133629-91-1Relevant academic research and scientific papers
Single-step syntheses of no-carrier-added functionalized [ 18F]fluoroarenes as labeling synthons from diaryliodonium salts
Chun, Joong-Hyun,Pike, Victor W.
, p. 6300 - 6306 (2013/09/23)
Radiotracers labelled with short-lived fluorine-18 (t1/2 = 109.7 min) are keenly sought for biomedical imaging with positron emission tomography (PET). The radiotracers are mostly required at high specific radioactivities, necessitating their radiosyntheses from cyclotron-produced no-carrier-added [18F]fluoride ion. PET radiotracers encompass wide structural diversity and molecular weight. Hence, diverse 18F-labeling methodology is needed to accomplish the required radiosyntheses in a simple and rapid manner. A useful strategy is to introduce nucleophilic [ 18F]fluoride ion first into a labeling synthon that may then be applied to label the target radiotracer. Here, we show that various functionalized [18F]fluoroarenes may be rapidly synthesized as labeling synthons through single-step reactions of appropriate diaryliodonium salts with [18F]fluoride ion. Decay-corrected radiochemical yields (RCYs) varied with position of functional group, choice of electron-rich aryl ring in the diaryliodonium salt, and choice of anion. Under best conditions, 18F-labeled fluorobenzaldehydes, fluorobenzyl halides, fluorobenzoic acid esters and fluorophenyl ketones were obtained selectively in 40-73%, 20-55%, 46-89% and 81-98% RCYs, respectively. This versatile straightforward methodology will enhance the scope for producing structurally complex, yet useful, PET radiotracers.
Fast and reliable method for the preparation of ortho- and para-[ 18F]fluorobenzyl halide derivatives: Key intermediates for the preparation of no-carrier-added PET aromatic radiopharmaceuticals
Lemaire, Christian,Libert, Lionel,Plenevaux, Alain,Aerts, Jo?l,Franci, Xavier,Luxen, André
, p. 48 - 55 (2012/06/18)
A fast and reliable method suitable for the automated preparation of (substituted) [18F]fluorobenzyl halides from several [ 18F]fluorobenzaldehydes was developed. Aromatic nucleophilic substitution of trimethylammonium benzaldehyde t
