含2-三氟甲基苯并咪唑的1,2,4-三唑的合成

2-三氟甲基苯并咪唑-1-乙酰肼在无水乙醇中分别与苯基异硫氰酸酯、对甲苯基异硫氰酸酯、对甲氧苯基异硫氰酸酯和邻甲苯基异硫氰酸酯反应,得到相应的酰氨基硫脲(Ⅲa~d),收率分别为73.3%、87.3%、85.5%和64.3%。再于115~120℃下,与w(NH2NH2.H2O)=85%的水合肼反应4 h,制得3-(2-三氟甲基苯并咪唑-1-亚甲基)-4-氨基-5-芳胺基-1,2,4-三唑(Ⅳa~d),收率分别为53.5%、56.1%、61.8%和50.7%。该方法反应时间短,处理简单,产率较高。目标化合物经元素分析,IR和1HNMR进行了结构确证。

Synthesis of 1,2,4-Triazole Containing 2-Trifluoromethylbenzimidazole

Acylthiosemicarbazides(Ⅲ_(a~d)) were prepared by reaction of 2-trifluoromethylbenzimidazole-1-acetyl hydrazine(Ⅰ) with phenyl isothiocyanate,p-methylphenyl isothiocyanate,p-methoxyphenyl isothiocyanate and o-methylphenyl isothiocyanate in the presence of anhydrous ethanol respectively in 73.3%,87.3%,85.5% and 64.3% yield.ThenⅢ_(a~d) reacted with 85% hydrazine hydrate at 115~120 ℃ for 4h to give 3-(2-trifluoromethylbenzimidazole-1-methylene)-4-amino-5-arylamino-1,2,4-triazole(Ⅳ_(a~d)),respectively in 53.5%,56.1%,61.8% and 50.7% yield.Advantages of this method is short reaction time,simple reaction process and high yield.Structures of the products were confirmed by elementary analysis,IR and ~1HNMR.