PROCESS FOR THE PREPARATION OF LIFITEGRAST

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...

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Bibliographic Details
Main Authors Longoni, Davide, Sada, Mara, Bertolini, Giorgio, Feliciani, Lazzaro, Valli, Matteo
Format Patent
LanguageEnglish
Published 12.08.2021
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary: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.
Bibliography:Application Number: US201916972856