两步法无催化剂高效合成2-取代苯并咪唑  

Two-step Efficient Synthesis of 2-Substituted Benzimidazoles without Catalyst

作　　者：李维思[1] 石倩[1] 李振江[1] 

机构地区：[1]南京工业大学制药与生命科学学院,南京210009

出　　处：《应用化学》2009年第2期130-134,共5页Chinese Journal of Applied Chemistry

基　　金：国家重点基础研究发展计划(2003CB716004)资助项目

摘　　要：芳香醛与NaHSO3加成得到羟基磺酸盐,加入邻苯二胺或取代邻苯二胺在乙醇中回流反应,空气氧化直接得到2-取代苯并咪唑。在合成的15个化合物中,产率均超过80%。其中化合物2-(4-氯苯基)-6-甲氧基-1H-苯并咪唑尚未见报道。所有产物结构经元素分析、IR、1H NMR分析技术得到确证。合成方法无需任何催化剂,操作简单,条件温和,环境友好。Several aromatic aldehydes and sodium bisulfite were mixed to prepare hydroxyl sulfonates, which were added to o-phenylenediamine or substituted o-phenylenediamine in refluxing ethanol to afford 2-substituted benzimidazoles through oxidation by air directly. One of the fifteen synthesized compounds, 2-（4-chloro- phyenyl）-6-methoxyl-lH-benzimidazole has not been reported. All the compounds were identified by IR, ^1H NMR spectra and elemental analysis. The method is simple, mild, eco-friendly and requires no catalyst.

关 键 词：芳香醛 邻苯二胺 取代苯并咪唑 合成 

分 类 号：O621.3[理学—有机化学]