酰胺类乙螨唑新化合物的合成及杀螨活性  

Synthesis and Acaricidal Activity of New Amido-etoxazoles

作　　者：李玉峰[1] 卜洪忠[1] 倪钰萍[2] 郝春燕[1] 陈栋萍[1] 宋熊荣[1] 

机构地区：[1]南京工业大学理学院,南京211816 [2]江苏省农药研究所有限公司,南京210036

出　　处：《农药》2013年第11期800-802,817,共4页Agrochemicals

摘　　要：[方法]为寻求高活性的杀螨剂,以乙螨唑为先导化合物,以3-硝基-2,6-二氟苯甲酰胺(1)为起始原料,依次经历缩合反应、傅克烷基化、关环、还原、酰基化反应,制备系列酰胺类乙螨唑新化合物,其结构经核磁共振氢谱分析确证。[结果]以朱砂叶螨螨卵为活体靶标对新化合物进行了生物活性测试。[结论]化合物6a、6g、6l、6m、6p、6r在100 mg/L质量浓度下对螨卵的抑制活性达到100%。[Methods] With etoxazole as the lead compound, a series of new amido-etoxazoles were designed to search for highly active acaricides. Amido-etoxazoles were synthesized from 3-nitro-2,6-difluorobenzamide （1） through condensation, Friedel-Crafts alkylation, intramolecular substitutive cyclization, hydrogenolysis and acylation. The structures of amido-etoxazoles were confirmed by tH NMR spectra. [Results] The bioassay was performed with eggs of vermilion mite（Tetranychus cinnabarinus） as living targets. [Conclusions] At the concentration of 100 mg/L, the acaricidal activity of 6a, 6g, 61, 6m, 6p and 6r against Vermilion mite eggs reached 100%.

关 键 词：乙螨唑 酰胺类乙螨唑 合成 杀螨活性 

分 类 号：TQ454.2[化学工程—农药化工]