Functionalization of Unactivated Positions in α-Amino Acid Derivatives

Significance

The modification of natural amino acids is a straightforward route to useful unnatural or rare amino acids, which are constituents of important biologically active compounds. Herein, an elegant route for the functionalization of β- andγ-positions of natural leucine and isoleucine, based on an interesting Pd-mediated C-H activation, is described. It allows obtaining acetoxylated or arylated amino derivatives in very good yields and excellent diastereoselectivities in a single synthetic step.