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1. (WO2018051972) NAHLSGEN OPTICAL RESOLUTION METHOD

Pub. No.:    WO/2018/051972    International Application No.:    PCT/JP2017/032829
Publication Date: Fri Mar 23 00:59:59 CET 2018 International Filing Date: Wed Sep 13 01:59:59 CEST 2017
IPC: C07F 9/40
A61P 17/00
C07B 57/00
C07B 63/00
A61K 31/662
A61P 37/08
Applicants: KYOTO UNIVERSITY
国立大学法人京都大学
Inventors: HIRATAKE, Jun
平竹潤
WATANABE, Bunta
渡辺文太
YOSHIOKA, Ryuzo
吉岡龍藏
ISHIDA, Hideaki
石田英晃
Title: NAHLSGEN OPTICAL RESOLUTION METHOD
Abstract:
Provided is a method for separating the four optical isomers of Nahlsgen. According to the present invention, a method for producing a mixture of D-2-amino-4-[(Rp)-(3-carboxymethylphenoxy)(methoxy)phosphoryl]butanoic acid hydrate and L-2-amino-4-[(Sp)-(3-carboxymethylphenoxy)(methoxy)phosphoryl]butanoic acid hydrate is characterized by comprising a step of: subjecting a mixture of the four optical isomers represented by the following formula (1') to fractional crystallization using water or a mixed solvent of water and a water-soluble organic solvent, and causing a mixture of a compound represented by the following formula (1-1'-1) and a compound represented by the following formula (1-4'-1) to deposit.