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

Disclosed in the present invention 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 therefore, the trimming due to the process failure rate can be remarkably reduced. 本说明书公开了一种方法，该方法可利用Ellman手性助剂的选择性及光学异构体的重结晶和分离，以制备具高光学纯度的N-[4-[(1R)-1-[[(R)-(1,1-二甲基乙基)亚磺酰基]胺基]乙基]-2,6-二氟苯基]甲烷磺酰胺(INT028-2)。根据上述方法，通过改善实现高光学纯度所必须的低温工艺条件，可在室温下制备质量优良、具高光学纯度的N-[4-[(1R)-1-[[(R)-(1,1-二甲基乙基)亚磺酰基]胺基]乙基]-2,6-二氟苯基]甲烷磺酰胺，因此可显著减少由于工艺失败率导致的损失。