N-取代苯并噁唑啉酮及N-取代苯并噁嗪啉酮类化合物的合成和生物活性  

Synthesis and Bioactivity of Substituted 3H-Benzoxazol-2-ones and 4H-Benzoxazin-3-ones

作　　者：袁莉萍[1] 曹瑾[1] 陈亮[1] 沈宙[1] 倪长春[1] 张一宾[1] 

机构地区：[1]上海市农药研究所,上海200032

出　　处：《现代农药》2009年第1期15-19,共5页MODERN AGROCHEMICALS

基　　金：国家重点基础研究发展计划("973计划")项目(2003CB114401)

摘　　要：采用邻氨基酚为原料合成了一系列N-取代苯并噁唑啉酮类化合物和N-取代的苯并噁嗪啉酮类化合物,其化学结构经过1H核磁共振及元素分析确证。初步的生物活性试验结果表明,N-取代苯并噁唑啉酮类化合物具有一定的杀虫杀菌活性,其中化合物3b、4b、14b、19b在50mg/L浓度下对淡色库蚊的杀死率为100%,化合物20b、21b、24b、25b、26b、27b、30b在1000mg/L浓度下对朱砂叶螨的杀死率均达95%以上;N-取代苯并噁嗪啉酮类化合物具有良好的除草活性,如化合物3d,5d,6d,7d和8d在浓度为100mg/L时,对苋菜Ambrosia tricolor Linn的抑制率达90%。A series of novel N-substituted benzoxazol-2-ones and N-substituted benzoxazinone derivatives were designed and synthesized by the stating material 2-amino phenol Their structures were confirmed by ^1H NMR and elemental analysis. The preliminary bioassay showed that N-substituted benzoxazol-2-ones had insecticidal and fungicidal activities. The mortality of compounds 3b, 4b, 14b, 19b to Culex pipiens pallens Coqjllett at the concentration of 50 mg/L reached 100%, The mortality of compounds 20b, 21b, 24b, 25b, 26b, 27b, 30 b to Tetranychus cennbarinus at the concentration of 1 000 mg/L was all upwards 95%. Well, N-substituted benzoxazinone derivatives had herbicidal activity. The inhibition rate of 3d, 5d, 6d, 7d and 8d toAmbrosia tricolor Lima at the concentration of 100 mg/L was up to 90%.

关 键 词：苯并噁唑啉酮 苯并噁嗪啉酮 合成 生物活性 

分 类 号：O626[理学—有机化学]