发明名称 METHOD OF RACEMISATION OF UNDESIRED ENANTIOMERS
摘要 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 &bgr;-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.
申请公布号 EP3022183(A1) 申请公布日期 2016.05.25
申请号 EP20140739853 申请日期 2014.07.18
申请人 LEK PHARMACEUTICALS D.D. 发明人 STAVBER, GAJ;CLUZEAU, JEROME
分类号 C07D223/16;C07C33/20;C07C211/27;C07C211/29;C07C233/66;C07C271/14 主分类号 C07D223/16
代理机构 代理人
主权项
地址