Copper-Catalyzed Synthesis of -Amino Acids Featuring Quaternary Stereocenters

The first general asymmetric synthesis of -disubstituted -amino acids via Cu-catalyzed ring opening of non-strained lactones with amines is reported. This approach features ample scope, operational simplicity and wide functional group diversity. The catalytic process allows to access a series of highly functionalized enantioenriched -amino acids featuring quaternary stereocenters with excellent enantiomeric ratios up to 98:2 and excellent yields up to 98%