Palladium(0)-catalyzed Mizoroki–Heck reaction and Rh(I)-catalyzed asymmetric hydrogenation of polymer-supported dehydroalanine system

We have developed a practical route for the synthesis of peptides containing unnatural amino acids. Mizoroki–Heck reaction of polymer-supported dehydroalanine, followed by asymmetric hydrogenation was accomplished using Pd(0) and Rh(I)–DuPHOS catalysts, respectively, leading to 36 dipeptides containing phenylalanine derivatives with high stereocontrol.