公开(公告)号：US20220411369A1

公开(公告)日：2022-12-29

申请号：US17777943

申请日：2020-11-18

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Atsuko NISHIGUCHI ,  Osamu YABE ,  Yoshihiro BANNO

IPC: C07D207/14

Abstract: The present invention provides a production method suitable for industrial production of (2S,3S)-3-amino-2-(3-bromo-2-fluorobenzyl)pyrrolidine having a protecting group at the 1-position.
The present invention is a method for producing N-[(4-methylphenyl)sulfonyl]-L-phenylalanine salt of (2S,3S)-3-amino-2-(3-bromo-2-fluorobenzyl)pyrrolidine having a protecting group at the 1-position, which comprises Step 2: a step of subjecting 2-(3-bromo-2-fluorobenzyl)-3-(methoxyimino)pyrrolidine having a protecting group at the 1-position to a reduction reaction; and Step 3: a step of subjecting the product obtained in Step 2 to optical resolution using salt formation with N-[(4-methylphenyl)sulfonyl]-L-phenylalanine.