Back to Search Start Over

Zinc‐Mediated Radiosynthesis of Unprotected Fluorine‐18 Labelled α‐Tertiary Amides.

Authors :
Wright, Jay S.
Ma, Richard
Webb, E. William
Winton, Wade P.
Stauff, Jenelle
Cheng, Kevin
Brooks, Allen F.
Sanford, Melanie S.
Scott, Peter J. H.
Source :
Angewandte Chemie; 1/8/2024, Vol. 136 Issue 2, p1-8, 8p
Publication Year :
2024

Abstract

This report describes the development of a Zn(OTf)2‐mediated method for converting α‐tertiary haloamides to the corresponding fluorine‐18 labelled α‐tertiary fluoroamides with no‐carrier‐added [18F]tetramethylammonium fluoride. 1,5,7‐Triazabicyclo[4.4.0]dec‐5‐ene is an essential additive for achieving high radiochemical conversion. Under the optimised conditions, radiofluorination proceeds at sterically hindered tertiary sites in high radiochemical conversions, yields, and purities. This method has been successfully automated and applied to access >200 mCi (>7.4 GBq) of several model radiofluorides. Mechanistic studies led to the development of a new, nucleophilic C−H radiofluorination process using N‐sulphonyloxyamide substrates. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
00448249
Volume :
136
Issue :
2
Database :
Complementary Index
Journal :
Angewandte Chemie
Publication Type :
Academic Journal
Accession number :
174635114
Full Text :
https://doi.org/10.1002/ange.202316365