Strained Ammonium Precursors for Radiofluorinations

Published on Jun 1, 2022in ChemistryOpen
· DOI :10.1002/open.202200039
Falco Reissig6
Estimated H-index: 6
(HZDR: Helmholtz-Zentrum Dresden-Rossendorf),
Constantin Mamat17
Estimated H-index: 17
(HZDR: Helmholtz-Zentrum Dresden-Rossendorf)
The increasing application of positron emission tomography (PET) in nuclear medicine has stimulated the extensive development of a multitude of novel and versatile techniques to introduce fluorine-18, especially for the radiolabelling of biologically or pharmacologically active molecules. Taking into consideration that the introduction of fluorine-18 (t1/2 =109.8 min) mostly proceeds under harsh conditions, radiolabelling of such molecules represents a challenge and is of enormous interest. Ideally, it should proceed in a regioselective manner under mild physiological conditions, in an acceptable time span, with high yields and high specific activities. Special attention has been drawn to 2-fluoroethyl and 3-fluoropropyl groups, which are often the active sites of radiofluorinated compounds. Precursors containing an ammonium leaving group - such as a strained azetidinium or aziridinium moiety - can help to overcome these obstacles leading to a convenient and mild introduction of [18 F]fluoride with high radiochemical yields.
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