新型1H-吡唑-4-甲酰胺类衍生物的合成及杀螨活性  

Synthesis and Acaricidal Activity of New 1H-Pyrazole-4-carboxamide Derivatives

作　　者：谢峰[1] 刘婷婷[1] 杨果[1] 袁静[2] 孔小林[1,2] 许天明[2] 谭成侠[1] 

机构地区：[1]浙江工业大学化学工程与材料学院,杭州310014 [2]中化蓝天浙江省化工研究院有限公司,杭州310023

出　　处：《有机化学》2013年第12期2596-2601,共6页Chinese Journal of Organic Chemistry

基　　金："十二五"国家科技攻关计划项目(No.2011BAE06B03-01);浙江省重点科技创新团队(No.2010R50018)资助项目~~

摘　　要：为寻求具有较高生物活性的农药新品种,采用活性基团拼接法,将1,3,5-三甲基-1H-吡唑-4-甲酰胺结构和二芳基醚结构进行活性亚结构拼接,设计并合成了10个未见文献报道的N-烷氧羰基-N-芳基取代的1H-吡唑-4-甲酰胺类化合物,其结构均经1H NMR,MS和元素分析确证,同时对所有化合物进行了初步杀螨活性测试.活性测试结果表明,在500 mg/L质量浓度下,目标化合物对朱砂叶螨均有较强的抑制作用,且大部分化合物对朱砂叶螨的致死率达90.0%以上.To find new lead compounds with high acaricidal bioactivity, ten new 1H-pyrazole-4-carboxamide derivatives were designed and synthesized by combining with the 1,3,5-trimethyl-1H-pyrazole-4-carboxamide moiety in pyflubumide and diaryl ether moiety in flufenoxuron. Their structures were c0iafirmed by 1H NMR, MS and elemental analyses. The acaricidal activities of these compounds were evaluated by pesticide bioassay procedure. The results showed that most of title com- pounds exhibited significant effect against Tetranychus cinnabarinus with 90.0% death rate at 500 mg/L.

关 键 词：1H-吡唑-4-甲酰胺 合成 杀螨活性 

分 类 号：TQ454.2[化学工程—农药化工] O626.21[理学—有机化学]