METHOD FOR RACEMIZING ENANTIOMERS OF N-[4-(1-AMINO-ETHYL)-2,6-DIFLUORO-PHENYL]-METHANESULFONAMIDE

• Main Authors: WOO, Byoung Young, PARK, Young-Ho, LEE, Ki-Wha, PARK, Miyoung
• Format: Patent
• Language: English; French; Korean
• Published: 28.06.2018
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

Disclosed in the specification is a method which selectively separates an R type enantiomer contained in a racemate (R/S=1/1) of N-[4-(1-amino-ethyl)-2,6-difluoro-phenyl]-methanesulfonamide, and then can convert the same back into the racemate (R/S=1/1) of N-[4-(1-amino-ethyl)-2,6-difluoro-phenyl]-methanesulfonamide through racemization of the remaining S type enantiomer. According to the method, S type enantiomers which were discarded in the past can be recycled, which is economical, and the S type enantiomers can be racemized without contamination due to material changes at a higher yield than the existing recycling technology. La présente invention concerne un procédé qui sépare sélectivement un énantiomère de type R contenu dans un racémate (R/S = 1/1) de N-[4-(1-amino-éthyl)-2,6-difluoro-phényl]-méthanesulfonamide, et permet ensuite de le convertir en racémate (R/S = 1 /1) de N-[4-(1-amino-éthyl)-2,6-difluoro-phényl]-méthanesulfonamide par racémisation de l'énantiomère de type S restant. Selon le procédé, des énantiomères de type S qui étaient rejetés dans le passé peuvent être recyclés, ce qui est économique, et les énantiomères de type S peuvent être soumis à une racémisation sans contamination en raison de changements de matériau à un rendement supérieur à celui de la technologie de recyclage existante. 본 명세서에는 N-[4-(1-아미노-에틸)-2,6-다이플루오로-페닐]-메테인설폰아마이드의 라세미체(R/S=1/1)에 포함된 R형 거울상 이성질체를 선택적으로 분리 후 남은 S형 거울상 이성질체를 라세미화를 통해 다시 N-[4-(1-아미노-에틸)-2,6-다이플루오로-페닐]-메테인설폰아마이드의 라세미체(R/S=1/1)로 전환시킬 수 있는 방법이 개시된다. 상기 방법에 따르면 기존에 버려지던 상기 S형 거울상 이성질체를 재활용할 수 있어 경제적이며, 기존의 재활용 기술보다 더 높은 수율로 물질 변화에 의한 오염없이 S형 거울상 이성질체를 라세미화 할 수 있다.