含3-氯-5-三氟甲基吡啶基丙烯腈类化合物的设计、合成及杀螨活性

Design, Synthesis and Acaricidal Activity of 3-Chloro-5-trifluoromethylpyridyl Acrylonitrile Derivatives

[目的]合成一系列新型吡啶丙烯腈类化合物,寻找高生物活性分子。[方法]以2,3-二氯-5-三氟甲基吡啶为起始原料,经取代、脱酯、加成反应合成一系列目标化合物。[结果]合成11个结构新颖的3-氯-5-三氟甲基吡啶基丙烯腈类化合物,经~1H NMR和元素分析手段,确定了目标化合物结构。生物活性测定结果表明:化合物V-1、V-2、V-3、V-6和V-7在质量浓度为100 mg/L时,对朱砂叶螨(T. cinnabarinus)若螨的致死率均高于80%,化合物V-3在10 mg/L时对朱砂叶螨卵螨的致死率为89.6%,略高于对照药剂。[结论]筛选出的高活性化合物具有进一步优化的前景,为此类化合物的进一步研究提供了参考。

[Aims] To search high bioactive molecules, a series of novel pyridyl acrylonitrile derivatives were designed.[Methods] A series of target compounds were synthesized by substitution, degreasing and addition reaction using2,3-dichloro-5-trifluoromethylpyridine as raw material. [Results] Eleven novel 3-chloro-5-trifluoromethylpyridyl crylonitrile derivatives were synthesized. The structures of the compounds were determined by -1H NMR and elemental analysis. Bioassay showed that the lethality rates of target compounds V-1, V-2, V-3, V-6 and V-7 against T.cinnabarinus nymphs were all over 80% at 100 mg/L. When the concentration of compound V-3 was 10 mg/L, the lethality rate of T. cinnabarinus eggs was 89.6%, which was slightly higher than that of control group. [Conclusions] The screened highly active compounds has the prospect of further optimization, providing a basis for further research of such compounds.