羟基酪醇的合成方法  

Synthetic procedure for hydroxytyrosol

作　　者：肖艳[1] 张杨[2] 杨郁[2] 任凤霞[2] 崔广智[1] 赵毅民[2] 

机构地区：[1]天津中医药大学,天津300193 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《国际药学研究杂志》2013年第3期335-337,共3页Journal of International Pharmaceutical Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2012ZX09301003-001)

摘　　要：目的探索羟基酪醇的简便合成方法。方法以邻苯二酚和乙醛酸为原料,经3,4-二羟基扁桃酸合成羟基酪醇。尝试用亚硫酸氢钠或焦亚硫酸钠为还原剂脱除3,4-二羟基扁桃酸的α-羟基,考察了温度、反应时间等因素对收率的影响。结果利用改进的合成路线,经四步反应合成了羟基酪醇,总收率52.7%。结论改进后的合成路线成本较低,简便易行,有利于羟基酪醇的规模化制备。Objective To explore the possibility for convenient synthesis of hydroxytyrosol.Methods Based on catechol and glyoxylic acid,hydroxytyrosol was synthesized through the intermediate 3,4-dihydroxyamygdalic acid.Sodium bisulfite or sodium metabisulfite were used for the dehydroxylation of 3,4-dihydroxyamygdalic acid.The influences of the temperature and reaction time on the yield of the dehydroxylation were investigated.Results Hydroxytyrosol was synthesized in four steps by using the ameliorated method with a total yield of 52.7%.Conclusion The ameliorated method is economical,easy to carry out and possible to scale up for the preparation of hydroxytyrosol.

关 键 词：羟基酪醇 邻苯二酚 乙醛酸 化学合成 

分 类 号：R914[医药卫生—药物化学]