D. Zhong, B. Blough, M. Kuhar
Feb 1, 2000
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
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.