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为了发现具有良好生物活性的新型先导化合物,在综合多种高活性化合物结构特点的基础上,设计合成了一系列含4-取代-1,3-环戊二酮结构的三酮类化合物.以1,3-环戊二酮为原料,经六步反应制得目标物,其结构经IR,~1H NMR及高分辨质谱确证,并对该类化合物合成方法进行了探讨.初步室内生测结果表明,部分化合物对油菜表现出明显的抑制活性,在100 mg/L浓度下对油菜的抑制率达到80%以上.在1500 g/ha施药量情况下,部分化合物对油菜的土壤处理和茎叶处理均呈现出很好的防除效果,抑制率达到90%以上.
In order to find novel lead compounds with good biological activity, a series of 4-substituted-1,3-cyclopentadienone-based triketones were designed and synthesized based on the structural features of many highly active compounds. 1,3-cyclopentadione as raw material, the target compound was obtained through six steps, the structure was confirmed by IR, 1H NMR and high resolution mass spectrometry, and the synthetic methods of the compounds were also discussed. The results showed that some of the compounds showed obvious inhibitory activity on rapeseed, and the inhibition rate of rapeseed was above 80% at the concentration of 100 mg / L. Under the application rate of 1500 g / ha, Leaf treatment showed a good control effect, inhibition rate reached 90%.