The Facile Synthesis of Dialkyl 1-Aminoalkylphosphonates

Abstract

During past several years we have been engaged in the synthesis of phosphono peptides, peptide analogues with phosphonic acid replacing C-terminal carboxylate moiety. They became increasingly important since they appeared useful as carriers of toxic aminoalkylphosphonic acids through bacterial cell wall^1–4 or into plant tissues.^1,5 The most succesful method for the synthesis of these peptides is the condensation of N-blocked amino acids with dialkyl 6,7 or diphenyl 8.9 esters of aminoalkylphosphonic acids followed by removal of protecting groups.