18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands

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18F-Labelling of electron rich iodonium ylides : application to the radiosynthesis of potential 5-HT2A receptor PET ligands. / Petersen, I N; Villadsen, J; Hansen, H D; Madsen, J; Jensen, A A; Gillings, N; Lehel, Szabolcs; Herth, M M; Knudsen, G M; Kristensen, J L.

In: Organic & Biomolecular Chemistry, Vol. 15, 04.2017, p. 4351-4358.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Petersen, IN, Villadsen, J, Hansen, HD, Madsen, J, Jensen, AA, Gillings, N, Lehel, S, Herth, MM, Knudsen, GM & Kristensen, JL 2017, '18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands', Organic & Biomolecular Chemistry, vol. 15, pp. 4351-4358. https://doi.org/10.1039/c7ob00628d

APA

Petersen, I. N., Villadsen, J., Hansen, H. D., Madsen, J., Jensen, A. A., Gillings, N., ... Kristensen, J. L. (2017). 18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands. Organic & Biomolecular Chemistry, 15, 4351-4358. https://doi.org/10.1039/c7ob00628d

Vancouver

Petersen IN, Villadsen J, Hansen HD, Madsen J, Jensen AA, Gillings N et al. 18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands. Organic & Biomolecular Chemistry. 2017 Apr;15:4351-4358. https://doi.org/10.1039/c7ob00628d

Author

Petersen, I N ; Villadsen, J ; Hansen, H D ; Madsen, J ; Jensen, A A ; Gillings, N ; Lehel, Szabolcs ; Herth, M M ; Knudsen, G M ; Kristensen, J L. / 18F-Labelling of electron rich iodonium ylides : application to the radiosynthesis of potential 5-HT2A receptor PET ligands. In: Organic & Biomolecular Chemistry. 2017 ; Vol. 15. pp. 4351-4358.

Bibtex

@article{e95ed52a8c0a4a8682f38b9f7f4cd550,
title = "18F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT2A receptor PET ligands",
abstract = "(18)F-Labelling of aromatic moieties was limited to electron deficient aromatic systems for many years but recent developments have provided access to the direct labelling of electron rich aromatic systems. Herein we report the synthesis and (18)F-labelling of iodonium ylide precursors in the pursuit of (18)F-labelled 5-HT2A receptor agonist PET-ligands. Subsequent evaluation in pigs showed high brain uptake of the PET ligands but a blocking dose of ketanserin did not significantly reduce the signal in relevant brain regions - indicating that the ligands do not interact specifically with the 5-HT2A receptor in vivo.",
keywords = "Journal Article",
author = "Petersen, {I N} and J Villadsen and Hansen, {H D} and J Madsen and Jensen, {A A} and N Gillings and Szabolcs Lehel and Herth, {M M} and Knudsen, {G M} and Kristensen, {J L}",
year = "2017",
month = "4",
doi = "10.1039/c7ob00628d",
language = "English",
volume = "15",
pages = "4351--4358",
journal = "Organic & Biomolecular Chemistry",
issn = "1477-0520",
publisher = "Royal Society of Chemistry",

}

RIS

TY - JOUR

T1 - 18F-Labelling of electron rich iodonium ylides

T2 - application to the radiosynthesis of potential 5-HT2A receptor PET ligands

AU - Petersen, I N

AU - Villadsen, J

AU - Hansen, H D

AU - Madsen, J

AU - Jensen, A A

AU - Gillings, N

AU - Lehel, Szabolcs

AU - Herth, M M

AU - Knudsen, G M

AU - Kristensen, J L

PY - 2017/4

Y1 - 2017/4

N2 - (18)F-Labelling of aromatic moieties was limited to electron deficient aromatic systems for many years but recent developments have provided access to the direct labelling of electron rich aromatic systems. Herein we report the synthesis and (18)F-labelling of iodonium ylide precursors in the pursuit of (18)F-labelled 5-HT2A receptor agonist PET-ligands. Subsequent evaluation in pigs showed high brain uptake of the PET ligands but a blocking dose of ketanserin did not significantly reduce the signal in relevant brain regions - indicating that the ligands do not interact specifically with the 5-HT2A receptor in vivo.

AB - (18)F-Labelling of aromatic moieties was limited to electron deficient aromatic systems for many years but recent developments have provided access to the direct labelling of electron rich aromatic systems. Herein we report the synthesis and (18)F-labelling of iodonium ylide precursors in the pursuit of (18)F-labelled 5-HT2A receptor agonist PET-ligands. Subsequent evaluation in pigs showed high brain uptake of the PET ligands but a blocking dose of ketanserin did not significantly reduce the signal in relevant brain regions - indicating that the ligands do not interact specifically with the 5-HT2A receptor in vivo.

KW - Journal Article

U2 - 10.1039/c7ob00628d

DO - 10.1039/c7ob00628d

M3 - Journal article

C2 - 28474719

VL - 15

SP - 4351

EP - 4358

JO - Organic & Biomolecular Chemistry

JF - Organic & Biomolecular Chemistry

SN - 1477-0520

ER -

ID: 177414505