含1,2,4-三唑杂环的新型Strobilurins衍生物的合成及杀菌活性有机化学.pdfVIP

2008 年第 28 卷 有 机 化 学 Vol. 28, 2008 第 5 期, 875～880 Chinese Journal of Organic Chemistry No. 5, 875～880 ·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 (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) 摘要 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 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* (Key Laboratory of Pesticide and Chemical Biology, Ministry of Education , College of Chemistry, Central China Normal University, Wuhan 430079) Abstract In order to find highly active lead compounds, fourteen novel derivatives of strobilurins were 1 designed and synthesized. Their structures were characterized by MS, H NMR spectra and elemental analy- sis. The single crystal structure of compound 5i was determined by X-ray diffraction analysis, which re- vealed 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. Keywords strobilurins; fungici