18F-Labelled Inorganic Fluorides & Radiopharmaceuticals

Since our initial collaborations with Prof. E. S. Garnett and Prof. R. V. Chirakal (McMaster Nuclear Medicine) in 1981, the expertise and techniques developed in our fundamental fluorine chemistry programs have been transferred to the field of Nuclear Medicine and to the syntheses of [¹⁸F]-radiopharmaceuticals (¹⁸F; a positron-emitting isotope of high specific activity and short half-life, 110 min, that is prepared using the Nuclear Medicine's cyclotron). Both [¹⁸F]F₂, and [¹⁸F]XeF₂ have been utilized for electrophilic radiofluorinations of a variety of compounds of biological interest, and in particular those which are of use for in vivo imaging of the human brain, e.g., [¹⁸F]fluorodopamine, [¹⁸F]fluoro-5-hydroxy-tryptophan, [¹⁸F]6-fluoro-3,4-dihydroxy-phenyl serine and [¹⁸F]2-deoxy-2-fluoro-glucose). These and other [¹⁸F]-labelled radiopharmaceuticals developed in collaboration with Prof. Chirakal's team to investigate, non-invasively, cerebral metabolism and disorders of the human brain such as Parkinson's disease and schizophrenia by positron emission tomography (P.E.T.). Recently, a reliable procedure for the formation of the ¹⁸F-labelled rare sugar, allose, was developed and shown, in an animal study, to have potential for breast tumor imaging and the assessment of lung fibrosis. Another recent discovery that melanoma tumors in mice can be imaged using an ¹⁸F-radiotracer is equally exciting.