Process for the preparation of rotigotine
US8519160B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 24, 2009 |
| Grant date | Aug 27, 2013 |
| Priority date | — |
| Expiry date | Mar 5, 2030 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C2602/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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-methoxynaphthalene (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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.