高等学校化学学报

高等学校化学学报

• 研究论文 • 上一篇    下一篇

N-苄氧/烷氧苯基-4,6-二取代嘧啶胺类化合物的合成、晶体结构及除草活性

乌婧, 王宝雷, 李永红, 宋海滨, 王素华, 李正名   

  1. 南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 天津市农药科学重点实验室, 天津 300071
  • 收稿日期:2007-10-08 修回日期:1900-01-01 出版日期:2008-08-10 发布日期:2008-08-10
  • 通讯作者: 李正名

Synthesis, Crystal Structure and Biological Activity of N-(4-Benzyloxy/alkyloxyphenyl)-4,6-disubstituted-2-pyrimidinyl-amine Derivatives

WU Jing, WANG Bao-Lei, LI Yong-Hong, SONG Hai-Bin, WANG Su-Hua, LI Zheng-Ming*   

  1. Institute of Elemento-Organic Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Tianjin Key Laboratory of Pesticide Science, Nankai University, Tianjin 300071, China
  • Received:2007-10-08 Revised:1900-01-01 Online:2008-08-10 Published:2008-08-10
  • Contact: LI Zheng-Ming

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摘要： 以5种苄氧基/烷氧基苯胺为基础, 设计合成了系列新颖的N-苄氧/烷氧苯基-4,6-二取代嘧啶胺类化合物, 其结构经1H NMR、MS及元素分析确证, 其中化合物5r的单晶结构经X射线单晶衍射分析确证. 油菜平皿法和稗草小杯法测试除草活性结果表明, 4种苄氧基/烷氧基苯胺3a, 3b, 3d, 3e具有较好的除草活性, 在100 μg/mL浓度下对单子叶稗草生长抑制率可达到77.3%—88.5%. KARI活性测试结果表明, 化合物5a—5s有较弱的KARI抑制活性.

关键词: 嘧啶胺, 晶体结构, 除草活性, KARI活性

Abstract: On the basis of the structures of five 4-benzyloxy/alkyloxy-anilines, 19 N-(4-benzyloxy/alkyloxy-phenyl)-(4,6-disubstituted-pyrimidin-2-yl)-amine derivatives were designed and synthesized. The structures of all the compounds were characterized by 1H NMR, MS and elemental analyses. The single crystal structure of compound 5r was determined to further elucidate the structure. The herbicidal activity of the title compounds was evaluated through barnyardgrass cup, rape root methods and KARI test. Herbicidal assay indicate that substituted-anilines 3a, 3b, 3d, 3e exhibited good growth inhibitory activities against barnyardgrass, which are 88.5%, 77.3%, 82.4%, and 80.2%, respectively at the mass concentration of 100 μg/mL. The KARI test of compounds 5a—5s show that the compounds have a weak inhibitory effect on KARI enzyme.

Key words: Pyrimidin-2-yl-amine, Crystal structure, Herbicidal activity, KARI activity

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