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

Hoffmann-la Roche Inc.

Siro Serafini

Pierluigi Padovan

Andrea Castellin

Ottorino De Lucchi

Marco Galvagni

Riccardo Motterle

Elena Brasola

Filippo Tomasi

Giuseppe Zagotto

Simone Zaramella

Emiliano Rossi

Claudio Dal Santo

Roberto Bortolaso

Object of the present invention is an improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts.

Process for the preparation of eslicarbazepine and eslicarbazepine acetate

An improved process for the preparation of the active pharmaceutical ingredient Clomiphene and, in particular, trans-Clomiphene, using acetic acid or trifluoroacetic acid is disclosed.

Process for the preparation of Clomiphene

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 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. 

Process for the synthesis of quetiapine

A process for the preparation of &#x3c9;-alkoxycarbonylamino-&#x3b1;-aminoacids and &#x3b1;,&#x3c9; orthogonally diprotected diaminoacids from &#x3b1;,&#x3c9;-diaminoacids using 1-alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of &#x3b5;-alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of &#x3c9;-alkoxycarbonylamino-&#x3b1;-aminoacids with benzotriazoles are also disclosed.

Process for the preparation of &#x3b5;-alkoxycarbonyllysines and their analogues

The present invention relates to a process for preparing the cyclohexylamine salt of (+)-threo-2-hydroxy-3-(2'-aminophenylthio)-3-(4'-methoxyphenyl)-propionic acid and of its optical (-)-antipode, by starting from the racemate acid by means of a first crystallization from a suitable chiral base and a second crystallization from a cyclohexylamine-containing solvent. Said salt is an intermediate in the synthesis of diltiazem, a well-known calcium-antagonist drug.

Process for preparing the cyclohexylamine salt of (+) -

4-Dimethylamino-3,5-dimethoxy-benzaldehyde, an intermediate for the preparation of the antibacterially active aditoprim (4-dimethylamino-3,5-dimethoxybenzoldehyde) a known antibacterially active compound, is obtained from 4-dimethylaminobenzonitrile by bromination or chlorination, replacement of the halogen by the methoxy group and reduction of the nitrile group.

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Vicenza, Italy

Siro Serafini