The first synthesis of unnatural β2,3,3-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 β2,3,3-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.
Keywords: C−C Cleavage; C−H Activation; One Pot Reaction; β-Amino Acids.
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