Aliphatic 18 F-Radiofluorination: Recent Advances in the Labeling of Base-Sensitive Substrates

Aliphatic fluorine-18 radiolabeling is the most commonly used method to synthesize tracers for PET-imaging. With an increasing demand for F-radiotracers for clinical applications, new labeling strategies aiming to increase radiochemical yields of established tracers or, more importantly, to enable F...

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Bibliographic Details
Published inChemMedChem Vol. 16; no. 17; pp. 2612 - 2622
Main Authors Bratteby, Klas, Shalgunov, Vladimir, Herth, Matthias Manfred
Format Journal Article
LanguageEnglish
Published Germany 06.09.2021
Subjects
Fluorine Radioisotopes
Halogenation
Humans
Molecular Conformation
Positron-Emission Tomography
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
aliphatic
fluorine-18
SN2
base sensitivity
radiochemistry
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Summary:Aliphatic fluorine-18 radiolabeling is the most commonly used method to synthesize tracers for PET-imaging. With an increasing demand for F-radiotracers for clinical applications, new labeling strategies aiming to increase radiochemical yields of established tracers or, more importantly, to enable F-labeling of new scaffolds have been developed. In recent years, increased attention has been focused on the direct aliphatic F-fluorination of base-sensitive substrates in this respect. This minireview gives a concise overview of the recent advances within this field and aims to highlight the advantages and limitations of these methods.
Bibliography:ObjectType-Article-2
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ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.202100303