Process for preparation of Rotigotine and intermediates thereof

Process for preparation of Rotigotine and intermediates thereof

To provide a novel process for preparing rotigotine and an intermediate thereof.SOLUTION: Provided is a novel process for preparing rotigotine and an intermediate thereof, including: (i) a step of obtaining (2S)-N-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-N-propyl-2-thiophen-2-yl-acetamide or a...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Irudayaraj, Victor Paul Raj, Govindaraj, Vedhachalam, Subramani, Senthilkumar, Jayaraman, Boopathy, Jayavelu, Jeyakanthan, Ray, Uttam Kumar, Vittal, Tangirala
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:To provide a novel process for preparing rotigotine and an intermediate thereof.SOLUTION: Provided is a novel process for preparing rotigotine and an intermediate thereof, including: (i) a step of obtaining (2S)-N-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-N-propyl-2-thiophen-2-yl-acetamide or a salt thereof (compound III) by reacting, in the presence of a base, (S)-1,2,3,4-tetrahydro-5-methoxy-N-propyl-2-naphthalenamine or a salt thereof (compound IV) with a 2-thienyl acetic acid derivative or a salt thereof; (ii) a step of obtaining (2S)-N-(5-hydroxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-N-propyl-2-thiophene-2-yl-acetamide or a salt thereof (compound II) by demethylating compound III with aluminum chloride; and (iii) a step of obtaining rotigotine of formula (I) or a salt thereof by reducing compound II with a suitable reducing agent in a solvent.SELECTED DRAWING: None