165950-84-5Relevant articles and documents
IMPROVED PROCESS FOR THE PREPARATION OF CRYSTALLINE FORM II OF ROTIGOTINE
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Page/Page column 3, (2015/12/24)
The present invention relates to an improved, environment friendly and cost effective process for the preparation of crystalline Form II of Rotigotine. Rotigotine, i.e. (6S)-6-{propyl[2-(2-thienyl) ethyl]amino}-5,6,7,8-tetrahydro-l-naphthalenol represented by structural formula (I), is used for the treatment of Parkinson's disease and Willis-Ekbom disease.
Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives
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, (2013/05/08)
The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R1, R2 and R3 are as defined for compound of formula (I).
PROCESS FOR THE PREPARATION OF ROTIGOTINE
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Page/Page column 2-3, (2011/10/10)
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 obtain 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.