EP 3022183 A1 20160525 - METHOD OF RACEMISATION OF UNDESIRED ENANTIOMERS
Title (en)
METHOD OF RACEMISATION OF UNDESIRED ENANTIOMERS
Title (de)
VERFAHREN ZUR RACEMISIERUNG UNERWÜNSCHTER ENANTIOMERE
Title (fr)
PROCÉDÉ DE RACÉMISATION D'ÉNANTIOMÈRES INDÉSIRABLES
Publication
Application
Priority
- EP 13177295 A 20130719
- EP 2014065539 W 20140718
- EP 14739853 A 20140718
Abstract (en)
[origin: WO2015007897A1] The present invention provides a very simple, efficient and economic technology for racemisation of amines, alcohols or thioalcohols where the chiral carbon (benzylic position) is located at the β-position of the heteroatom (amino, hydroxyl or mercapto group) or even more distant therefrom. Special focus is oriented in efficient and simple racemisation of an undesired enantiomer of a chiral pharmaceutically active ingredient, preferably lorcaserin or a salt thereof, preferably the hydrochloride salt thereof. The approach according to the invention enables a use of cheaper and shorter racemic synthetic schemes not requiring expensive and toxic reagents and catalysts. Present methodology enables industrialy convenient process.
IPC 8 full level
C07C 33/20 (2006.01); C07C 211/27 (2006.01); C07C 211/29 (2006.01); C07C 233/66 (2006.01); C07C 271/14 (2006.01); C07D 223/16 (2006.01)
CPC (source: EP)
C07C 29/56 (2013.01); C07C 209/68 (2013.01); C07C 209/88 (2013.01); C07C 233/66 (2013.01); C07C 271/14 (2013.01); C07D 223/16 (2013.01); C07B 2200/07 (2013.01)
Citation (search report)
See references of WO 2015007897A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated extension state (EPC)
BA ME
DOCDB simple family (publication)
WO 2015007897 A1 20150122; CN 105555769 A 20160504; EP 3022183 A1 20160525
DOCDB simple family (application)
EP 2014065539 W 20140718; CN 201480051490 A 20140718; EP 14739853 A 20140718