VERFAHREN ZUR ERZEUGUNG VON METALLCHELATAFFINITÄTSLIGANDEN

摘要

The present invention relates to a method of generating at least one polydentate metal chelating affinity ligand, which method comprises the steps of (a) providing at least one cyclic scaffold comprising a carbonyl, an adjacent sulphur and a nucleophile; (b) providing at least one polydentate metal chelating affinity ligand arm, optionally in a form wherein the metal chelating functionalities are protected, on each scaffold by derivatisation of the nucleophile of said scaffolds, while retaining the cyclic structure of the scaffold; (c) ring-opening at the bond between the carbonyl and the sulphur of the derivatised scaffold by adding a reagent that adds one or more metal chelating affinity ligand arms to the scaffold; and, if required, (d) deprotecting the functionalities of the ligand arm(s) provided in step (b). In the most preferred embodiment of the method, steps (c) and (d) are performed simultaneously as one single step.