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新型4,4-二甲基异噁唑-3-酮衍生物的合成及生物活性研究
引用本文:杨桂秋,孙挺,于秀兰.新型4,4-二甲基异噁唑-3-酮衍生物的合成及生物活性研究[J].化学通报,2006,69(12):921-925.
作者姓名:杨桂秋  孙挺  于秀兰
作者单位:东北大学理学院,东北大学理学院,沈阳化工学院制药工程系 沈阳110004,沈阳化工学院制药工程系,沈阳110142,沈阳110004,沈阳110142
摘    要:以Baylis-Hillman加成物为起始原料,设计并合成了5个结构新颖的4,4-二甲基异唑-3-酮衍生物。所合成的化合物经IR、1HNMR和元素分析确证。生物活性测试结果表明,所合成的目标产物在2000gai/ha的剂量下均具有较好的除草活性。中间体1-(2,4-二氯苯基)-2-溴甲基丙烯酸乙酯具有杀虫活性,在600gai/ha的剂量下对朱砂叶螨防效为100%。

关 键 词:Baylis-Hillman加成物  N-取代-4  4-二甲基异噁唑-3-酮  合成  生物活性
收稿时间:2006-02-27
修稿时间:2006-02-272006-09-25

Synthesis and Biological Activity of Novel 4,4-Dimethylisoxazolidin-3-one Derivatives
Yang Guiqiu,Sun Ting,Yu Xiulan.Synthesis and Biological Activity of Novel 4,4-Dimethylisoxazolidin-3-one Derivatives[J].Chemistry,2006,69(12):921-925.
Authors:Yang Guiqiu  Sun Ting  Yu Xiulan
Institution:1.School of Sciences, Northeastern University, Shenyang 110004; 2.Department of Pharmaceutical Engineering, Shenyang Institute of Chemical Technology, Shenyang 110142
Abstract:Five novel 4,4-dimethylisoxazolidin-3-one derivatives were designed and synthesized utilizing Baylis-Hillman adducts as starting materials. Their structures were confirmed by IR, ~1H NMR and elemental analysis. Evaluation of their biological activities indicated that the target compounds exhibited efficient herbicidal activity at 2000g ai/ha, while the intermediate ethyl 1-(2,4-dichlorophenyl)-2-bromomethyl-acrylate showed insecticidal activity with 100% control of tetranychus cinnabarinus at 600g ai/ha.
Keywords:Baylis-Hillman adduct  N-Substituted-4  4-dimethylisoxazolidin-3-one  Synthesis  Biological activity
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