公开(公告)号：US20170174622A1

公开(公告)日：2017-06-22

申请号：US15129927

申请日：2015-03-23

Applicant: KANEKA CORPORATION

Inventor： Koji MACHIDA ,  Kohei MORI ,  Narumi KISHIMOTO ,  Toshihiro TAKEDA

IPC: C07C277/08

CPC classification number: C07C277/08 ,  C07C279/24

Abstract: A tri-carbobenzoxy-arginine represented by the following formula (2): is produced by carbobenzoxylating the arginine or arginine derivative (1) represented by the following formula (1), or a salt thereof: by adding carbobenzoxy chloride and a base in a water/organic solvent bilayer system to an arginine or arginine derivative (1) represented by the formula (1), or a salt thereof.

公开(公告)号：US20130079525A1

公开(公告)日：2013-03-28

申请号：US13682840

申请日：2012-11-21

Applicant: KANEKA CORPORATION

Inventor： Kohei MORI ,  Masutoshi NOJIRI ,  Akira NISHIYAMA ,  Naoaki TAOKA

IPC: C07D211/56 ,  C07D211/60

CPC classification number: C07D211/60 ,  C07B57/00 ,  C07D211/56 ,  C12P17/12 ,  C12P41/006

Abstract: The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.