METHOD FOR PREPARING (R)-N-[4-(1-AMINO-ETHYL)-2,6-DIFLUORO-PHENYL]-METHANESULFONAMIDE

Disclosed in the present specification is a method capable of preparing N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide (INT028-2) with high optical purity, through the selection of Ellman-chiral auxiliaries and the re-crystallization and separation...

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Hauptverfasser: WOO, Byoung Young, RAMAMOHAN, M, REGATI, Sridhar, LEE, Jihae, JAYAPRAKASH, Sarva, PARK, Young-Ho, SRINIVAS, Mamidi, LEE, Ki-Wha, CHOI, Chang Soon, PARK, Miyoung, PATEL, Krushnakant
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creator WOO, Byoung Young
RAMAMOHAN, M
REGATI, Sridhar
LEE, Jihae
JAYAPRAKASH, Sarva
PARK, Young-Ho
SRINIVAS, Mamidi
LEE, Ki-Wha
CHOI, Chang Soon
PARK, Miyoung
PATEL, Krushnakant
description Disclosed in the present specification is a method capable of preparing N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide (INT028-2) with high optical purity, through the selection of Ellman-chiral auxiliaries and the re-crystallization and separation of optical isomers. According to the above method, high-purity N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide with excellent quality can be produced at room temperature by improving cryogenic process conditions necessary for realizing high optical purity, and thus the trimming due to the process failure rate can be remarkably reduced.
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PERFORMING OPERATIONS
PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
SEPARATION
TRANSPORTING
title METHOD FOR PREPARING (R)-N-[4-(1-AMINO-ETHYL)-2,6-DIFLUORO-PHENYL]-METHANESULFONAMIDE
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