Stereodivergent Synthesis of 3‐Hydroxyprolines and 3‐Hydroxypipecolic Acids via Ketoreductase‐Catalyzed Dynamic Kinetic Reduction

Abstract We report a practical enzymatic approach for the stereoselective synthesis of hydroxylated cyclic amino acids. Using ketoreductases, cyclic ketoesters are converted with high diastereo‐ and enantioselectivity to all isomers of 3‐hydroxyproline and 3‐hydroxypipecolic acid via a dynamic kinetic reduction reaction. This work highlights the ability of enzymes to provide solutions to challenges in stereoselective synthesis. magnified image