686768-53-6Relevant articles and documents
Enhanced copper-mediated 18F-fluorination of aryl boronic esters provides eight radiotracers for PET applications
Preshlock, Sean,Calderwood, Samuel,Verhoog, Stefan,Tredwell, Matthew,Huiban, Mickael,Hienzsch, Antje,Gruber, Stefan,Wilson, Thomas C.,Taylor, Nicholas J.,Cailly, Thomas,Schedler, Michael,Collier, Thomas Lee,Passchier, Jan,Smits, René,Mollitor, Jan,Hoepping, Alexander,Mueller, Marco,Genicot, Christophe,Mercier, Jo?l,Gouverneur, Véronique
supporting information, p. 8361 - 8364 (2016/07/07)
[18F]FMTEB, [18F]FPEB, [18F]flumazenil, [18F]DAA1106, [18F]MFBG, [18F]FDOPA, [18F]FMT and [18F]FDA are prepared from the corresponding arylboronic esters and [18
Syntheses of mGluR5 PET radioligands through the radiofluorination of diaryliodonium tosylates
Telu, Sanjay,Chun, Joong-Hyun,Simeon, Fabrice G.,Lu, Shuiyu,Pike, Victor W.
experimental part, p. 6629 - 6638 (2011/11/04)
3-Fluoro-1-((thiazol-4-yl)ethynyl)benzenes constitute an important class of high-affinity metabotropic glutamate subtype 5 receptor (mGluR5) ligands, some of which have been labeled with fluorine-18 (t1/2 = 109.7 min), to provide radioligands for molecular imaging of brain mGluR5 in living animal and human subjects with positron emission tomography (PET). Labeling in the 3-fluoro position of such ligands can be achieved through aromatic nucleophilic substitution of a halide leaving group with [18F]fluoride ion when a weakly activating m-nitrile group is present, but is generally very low yielding (8%). Here we used a microfluidic reaction platform to show that greatly enhanced (up to 6-fold) radiochemical yields can be achieved from suitably synthesized diaryliodonium tosylate precursors. The presence of a m-nitrile or other activating group is not required. Similar conditions were adopted in a more conventional automated radiochemistry platform having a single-pot reactor, to produce mGluR5 radioligands with useful radioactivities for PET imaging.
