Radiosynthesis of 5-[18f]fluoro-1,2,3-triazoles through aqueous iodine–[18f]fluorine exchange reaction
In this report, a simple and efficient process to achieve fluorine-18-labeled 1,2,3-triazole is reported. The heteroaromatic radiofluorination was successfully achieved through an iodine– fluorine-18 exchange in an aqueous medium requiring only trace amounts of base and no azeotropic drying of fluorine-18. This methodology was optimized on a model reaction and further validated on multiple 1,2,3-triazole substrates with 18–60% radiochemical conversions. Using this strategy—the radiosynthesis of a triazole-based thiamin analogue—a potential positron emission tomography (PET) probe for imaging thiamin-dependent enzymes was synthesized with 10–16% isolated radiochemical yield (RCY) in 40 min (uncorrected, n > 5).
Zhang, X., Basuli, F., Abdelwahed, S., Begley, T., & Swenson, R. (2021). Radiosynthesis of 5-[18f]fluoro-1,2,3-triazoles through aqueous iodine–[18f]fluorine exchange reaction. Retrieved from https://digitalcommons.pvamu.edu/chemistry-physics-facpubs/1