有机化学 ›› 2015, Vol. 35 ›› Issue (12): 2610-2616.DOI: 10.6023/cjoc201508015 上一篇    下一篇

研究简报

新型含氮杂环结构的1,1-二氯丙烯类化合物的合成及其生物活性

戴红a, 葛书山a, 戴宝江b, 李钰a, 施磊a, 李阳a, 方源a, 石玉军a   

  1. a 南通大学化学化工学院 南通 226019;
    b 南通职业大学化学与生物工程学院 南通 226007
  • 收稿日期:2015-08-14 修回日期:2015-09-23 发布日期:2015-10-08
  • 通讯作者: 施磊, 石玉军 E-mail:zhanghj2801@163.com;yjshi2015@163.com
  • 基金资助:

    国家自然科学基金(Nos. 21202089, 21372135)和南通市科技计划(Nos. AS2013002, AS2014011)资助项目.

Synthesis and Biological Activity of Novel 1,1-Dichloropropene Derivatives Containing N-Heterocycles

Dai Honga, Ge Shushana, Dai Baojiangb, Li Yua, Shi Leia, Li Yanga, Fang Yuana, Shi Yujuna   

  1. a College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019;
    b School of Chemical and Biological Engineering, Nantong Vocational University, Nantong 226007
  • Received:2015-08-14 Revised:2015-09-23 Published:2015-10-08
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21202089, 21372135), and the Science and Technology Project Fund of Nantong City (Nos. AS2013002, AS2014011).

为了从1,1-二氯丙烯类化合物中寻找新的活性物质, 本文采用活性基团拼接方法, 制备了一系列未见文献报道的新型含氮杂环结构的1,1-二氯丙烯衍生物. 通过1H NMR, 13C NMR和元素分析等手段对目标化合物的结构进行了验证.初步的生物活性测试结果显示, 在测试浓度为500 μg/mL时大多数目标化合物表现出良好的杀粘虫活性, 其中化合物6a, 6b, 6c, 6d, 6e, 6f, 6i, 6l, 6m6o对粘虫的杀死率均为100%. 此外, 部分目标物还表现出一定的杀蚜虫活性.

关键词: 含氮杂环, 1,1-二氯丙烯, 合成, 生物活性

In search of novel 1,1-dichloropropene compounds with potent bioactivities, a series of novel 1,1-dichloropropene derivatives containing N-heterocycles were synthesized by the strategy of active substructure combination. The structures of the target compounds were confirmed by 1H NMR, 13C NMR and elemental analysis. Preliminary bioassay indicated that most of the title compounds showed good larvicidal activity against Oriental armyworm at the concentration of 500 μg/mL. For example, the inhibition rates against Oriental armyworm of compounds 6a, 6b, 6c, 6d, 6e, 6f, 6i, 6l, 6m and 6o were all 100%. Besides, some target compounds displayed certain insecticidal activity against Aphis craccivora at the concentration of 500 μg/mL.

Key words: N-heterocycle, 1,1-dichloropropene, synthesis, bioactivity