新型丹皮酚氨基酸酯Schiff碱衍生物的合成与表征

SYNTHESIS AND CHARACTERIZATION OF NOVEL AMINO ACID ESTER SCHIFF BASE DERIVATIVES OF PAEONOL

为了进一步提高丹皮酚的生物活性,以丹皮酚和L-氨基酸酯为原料,在二乙胺作用下合成了一系列丹皮酚的氨基酸酯Schiff碱衍生物,并且具有较高的产率,所有产物均通过IR、1H NMR、13C NMR、HR MS等方法进行了表征,部分化合物通过X-ray单晶结构的证实.此外,对该反应的条件进行了优化:以甲醇为溶剂,反应温度为45℃,反应时间为10 h,反应物的物质的量比为1∶2.5,目标产物最高产率可达85%.

In order to improve the biological activities of paeonol, we synthesized a series of amino acid ester Schiff base derivatives of paeonol from paeonol and L-amino acid esters in the presence of diethylamine. The result showed that the products had a high yield. All of the products were characterized by IR,1H NMR,1~3C NMR, HR MS and the like; and the structure of a portion of the compounds was confirmed by X-ray single crystal. In addition, the reaction conditions were optimized as follows： reaction temperature 45 ℃, reaction time 10 hours, the mass ratio of reactants 1：2.5, and methanol as solvent. Under the optimized conditions, the highest yield of the target product reached 85%.