2-氰基-3-N-烷氨基-3-(N-2-氟苯乙氨基)丙烯酸乙酯类化合物的合成及生物活性研究  

Syntheses and Bioactivities of Ethyl 2-Cyano-3-Substituted Amino-3-(N-2-Fluorophenylethylamino) Acrylates

作　　者：周进康[1,2] 宋宝安[1] 胡德禹[1] 薛伟[1] 金林红[1] 卢平[1] 周霞[1] 

机构地区：[1]贵州大学精细化工研究开发中心,贵阳550025 [2]贵州教育学院化学系,贵阳550003

出　　处：《化学通报》2009年第1期53-58,共6页Chemistry

基　　金：国家自然科学基金项目(20672024)资助

摘　　要：把由氰基乙酸乙酯、二硫化碳、硫酸二甲酯在乙醇钠作用下反应得到的2-氰基-3,3-二甲硫基丙烯酸乙酯中间体用邻氟苯乙胺胺化,再和甲胺等烷胺进行胺化反应,合成了含氟2-氰基丙烯酸乙酯类化合物。结构经元素分析、IR、1H NMR、13C NMR等证实,抗烟草花叶病毒(TMV)生物活性的初步测定表明,所合成的化合物有一定抗TMV活性。A series of ethyl 2-cyano-3-alkylamino-3-（ N-2-fluorophenylethylamino）acrylates were synthesized in threestep procedure. First, ethyl 2-cyano-3,3-dimethythioacrylate （1） was prepared from ethyl cyanoacetate with carbon disulfide and dimethyl sulfate. Then it reacted with 2-fluorophenylethylamine to yield ethyl 2-cyano-3-（ N-2-fluorophenethylamino）-3- methythioacrylate （3）. Lastly, the titled compounds were obtained by the reaction of 3 with relative alkylamine. The structures of as-synthesized compounds were confirmed by elemental analysis, IR, ^1 H NMR and ^13 C NMR. The tests of their bioactivity showed that they exhibited moderate anti-TMV activity.

关 键 词：2-氰基丙烯酸乙酯类化合物 氟 合成 生物活性 

分 类 号：TQ450.2[化学工程—农药化工]