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含杂环甲胺基的氰基丙烯酸酯类光合作用抑制剂的合成和活性研究进展
Synthesis and Herbicidal Activity of 2-Cyano-3-heterocyclomethylaminoacrylates
【摘要】 氰基丙烯酸酯是一类PSII电子传递抑制剂,笔者发现在抑制剂分子疏水性基团苯环被吡啶替代能大大提高其抑制活性,对此先导结构进一步优化,设计合成以下系列新化合物:含2-氯(或烷氧基)-5-吡啶甲胺基的氰基丙烯酸酯、含2-氟-5-吡啶甲胺基的氰基丙烯酸酯、含2-氯-5-噻唑甲胺基的氰基丙烯酸酯、氮在吡啶环不同位置的吡啶甲胺基氰基丙烯酸酯、含烷硫基取代的吡啶甲胺基的氰基丙烯酸酯、含二茂铁甲胺基的氰基丙烯酸酯。生测结果表明:这些含杂环甲胺基的氰基丙烯酸酯类化合物对油菜等十字花科类杂草表现出很好的除草活性,且茎叶处理优于土壤处理。
【Abstract】 2-Cyanoacrylate compounds are an inhibitor of photosystem II eletron transport.Six series of 2-cyano-3-heterocyclomethylaminoacrylates were synthesized including 2-cyano-3-(2-chloro-5-pyridyl)methylaminoacrylates,2-cyano-3-(2-alkoxy-5-pyridyl)methylaminoacrylates,2-cyano-3-(2-fluoro-5-pyridyl)methylaminoacrylates,2-cyano-3-(2-chlorothiazol-5-yl)methylaminoacrylates,2-cyano-3-(2-methylthio-5-pyridylmethylamino)acrylates and 2-cyano-3-ferrocenemethyl aminoacrylates.Their herbicidal activities were evaluated.Some compounds exhibited excellent herbicidal activities against barnyardgrass,redroot amaranth and rapae,even at a dose of 75 g a.i./hm2,and the herbicidal activity at post-emergent treatment was superior to that at pre-emergent treatment.
【Key words】 2-cyanoacrylates; heterocycle; herbicidal activity; inhibitors of PSII electron transport;
- 【文献出处】 精细化工中间体 ,Fine Chemical Intermediates , 编辑部邮箱 ,2006年05期
- 【分类号】TQ457
- 【被引频次】5
- 【下载频次】256