Chiral resolution method of n-[4-(1-aminoethyl)-phenyl]-sulfonamide derivatives

Verfahren zur chiralen auflösung von n-[4-(1-aminoethyl)-phenyl]-sulfonamid-derivaten

Procédé de résolution chirale de dérivés n-[4-(1-aminoéthyl)-phényl]-sulfonamide

Abstract

The present specification relates to a chiral resolution method of a stereoisomer mixture, comprising a step of mixing a stereoisomer mixture of compounds, in which an amine group is bound to an asymmetric carbon atom, with a chiral auxiliary and salt-forming auxiliary compound, wherein the chiral auxiliary is an O,O' -diacyltartaric acid derivative, more specifically, a 2,3-dibenzoyl-tartaric acid or O,O' -di- p -toluoyl tartaric acid, the salt-forming auxiliary compound is mandelic acid or camphorsulfonic acid, and an optical isomer having a high level of optical purity can be obtained by using the method. Therefore, according to one aspect of the present invention, the method can be useful in pharmaceutical or cosmetic field when preparing an optical isomer having a high optical purity.

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