Sk Corporation

Sk Holdings Co., Ltd.

Sang-Chul Lim

Jong-Ho Lim

Ki-Nam Uhm

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.

Method for optically resolving a racemic &agr;-substituted heterocyclic carboxylic acid using enzyme

Disclosed is a method for preparing an R- or S-forms of &agr;-substituted heterocyclic carboxylic acid (&agr;-HCCA) and a counter enantiomeric form of &agr;-substituted heterocyclic carboxylic acid ester thereto by use of an enzyme. A racemic &agr;-HCCA is reacted with alcohol to give a racemic &agr;-HCCA ester, which is then brought into contact 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. Thus, a certain enantiomeric form of &agr;-HCCA and a counter enantiomeric form of &agr;-HCCA ester thereto, respectively can be prepared with high optical purity at high yields as well as at low cost.

Method for preparing an R- or S-form of &agr;-substituted heterocyclic carboxylic acid and a counter enantiomeric form of &agr;-substituted heterocyclic carboxylic acid ester thereto using enzyme

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Taejon, South Korea

Sang-Chul Lim