摘要
目的合成抗痛风药非布索坦并优化其工艺。方法以对羟基苯腈为原料,经加成、环合、甲酰化、烃化、氰化、水解6步反应制得目标产物。结果目标化合物的结构经1H-NMR、MS和元素分析确证,总收率33%。结论与文献报道的工艺比较,新工艺操作简单,反应时间缩短,成本降低,适合工业化生产。
Aim To improve the synthesis of antipodagric febuxostat and to optimize its procedure.Methods Antipodagric febuxostat was prepared starting from 4hydroxybenzonitrile via addition,cyclization,formylation,alkylation,cyanation,and hydrolysis.Results The overall yield of target compound was 33%,and its structure was confirmed by 1H-NMR,MS and elementary analysis.Conclusion In comparison with the reported procedure,the new route is simple,economic,and suitable for industrial production.
出处
《中国药物化学杂志》
CAS
CSCD
2010年第4期282-284,共3页
Chinese Journal of Medicinal Chemistry
关键词
抗通风药
非布索坦
合成
优化工艺
antipodagric
febuxostat
synthesis
procedure improvement
