Strategies for the Production of [11C]LY2795050 for Clinical Use

Strategies for the Production of [11C]LY2795050 for Clinical Use

This report describes a comparison of four different routes for the clinical-scale radiosynthesis of the κ-opioid receptor antagonist [11C]­LY2795050. Palladium-mediated radiocyanation and radiocarbonylation of an aryl iodide precursor, as well as copper-mediated radiocyanation of an aryl iodide and...

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Veröffentlicht in:Organic process research & development 2023-02, Vol.27 (2), p.373-381
Hauptverfasser: Kaur, Tanpreet, Shao, Xia, Horikawa, Mami, Sharninghausen, Liam S., Preshlock, Sean, Brooks, Allen F., Henderson, Bradford D., Koeppe, Robert A., DaSilva, Alexandre F., Sanford, Melanie S., Scott, Peter J. H.
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container_end_page 381
container_issue 2
container_start_page 373
container_title Organic process research & development
container_volume 27
creator Kaur, Tanpreet
Shao, Xia
Horikawa, Mami
Sharninghausen, Liam S.
Preshlock, Sean
Brooks, Allen F.
Henderson, Bradford D.
Koeppe, Robert A.
DaSilva, Alexandre F.
Sanford, Melanie S.
Scott, Peter J. H.
description This report describes a comparison of four different routes for the clinical-scale radiosynthesis of the κ-opioid receptor antagonist [11C]­LY2795050. Palladium-mediated radiocyanation and radiocarbonylation of an aryl iodide precursor, as well as copper-mediated radiocyanation of an aryl iodide and an aryl boronate ester, have been investigated. Full automation of all four methods is reported, each of which provides [11C]­LY2795050 in sufficient radiochemical yield, molar activity, and radiochemical purity for clinical use. The advantages and disadvantages of each radiosynthesis method are compared and contrasted.
doi_str_mv 10.1021/acs.oprd.2c00388
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