Asymmetric Synthesis of β²‐Aryl Amino Acids through Pd‐Catalyzed Enantiospecific and Regioselective Ring‐Opening Suzuki–Miyaura Arylation of Aziridine‐2‐carboxylates

Abstract

Abstract A Pd‐catalyzed enantiospecific and regioselective ring‐opening Suzuki–Miyaura arylation of aziridine‐2‐carboxylates was developed. The cross‐coupling allows for the asymmetric preparation of enantioenriched β 2 ‐aryl amino acids, starting from commercially available enantiopure d ‐ and l ‐serine esters. The mechanism and selectivity of the reaction was rationalized based on computational models.