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Inventor/a - Autor/a Berzosa Rodríguez, X. |
Entidades titulares 2508 - INTERQUIM S.A. |
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Tipo Solicitud 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) |
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Fecha solicitud / Prioridad 2019-01-31 |
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Número de solicitud WO2019020580 |
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Países de prioridad - |
