METHODS FOR INCORPORATING METAL CHELATORS AT CARBOXYL-TERMINAL SITE OF PEPTIDES

摘要

Methods for incorporating metal chelators at carboxyl-terminal sites of peptides are presented. In a first method, a metal chelator which is a polyazacarboxylate with two free carboxyl groups is attached to a functionalized resin via one carboxyl group and to a diamine or orthogonally protected diamine via a second carboxyl group. The protecting group is removed and a sequence of amino acids is added to the diamine residue on solid support to form the desired peptide. After addition of the amino acid or peptide, the compound is cleaved from the resin and blocking groups are removed. In a second method, an orthogonally protected polyazacarboxylate with a free carboxyl and protected amine groups is reacted with a functionalized resin. The amine protecting group is removed and amino acids are added to obtain the desired peptide. The compound is then cleaved from the resin and blocking groups are removed. The cleavage from the resin and removal of blocking groups can be performed simultaneously.