有机化学 ›› 2014, Vol. 34 ›› Issue (3): 495-506.DOI: 10.6023/cjoc201310012 上一篇    下一篇

综述与进展

苯并咪唑类化合物的合成方法进展

朱观明, 杨柳阳, 崔冬梅   

  1. 浙江工业大学药学院 杭州 310014
  • 收稿日期:2013-10-13 修回日期:2013-11-16 发布日期:2013-11-28
  • 通讯作者: 崔冬梅 E-mail:cuidongmei@zjut.edu.cn
  • 基金资助:

    浙江省自然科学基金(No. Y4100558)资助项目.

Advances in the Synthetic Methods of Benzimidazoles

Zhu Guanming, Yang Liuyang, Cui Dongmei   

  1. College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014
  • Received:2013-10-13 Revised:2013-11-16 Published:2013-11-28
  • Supported by:

    Project supported by the Natural Science Foundation of Zhejiang Province (No. Y4100558).

苯并咪唑类化合物具有抗HIV-1、抗肿瘤、抗细胞增殖、抗寄生虫、抗炎症、抗氧化和抗癫痫方面的生物活性,因此这类化合物的合成备受化学家们的关注. 首次按照反应中间体将近5年合成这类化合物的方法分为以N-亚甲基邻苯二胺(或N-亚甲基邻硝基苯胺)为中间体,以N-酰基邻苯二胺为中间体和以芳基脒(胍)为中间体三类. 通过从这个角度论述这些合成方法,期望能够为设计出更好的合成方法提供启发.

关键词: 苯并咪唑, N-亚甲基邻苯二胺, N-亚甲基邻硝基苯胺, N-酰基邻苯二胺, 芳基脒(胍), 催化剂

Benzimidazoles possess various bioactivities, such as anti-HIV-I, antineoplastic, antiproliferation, antiparasitic and so on, hence the synthetic methods of this class of compounds have attracted much attention. In order to provide some inspiration of better synthetic method design, in this review these methods reported during past five years will be firstly classified into three types according to the reaction intermediates, namely N-methene o-diaminobenzene (or N-methene-o-nitroaniline), N-acyl o-diaminobenzenes and arylamidine (aryl guanidine).

Key words: benzimidazole, N-methene o-diaminobenzene, N-methene-o-nitroaniline, N-acyl o-diaminobenzene, aryl amidine (aryl guanidine), catalyst