Zambon Group S.p.a.

Italfarmaco Spa

Euticals Spa

Archimica S.r.l.

Clariant Life Science Molecules (italy) S.p.a.

Curia Italy S.r.l.

Giorgio Bertolini

Francesco Santangelo

Cesare Casagrande

Domenico Vergani

Marco Frigerio

Giuseppe Motta

Stefania Montanari

Maurizio Velati

Paolo Mascagni

Claudio Semeraro

Flavio Leoni

Alberto Sala

Gianni Gromo

Francesco Marchini

Gianfranco Pavich

Mauro Biffi

Jacques Mizrahi

Maurizio Deleo

Massimo Losa

Gabriele Pietro Norcini

Francesca Benedini

Franco Pellacini

Annibale Gazzaniga

Silvio Levi

Maurizio Gallina

Patrizia Castoldi

Flavio Somenzi

Fabrizio Marcucci

Luciano Soldati

Giancarlo Dona

Alberto Bologna

Roberto Barani

Giuliana Porro

Maria Letizia Marchetti

Nicola Landoni

Luigi Petrucciani

Barbara Verzola

A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-&#x3b1;,&#x3b1;-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-&#x3b1;,&#x3b1;-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralization of the solution.

Process for preparing fexofenadine

A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

Process for the preparation of lacosamide

The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention. Still another object of the invention is represented by the crystalline forms I and II of the tapentadol free base. A further object of the present invention is the mixture of the crystalline forms I and II of the tapentadol free base. 

Process for the synthesis of tapentadol and intermediates thereof

The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below using the (2R,3R)&#x2014;O,O'-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

Process for the preparation of tapentadol and intermediates thereof

The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II: 

Process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine

A novel process for preparing emtricitabine, and more particularly a process for preparing emtricitabine involving the formation and isolation of intermediate compounds in salified form, is described.

Process and intermediates for preparing emtricitabine

A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.

The present invention relates to a process for preparing 5&prime;-acetylstavudine, an intermediate which is useful in the preparation of 2&prime;,3&prime;-didehydro-3&prime;-deoxythymidine, an active principle with antiviral action which is commonly known as stavudine (D4T).

Process for preparing 5&prime;-acetylstavudine

Compounds with anti-inflammatory and immunosuppressive activities

Analogues of the active metabolite of leflunomide, and to the use thereof as immunosuppressive and/or antinflammatory agents.

Analogues of the active metabolite of leflunomide

Diesters of carbonic acid disubstituted with primary, secondary or tertiary amine groups, pharmaceutically acceptable salts thereof, and their use as antiviral and inti-inflammatory agents.

Diesters of carbonic acid endowed with antiviral and anti-inflammatory

Pharmaceutical compositions for the treatment of cataract containing N-acetyl-L-cysteine derivatives of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification) are described.

Pharmaceutical compositions containing N-acetyl-cysteine derivatives

Compounds of formula I ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, methylene-dioxy or phenyl, which may be substituted by one or two groups independently selected from hydroxy, halogen, nitro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, COOR.sub.3, --CONR.sub.4 R.sub.5, ##STR2## --OCONR.sub.4 R.sub.5, --OCOR.sub.3, --NR.sub.4 R.sub.5, --OCOOR.sub.6, --NR.sub.3 COR.sub.7, --NR.sub.CONR.sub.4 R.sub.5, --N.dbd.CH--NR.sub.4 R.sub.5, NO.sub.2, CN, OH, SR.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 and R.sub.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, with the proviso that R.sub.1 and R.sub.2 cannot be hydrogen at the same time; X is oxygen or sulphur; Y represents a C.sub.2 -C.sub.6 alkylene chain or a C.sub.5 -C.sub.7 cycloalkylene group; and their pharmaceutically acceptable salts are provided and their use in pharmaceutical compositions which may be used in the treatment of cardiovascular diseases.

Benzoxazinone and benzothiazinone derivatives having cardiovascular

Derivatives of 2-amino-1,2,3,4-tetrahydronaphthalene and their use in therapeutic field are described. The compounds are particularly useful in the treatment of arterial hypertension, cardiac decompensation and renal failure, in the treatment of peripheral arteriopathies and in cerebrovascular insufficiency.

2-amino-1,2,3,4-tetrahydronaphthalene derivatives active on the

Steroid compounds active on the cardiovascular system of formula ##STR1## wherein X, n, R, R.sub.1 and R.sub.2 have the meanings mentioned in the description are described.

Steroid compounds active on the cardiovascular system

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Sesto San Giovanni, Italy

Giorgio Bertolini