Improved process

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/04 (2006.01) A61K 31/45 (2006.01)

Patent

CA 2753241

The present invention relates to improved processes for preparing 3-(4-amino-1- oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (I) (lenalidomide) and its intermediate 3-(1-oxo- 4-nitro-1,3-dihydro-isoindol- 2-yl)-piperidine-2,6-dione. The present invention further relates to improved processes for preparing lenalidomide crystalline form A, use of said crystalline form A as an active pharmaceutical ingredient or as an intermediate in the preparation of further crystalline or amorphous forms of lenalidomide, compositions comprising lenalidomide crystalline form A and their use in the treatment of disease.

La présente invention porte sur des procédés améliorés pour préparer la 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-pipéridine-2,6-dione (I) (lénalidomide) et son intermédiaire 3-(1-oxo-4-nitro-1,3-dihydro-isoindol-2-yl)-pipéridine-2,6-dione. La présente invention porte en outre sur des procédés améliorés de préparation de la forme cristalline A de lénalidomide, sur l'utilisation de ladite forme cristalline A en tant que principe pharmaceutique actif ou en tant qu'intermédiaire dans la préparation d'autres formes cristallines ou amorphes de lénalidomide, sur des compositions comprenant la forme cristalline A de lénalidomide et sur leur utilisation pour le traitement d'une maladie.

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