Synthesis of N-(2-[18F]fluoroethyl)-N′-methylthiourea:: a hydrogen peroxide scavenger

被引：0
|
作者：
Gilissen, C [1 ]
Bormans, G [1 ]
de Groot, T [1 ]
Verbruggen, A [1 ]
机构：
[1] Catholic Univ Louvain, Lab Radiopharmaceut Chem FFW, B-3000 Louvain, Belgium
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1998年 / 41卷 / 06期
关键词：
DMTU; hydrogen peroxide; fluorine-18; oxidative stress;
D O I：
10.1002/(SICI)1099-1344(199806)41:6<491::AID-JLCR102>3.0.CO;2-9
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
N-(2-[F-18]fluoroethyl)-N'-methylthiourea ([F-18]FEMTU), a fluorine-18 labelled derivative of the hydrogen peroxide scavenger dimethylthiourea (DMTU), has been synthesized by reaction of 2-[F-18]fluoroethylamine with methylisothiocyanate. 2-[F-18]Fluoroethylamine was obtained in modest radiochemical yields (39+/-6%, mean+/-sd, n=5, decay corrected) by nucleophilic substitution with [F-18]fluoride on N-[2(p-toluenesulfonyloxy)ethyl] phthalimide followed by deprotection with hydrazine and distillation. The distilled 2-[F-18]fluoroethylamine was trapped in CH2Cl2 and reacted with methylisothiocyanate to yield [F-18]FEMTU that was purified by reversed phase HPLC. The total synthesis takes 150 min and provides [F-18]FEMTU with a specific activity of 3.3+0.5 GBq/mu mol (mean+/-sd, n=3) at end of synthesis, with an overall decay corrected radiochemical yield of 25+/-8% (mean+/-sd, n=5).
引用
收藏
页码：491 / 502
页数：12
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