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Synthesis of [ 125 I]‐3β‐(4‐ethyl‐3‐iodophenyl)nortropane‐2β‐carboxylic acid methyl ester ([ 125 I]EINT)
Author(s) -
Zhong Dsong,
Blough Bruce E.,
Kuhar Michael J.,
Carroll F. Ivy
Publication year - 2000
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(200002)43:2<137::aid-jlcr300>3.0.co;2-n
Subject(s) - chemistry , carboxylic acid , yield (engineering) , iodine , iodide , derivative (finance) , high performance liquid chromatography , methyl iodide , nuclear chemistry , ethyl iodide , chromatography , organic chemistry , materials science , economics , financial economics , metallurgy
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 [ 125 I]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 Na 125 I used). Copyright © 2000 John Wiley & Sons, Ltd.