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

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.