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US 2026/0297022 A1Published application
Process for the preparation of sulfamoylbenzoic acid derivatives
AssigneeIama Therapeutics S.R.L.
InventorsMarco BORGOGNO, Annalisa SAVARDI, Andrea PATRICELLI MALIZIA, Marco DE VIVO, Laura CANCEDDA, Tommaso ANGELINI, Riccardo GARZELLI
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Abstract
The present invention relates to a method for the preparation of derivatives of the sulfamoylbenzoic acid, in particular of the (3-(dimethylsulfamoyl)-4-(8, 8, 8-trifluorooctylamino) benzoic acid.
Claims10
A method for the preparation of a compound of formula (I) or its salts, pharmaceutically acceptable stereoisomers, enantiomers, diastereoisomers, tautomers, geometric zwitterions:
- wherein:
- R1 and R2 are, independently, H, substituted or unsubstituted, linear or branched C1-10-alkyl optionally comprising one or more unsaturations;
- substituted or unsubstituted C3-8-cycloalkyl;
- substituted or unsubstituted, linear or branched C4-10-cycloalkyl-alkyl;
- C3-8-heterocycle;
- or, together with the nitrogen atom to which they are bound, R1 and R2 form a substituted or unsubstituted saturated heterocycle;
- R3 and R4 are, independently, hydrogen;
- substituted or unsubstituted C1-10-alkyl optionally comprising one or more unsaturations;
- C3-10-cycloalkyl;
- C4-10-cycloalkyl-alkyl;
- C2-8-haloalkyl;
- substituted or unsubstituted, linear or branched C2-8-heteroalkyl;
- optionally substituted phenyl;
- provided that at least one of R3 and R4 is other than hydrogen;
- R5 is hydrogen;
- halogen;
- hydroxyl;
- thiophenol;
- —NO2;
- R6 is —COOH;
- including the steps of:
- a) reacting, in aqueous solution, a compound of formula (II) with an amine of formula (III) to obtain a compound of formula (IV):
- wherein X and Y are independently a halogen;
- b) reacting, in aqueous solution and in the presence of a base, the compound of formula (IV) with a compound of formula (V) to obtain a compound of formula (I)
21 more elements
Dependencies are inferred from the claim text.