A Transmetalation Reaction Enables the Synthesis of [18F]5-Fluorouracil from [18F]Fluoride for Human PET Imaging

Translation of new 18F-fluorination reactions to produce radiotracers for human positron emission tomography (PET) imaging is rare because the chemistry must have useful scope and the process for 18F-labeled tracer production must be robust and simple to execute. The application of transition metal...

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Veröffentlicht in:Organometallics. - 1998. - 35(2016), 7 vom: 11. Apr., Seite 1008-1014
1. Verfasser: Hoover, Andrew J (VerfasserIn)
Weitere Verfasser: Lazari, Mark, Ren, Hong, Narayanam, Maruthi Kumar, Murphy, Jennifer M, van Dam, R Michael, Hooker, Jacob M, Ritter, Tobias
Format: Aufsatz
Sprache:English
Veröffentlicht: 2016
Zugriff auf das übergeordnete Werk:Organometallics
Schlagworte:Journal Article
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520 |a Translation of new 18F-fluorination reactions to produce radiotracers for human positron emission tomography (PET) imaging is rare because the chemistry must have useful scope and the process for 18F-labeled tracer production must be robust and simple to execute. The application of transition metal mediators has enabled impactful 18F-fluorination methods, but to date none of these reactions have been applied to produce a human-injectable PET tracer. In this article we present chemistry and process innovations that culminate in the first production from [18F]fluoride of human doses of [18F]5-fluorouracil, a PET tracer for cancer imaging in humans. The first preparation of nickel σ-aryl complexes by transmetalation from arylboronic acids or esters was developed and enabled the synthesis of the [18F]5-fluorouracil precursor. Routine production of >10 mCi doses of [18F]5-fluorouracil was accomplished with a new instrument for azeotrope-free [18F]fluoride concentration in a process that leverages the tolerance of water in nickel-mediated 18F-fluorination 
650 4 |a Journal Article 
700 1 |a Lazari, Mark  |e verfasserin  |4 aut 
700 1 |a Ren, Hong  |e verfasserin  |4 aut 
700 1 |a Narayanam, Maruthi Kumar  |e verfasserin  |4 aut 
700 1 |a Murphy, Jennifer M  |e verfasserin  |4 aut 
700 1 |a van Dam, R Michael  |e verfasserin  |4 aut 
700 1 |a Hooker, Jacob M  |e verfasserin  |4 aut 
700 1 |a Ritter, Tobias  |e verfasserin  |4 aut 
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