Expedited synthesis of ?-amino acids by single-step enantioselective ?-amination of carboxylic acids

Abstract The conversion of C?H bonds to C?N offers a sustainable and economical strategy for the synthesis nitrogen-containing compounds. However, challenges regarding control regio- stereoselectivity currently limit broad applicability intermolecular C( sp 3 )?H amination reactions. We address these restrictions by directed nitrene-mediated insertion using metal-coordinating functional group. report highly stereocontrolled, iron-catalysed direct ?-amination abundant carboxylic acid feedstock molecules. method provides in single step high-value N -Boc-protected ?-monosubstituted ?,?-disubstituted ?-amino acids, which can then be immediately used applications including solution- solid-phase peptide synthesis. This fulfils important aspects sustainability being efficient utilizing non-toxic, Earth-abundant iron as catalytic metal.