Reductive amination

A solution of amine compound (0.19 M in dichloroethane, 400 μL, 75 μmol) was placed in an 8 mL vial and treated with the aldehyde component (0,25 M solution so dichloroethane, 300 μL, 75 μmol). Sodium triacetoxyborohydride (225 μmol) was added to each vial, which was then capped and shaken at 30°C for 16 hours. Solvent was removed using a SpeedVac system, and the crude products were purified by preparative HPLC. 


Patent reference: WO2010058333 (Pfizer)