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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苯甲酰基乙烯醇结构的2-取代苯甲酰基-5-烷基-环戊酮类化合物.以己二酸二乙酯为原料,经6步反应制得目标产物,其结构经IR,1H NMR,X射线及元素分析或高分辨质谱确证,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100μg/mL浓度下对油菜的抑制率达到60%以上.
In order to find out the new lead compounds with good biological activities, a series of 2-substituted benzoyl-5-alkyl-rings with benzoyl vinyl alcohol structure were designed and synthesized based on the structural features of many highly active compounds. Pentanones, diethyl adipate as raw materials, the target product was obtained after 6 steps, the structure of which was confirmed by IR, 1H NMR, X-ray and elemental analysis or high resolution mass spectrometry. The preliminary bioassay results showed that some compounds showed obvious inhibitory activity on rapeseed, and the inhibition rate of rapeseed reached more than 60% at the concentration of 100μg / mL.