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

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. Make a choice, make it right: Novel one‐pot deracemization cascade, employing amine dehydrogenase and ω‐transaminase, is reported for the synthesis of enantiopure amines with excellent conversions