抗痛风药物非布司他中间体的工艺研究  

Study on the Technology of the Intermediate of Anti Gout Remedy Febuxostat

作　　者：王鹏 蒋岩 吴作伟 吴晓桐 Wang Peng;Jiang Yan;Wu Zuowei;Wu Xiaotong(Jiangsu Xingnuo Pharmaceutical Technology Co.,Ltd.,Xuzhou 221000,China)

机构地区：[1]江苏星诺医药科技有限公司,江苏徐州221000

出　　处：《广东化工》2020年第15期57-58,60,共3页Guangdong Chemical Industry

摘　　要：为了适应工业化生产,对非布司他中间体2-[(3-醛基-4-羟基)苯基]-4-甲基噻唑-5-甲酸乙酯的合成工艺进行研究,结果发现,乙腈为最佳溶剂,在回流温度下,采用多聚甲醛﹑无水氯化镁﹑三乙胺体系,反应5 h,经过后处理得到该中间体,纯度和收率能达到生产的要求。该合成方法,能有效避免使用常用溶剂多聚磷酸产生的污染。In order to adapt to industrial production, the synthesis process of 2-[(3-aldehyde-4-hydroxy) phenyl]-4-methylthiazol-5-carboxylic acid ethyl ester was studied. The results showed that acetonitrile was the best solvent. Under reflux temperature, Paraformaldehyde, anhydrous magnesium chloride and triethylamine system were used to react for 5 hours, and the intermediate was obtained through post-treatment. The purity and yield can meet the production requirements. This synthesis method, can effectively avoid the pollution caused by the use of common solvent polyphosphate.

关 键 词：非布司他中间体 乙腈 回流 多聚甲醛 无水氯化镁 

分 类 号：TQ[化学工程]