Journal of labelled compounds and radiopharmaceuticals p. 835 - 845 (1996)
Update date:2022-08-12
Topics:
Katsifis, Andrew
Mattner, Filomena
McPhee, Meredith
Kassiou, Michael
Najdovski, Ljubco
Dikic, Branko
The (S) and (R)-[123I]iodinated analogues of the benzodiazepine receptor partial agonist bretazenil have been synthesised for study of the central benzodiazepine receptor using SPECT. (S)- and (R)-[123I]iodobretazenil were prepared from the appropriate tin precursors by electrophilic iododestannylation with Na[123I] in the presence of Chloramine-T. The products were purified by semi-preparative reverse-phase HPLC with radiochemical yields of 80% in a total synthesis time of 50 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%. The enantiomeric purity of the (S) and (R) isomers were greater than 97% as assessed by analytical chiral HPLC analysis.
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