ArticleOrganic & biomolecular chemistry2011
Syntheses of mGluR5 PET radioligands through the radiofluorination of diaryliodonium tosylates.
Article in Organic & biomolecular chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- The Current Role of Microfluidics in Radiofluorination Chemistry.Molecular imaging and biology · 2020Review
- Hypervalent aryliodine compounds as precursors for radiofluorination.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- Crystal Structures of Diaryliodonium Fluorides and Their Implications for Fluorination Mechanisms.Chemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
- Unexpected Behavior of the Heaviest Halogen Astatine in the Nucleophilic Substitution of Aryliodonium Salts.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
- Iodonium ylide-mediated radiofluorination of 18F-FPEB and validation for human use.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2015Article
- Fluorine-18 radiochemistry, labeling strategies and synthetic routes.Bioconjugate chemistry · 2015Review
- Microfluidic continuous-flow radiosynthesis of [MedChemComm · 2014Article
- Radiosyntheses using fluorine-18: the art and science of late stage fluorination.Current topics in medicinal chemistry · 2014Review
- Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).Journal of medicinal chemistry · 2013Article
- Single-step syntheses of no-carrier-added functionalized [18F]fluoroarenes as labeling synthons from diaryliodonium salts.Organic & biomolecular chemistry · 2013Article
- 4-[18F]Fluoro-m-hydroxyphenethylguanidine: a radiopharmaceutical for quantifying regional cardiac sympathetic nerve density with positron emission tomography.Journal of medicinal chemistry · 2013Article
- Radiofluorination of diaryliodonium tosylates under aqueous-organic and cryptand-free conditions.Organic & biomolecular chemistry · 2013Article
- Microfluidics: a groundbreaking technology for PET tracer production?Molecules (Basel, Switzerland) · 2013Review
- No-carrier-added [18F]fluoroarenes from the radiofluorination of diaryl sulfoxides.Chemical communications (Cambridge, England) · 2013Article
- Selective syntheses of no-carrier-added 2- and 3-[18F]fluorohalopyridines through the radiofluorination of halopyridinyl(4'-methoxyphenyl)iodonium tosylates.Chemical communications (Cambridge, England) · 2012Article
- Single-step Radiosyntheses of 'European journal of organic chemistry · 2012Article
- Regiospecific syntheses of functionalized diaryliodonium tosylates via [hydroxy(tosyloxy)iodo]arenes generated in situ from (diacetoxyiodo)arenes.The Journal of organic chemistry · 2012Article
Corrections and comments
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5 authors.
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Abstract
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 [(18)F]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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