发明名称 |
OPTICAL RESOLUTION OF ALKYL 1,4-BENZODIOXAN-2-CARBOXYLATES USING ESTERASE FROM SERRATIA MARCESCENS |
摘要 |
<p>A process for resolving racemic alkyl 1,4-benzodioxan-2-carboxylates useful as intermediates in the synthesis of optically pure pharmaceutical compounds such as (S)-doxazosin is disclosed. The process utilizes a microbial enzyme derived from Serratia marcescens to catalyze the enantioselective hydrolysis of the alkyl (S)-1,4-benzodioxan-2-carboxylate enantiomer of the racemic mixture to its corresponding carboxylic acid at a faster rate than the R-enantiomer. An enantiomerically pure S-configured carboxylic acid is thereby formed for subsequent pharmaceutical synthesis. The nonhydrolyzed alkyl (R)-1,4-benzodioxan-2-carboxylate enantiomer can also be isolated and racemized, and the enzymatic hydrolysis reaction repeated.</p> |
申请公布号 |
EP0833937(B1) |
申请公布日期 |
2002.01.23 |
申请号 |
EP19960918471 |
申请日期 |
1996.06.07 |
申请人 |
SEPRACOR, INC. |
发明人 |
ROSSI, RICHARD, F., JR.;ZEPP, CHARLES, M.;HEEFNER, DONALD, L. |
分类号 |
C12P17/06;C12P41/00;(IPC1-7):C12P41/00 |
主分类号 |
C12P17/06 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|