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US 10,294,502 B2Granted
Methods for the synthesis of chiral kynurenine compounds
AssigneeVistagen Therapeutics, Inc.
InventorsStefan Abele, Klaus Laue, Roland A. Breitenmoser
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Abstract
Provided are methods for synthesizing compounds, including chiral kynurenine compounds. The methods are suitable for large-scale manufacture and produce the chiral kynurenines compounds in high chemical purity and high chiral purity.
Claims6
A method of preparing a compound of Formula I or a pharmaceutically acceptable salt, polymorph, hydrate, solvate, tautomer, or stereoisomer thereof:
- wherein each R is independently selected from the group consisting of hydrogen, halogen, alkyl, and substituted alkyl;
- and
- wherein n =0−4;
- the method comprising the step of:
- resolving the acylated kynurenine compound of Formula V with an acylase enzyme to afford the compound of Formula I:
2 more elements
A method of preparing a compound of Formula la or a pharmaceutically acceptable salt, polymorph, hydrate, solvate, tautomer, or stereoisomer thereof:
- the method comprising the step of:
- resolving 2-acetylamino-4-(2-amino-4-chloro-phenyl)-4-oxo-butyric acid (compound of Formula Va) with an acylase enzyme to the compound of Formula la:
Dependencies are inferred from the claim text.