有机化学 ›› 2006, Vol. 26 ›› Issue (11): 1600-1605. 上一篇    下一篇

研究简报

4-吡唑基-2-芳氧基嘧啶类化合物的合成及除草活性

刘卫敏,邹小毛,宋洪海,汪义丰,朱有全,杨华铮*   

  1. (南开大学元素有机化学国家重点实验室 元素有机化学研究所 天津 300071)
  • 收稿日期:2006-03-30 修回日期:1900-01-01 发布日期:2006-10-27
  • 通讯作者: 杨华铮

Synthesis and Herbicidal Activity of 4-Pyrazolyl-2-aryloxypyrimidine Derivatives

LIU Wei-Min,ZOU Xiao-Mao,SONG Hong-Hai,WANG Yi-Feng
ZHU You-Quan,YANG Hua-Zheng*   

  1. (State Key Laboratory of Elemento-organic Chemistry, Institute of Elemento-organic Chemis-try,
    Nankai University, Tianjin 300071)
  • Received:2006-03-30 Revised:1900-01-01 Published:2006-10-27
  • Contact: YANG Hua-Zheng

以2,4-二氯嘧啶为起始原料, 利用两个氯原子的活性差异, 经4-吡唑基-2-氯嘧啶合成了一系列4-吡唑基-2-芳氧基嘧啶类化合物, 通过1H NMR和元素分析对所合成的化合物进行了结构表征. 初步生物活性测定结果表明, 所合成的化合物都表现出一定的除草活性. 当嘧啶环2位的氯原子被芳氧基取代后, 化合物的除草活性均有不同程度的提高, 例如5c4a相比, 100 μg•mL-1时化合物对油菜的抑制率由15.7%提高到85.4%, 对稗草的抑制率由原来的11.6%提高到84.0%.

关键词: 嘧啶, 吡唑, 除草活性, 合成

In order to search for novel compounds with herbicidal activity, a series of 4-pyrazolyl- 2-aryloxypyrimidine derivatives were designed and synthesized using 2,4-dichloropyrimidine as a starting material. All compounds synthesized were confirmed by 1H NMR and elementary analysis. Preliminary bioassay results indicated that some compounds display herbicidal activity. For example, compound 5c exhibit igher than 80% inhibition activity against rape and barnyard grass in dosage of 100 μg•mL-1.

Key words: pyrazole, synthesis, herbicidal activity, pyrimidine