新型含氟吡啶哌嗪类衍生物的设计、合成与生物活性  

Design, Synthesis and Biological Activity of Novel Fluoropyridine Piperazine Derivatives

作　　者：彭壮 王明慧[1] PENG Zhuang, WANG Ming-hui(College of Chemistry and Molecular Engineering of Qingdao University of Science ＆ Technology, Qingdao 266042, Shandong, China)

机构地区：[1]青岛科技大学化学与分子工程学院,山东青岛266042

出　　处：《农药》2018年第9期641-644,共4页Agrochemicals

摘　　要：[目的]合成一系列新化合物,寻找环境友好型高生物活性分子。[方法]以哌嗪为桥链,通过活性亚结构拼接方法合成1-(3-氯-5-三氟甲基)-2-吡啶基哌嗪,并以此化合物为中间体将活性结构拼接合成一系列含氟吡啶哌嗪类衍生物。[结果]结构通过元素分析和1H NMR确证。生测结果表明:化合物Ⅳ3、Ⅳ13、Ⅳ14在质量浓度为5 mg/L时对小菜蛾(Plutella xylostella)的致死率高于94%,对甜菜夜蛾(Spodoptera exigua)的致死率高于80%,尤其化合物Ⅳ3表现出的生物活性优于对照化合物啶虫隆。[结论]筛选出环境友好型、高效杀虫剂,为含氟吡啶哌嗪类衍生物的活性研究提供参考。[Aims] The research aims to synthesize a series of new compounds and search for environmental friendly and high bioactive molecules. [Methods] 1-（3-Chloro-5-trifluoromethyl）-2-pyridylpiperazine was synthesized by the active substructure splicing method with piperazine as the bridge chain, and this compound was used as the intermediate to splice the active structure into a series of fluoropyridine piperazine derivatives. [Results] The structure was confirmed by elemental analysis and 1 H NMR. The bioassay showed that compounds IV3, IV13 and IV14 showed more than 94%mortality against diamond Plutella xylostella at 5 mg/L and showed more than 80% mortality against diamond Spodoptera exigua at the same concentration, especially the biological activity of compound IV3 was better than that of chlorfiuazuron. [Conclusions] The environment-friendly and highly effective insecticides were screened out, which provides a guide for the drug-resistance study for fluoropyridine piperazine derivatives.

关 键 词：哌嗪 含氟吡啶 杀虫剂 合成 生物活性 

分 类 号：TQ460.3[化学工程—制药化工]