2-氰基-3-取代胺基-3-[2-(4-氟苯基)-乙胺基]丙烯酸乙酯类化合物的合成及生物活性研究  

Synthesis and Bioactivity of Ethyl 2-Cyano-3-substituted-amino-3-[2-(4-fluorophenyl)-ethylamino]-acrylates

作　　者：周进康[1] 宋宝安[2] 薛伟[2] 金林红[2] 干正洋[1] 

机构地区：[1]贵州师范学院化学与生命科学学院,贵阳550018 [2]贵州大学精细化工研究开发中心,贵阳550025

出　　处：《有机化学》2011年第6期865-869,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.20672024)资助项目

摘　　要：以氰基乙酸乙酯为原料,经与二硫化碳、硫酸二甲酯反应合成了2-氰基-3,3-二甲硫基丙烯酸乙酯(1),然后引入对氟苯乙胺得到化合物(3),其与脂肪胺反应合成了新型含对氟苯乙氨基的2-氰基丙烯酸乙酯类化合物5a～5h,其结构经元素分析,IR,1H NMR和13C NMR等确证.初步生物活性试验表明,部分化合物具有一定抗烟草花叶病毒活性.A series of ethyl 2-cyano-3-substituted-amino-3-[2-（4-fluorophenyl）-ethylamino]-acrylates were synthesized in three steps.Firstly,ethyl 2-cyano-3,3-dimethythioacrylate（1） was prepared from reactions of ethyl cyanoacetate with carbon disulfide and dimethyl sulfate.Secondly,it reacted with 4-fluorophenethyl-amine to yield ethyl 2-cyano-3-methythioacrylate-3-[2-（4-fluorophenyl）-ethylamino]-acrylate（3）.Thirdly,the title compounds 5a-5h were obtianed by the reactions of 3 with corresponding alkylamines.The struc-tures of as-synthesized compounds were confirmed by elemental analysis,IR,1H NMR and 13C NMR tech-niques.Preliminary bioassay test indicated that some compounds showed moderate antivirus activity against Tobacco mosaic virus.

关 键 词：2-氰基丙烯酸乙酯类化合物 4-氟苯乙胺 合成 结构 生物活性 

分 类 号：TQ463.5[化学工程—制药化工]