“一锅法”制备2-芳环取代咪唑化合物

A One-pot Method for the Preparation of 2-Aryl-substituted Imidazoles

以氰基取代的芳环化合物为起始原料,采用一锅法经加成、缩合、闭环3步反应合成了6个2-芳环取代咪唑化合物。同时考察了反应过程中甲醇钠用量、闭环反应温度和反应时间对目标产物收率的影响,得到的最佳反应条件:n(甲醇钠)∶n(氰基化合物)=(0.08～0.12)∶1,反应温度80～90℃,反应时间3～8 h。产物结构通过熔点、核磁、质谱、元素分析进行了确证。

Six 2-aryl-substituted imidazoles were prepared by a three-step one-pot method from corresponding nitriles reacted with aminoacetaldehyde dimethyl acetal. A study was carried out on the effect of the amount of sodium methoxide, temperature and time of cycfization reaction on the yield of the target products. The optimum reaction conditions were identified as follows：the mole ratio of the amount of sodium methoixde to the starting nitriles was （0.08 - 0. 12 ） ： 1, the cyclization reaction temperature was 80 - 90 ℃ and the cyclization reaction time was 3 - 8 h. The structures of all products were characterized by means of melting point,mass, ^1HNMR and elementary analysis.