A convenient one-pot synthesis of phosphino-dipeptide analogs

A general one-pot synthesis is described for the preparation, in good overa ll yields, of phosphinopeptides as building blocks for peptide synthesis in the field of new enzyme inhibitors. This method, consisting of the additio n of alkyl hypophosphites to imines and then in the Michael-addition of the resulting alkyl alpha -aminophosphonites on acrylates, affords the possibi lity of variations for the substituents in alpha and beta position to the p hosphorus atom and in alpha position to the nitrogen atom. (C) 2001 Elsevie r Science Ltd. All rights reserved.