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

Amgen Inc.

Elena Brasola

Nicolas Tesson

Pierluigi Padovan

Ottorino De Lucchi

Marco Galvagni

Francesco Fontana

Riccardo Motterle

Paolo Stabile

Filippo Tomasi

Siro Serafini

Montserrat Trilla Castaño

Loris Peruzzi

Marco Di Silvestro

The present invention refers to a crystalline 2-fluoro-3-nitrotoluene compound of formula (I), and a process for the preparation thereof. Furthermore, the present invention relates to a process for the synthesis of a compound of formula (II) or salts thereof by means of the crystalline 2-fluoro-3-nitrotoluene.

Crystalline 2-fluoro-3-nitrotoluene and process for the preparation thereof

Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.

Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid

Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.

Dimer impurities of Apixaban and method to remove them

Dimer impurities of apixaban and method to remove them

Object of the present invention is an improved process for the preparation of Apixaban, through new intermediates which undergo to a faster amidation reaction. Impurities of Apixaban are also identified and quantified.

Key intermediates and impurities of the synthesis of Apixaban: Apixaban glycol esters

Key intermediates and impurities of the synthesis of apixaban: apixaban glycol esters

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

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Elena Brasola