溴莫普林的合成  

Synthesis of Brodimoprim

作　　者：金熔[1] 王尔华[1] 杨友田 

机构地区：[1]中国药科大学医药化工研究所,南京210009

出　　处：《中国药科大学学报》2000年第1期1-2,共2页Journal of China Pharmaceutical University

摘　　要：以 4 溴 3,5 二羟基苯甲酸为起始原料 ,经甲基化 酯化、肼化、氧化得 4 溴 3,5 二甲氧基苯甲醛 ,与丙烯腈缩合 ,再与硝胍环合得标题化合物 ,总收率为 2 9%。An improved process for the preparation of brodimoprim(1) was described. Compound 1 was synthesized from 4 bromo 3,5 dimethoxy benzoic aldehyde(5) by condensation with acrylonitrile and cyclization with guanidine nitrate. The compound 5 was prepared form 4 bromo 3,5 dihydroxy benzoic acid through methylation esterification, hydrazination and oxidation. The overall yield was 29%.

关 键 词：溴莫普林 甲氧苄氨嘧啶 合成 二羟基苯甲酸 

分 类 号：R914[医药卫生—药物化学]