Direct asymmetric reductive amination of α-keto acetals: a platform for synthesizing diverse α-functionalized amines

We report an efficient and straightforward method to synthesize enantio-enriched N -unprotected α-amino acetals via ruthenium-catalyzed direct asymmetric reductive amination. The α-amino acetal products are versatile and valuable platform molecules that can be converted to the corresponding α-amino acids, amino alcohols, and other derivatives by convenient transformations. A highly enantioselective synthesis of synthetically valuable and versatile α-functionalized chiral primary amines was achieved via Ru-catalyzed direct asymmetric reductive amination of easily available α-keto acetals with ammonium salts and H 2 .