Synthesis of phosphinodepsipeptides via the pseudo-four-component condensation reaction

Phosphinodepsipeptides are recognized as an important class of enzyme inhibitors as tetrahedrally structural transition-state analogues to natural peptides. A series of phosphinodepsipeptides was synthesized in satisfactory yields via pseudo-four-component condensation reaction of 2-(N-benzoxycarbonylamino)alkanamides/peptide amides, aldehydes, and aryldichlorophosphines, followed by alcoholysis with hydroxyl esters.