Synthesis of [123I]N',N'-dimethyl-6-methyl-(4'-iodophenyl)imidazo[1,2-a]pyridine-3-acetamide for the study of peripheral benzodiazepine receptors using SPECT

Article abstract of DOI:10.1002/(SICI)1099-1344(20000330)43:4<385::AID-JLCR325>3.0.CO;2-K

The [¹²³I] labelled imidazo[1,2-a]pyridine [¹²³I]iodozolpidem 4 was found to exhibit preferential activity towards Peripheral rather than Central Benzodiazepine receptors in vivo and was synthesised for the potential study of the Peripheral Benzodiazepine Receptors (PBR) using SPECT. [¹²³I]Iodozolpidem was prepared from the corresponding tributyl tin precursor by iododestannylation with Na[¹²³I] in the presence of peracetic acid or chloramine-T. Purification by semipreparative C-18 RP HPLC gave the product in radiochemical yields of 60-85%. The product was obtained in > 97% chemical and radiochemical puritiy with a specific activity > 80 GBq/μmol.