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One‐pot radiosynthesis of [ 13 N]urea and [ 13 N]carbamate using no‐carrier‐added [ 13 N]NH 3
Author(s) -
Kumata Katsushi,
Takei Makoto,
Ogawa Masanao,
Kato Koichi,
Suzuki Kazutoshi,
Zhang MingRong
Publication year - 2009
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.1584
Subject(s) - chemistry , radiosynthesis , carbamate , isocyanate , urea , ligand (biochemistry) , triphosgene , nuclear chemistry , medicinal chemistry , phosgene , organic chemistry , positron emission tomography , medicine , biochemistry , receptor , polyurethane , radiology
Abstract The aim of this study was to develop a practical labeling method of [ 13 N]ligands using no‐carrier‐added [ 13 N]NH 3 with high specific activity. [ 13 N]urea analogues [ 13 N]1a and [ 13 N]2a or [ 13 N]carbamate [ 13 N]3a were synthesized by reacting isocyanate 5a, carbamoyl chloride 6a or chloroformate 7a with [ 13 N]NH 3 . The precursors 5a–7a were prepared by treating amines 8a and 9a and alcohol 10a with triphosgene in situ . These reaction mixtures were not purified and were used directly for [ 13 N]ammonolysis, respectively. Using the one‐pot method, we synthesized [ 13 N]carbamazepine ([ 13 N]4), a putative positron emission tomography ligand for brain imaging. Copyright © 2009 John Wiley & Sons, Ltd.