摘要
基于活性亚结构拼接法,将三氟甲基吡啶结构引入含氮杂环,合成了5个含三氟甲基吡啶结构的含氮杂环化合物,其中1个为新化合物,结构经过^(1)H NMR进行鉴定。对5-三氟甲基-2-溴吡啶与含氮杂环的C-N偶联反应进行探索,得出了最优的反应条件。对目标化合物针对南方根结线虫、松材线虫和水稻干尖线虫的离体杀虫活性进行了研究。结果显示,在200μg/mL的浓度下,所有目标化合物对三种线虫表现出一定的杀线虫活性,5-三氟甲基-2-(1H-咪唑-1-基)吡啶对水稻干尖线虫表现出较好的杀线虫活性,致死率为55.6%,高于对照药剂噻唑磷(36.4%),略低于对照药剂Tioxazafen(64.4%)。
According to the principle of combination of bioactive substructure,the structure of trifluoromethylpyridine was introduced into nitrogen-containing heterocycle compounds,and 5 nitrogen-containing heterocycle compounds containing trifluoromethylpyridine moiety were synthesized,including a new compound.The structures of the target compounds were characterized by ^(1)H NMR.The reaction condition of carbon-nitrogen coupling reaction of 2-bromo-5-(trifluoromethyl)pyridine with nitrogen-containing heterocycle compound has been investigated,and the optimal reaction condition was obtained.The nematocidal activities of the target compounds against Meloidogyne incognita,Bursaphelenchus xylophilus and Aphelenchoides besseyi in vitro were determined.The results showed that all the target compounds displayed certain inhibitory activities against the three nematodes.2-(1H-imidazol-1-yl)-5-(trifluoromethyl)pyridine showed good nematocidal activity against A.besseyi and the mortality rate was 55.6%at 200μg/mL,which is higher than fosthiazate(36.4%)and slightly lower than tioxazafen(64.4%).
作者
马小云
刘丹
杨香奉
MA Xiao-yun;LIU Dan;YANG Xiang-feng(School of Chemistry and Materials Science,Guizhou Education University,Guiyang,Guizhou,550018;Research and Development Centre for Fine Chemicals,Guizhou University,Guiyang,Guizhou,550025)
出处
《贵州师范学院学报》
2022年第6期8-13,共6页
Journal of Guizhou Education University
基金
贵州师范学院2020年度校级科学研究基金项目重点项目(2020ZD005)
贵州省普通高等学校青年科技人才成长项目(黔教合KY字[2021]238)
贵州省教育厅特色重点实验室建设项目“功能有机分子特色重点实验室”(黔教合KY字[2018]001)。
关键词
三氟甲基吡啶
C-N偶联反应
杀线虫活性
南方根结线虫
松材线虫
水稻干尖线虫
Trifluoromethylpyridine
C-N Coupling Reaction
Nematocidal Activity
Meloidogyne Incognita
Bursaphelenchus Xylophilus
Aphelenchoides Besseyi
