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Unlocking Ketone Activation for Enantioselective Aldol Reactions by 4-Oxalocrotonate Tautomerase
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AI
Y
Y
J
周
DOI：10.1002/cbic.70438.png)
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Abstract
En 中文
4-Oxalocrotonate tautomerase (4-OT) is a promising scaffold for asymmetric biocatalysis, but conventional 4-OT-catalyzed aldol reactions focus solely on aldehyde substrate activation. Herein, we report the directed evolution of a tandem-fused 4-OT enzyme that achieves efficient activation of ketone substrates for enantioselective aldol reactions with substituted benzaldehydes. The engineered biocatalyst yields a range of chiral β-hydroxy ketone products with up to 99% yield and moderate enantioselectivity, while enabling access to both target enantiomers. This work expands the substrate promiscuity and reaction scope of 4-OT, laying a foundation for rational design of next-generation 4-OT variants for advanced organic synthesis and industrial biocatalysis.
Keywords:
4-oxalocrotonate tautomerase
aldol reaction
asymmetric synthesis
biocatalysis
Journal
IF:
2.8
Papers:
854
Citations:
1.5W
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Cited Papers