含有异噁唑的S-三唑[3,4-b]-1,3,4-噻二嗪、咪唑[2,1-b]-1,3,4-噻二唑和咪唑[2,1-b]-1,3,4-噁二唑衍生物的合成

异噁唑衍生物作为一类重要的生物活性物质，其合成一直受到人们的关注，其中德国HMR公司开发研制的新型抗内风湿性关节炎药来氟米特(Leftunomide)已于1998年在美国率先上市，该药还具有很好的免疫调节作用．7H-均三唑3，4-b]-1，3，4-噻二嗪、咪唑并2，1-b]噻唑和咪唑并2，1-b]-1，3，4-噻二唑衍生物均表现出广谱的生物活性．

Synthesis of S-Triazolo-1,3,4-thiadiazine, Imidazolo- 1,3,4-thiadiazole and Imidazolo-1,3,4-oxadiazole Derivatives Containing Isoxazole

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.