18F-labeling using click cycloadditions.

Abstract:

:Due to expanding applications of positron emission tomography (PET) there is a demand for developing new techniques to introduce fluorine-18 (t 1/2 = 109.8 min). Considering that most novel PET tracers are sensitive biomolecules and that direct introduction of fluorine-18 often needs harsh conditions, the insertion of (18)F in those molecules poses an exceeding challenge. Two major challenges during (18)F-labeling are a regioselective introduction and a fast and high yielding way under mild conditions. Furthermore, attention has to be paid to functionalities, which are usually present in complex structures of the target molecule. The Cu-catalyzed azide-alkyne cycloaddition (CuAAC) and several copper-free click reactions represent such methods for radiolabeling of sensitive molecules under the above-mentioned criteria. This minireview will provide a quick overview about the development of novel (18)F-labeled prosthetic groups for click cycloadditions and will summarize recent trends in copper-catalyzed and copper-free click (18)F-cycloadditions.

journal_name

Biomed Res Int

authors

Kettenbach K,Schieferstein H,Ross TL

doi

10.1155/2014/361329

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

361329

eissn

2314-6133

issn

2314-6141

journal_volume

2014

pub_type

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