含吡啶(噻唑)甲基的哌嗪类化合物的合成及生物活性  

Synthesis of Piperazine Derivatives Containing Pyridinemethyl/Thiazolemethyl and Their Biological Activities

作　　者：李刚月[1] 阎圣刚[1] 蒋山[1] 钱旭红[2] 黄青春[2] 张蓉[3] 

机构地区：[1]大连海事大学材料科学与工程系高分子材料研究所,大连116026 [2]华东理工大学化学生物学上海重点实验室,上海200237 [3]大连理工大学精细化工国家重点实验室,大连116012

出　　处：《有机化学》2008年第11期2001-2006,共6页Chinese Journal of Organic Chemistry

基　　金：国家重点基础研究发展计划(973计划)(No.2003CB114400)资助项目.

摘　　要：采用活性基团拼接原理,分别以2-氯-5-氯甲基吡啶和2-氯-5-氯甲基噻唑为原料,经过氮烷基化和加成反应,得到系列含吡啶甲基或噻唑甲基的哌嗪类化合物.初步测试结果表明:部分化合物表现出较弱的除草活性和杀豆蚜活性,但对孑孓显示出较高的的杀灭活性,其中4f在50mg/L的浓度下对孑孓的杀死率可达100%.According to the principle of combination of active groups, a series of piperazine derivatives containing pyridinemethyl/thiazolemethyl were designed and synthesized from 2-chloro-5-（chloromethyl） pyridine or 2-chloro-5-（chloromethyl）thiazole via N-alkylation and addition reactions. Some compounds showed weak herbicidal activity and insecticidal activity against Aphis fabae but good insecticidal activity against Culex pipiens, among which compound 4f exhibited 100% mortality against Culex pipiens at 50 mg/L.

关 键 词：哌嗪衍生物 合成 生物活性 

分 类 号：TQ450.2[化学工程—农药化工]