[EN] SYNTHESIS OF ENANTIOMERICALLY PURE 2-HYDROXY-2-ARYL-ETHYLAMINES<br/>[FR] SYNTHÈSE DE 2-HYDROXY-2-ARYL-ÉTHYLAMINES ÉNANTIOMÉRIQUEMENT PURES
申请人:CAMBREX CHARLES CITY INC
公开号:WO2009086283A1
公开(公告)日:2009-07-09
The present invention relates to an improved process for preparing enantiomerically pure 2-hydroxy-2-aryl-ethylamines, and their pharmaceutically acceptable salts, by transition metal catalyzed asymmetric hydrogenation preferably using a ruthenium transition metal catalyst system having as a chiral, bidentate phosphine ligand ((R)-I -diphenylphosphino-2- [(S)-α-(N,N-dimethylamino)-o-diphenylphosphinophenyl)methyl] ferrocene), such as Chiralyst LM 1010 RS available from Umicore AG & Co., KG.
本发明涉及一种改进的制备对映纯2-羟基-2-芳基乙基胺及其药学可接受盐的方法,通过过渡金属催化不对称氢化,优选使用具有手性双齿膦配体的钌过渡金属催化剂体系(例如Chiralyst LM 1010 RS,由Umicore AG&Co. KG提供),该配体为((R)-I-二苯基膦酸-2- [(S)-α-(N,N-二甲基氨基)-o-二苯基膦酸苯基甲基]二茂铁)。