OPTICALLY ACTIVE PIPERIDINE DERIVATIVE AND ITS PRODUCTION

PROBLEM TO BE SOLVED: To produce a diasteremoer salt useful as an intermediate for syntheses of pharmaceuticals having antihistaminic and antiallergic activities by optically resolving a specific piperazine derivative by using L(+)-tartaric acid. SOLUTION: This diastereomer, which consists of (S)-(-...

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Bibliographische Detailangaben
Hauptverfasser: KITA JUNICHIRO, TAKAMURA SHINJI
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To produce a diasteremoer salt useful as an intermediate for syntheses of pharmaceuticals having antihistaminic and antiallergic activities by optically resolving a specific piperazine derivative by using L(+)-tartaric acid. SOLUTION: This diastereomer, which consists of (S)-(-)-4-[(4-chlorophenyl)(2- pyridyl)methoxyl]piperidine.L(+)-tartarate of formula I, is obtained by making a racemic modification of formula II react with L(+)-tartaric acid, and fractivonally crystallizing the formed salt. Furthermore, by treating this diastereomer slat with an alkali to decompose, (S)-(-)-4-[(4-chlorophenyl)(2- pyrizyl)methoxyl]piperidine can be obtained.