IP Library Granted Patent US 9,981,984
Granted Patent B2
US 9,981,984 · App. 14/431,141 · Granted May 29, 2018

Method for producing cis-5-hydroxy-2-piperidinecarboxylic acid derivative, and method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid

Inventors: Tomoko Maeda (Kanagawa, JP); Hisatoshi Uehara (Kanagawa, JP); Yasuyo Saito (Kanagawa, JP); Masato Murai (Fukuoka, JP)
Assignee: API Corporation
C07D498/08C07D211/60C12P17/12Y02P20/55
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Quick Facts
Patent No.
US 9,981,984
App. No.
14/431,141
Granted
May 29, 2018
Kind
B2
Abstract

The present invention aims to provide a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid with high purity, and a method for producing its derivative. The present invention provides a method for producing a cis-5-hydroxy-2-piperidinecarboxylic acid derivative, which method comprises a step of converting cis-5-hydroxy-2-piperidinecarboxylic acid into a compound(s) of Formula (1) and/or Formula (2) (wherein R 1 represents a protective group for an amino group, and R2 represents a C 1 -C 6 alkyl group), and a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid.

Claims (13)

1. A method for producing a compound of Formula (1), said method comprising a step of reacting a mixture containing cis-5-hydroxy-2-piperidinecarboxylic acid and an impurity with a single kind of an acid halide, an acid anhydride, an acid halide and an acid anhydride in a single reactor to convert said cis-5-hydroxy-2-piperidinecarboxylic acid into a compound of Formula (1) by protecting and lactonizing said cis-5-hydroxy-2-piperidinecarboxylic acid with the single kind of the acid halide, the acid anhydride, or the acid halide and the acid anhydride in the single reactor,

wherein R 1 represents a protective group for an amino group, and

wherein the impurity comprises trans-5-hydroxy-2-piperidinecarboxylic acid.

2. The method according to claim 1 , further comprising the step of synthesizing cis-5-hydroxy-2-piperidinecarboxylic acid by bacterial reaction and/or enzymatic reaction.

3. The method according to claim 1 , further comprising a step of separating the compound of Formula (1) by crystallization or solvent extraction.

4. The method according to claim 1 , wherein said impurity further comprises (2S,3S)-3-hydroxy-2-piperidinecarboxylic acid.

5. The method according to claim 1 , wherein a mixture containing cis-5-hydroxy-2-piperidinecarboxylic acid and an impurity is reacted with a single kind of an acid halide.

6. The method according to claim 5 , wherein said acid halide comprises benzyloxycarbonyl chloride.

7. The method according to claim 1 , wherein:

the single kind of the acid halide, the acid anhydride, or the acid halide and the acid anhydride comprises the R 1 protective group;

the single kind of the acid halide, the acid anhydride, or the acid halide and the acid anhydride protects the amino group with the R 1 protective group in the compound of Formula (1); and

the single kind of the acid halide, the acid anhydride, or the acid halide and the acid anhydride allows the lactonization of the cis-5-hydroxy-2-piperidinecarboxylic acid to convert the cis-5-hydroxy-2-piperidinecarboxylic acid into the compound of Formula (1).

8. The method according to claim 1 , further comprising a step of separating the compound of Formula (1) by solvent extraction.

Assignments (3)
CHANGE OF ADDRESS Recorded Aug 21, 2025
From: API CORPORATION
To: API CORPORATION
Reel/Frame 072498/0511 →
MERGER Recorded Aug 21, 2025
From: API CORPORATION
To: UBE CORPORATION
Reel/Frame 072554/0211 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2015
From: MAEDA, TOMOKO; UEHARA, HISATOSHI; SAITO, YASUYO; MURAI, MASATO
To: API CORPORATION
Reel/Frame 035265/0727 →
Priority Claims (1)
JP 2012-278314 · Dec 20, 2012 · national
Continuity (1)
Related Publication 20150239906A1 · Aug 27, 2015