Asymmetric Synthesis of Chiral C ₃ -Aminomethyl Cyclopentanones by Ene-Reductase-Catalyzed Kinetic Resolution via Desaturation

Chiral C₃-aminomethyl cyclopentanones are key intermediates in organic chemistry, yet their synthesis remains challenging. In this study, we present a kinetic resolution catalyzed by ene-reductases─OYE1 mutants─enabling C₃-aminomethyl cyclopentanones to be resolved into R-C₃-aminomethyl cyclopentanones (up to 99% e.e.) and corresponding α,β-unsaturated cyclopentanones via desaturation reactions. Remarkably, the reaction remains viable at the gram scale even with lower catalyst loadings, demonstrating potential for industrial-scale implementation.