@@ Phosphinopeptides are important phosphorus analogues of naturally occurring peptides. They have been widely used as enzyme inhibitors and as haptens for catalytic antibody research because they can be considered as stable mimetics of tetrahedral transition states in ester and amide hydrolysis and formation[1]. Several phosphonopeptides have also shown potent antibacterial activity and can be used as herbicidal agents[1,2]. To date, several efficient synthetic routes have been developed for synthesis of phosphinopeptides, including the reaction of N-protected aminoalkylphosphinic chlorides with amino acid esters or peptide esters, the direct condensation of aminoalkylphosphinic acids and amino esters or peptide esters in the presence of coupling reagents, such as DCC, BOP, DPPA, with additives HOBt or DMAP, in low yields, the enzyme-catalyzed condensation of phosphinate ethyl esters and amino esters in satisfactory yields[3]. However, N-protected aminoalkylphosphinic acid derivatives need to prepared firstly in all of the reported methods and the overall yields for the synthesis of phosphinopeptides are dissatisfactory in the most cases.
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