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US 2022/0194894 A1Published application
Process of making 3-(4'-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof
AssigneeNogra Pharma Limited
InventorsSalvatore Demartis, Francesca Viti, Marie McNulty
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Abstract
The disclosure provides a process for the preparation of 3-(4′-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof, contemplated to be capable of modulating the activity of receptors, e.g., PPARs receptors.
Claims51
A process for preparing a substantially optically pure compound of Formula (VII):
- the process comprising:
- reacting a compound of Formula (I):
- with an activating agent, in the optional presence of a base, to form an intermediate of Formula (I-A):
- wherein LG is a leaving group;
- treating the intermediate of Formula (I-A) with a base solution in the presence of an alcohol solvent, to eliminate the leaving group and thereby forming an intermediate of Formula (I-B):
- hydrolyzing the intermediate of Formula (I-B) to form a compound of Formula (IV):
- hydrogenating the compound of Formula (IV) to form a compound of Formula (V):
- resolving the compound of Formula (V) to form a substantially optically pure compound of Formula (VI):
- and
- acylating the compound of Formula (VI) to form the compound of Formula (VII).
7 more elements
The process of any one of claims 1-39, wherein acylating occurs at a temperature between 60-70° C.
41 The process of claim 40, wherein at least about 8 to 10 kg is obtained.
A process for preparing a compound of Formula (I):
- the process comprising, providing a mixture of a compound of Formula (II):
- and a compound of Formula (III):
- and contacting the mixture with a base;
- thereby forming a compound of Formula (I).
1 more element
A compound represented by:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.