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.