A simple and high yielding method for the integration of 1,5-benzodiazepines integrated with 5-methyl- 2-oxo-3-phenyl-△^4-1,3,4-oxadiazolines in 75%-90% yield by microwave irradiation is devised. Microwave-accelerate...A simple and high yielding method for the integration of 1,5-benzodiazepines integrated with 5-methyl- 2-oxo-3-phenyl-△^4-1,3,4-oxadiazolines in 75%-90% yield by microwave irradiation is devised. Microwave-accelerated reaction was compared with thermal method. All the compounds were characterized by physical, analytical and spectral （IR, 1^H NMR, MS） data. Title compounds were screened for preliminary pharmacological activities.展开更多
In search of novel herbicides with high activity, a series of 2-arylthio-1, 2, 4-triazolo[1,5-a] pyrimidines (3) were synthesized by cyclization of 5-amino-3-arylthio-1,2,4-triazoles with 1,3-diketones or by the nucle...In search of novel herbicides with high activity, a series of 2-arylthio-1, 2, 4-triazolo[1,5-a] pyrimidines (3) were synthesized by cyclization of 5-amino-3-arylthio-1,2,4-triazoles with 1,3-diketones or by the nucleophilic substitution of substituted thiophenols with 2-methylsulfonyl-1, 2, 4-triazolo [1, 5-a]-pyrimidine. The structures of all compounds prepared were confirmed by H-1 NMR and MS spectroscopy along with elemental analyses. Preliminary bioassays indicated that some of the compounds 3 had good herbicidal activity against rape. In addition, the regioselectivity in the reaction of 5-amino-3-substituted arylthio-1,2, 4-triazoles with benzoylacetone was studied.展开更多
文摘A simple and high yielding method for the integration of 1,5-benzodiazepines integrated with 5-methyl- 2-oxo-3-phenyl-△^4-1,3,4-oxadiazolines in 75%-90% yield by microwave irradiation is devised. Microwave-accelerated reaction was compared with thermal method. All the compounds were characterized by physical, analytical and spectral （IR, 1^H NMR, MS） data. Title compounds were screened for preliminary pharmacological activities.
基金Project Supported by the National Natural Science Foundation of China (No: 29802002), the Natural Science Foundation of Hubei Province and the Dawn Plan of Science and Technology for Young Scientists of Wuhan City.
文摘In search of novel herbicides with high activity, a series of 2-arylthio-1, 2, 4-triazolo[1,5-a] pyrimidines (3) were synthesized by cyclization of 5-amino-3-arylthio-1,2,4-triazoles with 1,3-diketones or by the nucleophilic substitution of substituted thiophenols with 2-methylsulfonyl-1, 2, 4-triazolo [1, 5-a]-pyrimidine. The structures of all compounds prepared were confirmed by H-1 NMR and MS spectroscopy along with elemental analyses. Preliminary bioassays indicated that some of the compounds 3 had good herbicidal activity against rape. In addition, the regioselectivity in the reaction of 5-amino-3-substituted arylthio-1,2, 4-triazoles with benzoylacetone was studied.
