Process for preparing and purifying the LFA-1 antagonist Lifitegrast

Inventor/a - Autor/a

Berzosa Rodríguez, X.; Marquillas Olondriz, F.

Entitats titulars

2508 - INTERQUIM S.A.

Espacenet

Tipus

Sol·licitud PCT 

Abstract

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

Data sol·licitud / Prioritat

2019-01-31

Número de sol·licitud

WO2019020580

Països de prioritat

-