有机化学 ›› 2008, Vol. 28 ›› Issue (05): 875-880. 上一篇    下一篇

研究简报

含1,2,4-三唑杂环的新型Strobilurins衍生物的合成及杀菌活性

赵培亮,章博,王亚洲,杨光富*   

  1. (华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079)
  • 收稿日期:2007-09-12 修回日期:2007-10-15 发布日期:2008-05-20
  • 通讯作者: 杨光富

Synthesis and Fungicidal Activities of Novel Analogues of Strobilurins Containing 1,2,4-Triazol Moiety

ZHAO Pei-Liang,ZHANG Bo,WANG Ya-Zhou,YANG Guang-Fu*   

  1. (Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry,
    Central China Normal University, Wuhan 430079)
  • Received:2007-09-12 Revised:2007-10-15 Published:2008-05-20
  • Contact: YANG Guang-Fu

为了寻找新的高活性先导化合物, 设计合成了14个未见文献报道的Strobilurins类衍生物, 结构经MS, 1H NMR, 元素分析确认. 并用X-ray单晶衍射测定了(E)-3-甲氧基-2-[(5-甲基-4-邻溴代苯亚甲基亚胺基-1,2,4-三唑)-3-硫亚甲基]-苯基丙烯酸甲酯(5i)的晶体结构, 证实了分子中的两个C=C均为E-式构型. 初步生物活性测试结果表明, 在实验浓度下部分化合物具有一定的杀菌活性.

关键词: Strobilurins, 杀菌活性, 晶体结构

In order to find highly active lead compounds, fourteen novel derivatives of strobilurins were designed and synthesized. Their structures were characterized by MS, 1H NMR spectra and elemental analy-sis. The single crystal structure of compound 5i was determined by X-ray diffraction analysis, which revealed that the two carbon-carbon double bonds in the molecule were of E,E-configurations. The preliminary bioassay showed that some of them exhibited certain fungicidal activities.

Key words: fungicidal activity, crystal structure, strobilurins