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

Robert H. Mach, S. Todd Elder, Thomas E. Morton, Peggy A. Nowak, Paul H. Evora, James G. Scripko, Robert T. Luedtke, Christopher D. Unsworth, Theresa Filtz, Anand V. Rao, Perry B. Molinoff, Richard L.E. Ehrenkaufer

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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.

Original languageEnglish
Pages (from-to)777-794
Number of pages18
JournalNuclear Medicine and Biology
Volume20
Issue number6
DOIs
Publication statusPublished - 1 Jan 1993

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