Zach Systems S.p.a.

Zach System

Wyeth

Zambon S.p.a.

F.i.s. Fabbrica Italiana Sintetici S.p.a.

Ivan Michieletto

Livius Cotarca

Massimo Verzini

Paolo Maragni

Elisa Melotto

Raffaella Volpicelli

Roberto Brescello

Franco Massaccesi

Franco Pellacini

Mauro Napoletano

Dario Braga

Gabriele Morazzoni

Giorgio Soriato

Vincenzo Cannata

Johnny Foletto

Andrea Nicoli

Angelo Restelli

Nicola Catozzi

Alfonso Melloni

Paolo Andreella

Ilaria Munari

Mauro Andretto

Corrado Colli

Stefano Poli

Vincenzo Frega

Alessandro Di Maria

Franco Brazzarola

Paolo Fornasari

Mauro Maffini

Dario Università Di Bologna Braga

The present invention relates to a process for preparing a ketosulfone derivative and, more particularly, to an improved method for synthesizing 1-(6-methylpyridin-3-yl)-2-[(4-methylsulfonyl)-phenyl]ethanone by means of Pd-catalized alpha arylation process of a heteroaromatic ketone derivative.

Process for preparing a ketosulfone derivative

The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.

Process for preparing Bosentan monohydrate and it's intermediates

The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved method of debenzylation of a compound of formula (II) useful for preparing nebivolol endowed with high purity. 

Process for preparing Nebivolol

A process for resolving dorzolamide trans racemate, which comprises reacting said racemate with (1S)-(+)-10-camphorsulfonic acid so obtaining the (4S,6S) enantiomer by selectively precipitating and recovering the camphorsulfonic acid salt thereof (dorzolamide camphorsulfonate), and neutralizing dorzolamide camphorsulfonate to obtain dorzolamide.

Process for preparing dorzolamide

The present disclosure relates to polymorphic Form D of bazedoxifene acetate, pharmaceutical compositions and methods of treatment using the same, and methods of preparing the same.

Polymorphic Form D of bazedoxifene acetate and methods of preparing same

The present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.

Crystalline forms of macrolide compounds endowed with antiinflammatory activity

A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from 2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-3-methyl-pyridine, a new intermediate to obtain loratadine. 2-(4,4-dimethyl-4, 5-dihydrooxazol-2-yl)-3-methyl-pyridine is condensed with 3-chloro-benzyl-chloride and the resultant product is treated with Grignard reagent of 4-chloro-N-methyl-piperidine. [3-(2-(3-chloro-phenyl)-ethyl]-pyridin-2-yl]-1-(methyl-piperidin-4-yl)-methanone is obtained for subsequent hydrolysis. Starting from this last compound it is possible to obtain loratadine with known methods.

Process for the preparation of 4-(8-chloro-5 6-dihydro-11h-benzo-(5 6)-cyclohepta-(1 2b)-pyridin-11-ylidene-1-piperidiniecarboxylic acid ethyl ester (loratadine)

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Venice, Italy

Ivan Michieletto