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溴莫普林的合成
引用本文:林木荣,廖联安.溴莫普林的合成[J].中国新药杂志,2005,14(11):1318-1320.
作者姓名:林木荣  廖联安
作者单位:1. 福建省永春制药厂,泉州,362600
2. 厦门大学化学系,厦门,361005
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McFadyeh-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.

关 键 词:澳莫普林  药物合成  4-澳-3  5-二羟基苯甲酸  抗菌药
文章编号:1003-3734(2005)11-1318-03
收稿时间:2005-06-08
修稿时间:2005-06-08

Synthesis of Brodimoprim
LIN Mu-Rong,LIAO Lian-an.Synthesis of Brodimoprim[J].Chinese Journal of New Drugs,2005,14(11):1318-1320.
Authors:LIN Mu-Rong  LIAO Lian-an
Institution:1. Fujian Yongchun Pharmaceutical Factory, Quanzhou 362600, China; 2 Department of Chemistry, Xiamen University, Xiamen 361005, China
Abstract: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 hydrochloride.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.
Keywords:brodimoprim  synthesis  4-bromo-3  5-dihydroxy benzoic acid  antibacterial agent
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