Process for the preparation of lifitegrast

US11498917B2 · kind B2 · utility

Assignee

• OLON S.P.A. · IT

Inventors

• Giorgio Bertolini · Sesto San Giovanni, IT
• Lazzaro FELICIANI · Milano, IT
• Davide Longoni · Pioltello, IT
• Mara Sada · Segrate, IT
• Matteo Valli · Briavacca, IT

Key dates

• Filing date: Jun 13, 2019
• Grant date: Nov 15, 2022
• Expiry date: Jun 13, 2039

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.