3,5-二氯-4-吡啶酮乙酸合成工艺优化  

Optimize the synthesis of 3,5-dichloro-4-pyridone-N-acetic acid

作　　者：杨明波[1] 汪令[1] 贾爱琼[1] 李波[1] 赵经伟[1] 

机构地区：[1]抗生素研究与再评价四川重点实验室,四川抗菌素工业研究所,成都大学,成都610052

出　　处：《中国抗生素杂志》2017年第5期360-362,共3页Chinese Journal of Antibiotics

摘　　要：目的优化3,5-二氯-4-吡啶酮乙酸的合成工艺。方法以4-氨基吡啶为起始原料,经重氮化反应、水解、氯代、溴乙酸取代得3,5-二氯-4-吡啶酮乙酸。结果总收率为47.6%,含量为98.71%,产品结构经MS,1H-NMR和13C-NMR确证。结论本文设计的合成路线,起始原料便宜且操作简单,为工业放大生产提供了依据。Objective To optimize the synthesis of 3, 5-dichloro-4-pyridine-N-acetic acid. Methods 3, 5-Dichloro-4-pyridone-N-acetic acid was synthesized form 4-aminopyridine via diazotization, hydrolysis, chlorination and the bromoacetic acid substitution. Results The overall yield was 47.6% and the purity was 98.71%. The structure was confirmed by MS, ^1H NMR and ^13C NMR. Conclusion In this synthetic route, the economical starting material and convenient operations make it suitable for the industrial production.

关 键 词：4-氨基吡啶 “一锅煮”合成 3 5-二氯-4-吡啶酮乙酸 

分 类 号：R978.1[医药卫生—药品]