Biocatalytic Synthesis of Chiral N-Functionalized Amino Acids

N‐Functionalized amino acids are important building blocks for the preparation of diverse bioactive molecules, including peptides. The development of sustainable manufacturing routes to chiral N‐alkylated amino acids remains a significant challenge in the pharmaceutical and fine‐chemical industries. Herein we report the discovery of a structurally diverse panel of biocatalysts which catalyze the asymmetric synthesis of N‐alkyl amino acids through the reductive coupling of ketones and amines. Reactions have been performed on a gram scale to yield optically pure N‐alkyl‐functionalized products in high yields.