文献类型：期刊文献

中文题名：2,6-二乙基-4-甲基苯基丙二酰胺的合成

英文题名：The Synthesis of 2-(2,6-diethyl-4-methylphenyl)malonamide

作者：陈立鹏[1];廖道华[1];高倩[1];李爱军[1];郭栋[1];岳航[1];杨帆[1]

机构：[1]华东理工大学药学院,上海200237

年份：2014

卷号：53

期号：8

起止页码：558

中文期刊名：农药

外文期刊名：Agrochemicals

收录：CSTPCD;;北大核心:【北大核心2011】；CSCD:【CSCD_E2013_2014】；

语种：中文

中文关键词：唑啉草酯;中间体;除草剂;合成

外文关键词：pinoxaden; intermediates; herbicides; synthesis

摘要：[目的]旨在探索并优化出一条适合工业化生产2,6-二乙基-4-甲基苯基丙二酰胺的工艺路线。[方法]2,6-二乙基-4-甲基苯胺经过Sandmeyer反应,得到2,6-二乙基-4-甲基溴苯,然后与丙二腈在氯化钯催化下偶合,得到2,6-二乙基-4-甲基苯基丙二腈,最后将其水解得到目标产物2,6-二乙基-4-甲基苯基丙二酰胺。[结果]反应总收率为71.8%,产物与中间体经1H NMR、MS等进行了表征。[结论]该路线收率较高,原料易得,实验步骤较少,适合工业生产。
[Aims] This article aims to explore and optimize a reasonable route of 2-（2,6-diethyl-4-methylphenyl） malonamide on industrial scale. [Methods] 2,6-Diethyl-4-methyl-bromobenzene was prepared from 2,6-diethyl-4-methyl-aniline by the Sandmeyer reaction, then coupled with malononitrile under palladium catalysis to give the 2,6-diethyl-4- methyl-phenyl-malononitrile, which was hydrolyzed to get the target product. [Results] The total yield of the process was 71.8%, and the important intermediate and products were characterized by MS and ＇H NMR. [Conclusions] The proposed synthetic route has many advantages, including high yield, easily available raw materials, few synthetic steps and it can be suitable for industrial production.