Journal
SYNLETT
Volume 26, Issue 16, Pages 2257-2260Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0034-1381055
Keywords
carbon-11; carbon dioxide; Mitsunobu reaction; symmetrical urea; DBU
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Funding
- Medical Research Council (MRC) [MR/K022733/1]
- Department of Health through the National Institute for Health Research (NIHR) comprehensive Biomedical Research Centre award
- EPSRC
- European Commission [FP7-PEOPLE-2012-ITN, 316882]
- Medical Research Council [MR/K022733/1] Funding Source: researchfish
- MRC [MR/K022733/1] Funding Source: UKRI
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An efficient method to radiolabel symmetrical [C-11] ureas using 1,8-diazabicycloundec-7-ene (DBU) and cyclotron-produced [C-11]CO2 has been developed. [C-11] urea derivatives were obtained when aliphatic and aromatic amines were used with excellent radiochemical yields (RCYs) of over 70%. The mechanism of the reaction is proposed on the basis of control experiments. This simple and robust methodology provides a powerful tool to prepare C-11-labelled ureas previously inaccessible by existing methods and enable their utilisation for in vivo molecular imaging applications.
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