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2,3-二甲基喹啉类化合物的合成及其生物活性

Synthesis and Biological Activity of 2,3-dimethylquinoline Derivatives

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【作者】 范文玉; 姜艾汝; 田俊峰; 郝树林; 徐英; 李志念;

【Author】 FAN wen-yu1,JIANG ai-ru1,2,TIAN jun-feng2,HAO Shu-lin2,XU ying2,LI Zhi-nian2 (1.Shenyang University of Chemical Technology,Shenyang 110142,China;2.State Key Laboratory of the Discovery and Development of Novel Pesticide,Shenyang Research Institute of Chemical Industry Co.,Ltd.,Shenyang 110021,China)

【机构】 沈阳化工大学; 沈阳化工研究院有限公司新农药创制与开发国家重点实验室;

【摘要】 [目的]喹啉类化合物具有广泛的生物活性,寻找更好的高活性化合物并进行先导结构优化。[方法]以取代的2,3-二甲基-4-羟基喹啉作为中间体,利用中间体衍生化方法进行合成。[结果]合成了喹啉酯、喹啉醚及喹啉胺3类新化合物,其结构得到了NMR的表征和确认。[结论]生测结果表明,部分目标化合物对水稻稻瘟病、小麦白粉病有较好的防效。

【Abstract】 Quinolines possess a broad spectrum of biological activity,the purpose of this article is to search for better compound with high activity and then to carry out optimization around the lead structure.[Methods] The intermediate derivatization methods was adopted to synthesize the target compounds based on 2,3-dimethyl-4-hydroxy quinoline as intermediates.[Results] Quinoline ester,quinoline ether and quinoline amines were synthesized in this paper.All structures of the synthesized compounds were confirmed by 1H NMR.[Conclusions] Preliminary bioassay indicated that,some synthesized compounds have good fungicidal activities against Rice Blast and Wheat powdery mildew.

【基金】 国家重点基础研究发展规划项目(973项目:2010CB126105,2010CB735601,2012CB724501);国家“十二五”科技支撑计划项目(2011BAE06B00,2011BAE06B01,2011BAE06B02,2011BAE06B03,2011BAE06B05)
  • 【分类号】TQ450.6
  • 【被引频次】1
  • 【下载频次】212
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