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Synthesis of 11C-Labelled Symmetrical Ureas via the Rapid Incorporation of [11C]CO2 into Aliphatic and Aromatic Amines
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2015
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Combinatorial ChemistryNovel OrganocatalystsEngineering11C-labelled Symmetrical UreasBiochemistryNatural SciencesDiversity-oriented SynthesisAromatic AminesRadiopharmaceutical TherapyOrganic ChemistryExcellent Radiochemical YieldsChemistryRobust MethodologySynthetic ChemistryRapid IncorporationBiomolecular Engineering
An efficient method to radiolabel symmetrical [<sup>11</sup>C]ureas using 1,8-diazabicycloundec-7-ene (DBU) and cyclotron-produced [<sup>11</sup>C]CO<sub>2</sub> has been developed. [<sup>11</sup>C]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 <sup>11</sup>C-labelled ureas previously inaccessible by existing methods and enable their utilisation for in vivo molecular imaging applications.