The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Mar. 29, 2022

Filed:

May. 19, 2020
Applicant:

Interquim, S.a., Sant Cugat del Valles, ES;

Inventors:
Assignee:

INTERQUIM, S.A., Sant Cugat del Vallès, ES;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 405/06 (2006.01); C07D 217/02 (2006.01);
U.S. Cl.
CPC ...
C07D 405/06 (2013.01); C07D 217/02 (2013.01);
Abstract

It relates to a process for the preparation of lifitegrast (I) by: a) reacting benzofuran-6-carboxylic acid (II) with a non-chlorinated carboxyl activating agent; b) reacting the activated compound of formula (II) obtained in step a) with compound (III) or a salt thereof to give lifitegrast or a salt thereof; and c) optionally isolating the obtained lifitegrast. It also relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast (I) with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (Ia); ii) isolating the compound of formula (Ia) from the reaction medium; iii) converting the dicyclohexylamine salt into lifitegrast by the treatment with an acid; and iv) isolating the compound of formula (I) from the reaction medium. It also relates to dicyclohexylamine salt of lifitegrast and to a process for its preparation.


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