2-取代苯并咪唑类化合物具有抗肿瘤、抗菌等多种生物活性,广泛应用于医药、农药和化工等领域。综述近年来2-取代苯并咪唑合成方法的最新进展,重点从烷基取代、芳环取代、巯基取代、胺基取代和杂环取代等几个方面进行了详细归纳。指出苯并咪唑衍生物未来的合成方向可以从减少强酸强氧化剂使用,采用微波辐射和固体催化剂等方面进行开展。 2-Substituted benzimidazoles have many biological activities such as anti-tumor, anti-bacterial and are widely used in the fields of medicine, pesticide and chemical industry. In this paper, the recent progress in the synthesis of 2-substituted benzimidazoles is summarized. The emphasis is given in detail from the aspects of alkyl substitution, aromatic substitution, mercapto substitution, amine substitution and heterocyclic substitution. It is pointed out that the future synthesis direction of benzimidazole derivatives can be reduced from the use of strong acid and strong oxidants, using microwave radiation and solid catalyst.