LIGATION METHOD AND REAGENTS TO FORM AN AMIDE BOND

摘要

Methods and reagents for the formation of amide bonds between an activatedcarboxylic acid derivative and an azide useful in the synthesis of peptides,proteins and derivatized or labeled amino acids, peptide or proteins. Themethod involves the formation of a phosphinothioester which reacts with anazide resulting in amide formation. The invention provides phosphinothiolreagents which convert activated carboxylic acid derivatives tophosphinothioesters which then react with azides to form an amide bond. Themethods and reagents of the invention can be used for stepwise synthesis ofpeptides on solid supports or for the ligation to two or more amino acids, twoor more peptide or two or more protein fragments.