R-N-[4-1---26--]- Method for manufacturing R-N-[4-1-AMINOETHYL-26-difluoro-PHENYL]- METHANESULFONAMIDE

R-N-[4-1---26--]- Method for manufacturing R-N-[4-1-AMINOETHYL-26-difluoro-PHENYL]- METHANESULFONAMIDE

The present specification discloses a method for manufacturing N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide (INT028-2) of high optical purity through selectivity of Ellman chiral auxiliary and recrystallization separation of optical isomers. Acco...

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Bibliographische Detailangaben
Hauptverfasser: PATEL KRUSHNAKANT, LEE JIHAE, JAYAPRAKASH SARVA, CHOI CHANG SOON, PARK MIYOUNG, WOO BYOUNG YOUNG, PARK YOUNG HO, LEE KI WHA, SRINIVAS MAMIDI, RAMAMOHAN M, REGATI SRIDHAR
Format: Patent
Sprache:eng ; kor
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PERFORMING OPERATIONS
PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SEPARATION
TRANSPORTING
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Zusammenfassung:The present specification discloses a method for manufacturing N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide (INT028-2) of high optical purity through selectivity of Ellman chiral auxiliary and recrystallization separation of optical isomers. According to the method, cryogenic process conditions necessary for realizing high optical purity are enhanced to manufacture N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide of high purity and excellent quality at room temperature, so that trimming due to process failure rate can be remarkably reduced. 본 명세서에는 엘만 키랄 보조체의 선택성과 광학이성질체의 재결정 분리를 통해서, 높은 광학순도의 N-[4-[(1R)-1-[[(R)-(1,1-디메틸에틸)설피닐]아미노]에틸]-2,6-디플루오로페닐]-메탄설폰아미드(INT028-2)를 제조할 수 있는 방법이 개시된다. 상기 방법에 따르면 높은 광학순도를 구현하기 위해 필요한 극저온의 공정조건을 개선하여 상온에서 높은 순도의 N-[4-[(1R)-1-[[(R)-(1,1-디메틸에틸)설피닐]아미노]에틸]-2,6-디플루오로페닐]-메탄설폰아미드를 우수한 품질로 제조할 수 있으므로 공정 실패율에 따른 손질을 현저하게 감소시킬 수 있다.