Olon S.p.a.

Antibioticos S.p.a.

Basilea Pharmaceutica Ag

Davide Longoni

Walter Cabri

Marco Alpegiani

Enrico Siviero

Loris Sogli

Ermanno Bernasconi

Giovanni Pozzi

Daniele Mario Terrassan

Samuele Frigoli

Francisco Salto

Markus Heubes

Michael Schleimer

Claudio Fuganti

Giorgio Bertolini

Mara Sada

Lazzaro Feliciani

Stefano Serra

Claudio Felisi

Marco Alpegiani, Jr

Tamara Danelli

Matteo Valli

Paola Luigia Daverio

Tania Cristiano

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

Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl. 

Process for the preparation of enzalutamide

Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate. 

Crystalline salts of asenapine

A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril. 

Crystalline (6R,7R)-7-{2-(5-amino-[1,2,4] thiadiazol-3-yl)-2-[(Z)-trityloxyimino]-acetylamino}-3-[(R)-1'-tert-butoxycarbonyl-2-oxo-[1,3&#x2032;]bipyrrolidinyl-(3E)-ylidenemethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester; its manufacture and use

The invention is directed towards a process for the preparation of Cefuroxime acid or for a corresponding pharmaceutically acceptable salt or ester. The process comprises the carbamoylation of a Cefuroxime precursor with an activated isocyanate. Additionally, the process is characterized by the fact that a carbonic C -C alkyl ester is used as a solvent for the carbamoylation reaction.

Process for the synthesis of beta-lactam derivatives

A compound having the following general formula (I): ##STR1## where R is a hydrogen atom; a linear or branched C.sub.1 -C.sub.4 alkyl group, unsubstituted or substituted by at least a phenyl group or at least a hydrogen atom; a benzyl group substituted by at least a linear or branched C.sub.1 -C.sub.4 alkyl or alkoxy group or a nitro group; a silyl substituted by at least a linear or branched, unsubstituted or substituted C.sub.1 -C.sub.4 alkyl group; n is 0 or 1; and Y is a radical of formula ##STR2## wherein A is H, OH, Cl, CH.sub.2, CH.sub.2 X, where X is F, Cl, Br, I, OH or OR' and R' is COCH.sub.3 or a linear or branched, unsubstituted or substituted C.sub.1 -C.sub.4 alkyl group and - - - represents a single or a double bond, with the proviso that when n=0 and R is H, R' is not a methyl group.

Glutaryl 7-ACA derivatives and processes for obtaining them

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Rodano, Italy

Davide Longoni