Olon S.p.a.

Lazzaro Feliciani

Giorgio Bertolini

Mara Sada

Federico Gassa

Alberto Mazza

Marco Quaroni

Stefano Maiorana

Davide Longoni

Corrado Colli

Federica Colombo

Aldo Bianchi

Filippo Nisic

Paolangelo Cerea

Matteo Valli

Giuseppe Cremonesi

Christian Invernizzi

The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R, Rand Rare independently selected from straight or branched C-Calkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water. 

Process for the preparation of lifitegrast

The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III): 

Process for the preparation of Crisaborole in a stable crystal form

The present invention relates to a process for the preparation of crisaborole of formula (I):  

Process for the preparation of crisaborole

Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I): 

Process for the preparation of indanamine derivatives and new synthesis intermediates

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Casaletto Lodigiano, Italy

Lazzaro Feliciani