Straightforward Access to Free β^2,3,3-Amino Acids through One Pot C-H Activation/C−C Cleavage

The first synthesis of unnatural β^2,3,3-amino acids with a spirocyclic backbone by one-pot protocol has been presented. This reaction features wide functional group tolerance and feasibility of post-functionalization of natural products and biologically important molecules. Novel dipeptide and tripeptide structures were assembled using this newly developed β^2,3,3-amino acid in high efficiency. The combination of C−H activation and C−C cleavage for the synthesis of β-amino acids would trigger more promising synthetic routes for this compound.