The use of [18F]4-fluorobenzyl iodide (FBI) in PET radiotracer synthesis: model alkylation studies and its application in the design of dopamine D1 and D2 receptor-based imaging agents |
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Authors: | RH Mach ST Elder TE Morton PA Nowak PH Evora JG Scripko RR Luedtke CD Unsworth T Filtz AV Rao |
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Affiliation: | Cerebrovascular Research Center, University of Pennsylvania, Philadelphia 19104-6063. |
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Abstract: | [18F]4-Fluorobenzyl iodide ([18F]FBI) was prepared, and a series of model alkylation studies were conducted to determine its chemical reactivity toward nitrogen and sulfur nucleophiles of varying nucleophilicities. [18F]FBI was found to react rapidly with secondary amines and anilines to give the corresponding N-[18F]4-fluorobenzyl analogue in high yield. Amides and thiol groups required the use of a base catalyst. The utility of [18F]FBI was documented by investigation of dopamine D1 and D2 receptor-based radiotracers. |
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