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

H. Lundbeck A/s

Other

Dipharma Francis S.r.l.

Phf S.a.

Andrea Castellin

Marco Galvagni

Ottorino De Lucchi

Clark Ferrari

Federico Sbrogiò

Riccardo Motterle

Stefano Fogal

Andrea Caporale

Giancarlo Arvotti

Elisabetta Bergantino

Nicolas Tesson

Pierluigi Padovan

Lin Feng

Jacopo Zanon

Francesco Fontana

Paolo Stabile

Siro Serafini

Stefano Tartaggia

Poul Dahlberg Nielsen

Rikke E Humble

Alessandro Falchi

Claudio Dal Santo

Llorenç Rafecas

Steen Sogaard

Giulio Volpe

Jordi De Mier

Michele Maggini

Paola Donnola

Liu Jiageng

Yibo Zhou

Thomas Pittelkow

Jacobo Zanon

Oscar Martini

Francesco Ciardella

Luca Gregori

A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

Process for the preparation of olopatadine

The present invention relates to a novel process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.

Co-crystal intermediates of rosuvastatin and methods of using same

The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%. 

Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine

A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.

Process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of etoricoxib

An alternative method for the preparation of Erlotinib through a new chemical reaction for the preparation of the 4-(3-aminophenyl)-2-methyl-3-butyn-2-ol key intermediate of formula (IV) according to the following scheme. 

Method for the preparation of erlotinib

The present invention relates to an industrial process for the reduction of 4-androstene-3,17-dione in order to obtain testosterone using a particularly stable and selective enzyme produced in a recombinant manner.

Process for the preparation of testosterone

The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.

Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof

The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt. 

Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole

The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1,2-thiazin-6-sulfonamide, 4-(ethyl amino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1,2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.

Process for the preparation of brinzolamide

The present invention relates to a process for the synthesis of Moxifloxacin of Formula (I) and salts thereof by means of a process providing the coupling reaction of 1-cyclopropril-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo -3-quinolinic acid or ester thereof with (4aS, 7aS) -octahydro-1H-pyrrole[3,4-b]pyridine using a magnesium salt.

Process for preparing Moxifloxacin and salts thereof

Methods for manufacture of 5-alkoxycarbonylphthtalides are disclosed. The 5-alkoxycarbonylphthtalides are useful in syntheses of the well-known antidepresssants citalopram and escitalopram.

Intermediates for the preparation of citalopram and escitalopram

A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound. 

Process for the preparation of ziprasidone

A process for the preparation of citalopram of formula (I)in which a compound of formula (II)wherein Z is iodo, bromo, chloro or CF&#x2014;(CF)&#x2014;SO&#x2014;O&#x2014; n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction in which the group Z is exchanged with cyanide by reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and the crude citalopram base is subsequently subjected to a film distillation process; the resulting citalopram product is then optionally further purified and worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

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Mestrino, Italy

Andrea Castellin