OPTICAL RESOLUTION OF PIPERIDINE DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To efficiently optically resolve a racemic piperidine derivative by reacting the racemic piperidine derivative with an optically active propionic acid compound, separating and collecting the produced two kinds of diastereomer salts by utilizing the difference of solubility. SOLUTION: A racemic compound of formula I (X is a halogen) 4-[(4- halogenophenyl)(2-pyridyl)methoxy]piperidine} is reacted with an optically active propionic acid compound of formula II (Y is H or a halogen; Z is a lower alkoxy; * is an asymmetric carbon) [e.g. (2R,3R)-2-hydroxy-3-(4- methoxyphenyl)-3-(2-nitro-5-chlorophenylthio)propionic acid] to produce two kinds of diastereomer salts and either one of diastereomers is separated and collected by utilizing the difference of solubility of the resultant two kinds of diastereomer salts to optically resolve a racemic compound of formula I. The optically active substance of the compound of formula I is useful as a producing intermediate for optically active substances of a piperidine derivative of formula III (A is a 2-6C alkylene or the like; B is hydroxyl or the like).