A one-step automated high-radiochemical-yield synthesis of 18F-FECNT from mesylate precursor

被引：16

作者：

Chen, Zheng Ping ^{[1
,2
]}

Wang, Song Pei ^{[2
]}

Li, Xiao Min ^{[2
]}

Liu, Chun Yi ^{[2
]}

Tang, Jie ^{[2
]}

Cao, Guo Xian ^{[2
]}

Luo, Shi Neng ^{[2
]}

Zhang, Lian Fen ^{[1
]}

Jin, Jian ^{[1
]}

机构：

[1] Jiangnan Univ, Sch Med & Pharmaceut, Wuxi 214122, Peoples R China

[2] Jiangsu Inst Nucl Med, Minist Hlth PRC, Key Lab Nucl Med, Wuxi 214063, Peoples R China

来源：

APPLIED RADIATION AND ISOTOPES | 2008年 / 66卷 / 12期

基金：

中国国家自然科学基金;

关键词：

F-18-FECNT; Automated synthesis; One-step; Dopamine transporter; PET;

D O I：

10.1016/j.apradiso.2008.05.002

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

2 beta-Carbomethoxy-3 beta-(4-chlorophenyl)-8-(2-[F-18]fluoroethyl)nortropane (F-18-FECNT) is a potential dopamine transporter imaging agent. In this article, a new mesylate precursor was prepared and a one-step automated synthesis of 18F-FECNT was developed. The mesylate precursor (4) was synthesized from 2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropane (1) by N-demethylation, hydroxyethylation followed by mesylation at a total yield of 47%. [ F-18]fluorination was performed by heating 4 ring mesylate precursor and K[F-18] in 1 ml acetonitrile at (90)degrees C for 20 min. The crude F-18-FECNT was obtained with a radiolabeling yield of 48%. After purification by preparative high performance liquid chromatography (HPLC), the final 18 F-FECNT product was obtained with a radiochernical purity of 98.4% and a decay corrected radiochemical yield of 33 +/- 9% (and the uncorrected radiochernical yield was 19 +/- 5%, n = 5). The duration of the total procedure was 80-90 min. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：1881 / 1885

页数：5

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