1044740-01-3Relevant academic research and scientific papers
Facile radiosynthesis of fluorine-18 labeled β-blockers. Synthesis, radiolabeling, and ex vivo biodistribution of [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol
Stephenson, Karin A.,Wilson, Alan A.,Meyer, Jeffrey H.,Houle, Sylvain,Vasdev, Neil
experimental part, p. 5093 - 5100 (2009/09/08)
An efficient and general method has been developed for fluorine-18 labeling of β-blockers that possess the propanolamine moiety. A new synthetically versatile intermediate, 3-(1-(benzyloxy)propan-2-yl)-2-oxooxazolidin-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, [18F]-(2S and 2R)-1-(1-fluoropropan-2-ylamino)-3-(m-tolyloxy)propan-2-ol ((2S and 2R)-[ 18F]1). The radiosyntheses were accomplished in 96% radiochemical and >99% enantiomeric purities, with specific activities of 0.9-1.1 Ci/μmol (EOS). Ex vivo biodistribution studies with the radiotracers demonstrated excessively rapid washout that may limit their use for cerebral PET imaging.
