较高光学纯度丹参素的制备方法研究  

Study on Preparation of Danshensu With High Enantiomeric Purity

作　　者：王黎[1] 尤静[1] 王丹[1] 雷媛 李永新 WANG Li;YOU Jing;WANG Dan;LEI Yuan;LI Yong-xin(College of Pharmacy,Xi'an Medical University,Shaanxi Xi'an 710021,China)

机构地区：[1]西安医学院药学院,陕西西安710021

出　　处：《当代化工》2018年第12期2518-2520,2525,共4页Contemporary Chemical Industry

基　　金：陕西省自然科学基础研究计划项目(No.2017JM8060);2016年国家级;省级大学生创新创业训练计划项目(No.201611840007;No.2273)

摘　　要：重要中药活性物质丹参素分子中含有一个手性碳原子,可以使用手性原料D-酪氨酸通过重氮化反应进行制备。然而,丹参素分子中的手性仲醇在现有重氮化反应条件下容易发生外消旋化,导致产物的光学纯度下降,也会增加后处理的难度,降低反应收率。本研究简要考察了产生外消旋化问题的原因,以产物的ee值与收率为指标,改进了该步骤反应的工艺,使产物ee值由16.9%提高至64.2%,提高了D-酪氨酸法制备丹参素工艺的工业化实用价值。The molecule of Danshensu as an traditional Chinese medicine active substance contains a chiral carbon atom,which can be prepared by the diazotization reaction from chiral material D-tyrosine.However,the chiral secondary alcohols in the Danshensu molecule are prone to be racemized under the conditions of diazotization reaction, which leads to the decrease of the enantiomeric purity of the products.In this paper,causes of the racemization was investigated,and the reaction process was improved to increase the ee value from 16.9% to 64.2%.

关 键 词：丹参素 光学纯度 重氮化反应 外消旋化 

分 类 号：R9[医药卫生—药学] TQ463[化学工程—制药化工]