A facile enzymatic process for the preparation of (s)-Naproxen ester prodrug in organic solvents

被引:38
|
作者
Chang, CS [1 ]
Tsai, SW [1 ]
机构
[1] NATL CHENG KUNG UNIV,DEPT CHEM ENGN,TAINAN 70101,TAIWAN
关键词
prodrug; lipase; (s)-naproxen ester; esterification;
D O I
10.1016/S0141-0229(96)00222-0
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
A facile enzymatic synthesis process has been developed to directly prepare the 4-morpholinoethyl ester prodrug of (s)-Naproxen from racemic Naproxen using lipases as the biocatalysts in the organic solvent. With the careful selection of lipase (Lipase MY) and reaction medium (cyclohenane), a high enantiomeric ratio of 136 for the enzyme was obtained. A Ping-Pong Bi Bi mechanism with competitive inhibition by the alcohol was illustrated from the variation of initial rates with substrate concentrations. (C) 1997 by Elsevier Science Inc.
引用
收藏
页码:635 / 639
页数:5
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