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.