溴莫普林的合成

Synthesis of Brodimoprim

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%.