US 2026/0132101 A1 · METHOD FOR RESOLVING PHENYLALANINE DERIVATIVE, AND INTERMEDIATE

Abstract

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.

Claims20

Dependent claims

A chiral resolution method of a phenylalanine derivative represented by formula (I):

in which X is selected from Br, I, F, Cl, CN, SCN, or OCN;
R1 and R2 are each independently selected from:
hydrogen or tert-butoxycarbonyl;
R3 is selected from tert-butyl;
and
n=1 or 2;
wherein the method comprises a resolving step, comprising reacting a resolving agent with the phenylalanine derivative represented by formula (I) in a reaction solvent to obtain a resolution intermediate;
wherein the resolving agent 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 ethanol, or acetone.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application

19/444,307Filed 9 Jan 2026

Priority

CN 202310903753.221 Jul 2023

Published

14 May 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification11 codes

C07C 227/34
Preparation of optical isomers: by separation of optical isomers
C07C 227/42
Separation; Purification: crystallisation
C07C 69/78
Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring: benzoic acid esters
C07C 229/34
Having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton: the carbon skeleton containing six-membered aromatic rings

Method for resolving phenylalanine derivative, and intermediate

Life of this patent

Method for resolving phenylalanine derivative, and intermediate

Life of this patent

Abstract

Claims20