5-烷基-2-氨基-1,3,4-噻二唑的合成及应用

用硫代氨基脲与甲酸、乙酸、丙酸、丁酸、异丁酸、异戊酸等在盐酸、磷酸、多聚磷酸、硫酸催化下 ,分别合成了 2 -氨基 -1 ,3 ,4-噻二唑 (a)、5 -甲基 -2 -氨基 -1 ,3 ,4-噻二唑 (b)、5 -乙基 -2 -氨基 -1 ,3 ,4-噻二唑 (c)、5 -丙基 -2 -氨基 -1 ,3 ,4-噻二唑 (d)、5 -异丙基 -2 -氨基 -1 ,3 ,4-噻二唑 (e)、5 -异丁基 -2 -氨基 -1 ,3 ,4-噻二唑 (f)。并对工艺条件进行了试验 ,结果表明 :最佳工艺条件为硫代氨基脲与酸的摩尔比为 1∶ 1 .4,合成 2 -氨基 -1 ,3 ,4-噻二唑为多聚磷酸催化 ,合成其它的为浓盐酸催化 ,回流 3 h,产率分别为 96.78%、74.3 4%、73 .67%、71 .68%、68.44%、67.5 4%。同时以 a～f为原料合成了具有抗菌作用的 5 -烷基 -1 ,3 ,4-噻二唑硫脲乙酸和 5 -烷基 -2 -苯基 -硫脲 -1 ,3 ,4-噻二唑的衍生物

Synthesis and Application of 5-Alkyl-2-amino-1,3,4-thiodiazole

Amino 1,3,4 thiodiazole(a), 2 amino 5 methyl 1,3,4 thiodiazole(b), 2 amino 5 ethyl 1,3,4 thiodiazole(c), 2 amino 5 propyl 1,3,4 thiodiazole(d), 2 amino 5 isopropyl 1,3,4 thiodiazole(e), 2 amino 5 isobutyl 1,3,4 thiodiazole(f) were synthesized using aminothiourea, formic acid, acetic acid, propionic acid, butyric acid, isobutyric acid and isopentanoic acid as raw materials and chlorhydric acid, phosphoric acid, polyphosphoric acid or sulfuric acid as catalyst. The results showed that the optimum conditions were: the molar ratio of aminothiourea and acid was 1∶1.4, and the reaction time was 3 h under refluxing, polyphosphoric acid was used as catalyst for synthesis of a chlorhydric acid was used as catalyst for synthesis of b~f. The yield of a~f is 96.78%、74.34%、73.67%、71.68%、68.44%、67.54%, respectively. New antibacterial compounds were synthesized from a~f.