PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE (S)-(-)-2-(N-PROPYLAMINO)-5-METHOXYTETRALINE AND (S)-(-)-2-(N-PROPYLAMINO)-5-HYDROXYTETRALINE COMPOUNDS

摘要

The present invention describes a novel process for the preparation ofoptically active (S)-(-)-2-(N-propylamino)-5-methoxytetraline and (S)-(-)-2-(N-propylamino)-5-hydroxytetraline compounds based on the optical resolution ofmixtures of the enantiomers of 2-(N-propylamino)-5-methoxytetraline and 2-(N-propylamino)-5-hydroxytetraline respectively.This process comprises (a) reacting a mixture of the enantiomers of saidcompounds with an optically active organic acid to formdiastereoisomeric salts and separating the salts by crystallization. Saidcompounds are useful in the preparation of (6S)-(-)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine).Rotigotine is a dopamine agonist and is indicated for thetreatment of Parkinson's disease.