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

Other

Marco Galvagni

Clark Ferrari

Andrea Castellin

Riccardo Motterle

Stefano Fogal

Ottorino De Lucchi

Stefano Tartaggia

Alex Comely

Marta Pontini

Rosa Maria Moreno

Nicolas Tesson

Francesco Fontana

Paolo Stabile

Elena Brasola

Siro Serafini

Filippo Tomasi

Ennio Grendele

Alessandro Leganza

Giancarlo Arvotti

Elisabetta Bergantino

Llorenç Rafecas

Jordi De Mier

Cristiano Grandini

Giovanni Lora

Massimo Peruffo

An improved process for the preparation of Triazole and salts thereof, a key intermediate for the synthesis of Sitagliptine is disclosed.

Process for the preparation of triazole and salt thereof

Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.

Convenient process for the preparation of statins

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 an efficient process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. Water is employed as reaction medium.

Very efficient process for preparing an intermediate of etoricoxib

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

The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO&#x2014;COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.

Process for the preparation of Efavirenz

The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base. 

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Verona, Italy

Marco Galvagni