新型吡唑联吡咯类杂环化合物的合成及杀菌活性  

Synthesis and Fungicidal Activity of New Pyrrolpyrazole Compounds

作　　者：王子时[1] 叶汉韬 肖丹[1] 马东升[1] 高金胜[1,2] 于颖慧[1] 侯广峰[2] 闫鹏飞[1] 

机构地区：[1]黑龙江大学化学化工与材料学院,哈尔滨150080 [2]黑龙江大学农药工程中心,哈尔滨150080

出　　处：《有机化学》2014年第10期2057-2062,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.21371052;21272061);黑龙江省教育厅科学研究基金(No.12531512)资助项目~~

摘　　要：为寻找具有更高生物活性、更环保的新农药杀菌剂,基于杀菌剂氟咯菌腈设计并合成了10个新型吡唑联吡咯类杂环化合物,以吡唑环代替氟咯菌腈上原有的苯环,以期提高其杀菌活性.采用1H NMR,FTIR,单晶X射线衍射、元素分析和熔点测定等测试手段对目标化合物及其中间体的结构进行了表征与确认,并通过挥发法培养得到了6个目标化合物的单晶.还对其中6个化合物进行了生物活性测试,测试结果表明各化合物对水稻纹枯病、黄瓜灰霉病、黄瓜霜霉病均表现出一定的抑菌效果,可作为先导化合物对其结构进行深入的研究,为新农药杀菌剂的开发提供了理论支持.With the aim of obtaining new potential fungicide candidates with higher biological activities and environmental safety, ten new pyrrolpyrazole compounds based on the structures of fludioxonil were designed and synthesized. The benzene ring in original fludioxonil structure is replaced by pyrazole ring to improve its bactericidal activity. All the structures of target products and their intermediates are characterized and confirmed by ^1H NMR, FTIR, single crystal diffraction, HPLC, elemental analysis and melting point determination. Six single crystals of final products are also achieved by volatilization under room temperature. Biological activity tests are conducted for six compounds. The results show that each compound exhibits certain antibacterial activity toward rhizoctonia, botrytis cinerea and cucumber downy mildew, which provides valuable information for further development of new pesticides fungicides.

关 键 词：氟咯菌腈 吡唑联吡咯类化合物 合成 反应条件 生物活性测试 

分 类 号：O626[理学—有机化学]