非布索坦的合成  

Synthesis of Febuxostat

作　　者：任月娇[1] 李晶[2] 张雷[2] 

机构地区：[1]华南理工大学化学与化工学院,广东广州510640 [2]华南理工大学生物科学与工程学院,广东广州510006

出　　处：《精细化工》2013年第10期1134-1137,共4页Fine Chemicals

基　　金：广东省科技厅国际合作项目(2012B050600013)~~

摘　　要：以4-羟基苯甲腈为原料,经硫化、环合、甲酰化、氰化、烷基化、水解反应制得非布索坦。改进后的工艺在氰化和烷基化时采用"一锅法"合成,同时考察了硫化反应中盐酸浓度以及苯环甲酰化反应过程中时间、温度、甲烷磺酸和三氟乙酸体积比对产物收率的影响。研究表明,该合成路线操作简单,反应条件温和,不引入剧毒物质,收率可达65.7%。Febuxostat was prepared from 4-hydroxybenzonitrile via sulfuration, cyclization, formylation, cyanation, alkylation and hydrolysis. The cyanation and alkylation reaction was performed in a one-pot reaction in the improved process, and the key factors, such as concentration of hydrochloric acid, reaction time, temperature, the ratio of methane sulfonic acid to trifluoroacetic acid, were explored. The improved process was convenient and boasting mild reaction conditions, and the total yield was as high as 65.7%.

关 键 词：非布索坦 抗痛风药 黄嘌呤氧化酶 硫化 甲酰化 一锅法 医药与日化原料 

分 类 号：R971.1[医药卫生—药品]