Radiosynthesis of 5-[18F]Fluoro-1,2,3-triazoles through Aqueous Iodine–[18F]Fluorine Exchange Reaction |
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| Authors: | Xiang Zhang Falguni Basuli Sameh Abdelwahed Tadhg Begley Rolf Swenson |
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| Institution: | 1.Chemistry and Synthesis Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD 20892, USA; (F.B.); (R.S.);2.Department of Chemistry, Prairie View A&M University, Prairie View, TX 77446, USA;3.Department of Chemistry, Texas A&M University, College Station, TX 77843, USA; |
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| Abstract: | 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). |
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| Keywords: | 1 2 3-triazole radiofluorination positron emission tomography halogen exchange thiamin azeotropic drying |
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