新型含氮氧杂环结构的吡唑肟醚衍生物的设计合成与杀虫活性研究

项目名称： 新型含氮氧杂环结构的吡唑肟醚衍生物的设计合成与杀虫活性研究

项目编号： No.21202089

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 有机化学

项目作者： 戴红

作者单位： 南通大学

项目金额： 25万元

中文摘要： 近年来，吡唑肟醚衍生物的研究已成为有关农药研究人员关注的重点研究领域，其研究内容广泛。本课题在总结分析国内外吡唑肟醚杀虫杀螨剂的结构特征、活性数据基础上，选择吡唑肟为母体结构，利用生物等排及活性亚结构拼接等方法，将具有多取代基或延长链的噻唑、吡啶、嘧啶、呋喃、噁二唑等含氮氧杂环单元，通过亚甲基以桥连方式同吡唑肟相连，构建多种具有含氮氧杂环取代的新型吡唑肟醚类化合物。通过对不同合成方法的研究与比较，确定高效、便捷、经济的合成路线。选择适当的虫害为作用对象及相应的生物活性测定模型，测试目标化合物的杀虫活性，进一步研究其构效关系,以期发现具有高活性的农药先导化合物。本研究既保留了吡唑肟类农药的基本结构特征，又突破了相关化合物的结构模式和专利覆盖面，拓展了研究领域。其研究成果可为高效、低毒、低生态风险的新农药创制准备工作基础，提供结构活性数据及新的选择模式。

中文关键词： 吡唑肟；氮氧杂环；合成；生物活性；

英文摘要： Recently, pyrazole oxime ether derivatives have attracted considerable attention in agrochemical research due to their excellent bioactivities. In this project, we choose the pyrazole oxime moiety as the mother backbone, based on analyzing the structural properties and biological activities of pyrazole oxime ether insecticide and acaricide. We want to construct novel pyrazole oxime ethers containing N-,O-heterocycles by introducing the substituted thiazole, pyridine, pyrimidine, furan, and oxadiazole rings into the pyrazole oxime skeleton, which not only remain the basic structural properties of pyrazole oximes, but also break down the structural modes and patent protection of the related compounds and increase the research range of pyrazole oximes. An effective, simple and economic synthetic route to obtain such compounds is one of the goals we pursued.The insecticidal activities and structure-activity relationships of the designed compounds will also be studied with the corresponding bioassay mode in order to find potent pesticide lead compounds. The research results of this project will make good preparation for the design and development of new agrochemicals with high activity,low toxicity and favorable safety profile,further provide more structure-activity data and novel selection modes.

英文关键词： pyrazole oxime；N;O-heterocycle；synthesis；bioactivity；