摘要
非布司他是一种疗效显著的抗痛风药物,研究其合成方法具有重要意义。通过2种不同方法合成了非布司他关键中间体2-(3-醛基-4-羟苯基)-4-甲基噻唑-5-甲酸乙酯,比较和分析2种方法的优缺点。研究发现,采用多聚甲醛进行甲酰化反应合成非布司他关键中间体时的产率较高;但采用六次甲基四胺进行甲酰化反应合成非布司他关键中间体方法的生产成本更低,更环保,适用于工业化生产,其中以冰醋酸作为质子化试剂的达夫(Duff)反应法具有更好的工业应用前景。
Febuxostat is an anti-gout drug with excellent curative effect,and its synthesis method research is of the vital significance. In this paper,two methods for the synthesis of Febuxostat’s key intermediate 2-( 3-Formyl-4-hydroxy-phenyl)-4-methyl-thiazole-5-carboxylic acid ethyl ester were performed,and the advantages and disadvantages of each method were compared and analyzed. Experimental results showed that the product yield of the formylation with paraformaldehyde was relatively higher. But from the aspects such as production cost and environmental protection,the method for the formylation with hexamethylenetetramine was more suitable for the industrial production. The Duff method using glacial acetic acid as protonation reagent should have a good prospect for industrial application.
作者
张勇
李毓桔
马志刚
徐来
隋宁
陈雪梅
ZHANG Yong;LI Yuju;MA Zhigang;XU Lai;SUI Ning;CHEN Xuemei(School of Chemistry and Chemical Engineering,Hubei Polytechnic University,Huangshi Hubei 435003;Shanghai EastForeign Language School Affiliated to SISU,Shanghai 200092;Huangshi Phamacy Co. ,Ltd. ,Huangshi Hubei 435000)
出处
《湖北理工学院学报》
2019年第1期36-39,共4页
Journal of Hubei Polytechnic University
基金
湖北省教育厅高校青年教师深入企业行动计划项目(项目编号:XD2014677)
