Chemi S.p.a.

Italfarmaco Spa

Zach System

Elio Ullucci

Stefano Turchetta

Lorenzo De Ferra

Maurizio Zenoni

Umberto Ciambecchini

Livius Cotarca

Oreste Piccolo

Paolo Maragni

Mara Sada

Johnny Foletto

Tiziana Benincori

Angela Tuozzi

Alessandra Verrazzani

Giorgio Berardi

Nakia Maulucci

Stefania Cocciolo

Francesco Sannicolo′

Simona Tollis

Simona Rizzo

A process for obtaining {{6-[(diethylamino)methyl]naphthalen-2-yl}methyl[4-(hydroxycarbamoyl)phenyl]carbamate and/or pharmaceutically acceptable salts thereof having high purity is described. This process allows to obtain a product having an amount of any single unknown impurity equal to or less than 0.10%, as well as a product having a purity greater than 99.5%, preferably equal to or greater than 99.6%. An HPLC method for determining the purity of the product and possible impurities thereof is also described.

Process for preparing {6-[(diethylamino)methyl]naphthalen-2-yl}methyl [4-(hydroxycarbamoyl)phenyl]carbamate having high purity

A process is described for preparing fesoterodine fumarate comprising the salification reaction of fesoterodine with fumaric acid in an organic solvent, preferably a ketone, at a temperature not greater than 45&#xb0; C. Such process allows obtaining products with high yields and purities, and in particular a product having a content of (2E)-4-[(3-(3-diisopropylamino-1-phenylpropyl)-4-(2-isobutyroyloxyphenyl)methoxy]-4-oxobut-2-enoic acid less than or equal to 0.15% by mole.

Method for preparing high-purity fesoterodine fumarate

A process is described for preparing fesoterodine and/or fesoterodine fumarate comprising the esterification of (R)-feso deacyl with isobutyric acid or a precursor thereof, such as an isobutyryl halide or the isobutyric acid anhydride to give fesoterodine, in a mixture of water at alkaline pH and/or at least one organic solvent. This process allows obtaining products with high yields and purities, and in particular a product having a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-isobutyroyloxymethyl-phenyl isobutyrate less than 1% by mole and a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol less than 0.05% by mole.

Method for preparing fesoterodine and/or fesoterodine fumarate

The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved process for synthesizing enantiomerically enriched 6-fluoro chroman alcohol or epoxide derivatives of formula, wherein R and X is defined in the description; as useful intermediates in the preparation of Nebivolol. 

Process for preparing Nebivolol

The present invention relates to a process for the preparation of Montelukast and the salts thereof comprising the following steps: (a) reaction of a compound A with a compound A in which n varies between 1 and 2 and, when n is 1, R is methyl and, when n is 2, R is a C-Calkyl or an aryl, and X is a leaving group, by nucleophilic substitution reactions in dipolar organic solvents to yield the compound A3 (b) reaction of the compound A3 with an inorganic acid HY, in which Y is Cl, Br, I, and subsequent isolation of the resultant salt A4; (c) optional conversion of the salt A4 into the compound A3;(d) methylation of the salt A4 and/or of the compound A3 to yield Montelukast.

Process for the preparation of Montelukast

Metallic catalysts of the general formula (I) and their precursors, suitable for chemo- regio- and stereoselective reactions, derived from ortho-bis-(1-phospholanyl)-heteroarenes. The new catalysts are characterized by the presence of two homo-morphic phospholanic rings set in adjacent positions of an aromatic pentatomic heterocycle 

Metallic catalysts for chemo-, regio- and stereoselective reactions, and corresponding precursors

A method for the resolution of etodolic acid by crystallization of its salt with optically active 1-phenylethylamine and subsequent recovery of the (R,S) etodolic acid from the mother liquors of crystallization by racemization and crystallization is described.

Method for the racemization of etodolic acid

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Latina, Italy

Elio Ullucci