N-氮杂环甲氧基-O-(4-芳氧基苯基)乳酸酰胺的合成与除草活性

Synthesis and Herbicidal Activity of Novel N-Hetrocyclo Containing Nitrogen Methoxy-O-(4-aryloxy-phenyl) Lactamide Derivatives

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.

The lead compound A8169 was modified, 12 N-hetrocyclo containing nitrogen methoxy-O-（4-aryloxy-phenyl） lactamide derivatives were designed and synthesized, and their structures were characterized by^ 1H NMR, ^13C NMR, LC/MS and IR. The bioassay results indicated that all compounds exhibited 100% activities against Digitaria sanguinalis, Echinochloa crus-galli L and Setaria Viridis at 2250 g/ha. In particular, （R）-（＋）-N-（（2-chlorothiazol-5-yl）methoxy）-O-（4-（（6-chloro-quinoxalin-2-yl）oxy）phenoxy） lactamide （2f） was much more effective against Digitaria sanguinalis （IC50=6.8 g/ha） and Echinochloa crus-galli （IC50=6.6 g/ha） than commercial clodinafop-propargyl and lead compound A8169.