A 18F-labeled dibenzocyclooctyne (DBCO) derivative for copper-free click labeling of biomolecules

The new prosthetic group F-18-TEG-DBCO (dibenzocyclooctyne) can be prepared within a total reaction time of 60 min including purification with an overall yield (n.d.c.) of 34 +/- 5%. Copper-free click cycloadditions with an azido-cRGD, a folate-azide and two alpha-MSH analogue azido-peptides resulted in very high RCYs and fast reaction kinetics.