Eight 5-substituted-1,3,4-oxadiazole-2-ones were synthesized using substituted benzoic hydrazides as starting materials and triphosgene as cyclization reagent at ambient temperature with high purity and good yields.Their structures were characterized by IR,MS,1H NMR and elemental analysis.The salient features of this method included the simple reaction set-ups,safety,short reaction time and high yields of products.展开更多
Acylation of 2-amio-5-aryl-1,3,4-oxadiazoles with acyl chlorides and trichloroacetic acid to afford eleven new -N--[5-aryl-1,3,4-oxadiazol-2-yl]-substituted amides. The required oxadiazole precursors are prepared by o...Acylation of 2-amio-5-aryl-1,3,4-oxadiazoles with acyl chlorides and trichloroacetic acid to afford eleven new -N--[5-aryl-1,3,4-oxadiazol-2-yl]-substituted amides. The required oxadiazole precursors are prepared by oxidative cyclization of corresponding aldehyde semicarbazones. The structures of the synthesized compounds are elucidated by elemental analysis、 1HNMR、IR and MS. They are screened for their larvicidal activities against wild fruit and antibiotic activities.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bis(phenylsulfonyl)-1,2,5-oxadiazole-2-oxide,the NO donor,was synthesized by etherealization of thiophenol,oxidation,and then cyclization with an overall yield of 70%. This process is simpler and the yield of product is higher than that previously reported.
文摘Eight 5-substituted-1,3,4-oxadiazole-2-ones were synthesized using substituted benzoic hydrazides as starting materials and triphosgene as cyclization reagent at ambient temperature with high purity and good yields.Their structures were characterized by IR,MS,1H NMR and elemental analysis.The salient features of this method included the simple reaction set-ups,safety,short reaction time and high yields of products.
文摘Acylation of 2-amio-5-aryl-1,3,4-oxadiazoles with acyl chlorides and trichloroacetic acid to afford eleven new -N--[5-aryl-1,3,4-oxadiazol-2-yl]-substituted amides. The required oxadiazole precursors are prepared by oxidative cyclization of corresponding aldehyde semicarbazones. The structures of the synthesized compounds are elucidated by elemental analysis、 1HNMR、IR and MS. They are screened for their larvicidal activities against wild fruit and antibiotic activities.
