Asymmetric catalytic cascade processes are powerful since they offer direct access to complex chiral molecules from simple substrates and in a single step. In biocatalysis, cascades are generally designed by combining multiple enzymes, each catalyzing individual steps of a reaction sequence. Herein, we report a different strategy for biocatalytic cascades based on a single multifunctional enzyme that can promote multiple stereoselective steps of a domino process by mastering distinct catalytic mechanisms of substrate activation in a sequential way. Specifically, we have used an engineered 4-oxalocrotonate tautomerase (4-OT) enzyme with the ability to form both enamine and iminium ion intermediates and combine these mechanisms of catalysis in a complex sequence. This approach allowed us to activate aldehydes and enals toward the synthesis of enantiopure cyclohexene carbaldehydes bearing multiple stereogenic centers. The multifunctional 4-OT enzymes could successfully promote both a two-component reaction and a triple cascade characterized by different mechanistic features and activation sequences. This study demonstrates that biocatalytic strategies can match and even surpass in efficiency the potential of organocatalytic cascade catalysis.
Enantioselective Biocascade Catalysis with a Single Multifunctional Enzyme
Angew. Chem. Int. Ed. 2022, DOI: 10.1002/anie.202212176.