SYNTHESIS OF I-123 AND I-125 LABELED 5-IODO-6-NITROQUIPAZINE

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