Process for the preparation of nonracemic syn-1-(4-hydroxy-phenyl)-2-(4-hydroxy-4-phenyl -piperidin-1-yl)-1-propanol compounds
申请人:DSM CATALYTICA PHARMACEUTICALS, INC.
公开号:US20030144521A1
公开(公告)日:2003-07-31
The present invention provides a process for the preparation of a nonracemic diastereomer of 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding nonracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanone using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.
本发明提供了一种制备非外消旋对映体1-(4-苯氧基苯基)-2-(4-羟基-4-苯基哌啶-1-基)-1-丙醇的方法,通过使用催化剂体系对相应的非外消旋1-(4-苯氧基苯基)-2-(4-羟基-4-苯基哌啶-1-基)-1-丙酮进行加氢反应,所述催化剂体系包括钌、非外消旋二膦配体、从氨基硫醚和非手性二胺中选择的双齿胺配体以及碱。