Preprint Review Version 1 Preserved in Portico This version is not peer-reviewed

Sweetening Pharmaceutical Radiochemistry by 18F-Fluoroglycosylation: Recent Progress and Future Prospects

Version 1 : Received: 14 October 2021 / Approved: 18 October 2021 / Online: 18 October 2021 (11:10:02 CEST)

A peer-reviewed article of this Preprint also exists.

Shinde, S.S.; Maschauer, S.; Prante, O. Sweetening Pharmaceutical Radiochemistry by 18F-Fluoroglycosylation: Recent Progress and Future Prospects. Pharmaceuticals 2021, 14, 1175. Shinde, S.S.; Maschauer, S.; Prante, O. Sweetening Pharmaceutical Radiochemistry by 18F-Fluoroglycosylation: Recent Progress and Future Prospects. Pharmaceuticals 2021, 14, 1175.

Abstract

In the field of 18F-chemistry for the development of radiopharmaceuticals for positron emission tomography (PET), various labeling strategies by the use of prosthetic groups have been im-plemented, including chemoselective 18F-labeling of biomolecules. Among those, chemoselec-tive 18F-fluoroglycosylation methods focus on the sweetening of pharmaceutical radiochemistry by offering a highly valuable tool for the synthesis of 18F-glycoconjugates with suitable in vivo properties for PET imaging studies. A previous review covered the various 18F-fluoroglycosylation methods that have been developed and applied as of 2014 [Maschauer and Prante, BioMed. Res. Int. 2014, 214748]. This paper is an updated review, providing the recent progress in 18F-fluoroglycosylation reactions and the preclinical application of 18F-glycoconjugates, including small molecules, peptides, and high-molecular-weight proteins.

Keywords

fluorine-18; prosthetic group; 18F-fluoroglycosylation; positron emission tomography; PET

Subject

Chemistry and Materials Science, Medicinal Chemistry

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