应用化学

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螺环季酮酸的羧酸酯衍生物的合成及其杀螨活性

高树坤*,石营,韩宗岭,傅海丰,许良忠,陈晓涛   

  1. (青岛科技大学化学与分子工程学院 青岛 266042)
  • 收稿日期:2011-09-19 修回日期:2011-11-22 出版日期:2012-08-10 发布日期:2012-08-10
  • 通讯作者: 高树坤; E-mail:mylover_gao@126.com; 研究方向:有机合成、药物中间体合成、新农药研发

Synthesis and Acaricidal Activity of Carboxylate Derivatives of Tetronic Acid Compounds

GAO Shukun*, SHI Ying, HAN Zongling, FU Haifeng, XU  Liangzhong, CHEN Xiaotao   

  1. (College of Chemistry and Molecular Engineering,Qingdao University of Science & Technology,Qingdao 266042,China)
  • Received:2011-09-19 Revised:2011-11-22 Published:2012-08-10 Online:2012-08-10

摘要: 采用类同合成、活性亚结构拼接方法,对螺环季酮酸类杀虫杀螨剂Spirodiclofen进行设计修饰,合成了18种螺环季酮酸羧酸酯的新衍生物,结构经1H NMR、IR和元素分析确证,并用X射线单晶衍射测定了化合物6d的晶体结构。 通过其生物活性测试,探讨了其构效关系。

关键词: 杀螨剂, 螺环季酮酸, 合成, 生物活性, 晶体结构

Abstract: Eighteen carboxylate derivatives of tetronic acid compounds were designed and synthesized by modifying the spirodiclofen of tetronic acid acaricide with bioisosterism and union of active group on the base of the structure-activity relationship. Their structures were characterized by 1H NMR, IR spectra and elemental analysis, and the single crystal structure of compound 6d was determined by X-ray diffraction analysis. The relationship between structures and activities has been analyzed by bioassay, several of them show high potential as novel acaricides.

Key words: acaricide, tetronic acid, synthesis, Bioactivity, Catalytic activity

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