1,2二取代苯并咪唑化合物的一种高效合成方法(英文)

Efficient Synthetic Method of 1,2-substituted benzimidazoles

苯并咪唑是一类具有广泛生理活性的化合物,许多药物分子中都含有苯并咪唑结构。笔者研究苯并咪唑化合物新的高效合成方法。以邻苯二胺和酮为原料,在微波条件下,经缩合,形成单席夫碱,然后再与其他醛反应,高产率的得到了5个1位、2位接有不同取代基的苯并咪唑化合物。单席夫碱生成咪唑过程中,发生1,3负氢迁移。

The benzimidazole exhibits widespread activities, and the benzimidazole nucleus is found in a variety of drugs. In this paper,we research a new and efficient synthetic method of 1,2-disubstituted benzimidazole, o-phenylenediamine and ketone form schiff bases having one free amine group with microwave ,and then schiff bases condensed with different aldehydes to give five 1,2-substituted benzimidazoles. The mechanism of reaction involves 1,3 shift of negative hydrogen ion.