Applied Radioisotopes

New aqueous fluorination techniques

New aqueous fluorination techniques: 18F is a key isotope for the production of many radiopharmaceuticals. For decades, the addition of 18F to radiopharmaceutical precursors required harsh (high temperature, anhydrous) chemical conditions in order to provide adequate yields of the desired products. These conditions typically degrade more sensitive biomolecules, such as antibodies, peptides and proteins. Over the past 5 years, TRIUMF has worked collaboratively with scientists at the University of British Columbia and Simon Fraser University to develop two novel aqueous fluorination methods. Efforts with Dr. David Perrin (UBC, Chemistry) enabled the development of aqueous aryltrifuloroborate chemistry for rapid, 1-step incorporation of 18F onto peptides and other biomolecules; while those with Dr. Robert Britton have resulted in a novel method that uses a light-activated catalyst to place fluorine atoms on very specific locations of certain amino acids. These methods give radiopharmaceutical chemists new tools by which to produce radiopharmaceuticals that have been, until now, inaccessible or too difficult to produce.