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2020 , Vol. 40 >Issue 12: 4315 - 4321

DOI: https://doi.org/10.6023/cjoc202008031

研究简报

含苯并三氮唑单元的新型吡唑肟衍生物的合成与生物活性

  • 朱玥 ,
  • 郑丹丹 ,
  • 缪何一 ,
  • 钱程 ,
  • 戴红 ,
  • 梁凯 ,
  • 周贝贝 ,
  • 石玉军 ,
  • 荀校 ,
  • 王阳
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  • 南通大学化学化工学院 南通 226019

收稿日期: 2020-08-18

  修回日期: 2020-09-27

  网络出版日期: 2020-10-15

基金资助

国家自然科学基金（Nos.21372135，21802075）、南通市科技计划（No.MS12019060）资助项目.

收起

Synthesis and Biological Activities of Novel Pyrazole Oxime Derivatives Containing Benzotriazolyl Moiety

  • Zhu Yue ,
  • Zheng Dandan ,
  • Miao Heyi ,
  • Qian Cheng ,
  • Dai Hong ,
  • Liang Kai ,
  • Zhou Beibei ,
  • Shi Yujun ,
  • Xun Xiao ,
  • Wang Yang
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  • College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019

Received date: 2020-08-18

  Revised date: 2020-09-27

  Online published: 2020-10-15

Supported by

Project supported by the National Natural Science Foundation of China (Nos. 21372135, 21802075), and the Science and Technology Project Fund of Nantong City (No. MS12019060).

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摘要

为了探寻新型含氮杂环活性物质，以杀螨剂唑螨酯为先导化合物，在吡唑肟的分子结构中引入苯并三氮唑单元结构，设计合成了17个未见文献报道的含苯并三氮唑结构的新型吡唑肟类衍生物.目标化合物的结构经1H NMR，13C NMR和元素分析确证.初步的生测数据表明，部分目标化合物显示出优良杀虫作用.在20 μg/mL浓度下，3个化合物对朱砂叶螨有70%~100%的防效.6个化合物在20 μg/mL浓度下对蚜虫的杀死率在90%~100%.另外，16个化合物在500 μg/mL浓度下对粘虫也呈现出较好的杀虫活性（致死率≥ 80%）.

关键词： 苯并三氮唑; 吡唑肟; 合成; 生物活性

本文引用格式

朱玥 , 郑丹丹 , 缪何一 , 钱程 , 戴红 , 梁凯 , 周贝贝 , 石玉军 , 荀校 , 王阳 . 含苯并三氮唑单元的新型吡唑肟衍生物的合成与生物活性[J]. 有机化学, 2020 , 40(12) : 4315 -4321 . DOI: 10.6023/cjoc202008031

Abstract

In search of new N-heterocyclic compounds possessing good biological activities, 17 novel pyrazole oxime derivatives were designed and synthesized by introducing benzotriazole moiety into pyrazole oxime skeleton based on fenpyroximate. Their structures were tested by 1H NMR, 13C NMR and elemental analysis. Preliminary bioassay data displayed that 3 compounds showed 70%~100% insecticidal activities towards Tetranychus cinnabarinus at 20 μg/mL. 6 compounds possessed 90%~100% mortality rates towards Aphis medicaginis at 20 μg/mL. Moreover, 16 compounds displayed more than 80% insecticidal activities against Mythimna separata (Walker) at 500 μg/mL.

Key words： benzotriazole; pyrazole oxime; synthesis; biological activity

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