Interquim, S.a.

Xavier Berzosa Rodríguez

Francisco Marquillas Olondriz

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. 

Process for preparing and purifying a LFA-1 antagonist

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 (Ia); 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 (Ia) and to a process for its preparation. (Formula I, III) 

Process for preparing and purifying the LFA-1 antagonist lifitegrast

The invention relates to a process for obtaining compounds derived from tetrahydro-&#x3b2;-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.

Growing community of inventors

Terrassa, Spain

Xavier Berzosa Rodríguez