Deracemization of Racemic Amines to Enantiopure (R)‐ and (S)‐amines by Biocatalytic Cascade Employing ω‐Transaminase and Amine Dehydrogenase

Abstract A one‐pot deracemization strategy for α‐chiral amines is reported involving an enantioselective deamination to the corresponding ketone followed by a stereoselective amination by enantiocomplementary biocatalysts. Notably, this cascade employing a ω‐transaminase and amine dehydrogenase enabled the access to both ( R )‐and ( S )‐amine products, just by controlling the directions of the reactions catalyzed by them. A wide range of ( R )‐and ( S )‐amines was obtained with excellent conversions (>80 %) and enantiomeric excess (>99 % ee ). Finally, preparative scale syntheses led to obtain enantiopure ( R )‐ and ( S )‐ 13 with the isolated yields of 53 and 75 %, respectively.