Synthesis and biodistribution of ¹³¹I-BIB

The synthesis and biodistribution of ¹³¹I-1-iodo-2,5-bis(4’-amino)styrylbenzene (¹³¹I-BIB) were reported. The chemical structure of the labeling precursor 1-tributylstannyl -2,5-bis(4’-amino)styrylbenzene and all its intermediates were verified by IR，¹H NMR and MS respectively. The radioiodinated compound was prepared using iododestannylation reaction by hydrogen peroxide. Labeling yield was more than 60% and radiochemical purity was more than 90% determined by thin layer chromatography (TLC). The in vivo biodistribution of ¹³¹I-BIB in ICR mice showed that the value of brain uptake was the highest in 30 min.