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有机化学 ›› 2006, Vol. 26 ›› Issue (11): 1539-1543. 上一篇    下一篇

研究论文

N-{2-氯-5-[3-甲基-2,6-二氧-4-三氟甲基-2,3-二氢嘧啶-1(6H)-基]苯基}酰胺类化合物的合成及除草活性

黄明智*,a,b，张泉a，任叶果b，雷满香b，黄路b
任竞b，杨光富*,a   

  1. (a华中师范大学化学学院 武汉 430079)
    (b湖南化工研究院 长沙 410007)
  • 收稿日期:2005-12-22 修回日期:1900-01-01 发布日期:2006-10-27
  • 通讯作者: 杨光富

Synthesis and Herbicidal Activity of N-{2-Chloro-5-[3-methyl-2,6-dioxo- 4-trifluoro-methyl-2,3-dihydropyrimidin-1(6H)-yl]phenyl} Amides

HUANG Ming-Zhi*,a,b,ZHANG Quana,REN Ye-Guob,LEI Man-Xiangb
HUANG Lub,REN Jingb,YANG Guang-Fu*,a   

  1. (a College of Chemistry, Central China Normal University, Wuhan 430079)
    (b Hunan Research Institute of Chemical Industry, Changsha 410007)
  • Received:2005-12-22 Revised:1900-01-01 Published:2006-10-27
  • Contact: YANG Guang-Fu

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为了寻找高效、安全的除草活性化合物, 合成了12个全新的N-{2-氯-5-[3-甲基-2,6-二氧-4-三氟甲基-2,3-二氢嘧啶-1(6H)-基]苯基}酰胺类化合物, 其化学结构经IR, 1H NMR, LC/MS和元素分析确证. 初步生物活性测定结果表明, 该类化合物具有一定的除草活性, 如7a, 7b, 7c, 7g, 7h, 7i, 7k和7l在有效成分75 g/hm2剂量下, 茎叶处理对苘麻(Abutilon theophrasti)、刺苋(Amaranthus spinosus)等阔叶杂草具有良好的除草活性, 其抑制率达100%.

关键词: 脲嘧啶, 原卟啉原氧化酶, 除草活性, 合成

In search of safer and more efficacious herbicidal compounds, twelve N-{2-chloro-5-[3-methyl-2,6-dioxo-4-trifluoromethyl-2,3-dihydropyrimidin-1(6H)-yl]phenyl} amides were synthesized. Their structures were confirmed by IR, 1H NMR, LC/MS spectra and elemental analysis. Preliminary bioassay showed that most of title compounds had good herbicidal ac-tivity, for example, 7a, 7b, 7c, 7g, 7h, 7i, 7k and 7l exhibited 100% inhibition to broad-leaved weeds, such as Abutilon theophrasti and Amaranthus spinosus at active ingredient 75 g/hm2.

Key words: protox, synthesis, herbicidal activity, uracil