Synthesis of iodine-123 labelled analogues of the partial agonist (S)- and (R)-bretazenil for the study of CNS benzodiazepine receptors using SPECT

✍ Scribed by Andrew Katsifis; Filomena Mattner; Meredith McPhee; Michael Kassiou; Ljubco Najdovski; Branko Dikic

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: French
• Weight: 673 KB
• Volume: 38
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/(sici)1099-1344(199609)38:9<835::aid-jlcr898>3.0.co;2-z

✦ Synopsis

The (S) and (R)- ['231]iodinated analogues of the benzodiazepine receptor partial agonist bretazenil have been synthesised for study of the central benzodiazepine receptor using SPECT. (S)and (R)-['Z31]iodobretnil were prepared from the appropriate tin precursors by electrophilic iododestannylation with Na['? 'I] 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 Cimmol. 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 c h i d HPLC analysis.