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以A8169为先导,设计并合成了12个新型的N-氮杂环甲氧基-O-(4-芳氧基苯基)乳酸酰胺化合物,其结构经1H NMR,13C NMR,LC/MS和IR确证.初步生物活性测定结果表明,化合物在2250 g/ha剂量下,对单子叶杂草马唐(Digitaria sanguinalis)、稗草(Echinochloa crus-galli)、狗尾草(Setaria viridis)等均具有100%的除草活性,进一步活性筛选发现,(R)-(+)-N-[(2-氯噻唑-5-基)甲氧基]-O-[4-((6-氯喹喔啉-2-基)氧基)苯氧基]乳酸酰胺(2f)除草活性(马唐IC50=6.8g/ha,稗草IC50=6.6 g/ha)远高于同类商品化除草剂炔草酯和先导化合物A8169.
A8169 as the leader, 12 novel N-azacymethoxy-O- (4-aryloxyphenyl) lactic acid amide compounds were designed and synthesized. Their structures were confirmed by 1H NMR, 13C NMR, LC / MS and IR.The results of preliminary bioassay indicated that the compound had 100% of the same density on Digitaria sanguinalis, Echinochloa crus-galli, Setaria viridis and so on under the dosage of 2250 g / ha, The results showed that the activity of (R) - (+) - N - [(2-chlorothiazol-5-yl) methoxy] -O- [4- (2f) herbicidal activity (Cotatum IC50 = 6.8g / ha, IC50 of barnyard grass = 6.6g / ha) is much higher than that of the similar commercial herbicides clodinafonate and lead compound A8169 .