Original and efficient method for the preparation of N-aminoamide pseudodipeptides in high optical purity

N-Aminoamide pseudodipeptides ZAAΨ[CO-N(NPht)]-AAOR can be easily obtained via the Mitsunobu protocol by using α-hydroxyesters as alcohol partners and aminoacid phthaloyl hydrazide derivatives as acidic partners. The direct conversion of the phthaloyl group into tert-butyloxycarbonyl can be performed in a three-stage one-pot protocol.