Synthesis of Phosphinopeptides and Phosphinodepsipeptides

Both phosphinopeptides and phosphinodepsipeptides are important phosphorus analogues of naturally occurring peptides. They have been widely applied as biological active peptides, such as enzyme inhibitors, haptens for production of catalytic antibodies, and antibiotics. Synthetic methods of phosphinopeptides and phosphinodepsipeptides are reviewed and classified on the basis of the structural characteristics of aminoalkylphosphinic acids. This review focuses on the synthetic methods to phosphinopeptides and phosphinodepsipeptides, including α‐, β‐, and γ‐phosphinopeptides and α‐phosphinodepsipeptides.