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Synthesis of iodine‐123 labelled analogues of imidazenil and ethyl‐imidazenil for studying benzodiazepine receptors using SPECT
Author(s) -
Katsifis Andrew,
Mattner Filomena,
Dikic Branko,
Najdovski Ljubco,
Kassiou Michael
Publication year - 1996
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/(sici)1099-1344(199612)38:12<1121::aid-jlcr948>3.0.co;2-v
Subject(s) - chemistry , iodine , high performance liquid chromatography , acetic acid , peracetic acid , methyl iodide , chloramine t , receptor , bromine , iodide , benzodiazepine , radiochemistry , nuclear chemistry , chromatography , medicinal chemistry , organic chemistry , biochemistry , hydrogen peroxide
The [ 123 I]iodinated analogues of the benzodiazepine receptor partial agonist imidazenil and N‐ethyl imidazenil have been synthesised for the study of the central benzodiazepine receptor using SPECT. [ 123 I]Iodoimidazenil and [ 123 I]N‐ethyliodoimidazenil were prepared by nucleophilic bromine‐iodine exchange in acetic acid at 150°. The products were purified by semi‐preparative reverse‐phase HPLC with average radiochemical yields of 80% in a total synthesis time of 80 minutes. The specific activity was determined to be greater than 2500 Ci/mmol. The radiochemical and chemical purity assessed by radio‐TLC and HPLC were found to be 98%. Alternatively, iododestannylation reactions via the trimethyltin precursors with Na[ 123 I] in the presence of Chloramine‐T or peracetic acid resulted in yields of only 20–25% with the bulk of activity being lost as volatile methyl [ 123 I]iodide.