Synthesis of [I-125]-3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester ([I-125]EINT)
A WIN 35,065‐2 analog, 3β‐(4‐ethyl‐3‐iodophenyl)nortropane‐2β‐carboxylic acid methyl ester (EINT), has been radiolabeled with iodine‐125 by radioiododestannylation of the trimethyltin derivative, N‐tert‐butoxycarbonyl‐3β‐(4‐ethyl‐3‐trimethyltinphenyl)nortropane‐2β‐carboxylic acid methyl ester (2), using carrier‐free sodium iodide‐125. The radiolabeling consists of a one‐pot, two‐step method entailing radioiododestannylation followed by nitrogen deprotection. Purification by reversed‐phase HPLC gives [125I]EINT in 34·2% yield with high radiochemical purity (>99%) and high specific activity (1988 mCi/μmol, 73·6 GBq/μmol, based on the specific activity of the Na125I used). Copyright © 2000 John Wiley & Sons, Ltd.
Zhong, D., Blough, B., Kuhar, M. J., & Carroll, F. (2000). Synthesis of [I-125]-3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester ([I-125]EINT). Journal of Labelled Compounds and Radiopharmaceuticals, 43(2), 137-146. https://doi.org/10.1002/(SICI)1099-1344(200002)43:23.0.CO;2-N