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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (11): 2001-2006. 上一篇    下一篇

研究简报

含吡啶(噻唑)甲基的哌嗪类化合物的合成及生物活性

李刚月*,a; 阎圣刚a ; 蒋 山a ; 钱旭红*,b ; 黄青春b; 张 蓉c   

  1. (a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)
    (b华东理工大学化学生物学上海重点实验室 上海 200237)
    (c大连理工大学精细化工国家重点实验室 大连 116012)
  • 收稿日期:2008-03-04 修回日期:2008-05-23 发布日期:2008-11-18
  • 通讯作者: 李刚月

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

LI, Gang-Yue*,a; YAN, Sheng-Gang a; JIANG, Shana; QIAN, Xu-Hong*,b;
HUANG, Qing-Chunb; ZHANG, Rongc
  

  1. (a Institute of Polymer Materials, Department of Materials Science and Engineering, Dalian Maritime University,
    Dalian 116026)
    (b Shanghai Key Laboratory of Chemical Biology, East China University of Science and Technology, Shanghai 200237)
    (c State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012)
  • Received:2008-03-04 Revised:2008-05-23 Published:2008-11-18
  • Contact: LI, Gang-Yue

PDF

1389

被引次数

46

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50 mg/L的浓度下对孑孓的杀死率可达100%.

关键词: 合成, 生物活性, 哌嗪衍生物

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.

Key words: synthesis, biological activity, piperazine derivative