溴莫普林的合成  

Synthesis of Brodimoprim

作　　者：林木荣 廖联安[2] 

机构地区：[1]福建省永春制药厂,泉州362600 [2]厦门大学化学系,厦门361005

出　　处：《中国新药杂志》2005年第11期1318-1320,共3页Chinese Journal of New Drugs

摘　　要：目的:合成溴莫普林。方法:以4-溴-3,5-二羟基苯甲酸一水化合物为起始原料,经甲基化-酯化、酰肼化、改进的McFadyen-Stevens反应、Knoevenagel缩合,再与盐酸胍环合制备溴莫普林。结果:目标化合物经核磁共振氢谱、质谱、红外光谱等确证,溴莫普林的总收率为35.2%。结论:本方法条件温和,操作简单。Objective：To synthesize brodimoprim. Methods： Brodimoprim was synthesized from 4- bromo-3, 5-dihydroxy benzoic acid via 5 chain reactions including methylation-esterification, hydrazination, modified Mcfadyen-Stevens reaction, Knoevenagel condensation and cyclization with guanidine hydroehloride. Results： The structure of target compound was verified by ^1H-NMR, MS and IR. The overall yield was 35.2 % . Conclusion：The easily manipulated synthetic procedure is good for pilot manufacture.

关 键 词：溴莫普林 药物合成 4-溴-3 5-二羟基苯甲酸 抗菌药 

分 类 号：R974.3[医药卫生—药品] R914.5[医药卫生—药学]