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以3,5-二取代异噁唑-4-甲酰肼为基本原料制备关键中间体1-(3-对甲氧基苯基-5-甲基异噁唑-4-基)-4-芳基氨基硫脲(3a～3c);3在不同条件下经关环反应制得含有3,5-二取代异噁唑的2-芳氨基噻二唑(4a～4c),2-芳氨基噁二唑(5a～5c)和3-[3’-(4″-甲氧基苯基)-5’-甲基-异噁唑-4’-基)-4-芳基-1,2,4-三唑-5-硫酮(6a～6c);6与碘甲(乙)烷反应合成了4-芳基-5-[3’-(4″-甲氧基苯基)-5’-甲基异噁唑-4’-基]-3-甲(乙)硫基-1,2,4-三唑(7a～8c),其结构经1H NMR,IR,MS和元素分析表征,其中4,5,7和8未见文献报道。
The key intermediate 1- (3-p-methoxyphenyl-5-methylisoxazol-4-yl) -4- Arylaminothioureas (3a ~ 3c); 3 2-arylaminothiadiazoles (4a ~ 4c) containing 3,5-disubstituted isoxazoles were prepared by ring closure reaction under different conditions, Oxadiazoles (5a-5c) and 3- [3 ’- (4 “-methoxyphenyl) -5’- methyl- isoxazol- 4’- yl) -4-aryl- 1, 2 4-triazole-5-thione (6a ~ 6c); 4-aryl-5- [3 ’- (4 ”-methoxyphenyl) -5 The title compound was characterized by 1H NMR, IR, MS and elemental analysis , Of which 4, 5, 7 and 8 have not been reported in the literature.