A convenient one-pot synthesis of phosphino-dipeptide analogs

A general one-pot synthesis is described for the preparation, in good overall yields, of phosphinopeptides as building blocks for peptide synthesis in the field of new enzyme inhibitors. This method, consisting of the addition of alkyl hypophosphites to imines and then in the Michael-addition of the resulting alkyl α-aminophosphonites on acrylates, affords the possibility of variations for the substituents in α and β position to the phosphorus atom and in α position to the nitrogen atom.