Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 9, Issue 19, Pages 6629-6638Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c1ob05555k
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Funding
- National Institutes of Health (NIMH)
- NATIONAL INSTITUTE OF MENTAL HEALTH [ZIAMH002793] Funding Source: NIH RePORTER
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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 (t(1/2) = 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 [F-18] 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.
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