含氟吡唑-4-肟酯乙酰胺类衍生物的合成及生物活性  

Synthesis and biological activity of fluorinated 1H-pyrazole-4-oxime ester-acetamides derivatives

作　　者：王赛荣[1] 谢峰[1] 刘婷婷[1] 杨果[1] 袁静[2] 黄红英[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：《农药学学报》2014年第1期97-101,共5页Chinese Journal of Pesticide Science

基　　金："十二五"国家科技支撑计划资助项目(2011BAE06B02)

摘　　要：为寻求具有较高生物活性的农药新品种,以杀螨剂pyflubumide为先导,在其母体结构中引入肟酯和二芳基醚结构,设计并合成了7个未见文献报道的1H-吡唑-4-肟酯乙酰胺类化合物,其结构均经核磁共振氢谱、质谱和元素分析确证。初步生物活性测试结果表明,在500 mg/L质量浓度下,所有目标化合物对朱砂叶螨Tetranychus cinnabarinus均有较强的杀灭作用,大部分化合物对其的致死率达100%,但药效低于对照药剂阿维菌素和炔螨特。To find new biological lead compounds ester-acetamides derivatives were designed and with high bioactivity, 7 new 1H-pyrazole-4-oxime synthesized by inserting the oxime esters and tolyloxybenzyl into mother structure of pyflubumide. Their structures were confirmed by I H NMR, MS and elemental analysis. The acaricidal activity of these compounds was evaluated. The results showed that most of title compounds exhibited inhibiting effect against Tetranychus cinnabarinus with 100% death rate at 500 mg/L. However, the effect is not as well as abamectin or propargite.

关 键 词：1H-吡唑4-肟酯乙酰胺 合成 生物活性 

分 类 号：O626.21[理学—有机化学]