2,6-二乙基-4-甲基苯基丙二酰胺的合成  

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] 

机构地区：[1]华东理工大学药学院,上海200237

出　　处：《农药》2014年第8期558-560,563,共4页Agrochemicals

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.

关 键 词：唑啉草酯 中间体 除草剂 合成 

分 类 号：TQ457[化学工程—农药化工]