文献类型：期刊文献

中文题名：甲氧苄啶的合成

英文题名：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：[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

年份：2008

卷号：16

期号：6

起止页码：716

中文期刊名：合成化学

外文期刊名：Chinese Journal of Synthetic Chemistry

收录：CSTPCD;;CSCD:【CSCD_E2011_2012】；

语种：中文

中文关键词：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

外文关键词：aniline ; trimethoprim; dihydrofolate reductase inhibitor; antibacterial synergist; drug synthesis

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.