POLYMER-SUPPORTED RADIOPHARMACEUTICALS - I-123 LABELED AND I-131-LABELED N-ISOPROPYL-4-IODOAMPHETAMINE

A trialkyltin chloride functionalized polystyrene has been reacted with p-bromophenyl lithium, the dilithio derivative from N-isopropyl-4-bromoamphetamine and the Grignard reagent from 2-(3-bromophenyl)-4,4-dimethyloxazoline. Reaction of the polymeric product bearing phenyloxazoline or N-isopropylamphetamine with iodine yielded 2-(3-iodophenyl)-4,4-dimethyloxazoline or N-isopropyl-4-iodoamphetamine in chemical yields consistent with about 0.4 meq/g of bound aromatics. Treatment with (NaI)-I-131 and an oxidant of the polymeric product bearing the p-bromophenyl group or the N-isopropylamphetamine group gave rise to no-carrier-added p-bromo[I-131]iodobenzene in 45% radiochemical yield or no-carrier-added N-isopropyl-4-[I-131]iodoamphetamine in 44% radiochemical yield. A similar reaction using (NaI)-I-123 gave N-isopropyl-4-[I-123]iodoamphetamine in 10% radio-chemical yield.