公开(公告)号：US20220144774A1

公开(公告)日：2022-05-12

申请号：US17594062

申请日：2020-04-03

申请人： YUHAN CORPORATION

发明人： Sang-Ho OH ,  Doo-Byung LEE ,  Kyoung-Chan KWON ,  Sang-Won KIM ,  Hyo-Ick HWANG ,  Kyeong-Sill LEE ,  Ik-Su JO ,  Ji-Hye CHOI ,  Sung-Hee CHO ,  Su-Young LEE

IPC分类号： C07D211/56 ,  C07D487/04

摘要： Provided are a novel process for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof, which is an intermediate useful for the preparation of tofacitinib, an intermediate used in the process, i.e., isopropanol solvate of methyl ((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)carbamate dibenzoyl-L-tartrate, an intermediate, having excellent stability, useful for the preparation of tofacitinib, i.e., (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine acetate, and a process for preparing tofacitinib or a pharmaceutically acceptable salt thereof.