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BioMed Research International
Volume 2014, Article ID 214748, 16 pages
Review Article

Sweetening Pharmaceutical Radiochemistry by 18F-Fluoroglycosylation: A Short Review

Molecular Imaging and Radiochemistry, Department of Nuclear Medicine, Friedrich Alexander University, Schwabachanlage 6, 91054 Erlangen, Germany

Received 19 March 2014; Accepted 15 April 2014; Published 1 June 2014

Academic Editor: Roland Haubner

Copyright © 2014 Simone Maschauer and Olaf Prante. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


At the time when the highly efficient [18F]FDG synthesis was discovered by the use of the effective precursor 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-β-D-mannopyranose (mannose triflate) for nucleophilic 18F-substitution, the field of PET in nuclear medicine experienced a long-term boom. Thirty years later, various strategies for chemoselective 18F-labeling of biomolecules have been developed, trying to keep up with the emerging field of radiopharmaceutical sciences. Among the new radiochemical strategies, chemoselective 18F-fluoroglycosylation methods aim at the sweetening of pharmaceutical radiochemistry by providing a powerful and highly valuable tool for the design of 18F-glycoconjugates with suitable in vivo properties for PET imaging studies. This paper provides a short review (reflecting the literature not older than 8 years) on the different 18F-fluoroglycosylation reactions that have been applied to the development of various 18F-glycoconjugate tracers, including not only peptides, but also nonpeptidic tracers and high-molecular-weight proteins.