6533b82efe1ef96bd12925c7

RESEARCH PRODUCT

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

K. KettenbachT. L. RossT. L. Ross

subject

Pharmacologychemistry.chemical_classificationbiology010405 organic chemistryBiomoleculeOrganic ChemistryPharmaceutical Sciencechemistry.chemical_element010402 general chemistry01 natural sciencesBiochemistryCombinatorial chemistryCopperCofactor0104 chemical sciencesChemical kineticschemistry.chemical_compoundchemistryYield (chemistry)Drug Discoverybiology.proteinMolecular MedicineDerivative (chemistry)

description

The new prosthetic group 18F-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 α-MSH analogue azido-peptides resulted in very high RCYs and fast reaction kinetics.

https://doi.org/10.1039/c5md00508f