Process for preparing and purifying the LFA-1 antagonist lifitegrast

The invention relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast (I) with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (la); ii) isolating the salt (Ia) from the reaction medium; iii) converting the isolated salt (Ia) into lifitegrast (I) b...

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Bibliographic Details
Main Authors Berzosa Rodríguez, Xavier, Marquillas Olondriz, Francisco
Format Patent
LanguageEnglish
Published 28.07.2020
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast (I) with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (la); ii) isolating the salt (Ia) from the reaction medium; iii) converting the isolated salt (Ia) into lifitegrast (I) by treatment with an acid; and iv) isolating lifitegrast (I) from the reaction medium. It also relates to the dicyclohexylamine salt of lifitegrast (Ia) and to a process for its preparation.
Bibliography:Application Number: US201816632057