Copper-catalysed 'click' chemistry is a highly utilised technique for radiolabelling small molecules and peptides for imaging applications. The usefulness of these reactions falls short, however, when metal catalysis is not a practically viable route; such as when using metal chelates as radioligands. Here, we describe a method for carrying out 'click-type' radiochemistry in the presence of DOTA chelates, by combining (68) Ga radiolabelling techniques with well-established bioorthogonal reactions, which do not rely upon metal catalysis.
Keywords: Bioorthogonal chemistry; DOTA; Gallium-68; azide; click chemistry; cyclooctyne; norbornene; strained alkene; tetrazine.
Copyright © 2013 John Wiley & Sons, Ltd.