苯并咪唑-5,6-二羧酸的合成

Studies for the Synthesis of Benzimidazole-5,6-dicarboxylic acid

设计了苯并咪唑 5 ,6 二羧酸的新合成路线 ;解决了已有方法中的原料来源少 ,价格高 ,且含有微量重金属离子等问题 ;实现了苯并咪唑 5 ,6 二羧酸由常用原料、普通试剂和通用方法的简便合成 ,得到了可满足医药工业要求的产品 .该路线以苯酐为起始原料 ,经氨解、硝化、还原、重氮化氯代、硝化、氨解、还原、环合、水解九步 ,得到苯并咪唑 5 ,6 二羧酸 .总收率达 9.7% .

This thesis developed a new method to prepare benzimidazole-5, 6-dicarbo-xylic acid. This method is low-priced and convenient. The product with no heavy metal ion can be used in pharmaceutical industry. Benzimidazole-5,6-dicarboxylic acid was prepared from phthalic anhydride by nine steps, which are amination, nitration, reduction, diazotisation, chlorination, nitration, amination, reduction, cyclization and hydration. The overall yield is 9.7%.