Process for the preparation of rotigotine

Details Process for the preparation of rotigotine Process for the preparation of rotigotine

C - Chemistry, Metallurgy

07

C

C07C 215/48 (2006.01) A61K 31/381 (2006.01) A61P 25/00 (2006.01) C07D 333/20 (2006.01)

Patent

CA 2738392

A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid- sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II) The process is advantageous from the industrial point of view in that it allows to ob-tain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-1-methoxy-naphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by--products. Furthermore, two novel crystalline forms are disclosed.

La présente invention concerne un procédé de préparation de la rotigotine (I) et de ses sels pharmaceutiquement acceptables, lequel comprend l'amination réductrice d'une amine de formule 6 avec le complexe acide 2-thiénylacétique-borohydrure de sodium et lequel utilise le bromhydrate 5 comme intermédiaire (II). Le procédé est avantageux du point de vue industriel du fait qu'il permet d'obtenir la Rotigotine avec une pureté énantiomérique élevée en partant du 5,6,7,8-tétrahydro-6-(S)-N-propylamino-1-méthoxy-naphthalène (2) optiquement actif, évitant ainsi l'utilisation de réactifs dangereux, le besoin d'effectuer une séparation chromatographique difficile ou la formation de produits secondaires. De plus, l'invention concerne deux nouvelles formes cristallines.

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