Zambon Group

Bracco International Bv

Teva Pharmaceuticals International Gmbh

Zach System

Sicor Inc.

Maurizio Paiocchi

Marco Villa

Claudio Giordano

Katiuscia Arrighi

Laura Coppi

Graziano Castaldi

Pietro Allegrini

Massimo Verzini

Silvia Cavicchioli

Giorgio Soriato

Aldo Belli

Vincenzo Cannata

Paolo Cavalleri

Andrea Nicoli

Pavel Kolesa

Marisa Martinelli

Antonio Nardi

Piero Paravidino

Francesco Corcella

Roberto Casagrande

Gaetano Marchioro

Francesco Ponzini

Giulio Perdoncin

Ettore Bigatti

Matteo Toso

Roberta Volonté

Aldo Di Caterino

Roberta VolontÉ

Simone Tosi

Andrea Giolito

Disclosed crystalline Siponimod fumaric acid, solid state forms (polymorphs) thereof, processes for preparation thereof and pharmaceutical compositions thereof.

Crystalline siponimod fumaric acid and polymorphs thereof

The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of &#x3b1;,-diaminocarbonyl-&#x3b2;,&#x3b2;-pentamethylene glutarimide.

Process for the preparation of gabapentin

A process for the nitration of conjugated alkenes of formula (I) wherein R, R1, R2, R3 and R4 have the meanings reported in the description, which allows to obtain the corresponding &#x3b2;-nitro-alkenes, characterised in that the nitrating agent is a mixture of an inorganic nitrite and iodine in the presence of an oxidising agent is described.

Process for the preparation of nitroalkenes

A process for purifying Iopamidol which uses a butanol as solvent is described. Iopamidol is obtained with high yields, also starting from aqueous solutions of the same and has characteristics in accordance with those required by pharmacopoeia.

Process for the purifying of iopamidol

A process for the preparation of heteroaryl-phenylalanines of formula (II) in which R is a hydrogen atom, a straight or branched C -C alkyl groups or a benzyl group; R is an optionally substituted 5 or 6 membered aromatic heterocyclic group with one or two heteroatoms selected among nitrogen, oxygen and sulphur; comprising a cross-coupling reaction among heteroaryl-zinc halide and phenylalanine derivatives is described. Compounds of formula (II) are intermediates useful for the preparation of compounds endowed with pharmacological activity.

Process for the preparation of heteroaryl-phenylalanines

A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.

Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes

A process for the preparation of the compound L-5-(2-acetoxypropionylamino)-2,4,6-triiodoisophthaloyl dichloride by reacting 5-amino-2,4,6-triiodoisophthaloyl dichloride with L-2-acetoxypropionyl chloride in N,N-dimethylacetamide as a solvent, characterized in that a catalytic amount of a lower alcohol is added to the reaction mixture.

Process for the preparation of an intermediate useful in the synthesis

A process for the preparation of (S)-N,N'-bis�2-hydroxy-1-(hydroxymethyl)ethyl!-5-(2-acetoxy-propionylamino )-2,4,6-triiodo-isophthalamide, an intermediate useful for the synthesis of iopamidol, by reaction between L-5-(2-acetoxy-propionylamino)-2,4,6-triiiodoisophthaloyl dichloride and 2-amino-1 ,3-propanediol in N-methylpyrrolidone and in the presence of a base, is described.

A process for the purification of 2,6-diisopropylphenol (Propofol) by transformation of the crude Propofol into its ester with a carboxylic or sulphonic acid, crystallization and hydrolysis, is described.

Process of purification of 2,6-diisopropylphenol

A process for the direct and regioselective functionalization of phenothiazine which allows one to introduce an SH group in position 2, said process comprising the sulfination or sulfonation of the phenothiazine N-protected with an alkoxycarbonyl, an alkylsulfonyl or an arylsulfonyl group, the reduction of the produce obtained to give the N-protected 2-mercapto-phenothiazine, and the deprotection of the nitrogen atom. The thus-obtained 2-mercapto-phenothiazine is an important intermediate for the preparation of pharmacological active compounds.

Process for the direct and regioselective functionalization in position

An improvement to a process for the preparation of L-5-(2-acetoxy-propionylamino)-2,4,6-triiodo-isophthalic acid dichloride by reacting 5-amino-2,4,6-triiodo-isophthalic acid dichloride with L-2-acetoxy-propionyl-chloride, is described.

Process for the preparation of

A process for the preparation of 4-(2,4-difluorophenyl)-phenyl 4-nitro-benzoate, an intermediate for the preparation of 5-(2,4-difluorophenyl)-salicylic acid, which is a drug known with the international non-proprietary name Diflunisal, is described.

Process for the preparation of 4-(2,4-difluorophenyl)-phenyl

Process for the preparation of (2S,3S)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H) -one of formula ##STR1## by direct cyclization of the compound of the formula ##STR2## with a catalytic amount of phosphonic acid.

Process for the preparation of benzothiazepines by cyclization with

A crystallization process of crude 5-(2',4'-difluorophenyl)-salicylic acid from a mixture of an aromatic hydrocarbon and an aliphatic ketone for preparing 5-(2',4'-difluorophenyl)-salicylic acid in form II substantially pure is described.

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Milan, Italy

Maurizio Paiocchi