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Rapid and efficient synthesis of [ 18 F]fluoronicotinamides, [ 18 F]fluoroisonicotinamides and [ 18 F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
Author(s) -
Al Jammaz I.,
AlOtaibi B.,
Okarvi S.,
Amartey J.
Publication year - 2011
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1869
Subject(s) - chemistry , benzamide , radiosynthesis , yield (engineering) , nucleophile , combinatorial chemistry , pet imaging , nicotinamide , imaging agent , chemical synthesis , radiochemistry , organic chemistry , in vivo , nuclear medicine , positron emission tomography , biochemistry , catalysis , medicine , materials science , microbiology and biotechnology , biology , metallurgy , in vitro , enzyme
In an attempt to simplify nucleophilic radiofluorination reactions to be amenable for automation, a series of [ 18 F]fluoronicotinamides, [ 18 F]fluoroisonicotinamides and [ 18 F]fluorobenzamides were synthesized using one‐step synthetic approach involving displacement reactions on trimethylammonium‐nicotinamide, trimethylammonium‐isonicotinamide and trimethylammonium‐benzamide precursors. Based on starting [ 18 F]‐fluoride, radiochemical yields and purities were found to be greater than 90 and 97%, respectively, within 20 min synthesis time and, without high‐performance liquid chromatography purification. This synthetic approach holds great promise as a rapid and simple method for the automated radiofluorination of [ 18 F]fluoronicotinamides, [ 18 F]fluoroisonicotinamides and [ 18 F]fluorobenzamides with high radiochemical yield and very short preparation time. Copyright © 2011 John Wiley & Sons, Ltd.

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