Frederick T. Chin, Ph.D.
Publication Details
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Efficient O- and N-(-fluoroethylation)s with NCA [18F]-fluoroethyl tosylate under microwave-enhanced conditions
Journal of Labelled Compounds and Radiopharmaceuticals. 2004; (5): 289-297
Reactions of no-carrier-added (NCA) [18F]-fluoroethyl tosylate with amine, phenol or carboxylic acid to form the corresponding [18F]N-(-fluoroethyl)amine, [18F]-fluoroethyl ether or [18F]-fluoroethyl ester, were found to be rapid (2-10 min) and efficient (51-89% conversion) under microwave-enhanced conditions. These conditions allow reactants to be heated rapidly to 150°C in a low boiling point solvent, such as acetonitrile, and avoid the need to use high boiling point solvents, such as DMSO and DMF, to promote reaction. The microwave-enhanced reactions gave about 20% greater radiochemical yields than thermal reactions performed at similar temperatures and over similar reaction times. With a bi-functional molecule, such as DL-pipecolinic acid, [18F]-fluoroethyl tosylate reacts exclusively with the amino group.
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