Chiral Phosphoric Acid Catalyzed Transfer Hydrogenation: Facile Synthetic Access to Highly Optically Active Trifluoromethylated Amines

摘要

Chiral amines represent an important structural motif that can be found in a vast number of biologically active compounds. Many well-established drugs that are applicable in a diverse number of areas rely on this prominent pharmacophore. Among them are Cinacalcet (1) and NPS R-568 (2; hyperparathyroidism), Rivastigmine (3; Alzheimer's and Parkinson's disease), and Odanacatib (4; cathepsin K inhibitor; Scheme 1).