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香豆素烟酸酯的合成及生物活性研究

         

摘要

以烟酸和香豆素为原料,通过缩合剂法合成香豆素烟酸酯.经过核磁共振氢谱、质谱确证目标化合物的化学结构.考察影响因素(反应溶剂、反应温度、反应时间、缩合剂种类)对酯化产物收率的影响,优选出最佳合成工艺.最佳合成工艺为反应温度为25 ℃、反应时间为24 h、最佳溶剂为乙腈、采用DCC/DMAP为缩合剂,生物活性测试表明,新合成的烟酸香豆素酯对肿瘤细胞具有一定的抑制作用.%Coumarin nicotinic acid ester was synthesized from nicotinic acid and coumarin by condensation agent method.Its chemical structure was confirmed by 1H NMR and MS spectroscopy.The influence factors(reaction solvents, reaction temperature, reaction time, condensing agents) were discussed on the yield of esterification product in order to select the optimal synthesis process.The results showed that the optimal synthetic conditions were as follows: reaction temperature 25 ℃, reaction temperature 24 h, dichloromethane as solvent and DCC/DMAP as condensation agent.The biological activity test showed that coumarin nicotinic acid ester had a certain inhibitory effect on tumor cells.

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