THE USE OF F-18! 4-FLUOROBENZYL IODIDE (FBI) IN PET RADIOTRACER SYNTHESIS - MODEL ALKYLATION STUDIES AND ITS APPLICATION IN THE DESIGN OF DOPAMINE-D(1) AND DOPAMINE-D(2) RECEPTOR-BASED IMAGING AGENTS
Rh. Mach et al., THE USE OF F-18! 4-FLUOROBENZYL IODIDE (FBI) IN PET RADIOTRACER SYNTHESIS - MODEL ALKYLATION STUDIES AND ITS APPLICATION IN THE DESIGN OF DOPAMINE-D(1) AND DOPAMINE-D(2) RECEPTOR-BASED IMAGING AGENTS, Nuclear medicine and biology, 20(6), 1993, pp. 777-794
F-18!4-Fluorobenzyl iodide (F-18!FBI) was prepared, and a series of
model alkylation studies were conducted to determine its chemical reac
tivity toward nitrogen and sulfur nucleophiles of varying nucleophilic
ities. F-18!FBI was found to react rapidly with secondary amines and
anilines to give the corresponding N-F-18!4-fluorobenzyl analogue in
high yield. Amides and thiol groups required the use of a base catalys
t. The utility of F-18!FBI was documented by investigation of dopamin
e D1 and D2 receptor-based radiotracers.