第 43 卷第 2 期Vol. 43 No. 2
2013 年 4 月Apr 2013

所属栏目:医药及中间体

(R)-(-)-α-甲氧基苯乙酸的2种合成方法
沈思思,王吕鸣,孙金涛,沙 宇 (沈阳药科大学,基于靶点的药物设计与研究教育部重点实验室,辽宁 沈阳 110016)
摘 要:(R)-(-)-α-甲氧基苯乙酸的2种合成方法均是以简单易得的扁桃酸为原料,经醚化,或者经酯化醚化、水解得单一构型(R)-(-)-α-甲氧基苯乙酸,其结构经MS、1H NMR、13C NMR分析确证。产品纯度99.3%(HPLC),反应收率52.0%。路线一方法与原有文献相比,后处理操作简单、耗时短、收率高,而路线二方法是无文献报道的全新方法。2种方法均利于工业化生产。
关键词:(R)-(-)-α-甲氧基苯乙酸;扁桃酸;醚化;酯化;水解
中图分类号:O625.52  文献标识码:A  文章编号:1009-9212(2013)02-0037-02
Two Synthetic Methods of (R)-2-Methoxy-2-phenylacetic Acid
SHEN Si-si,WANG Lü-ming,SUN Jin-tao,SHA Yu (Key Laboratory of Structure-Based Drug Design & Discovery,Ministry of Education,Shenyang Pharmaceutical University,Shenyang 110016,China)
Abstract:(R)-2-Methoxy-2-phenylacetic acid was synthesized from mandelic acid via esterification-etherification and hydrolysis,or via only a single step of etherification. Its structure was confirmed by MS,1H NMR and 13C NMR. The purity of the product was 99.3% (HPLC),and overall yield was 52.0%. The former method shows the advantages of convenient operation,time saving and high yield,whereas the latter is a novel way never reported. These two methods are both suitable for industrial process.
Key words:(R)-2-methoxy-2-phenylacetic acid;mandelic acid;etherification;esterification ;hydrolysis
基金项目:辽宁省教育厅资助项目(2009226015-5)。
作者简介:沈思思(1987-),女,辽宁锦州人,硕士研究生,主要从事药物化学研究。(E-mail:shensisi-1987@163.com)
联 系 人:沙 宇(1975-),男,吉林长春人,副教授,硕士生导师,主要从事药物化学研究。(E-mail:shayu@syphu.edu.cn)
收稿日期:2013-01-20