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

摘要: The (S) and (R)-[ 123 I]iodinated analogues of the benzodiazepine receptor partial agonist bretazenil have been synthesised for study central using SPECT. (S)- I]iodobretazenil were prepared from appropriate tin precursors by electrophilic iododestannylation with Na[ I] in presence Chloramine-T. products purified semi-preparative reverse-phase HPLC radiochemical yields 80% a total synthesis time 50 minutes. specific activity was determined to be greater than 2500 Ci/mmol. chemical purity assessed radio-TLC found 98%. enantiomeric (R) isomers 97% as analytical chiral analysis.