Zach System S.p.a.

Zach Systems S.p.a.

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

Raffaella Volpicelli

Livius Cotarca

Paolo Maragni

Johnny Foletto

Massimo Verzini

Franco Massaccesi

Mauro Andretto

Ivan Michieletto

Ilaria Munari

Antonio Nardi

Giorgio Soriato

Roberto Brescello

Elisa Melotto

Alfonso Melloni

Anna Smaniotto

Corrado Colli

The present invention relates to a chiral oxamide of formula (I) useful as an intermediate in the preparation of dorzolamide, and to the preparation thereof. The invention also relates to the preparation of dorzolamide, to the hydrochloride salt thereof, and to the active ingredient contained in a drug useful in the treatment of glaucoma, by means of the intermediate of formula (I). 

Process for preparing enantiomerically enriched oxamides

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 stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SOand Ris hydrogen or an SONHgroup, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof. 

Asymmetric reduction process

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

The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.

Process for preparing nebivolol

The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a diastereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (&#x2212;)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol. 

The present invention relates to a process for the preparation of Nebivolol and, more particularly, to an improved method of synthesizing 6-fluoro chroman epoxides of formula (I) key intermediates in preparing nebivolol. 

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Vicenza, Italy

Raffaella Volpicelli