2-[1-(1,2,4-三唑)甲基]-3-乙酰基-2,5-二取代芳基-1,3,4-噁二唑啉类化合物的合成

在冰醋酸存在下, 4-取代苯乙酮和溴素容易进行溴代反应, 得到α-溴-4-取代苯乙酮; 将其和1,2,4-三唑在丙酮中反应, 得到α-(1,2,4-三唑-1-基)-4-取代苯乙酮2; 在冰醋酸催化下, 2和4-取代苯甲酰肼1进行缩合, 得到相应酰腙衍生物3; 化合物3在乙酸酐的作用下环化生成一系列2-1-(1,2,4-三唑)甲基]-3-乙酰基-2,5-二取代芳基-1,3,4-噁二唑啉4. 化合物4的结构经IR, 1H NMR, MS, 元素分析和单晶衍射确证.

Synthesis of 3-Acetyl-2,5-di[(un)substituted phenyl]-2- (1,2,4-triazol-1-ylmethyl)-1,3,4-oxadiazoline

In the presence of glacial acetic acid, 4-substituted acetophenone was brominated easily to afford α-bromo-4-substituted acetophenone, which was reacted with 1,2,4-triazole in acetone to get α-(1,2,4-tria- zole-1-yl)-4-substituted acetophenone (2). Reaction of 4-substituted benzohydrazide (1) with compound 2 gave the corresponding hydrazones 3, which could be readily converted to their congener oxadiazolines 4 in good yields by treatment with acetic anhydride. Compounds 4 were confirmed by IR, 1H NMR, MS, ele-mental analysis and single crystal X-ray diffraction.