Automated synthesis of [18F]Florbetaben as Alzheimer's disease imaging agent based on a synthesis module system

被引：18

作者：

Wang, Hongliang ^{[1
,2
]}

Guo, Xinyan ^{[2
]}

Jiang, Shende ^{[2
]}

Tang, Ganghua ^{[1
]}

机构：

[1] Sun Yat Sen Univ, Affiliated Hosp 1, Dept Nucl Med, Guangzhou 510080, Guangdong, Peoples R China

[2] Tianjin Univ, Sch Pharmaceut Sci & Technol, Tianjin 300072, Peoples R China

来源：

APPLIED RADIATION AND ISOTOPES | 2013年 / 71卷 / 01期

基金：

国家高技术研究发展计划(863计划);

关键词：

F-18-labeling; Automated synthesis; F-18]Florbetaben; RADIATION-DOSIMETRY; AMYLOID-BETA; BRAIN; HYPOTHESIS;

D O I：

10.1016/j.apradiso.2012.09.014

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

An automated synthesis procedure of [F-18]Florbetaben ([F-18]BAY94-9172), a radiolabeled imaging agent in phase III study for in vivo mapping of fibrillar amyloid beta (A beta) with PET, was developed using the commercial PET-MF-2V-IT-1 synthesizer. The automated radiosynthesis was carried out via a one-step nucleophilic fluorination of methanesulfonic acid 2-[2-(2{4-[2-(4-methylamino-phenyl)-vinyl]-phenoxy}-ethoxy)-ethoxy]-ethyl ester, as a new precursor, and separation with semi-preparative high performance liquid chromatography (HPLC). The total synthesis time amounted to 50 min with 20-25% yield (uncorrected for decay) and radiochemical purities of more than 95% in all runs. The described automated radiosynthesis allows the production of [F-18]Florbetaben using a commercial radiosynthesis module and enables clinical trials of this compound. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：41 / 46

页数：6

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