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

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

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％．

In search of safer and more efficacious herbicidal compounds, twelve N-{2-chloro-5- [3-methyl-2,6-dioxo-4-trifluoromethyl-2,3-dihydropyrimidin-l（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 activity, for example, 7a, 7b, 7c, 7g, 7h, 7i, 7k and 71 exhibited 100% inhibition to broad-leaved weeds, such as Abutilon theophrasti and Amaranthus spinosus at active ingredient 75 g/hm^2.