Method for optically resolving a racemic &agr;-substituted heterocyclic carboxylic acid using enzyme
US6455302B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | May 31, 2001 |
| Grant date | Sep 24, 2002 |
| Priority date | — |
| Expiry date | May 31, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12P41/005
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Disclosed is a method for optically resolving a racemic &agr;-substituted heterocyclic carboxylic acid (&agr;-HCCA) by taking advantage of enantioselectivity of enzymes. &agr;-HCCA is reacted with alcohol to give a racemic &agr;-HCCA ester, which is then reacted with an enzyme with enantioselectivity, whereby either R-form or S-form of the racemate is hydrolyzed. Extraction with an organic solvent can obtain enantiomers of the &agr;-HCCA ester. The extracted enantiomeric &agr;-HCCA ester is converted to enantiomeric &agr;-HCCA by catalytic hydrogenation in an organic solution or by enzymatic hydrolysis in an aqueous solution. Thus, a racemic mixture of &agr;-HCCA can be optically resolved with high optical purity at high yields as well as at low cost.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.