Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 16, Pages 5093-5100Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800227h
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Funding
- Natural Sciences and Engineering Research Council of Canada (NSERC)
- Canadian Institutes for Health Research [CHRPJ 322787-06]
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An efficient and genral method has been developed for fluorine-18 labeling of beta-blockers that possess the propanolamine moiety. A new synthetically versatile intermediate, 3-(1-(benzyloxy)propan-2-yl)-2-oxoox-azolidin-5-yl)methyl 4-methylbenzenesulfonate (13), was prepared and can be conjugated to any phenoxy core. To demonstrate the synthetic methodology, fluorinated derivatives of toliprolol were prepared, namely, [(18)F]-(2S and 2R)-]-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ((2S and 2R)-[(18)F]1). The radiosyntheses were accomplished in < 1 h, with 20-24% (uncorrected for decay, n = 7) radiochemical yields, > 96% radiochemical and > 99% enantiomeric purities, with specific activities of 0.9-1.1 Ci/mu mol(EOS). Ex vivo biodistribution studies with the radiotracers demonstrated excessively rapid washout that May limit their use for cerebral PET imaging.
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