Synthesis of 123I and 125I-labelled 5-iodo-6-nitroquipazine

Article abstract of DOI:10.1002/jlcr.2580341003

The syntheses of the potent and selective serotonin reuptake complex radioligands [¹²³I]- and [¹²⁵I]5-iodo-6-nitroquipazine (5-iodo-6-nitro-2-piperazinylquinoline) are reported. A seven step synthetic sequence provided the BOC-protected 5-tributyltin-6-nitroquipazine precursor for radioiodination. End of synthesis radioiodination yields of -40% for ¹²³I and ~ 60% for ¹²⁵I were achieved resulting in labelled products with high specific activities (>4000 and >2000 Ci/mmol, respectively) and radiochemical purities (>98%).