新型含吡啶环取代的吡唑肟醚类化合物的合成及生物活性研究  

Synthesis and Biological Activities of Novel Pyrazole Oxime Ether Derivatives Containing Pyridyl Ring

作　　者：戴红[1,2] 刘建兵[1] 苗文科[1] 吴珊珊[1] 秦雪[1] 张欣[1] 王婷婷[1] 方建新[1] 

机构地区：[1]南开大学元素有机化学国家重点实验室,天津300071 [2]南通大学化学化工学院,南通226019

出　　处：《有机化学》2011年第10期1662-1667,共6页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.20772068);南通市科技计划(Nos.K2010016;AS2010005);南通大学自然科学基金(Nos.09Z010;09C001)资助项目

摘　　要：为了寻找新型高效低毒的农药先导化合物,通过N-吡啶基吡唑肟与2-氯-5-氯甲基吡啶的缩合反应,合成了一系列含吡啶环取代的吡唑肟醚类化合物.目标化合物的结构均经1H NMR,13C NMR和元素分析确证.初步生物活性试验结果表明,部分化合物具有一定的杀菌、杀虫和植物生长调节活性.如化合物5c在浓度为50μg/mL时对番茄早疫的抑制率为61.4%;化合物5j在浓度为50μg/mL时对花生褐斑的抑制率为60.2%;化合物5i在浓度为500μg/mL时对蚜虫表现出50.3%的杀死率;化合物5f在浓度为10μg/mL时对黄瓜子叶生根表现出71.0%的促进生长作用.In search of new low toxicity and potent pesticide lead compounds,a series of novel pyrazole oxime ether derivatives containing a pyridyl ring were synthesized by the condensation of N-pyridyl pyra-zole oximes with 2-chloro-5-chloromethyl pyridine.Their structures were determined by 1H NMR,13C NMR spectra and elemental analysis.Preliminary bioassay showed that some of the target compounds dis-played fungicidal,insecticidal,and plant growth regulatory activities to some extent.For example,com-pound 5c exhibited 61.4% inhibition rate against Alternaria solani at the concentration of 50 μg/mL,com-pound 5j showed 60.2% inhibition rate against Cercospora arachidicola at the concentration of 50 μg/mL,the mortality rate of compound 5i was 50.3% against Aphis craccivora at the concentration of 500 μg/mL,and compound 5f displayed 71.0% promotion effect on the radicle growth of cucumber cotyledons at the concentration of 10 μg/mL.

关 键 词：吡啶 吡唑肟醚 合成 生物活性 

分 类 号：TQ450.1[化学工程—农药化工]