Synthesis of [125I]-3β-(4-ethyl-3-iodophenyl)nortropane-2β-carboxylic acid methyl ester ([125I]EINT)

被引：0

作者：

Zhong, DS

Blough, BE

Kuhar, MJ

Carroll, FI

机构：

[1] Res Triangle Inst, Res Triangle Pk, NC 27709 USA

[2] Emory Univ, Yerkes Reg Primate Res Ctr, Atlanta, GA 30329 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2000年 / 43卷 / 02期

关键词：

radioiodination; iodine-125; labeling; serotonin transporter; iododestannylation; chloramine-T; I-125]EINT;

D O I：

10.1002/(SICI)1099-1344(200002)43:2<137::AID-JLCR300>3.0.CO;2-N

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A WIN 35,065-2 analog, 3 beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester (EINT), has been radiolabeled with iodine-125 by radioiododestannylation of the trimethyltin derivative, N-tert-butoxycarbonyl-3 beta- (4-ethyl-3-trimethyltinphenyl)nortropane-2 beta- 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 [I-125]EINT in 34.2% yield with high radiochemical purity (>99%) and high specific activity (1988 mCi/mu mol, 73.6 GBq/mu mol, based on the specific activity of the (NaI)-I-125 used).

引用

页码：137 / 146

页数：10

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