A new cystine-glutamate exchanger inhibitor was created through the development of a new catalytic asymmetric synthesis method. Rh-catalyzed catalytic asymmetric hydrogenation of dehydro amino acid esters was expanded to the synthesis of chiral amino acid esters with bis-carbamate protection. The new chemistry was successfully applied to the synthesis of N-benzoyl diamino suberic acid, which showed potent inhibitory effects for cystine-glutamate exchangers, a promising molecular target for cancer therapy. More information can be found in the Communication by T. Shinada et al. on page 5145.