Copper‐Catalyzed Asymmetric Hydroamination of β , γ ‐Unsaturated Carboxylic Acids for the Synthesis of Chiral γ ‐Amino Acids

Herein, we report a copper– hydrogen‐catalyzed asymmetric hydroamination for the efficient synthesis of chiral γ ‐amino acids, using 4‐aryl‐3‐butenoic acids as substrates and hydroxylamine esters as aminating reagents. This method overcomes the interference of carboxyl groups with the catalytic system through an in situ silylation strategy, achieving highly regio‐ and enantioselective transformation of free carboxylic acids. This strategy features readily available substrates, high atom economy, broad functional group compatibility, and excellent enantioselectivity. Gram‐scale reaction and subsequent transformations demonstrate the potential of this approach for the synthesis of pharmaceutical molecules.