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对氯苯乙酮肟醚衍生物的合成及生物活性

Synthesis and Bioactivity of 4-Chlorophenyl Methyl Ketone Oxime Ether Derivatives

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【作者】 许艳袁莉萍曹瑾倪长春沈宙陈亮张一宾

【Author】 XU Yan2, YUAN Li-ping1, CAO Jin1, NI Chang-chun1,SHEN Zhou1, CHEN Liang1, ZHANG Yi-bin1(1.Shanghai Pesticide Research Institute,Shanghai 200032,China;2.East China University of Science and Technology,Pharmaceutical Institute,Shanghai 200237,China)

【机构】 华东理工大学药学院上海市农药研究所上海市农药研究所 上海200237上海200032

【摘要】 为寻找高活性的新农药化合物,通过2-取代氨基-1-对氯苯乙酮-1-肟与卤代烃反应,设计并合成了35个对氯苯乙酮肟醚衍生物,其结构均经核磁共振氢谱和元素分析确证。初步的生物活性测定结果表明,该类化合物具有一定的杀虫、抑菌及除草活性,其中C9、C12在500mg/L时对蚜虫Aphis craccivaora的致死率达到100%;C10、C12、C15和C23在1000mg/L时对朱砂叶螨Tetranychus cinabarinus的致死率达到100%;C29、C30和C31在500mg/L时对黄瓜白粉病菌Sphaerotheca fuligineas的抑制率达到95%以上;C29、C30、C33和C35在100mg/L时对马唐Digitaria sanguinalis的抑制率达到90%以上。

【Abstract】 In search of novel pesticide leading compound with high bioactivity,thirty-five 4-chloro-phenyl methyl ketone oxime ether derivatives were designed and synthesized by the reaction of 2-substituted amino 4-chlorophenyl methyl ketone oxime with halohydrocarbon.The structure of all novel compounds was confirmed by 1H NMR and elemental analysis.Preliminary bioassays showed that some compounds exhibited certain insecticidal and herbicidal activities.The mortality of C9,C12 to Aphis craccivaora reached 100% at the concentration of 500 mg/L.The mortality of C10,C12,C15 and C23 to Tetranychus cinabarinus reached 100% at 1 000 mg/L.The inhibition rate of C29,C30 and C31 to Sphaerotheca fuligineas was over 95% at the concentration of 500 mg/L.The inhibition rate of C29,C30,C33 and C35 to Digitaria sanguinalis was over 90% at the concentration of 100 mg/L.

【关键词】 苯乙酮肟合成肟醚生物活性
【Key words】 phenyl methyl ketone oximesynthesisoxime etherbioactivity
【基金】 国家重点基础研究发展计划(“973”计划)项目(2003CB114401).
  • 【文献出处】 农药学学报 ,Chinese Journal of Pesticide Science , 编辑部邮箱 ,2007年01期
  • 【分类号】TQ450.21
  • 【被引频次】7
  • 【下载频次】484
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