水溶性葛根素衍生物的合成  

Synthesis of puerarin derivatives

作　　者：朱盼 张彬[1] 向纪明 ZHU Pan;ZHANG Bin;XIANG Ji-ming(College of Chemistry and Chemical Engineering,Shaanxi University of Science&Technolog,Xi’an 710000,china;College of Chemistry and Chemical Engineering,Ankang University,Ankang 725000,china)

机构地区：[1]陕西科技大学化学化工学院,陕西西安710021 [2]安康学院化学化工学院,陕西安康725000

出　　处：《化学研究与应用》2019年第4期732-735,共4页Chemical Research and Application

摘　　要：以葛根素为起始原料,分别经亲核取代反应和羟甲基化反应得到水溶性4′-羟乙基葛根素和3′,5′-二羟甲基葛根素,对首次得到的3′,5′-二羟甲基葛根素,用正交实验对的合成条件进行了优化,当n(葛根素)∶n(甲醛)∶n(氢氧化钠)=1∶2∶4,反应温度为60℃,反应时间为4.0 h,产率为69.0%。目标化合物的结构经IR、~1H NMR、^(13)C NMR和元素分析方法进行表征。经测试4′-羟乙基葛根素和3′,5′-二羟甲基葛根素水溶性分别是葛根素的5倍和10倍。Water-soluble 4′-hydroxyethyl puerarin and 3′,5′-dihydroxymethyl puerarin were synthesized by nucleophilic substitution and hydroxymethylation respectively from puerarin as raw materials.The optimum synthetic conditions of 3′,5′-dihydroxymethyl puerarin was studied for the first time by the four factors and three levels orthogonal experiment.The optimal mole ratio was n(puerarin)∶n(methanal)∶n(sodium hydroxide)=1∶2∶4,the reaction temperature 60℃and the reaction time 4h.The yield under the optimum conditions was up to 69.0%.The target molecules was characterized by IR,1H NMR,13 C NMR spectra and elemental analysis.The water solubility of 4′-hydroxyethyl puerarin and 3′,5′-dihydroxymethyl puerarin were 5 times and 10 times that of puerarin.

关 键 词：葛根素 水溶性葛根素 合成 

分 类 号：O621.3[理学—有机化学]