甲氧苄啶的合成  

Synthesis of Trimethoprim

作　　者：冀亚飞[1] 赵乘有[1] 万欢[1] 段梅莉[1] 许煦[2] 

机构地区：[1]华东理工大学药学院,上海200237 [2]华东理工大学化工学院,上海200237

出　　处：《合成化学》2008年第6期716-718,共3页Chinese Journal of Synthetic Chemistry

摘　　要：丙烯腈与苯胺经ZnCl2/AcOH体系催化加成得β-苯胺丙腈(2);2与3,4,5-三甲氧基苯甲醛在叔丁醇钾存在下缩合制得β-苯胺基-α-3,4,5-三甲氧基苯基丙烯腈(3);3在甲醇钠甲醇溶液中与硝酸胍环化合成了甲氧苄啶(TMP),总收率77.1%。3和TMP的结构经1HNMR和EI-MS表征。β-Anilinopropanenitrile （2） was prepared by the addition of propenenitrile with aniline using ZnCl2/AcOH as the catalyst.β-anilino-α-3,4,5-trimethoxybenzylpropenenitrile （ 3 ） were obtained by the condensation of 2 with 3,4,5-trimethoxybenzaldehyde in the presence of potassium t-butoxide. Trimethoprim（TMP） in overall yield of 77.1% was synthesized by the cyclization of 3 with guanidine nitrate in the presence of sodium methoxide. The structures of 3 and TMP were confirmed by 1H NMR and EI-MS.

关 键 词：苯胺 甲氧苄啶 二氢叶酸还原酶抑制剂 抗菌增效剂 药物合成 

分 类 号：R914.5[医药卫生—药物化学] O626.41[医药卫生—药学]