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Automated synthesis and purification of [ 18 F]fluoro‐[ di‐deutero ]methyl tosylate
Author(s) -
Beyerlein Friederike,
Piel Markus,
Höhnemann Sabine,
Rösch Frank
Publication year - 2013
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.3043
Subject(s) - chemistry , yield (engineering) , nucleophile , chemical synthesis , deuterium , total synthesis , radiochemistry , organic chemistry , nuclear chemistry , catalysis , biochemistry , materials science , physics , quantum mechanics , metallurgy , in vitro
Automated synthetic procedures of [ 18 F]fluoro‐[ di‐deutero ]methyl tosylate on a GE TRACERlab FX F‐N module and a non‐commercial synthesis module have been developed. The syntheses included azeotropic drying of the [ 18 F]fluoride, nucleophilic 18 F‐fluorination of bis(tosyloxy)‐[ di‐deutero ]methane, HPLC purification and subsequent formulation of the synthesized [ 18 F]fluoro‐[ di‐deutero ]methyl tosylate ( d 2 ‐[ 18 F]FMT) in organic solvents. Automation shortened the total synthesis time to 50 min, resulting in an average radiochemical yield of about 50% and high radiochemical purity (>98%). The possible application of this procedure to commercially available synthesis modules might be of significance for the production of deuterated 18 F‐fluoromethylated imaging probes in the future. Copyright © 2013 John Wiley & Sons, Ltd.