PROCESS FOR PRODUCING METOPROLOL ENANTIOMER FROM METOPROLOL RACEMATE

摘要

PURPOSE: A process of preparing enantiomer by adding menthyl chloroformate as an isomerizing agent to metoprolol racemate and hydrolyzing is provided which produces the title compound in high yield and at low cost. CONSTITUTION: A process comprises the steps of (1) obtaining ()-diastereomers by adding menthyl chloroformate as an isomerizing agent to metoprolol racemate, (2) separating (+), (-)-diastereomer from obtained ()-diastereomers using a high performance liquid chromatography, and (3) obtaining enantiomer by hydrolyzing the separated (+), (-)-diastereomer. The process can obtain high purity (+), (-)-diastereomer enantiomer as compared with conventional asymmetric synthesis or chiral chromatography.