以Suzuki反应合成抗痛风药非布索坦  

The preparation of febuxostat by Suzuki reaction

作　　者：曹前明 马小丽[1] 熊杰明[1] 郭盼[1] 谷崔迎 岳辉[1] 秦飞飞[1] 彭效明[1] 刘博[1] 居瑞军[1] 晁建平[1] 

机构地区：[1]北京石油化工学院化学工程学院,北京102600

出　　处：《中国新药杂志》2016年第9期1057-1060,共4页Chinese Journal of New Drugs

摘　　要：目的:研究一种合成非布索坦完整的新工艺。方法:以5-溴水杨醛和2-氨基-4-甲基噻唑-5-甲酸乙酯为起始原料,合成3-氰基-4-异丁氧基苯硼酸和2-溴-4-甲基噻唑-5-甲酸乙酯,两者再经过Suzuki反应偶联并水解得到非布索坦。结果:目标化合物经核磁共振、红外光谱确认了其化学结构。结论:该过程基于Suzuki芳基偶联反应,此工艺具有条件温和、高效、绿色、经济等优点并可用于工业化生产。Objective： To obtain a new synthesis process of febuxostat. Methods： 5-bromosalicylaldeyhde and ethyl 2-amino-4-methylthiazole-5-carboxylate were used as the starting materials to synthesize 3-cyano-4-isobutoxyphenyl boronic acid and ethyl 2-bromo-4-methyithiazole-5-carboxylate,then febuxostat was obtained via Suzuki coupling reaction and hydrolysis reaction. Results： The structue of febuxostat was verified by HNMR and IR analysis. Conclusion： The process based on the Suzuki coupling reaction has the advantages of mild conditions and high efficiency,and is green and economic. It can be used for industrial production.

关 键 词：非布索坦 合成 SUZUKI反应 

分 类 号：R914.5[医药卫生—药物化学]