2-巯基-5-硝基苯并咪唑的连续化合成研究

Study on Continuous Synthesis of 2-mercapto-5-nitrobenzimidazole

艾普拉唑是新一代的质子泵抑制剂,主要用于治疗十二指肠等消化性溃疡为主的肠胃疾病,具有抑酸效果强,作用持久等优势。已在27个国家申请了专利,并于2007年成功上市,2016年销售额达到1.2亿元。本文提供一种以4-硝基邻苯二胺为原料制备艾普拉唑关键中间体2-巯基-5-硝基苯并咪唑的连续化合成方法。本方法具有操作简便、安全环保、产率高等特点。

Epoprazole is a new generation of proton pump inhibitors, and mainly treats duodenal ulcer ano omer peptic ulcer-based gastrointestinal diseases. It has patent application in 27 countries, successfully reached annual sale of 120 million yuan in 2016. Flow chemistry was used to synthesize 2-mereapto-5-nitrobenzimidazole, which was the key intermediate of epoprazole, and a potent enviromently friendly way to make epoprazole was offered.