WO2025020992 - METHOD FOR RESOLVING PHENYLALANINE DERIVATIVE, AND INTERMEDIATE
National phase entry is expected:
Publication Number
WO/2025/020992
Publication Date
30.01.2025
International Application No.
PCT/CN2024/106107
International Filing Date
18.07.2024
Title **
[English]
METHOD FOR RESOLVING PHENYLALANINE DERIVATIVE, AND INTERMEDIATE
[French]
PROCÉDÉ DE RÉSOLUTION D'UN DÉRIVÉ DE PHÉNYLALANINE ET INTERMÉDIAIRE
[Chinese]
苯丙氨酸类衍生物的拆分方法和中间体
Applicants **
NEUBORON BIO-SCITECH CO., LTD.
Inventors
ZHOU, Ping
BIAN, Ya
WANG, Wei
CHEN, La-mei
CHEN, Lian-bao
LIU, Yuan-hao
Priority Data
202310903753.2
21.07.2023
CN
202410898850.1
05.07.2024
CN
Application details
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International Searching Authority |
CNIPA
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The Standard Agent's Assignment
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Legal Entity
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| Entry into National Phase under |
Chapter I
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1892 | |
| EPO | Filing, Examination, Granting | 13590 | |
| Japan | Filing, Examination, Granting | 2277 | |
| South Korea | Filing, Examination, Granting | 2431 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
24,930
The term for entry into the National Phase has expired. This quotation is for informational purposes only
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Abstract[English]
A method for resolving a phenylalanine derivative of formula (I), and an intermediate. The method comprises: a resolving step comprising using a resolving reagent to react with the phenylalanine derivative represented by formula (I) in a reaction solvent to obtain a resolved intermediate, wherein the resolving reagent is selected from N-acetyl-D-phenylalanine and/or (2R,3R)-(-)-dibenzoyl-L-tartaric acid, and the reaction solvent is selected from 90-99% aqueous ethanol, absolute ethyl alcohol, or acetone. The method uses a chiral reagent to perform salt formation and racemate resolution, and has the advantages of being easy to operate, requiring no special production devices, and being easy to scale up production.[French]
L'invention concerne un procédé de résolution d'un dérivé de phénylalanine de formule (I), et un intermédiaire. Le procédé comprend : une étape de résolution consistant à utiliser un réactif de résolution pour réagir avec le dérivé de phénylalanine représenté par la formule (I) dans un solvant de réaction pour obtenir un intermédiaire résolu, le réactif de résolution étant choisi parmi la N-acétyl-D-phénylalanine et/ou l'acide (2R,3R)-(-)-dibenzoyl-L-tartrique, et le solvant de réaction étant choisi parmi 90 à 99% d'éthanol aqueux, d'alcool éthylique absolu ou d'acétone. Le procédé utilise un réactif chiral pour effectuer une formation de sel et une résolution de racémate, et présente les avantages d'être facile à utiliser, ne nécessitant pas de dispositifs de production spéciaux, et d'être facile à mettre à l'échelle de production.[Chinese]
式(I)的苯丙氨酸类衍生物的拆分方法和中间体。所述方法包括拆分步骤：包括利用拆分试剂在反应溶剂中与式(I)所示苯丙氨酸类衍生物进行反应得到拆分中间体，所述拆分试剂选自N-乙酰-D-苯丙氨酸和/或(2R,3R)-(-)-二苯基甲酰基-L-酒石酸；所述反应溶剂选自90～99％的乙醇水溶液、无水乙醇或丙酮。所述方法使用手性试剂进行成盐拆分消旋体，具有操作简便，无需特殊的生产设备，生产规模易放大的优势。