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[目的]发现具有农用生物活性的新化合物,采用中间体衍生化方法,以2-氯-5-氯甲基吡啶为原料,设计合成含取代吡啶的吡唑酰胺类化合物并测定其生物活性。[方法]以2-氯-5-氯甲基吡啶为起始原料,首先合成2-(6-氯吡啶-3-基)乙腈,然后经过醚化、还原氢化,得到取代的吡啶乙胺,最后与4-氯-1,3-二甲基-1H-吡唑-5-甲酰氯反应合成9个目标化合物,经核磁验证了结构正确。[结论]生物活性测试结果表明:在普筛的条件下此类化合物对杀虫和杀菌都有良好活性,其中化合物A3对小菜蛾和桃蚜的致死率均为100%,同时对蔬菜霜霉病、小麦白粉病和玉米锈病都有很好的活性;化合物A9表现出了良好的杀菌活性,在25 mg/L的质量浓度下,对黄瓜霜霉病的活性为100%。
[Objective] The research aimed to find novel compounds with agricultural biological activity. The pyrazole amide compounds with substituted pyridine were designed and synthesized by 2-chloro-5-chloromethylpyridine by the method of intermediate derivatization and the biological activity was determined. [Method] Starting from 2-chloro-5-chloromethylpyridine, 2- (6-chloropyridin-3-yl) acetonitrile was synthesized and then subjected to etherification and reductive hydrogenation to obtain substituted pyridylethylamine. Finally, 9 target compounds were synthesized by the reaction of 4-chloro-1,3-dimethyl-1H-pyrazole-5-carboxylic acid chloride. The structures were confirmed by NMR. [Conclusion] The results of biological activity test showed that these compounds had good insecticidal and bactericidal activities under general screening conditions. The lethality of compound A3 to Plutella xylostella and Myzus persicae was 100% The activity of compound A9 showed good bactericidal activity, and its activity against cucumber downy mildew was 100% under the concentration of 25 mg / L.