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

被引：19

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

共 50 条

[21] In vivo PET imaging of beta-amyloid deposition in mouse models of Alzheimer's disease with a high specific activity PET imaging agent [18F]flutemetamol [J].

Snellman, Anniina ;

Rokka, Johanna ;

Lopez-Picon, Francisco R. ;

Eskola, Olli ;

Salmona, Mario ;

Forloni, Gianluigi ;

Scheinin, Mika ;

Solin, Olof ;

Rinne, Juha O. ;

Haaparanta-Solin, Merja .

EJNMMI RESEARCH, 2014, 4 :1-11

[22] Automated synthesis of 2′-deoxy-2′-[18F]fluoro-5-methyl-1-β-D-arabinofuranosyluracil ([18F]-FMAU) using a one reactor radiosynthesis module [J].

Li, Zibo ;

Cai, Hancheng ;

Conti, Peter S. .

NUCLEAR MEDICINE AND BIOLOGY, 2011, 38 (02) :201-206

[23] Limitations of Small Animal PET Imaging with [18F]FDDNP and FDG for Quantitative Studies in a Transgenic Mouse Model of Alzheimer's Disease [J].

Kuntner, Claudia ;

Kesner, Adam L. ;

Bauer, Martin ;

Kremslehner, Robert ;

Wanek, Thomas ;

Mandler, Markus ;

Karch, Rudolf ;

Stanek, Johann ;

Wolf, Tanja ;

Mueller, Markus ;

Langer, Oliver .

MOLECULAR IMAGING AND BIOLOGY, 2009, 11 (04) :236-240

[24] Ligand-based design of [18F]OXD-2314 for PET imaging in non-Alzheimer's disease tauopathies [J].

Lindberg, Anton ;

Murrell, Emily ;

Tong, Junchao ;

Mason, N. Scott ;

Sohn, Daniel ;

Sandell, Johan ;

Strom, Peter ;

Stehouwer, Jeffrey S. ;

Lopresti, Brian J. ;

Viklund, Jenny ;

Svensson, Samuel ;

Mathis, Chester A. ;

Vasdev, Neil .

NATURE COMMUNICATIONS, 2024, 15 (01)

[25] An Exposition of 11C and 18F Radiotracers Synthesis for PET Imaging [J].

Saxena, Priya ;

Mahmood, Tarique ;

Dixit, Manish ;

Gambhir, Sanjay ;

Ahsan, Farogh .

CURRENT RADIOPHARMACEUTICALS, 2021, 14 (02) :92-100

[26] Advances in the automated synthesis of 6-[18F]Fluoro-L-DOPA [J].

Ângela C. B. Neves ;

Ivanna Hrynchak ;

Inês Fonseca ;

Vítor H. P. Alves ;

Mariette M. Pereira ;

Amílcar Falcão ;

Antero J. Abrunhosa .

EJNMMI Radiopharmacy and Chemistry, 6

[27] Production of 6-l-[18F]Fluoro-m-tyrosine in an Automated Synthesis Module for 11C-Labeling [J].

Orlovskaya, Viktoriya V. ;

Craig, Austin S. ;

Fedorova, Olga S. ;

Kuznetsova, Olga F. ;

Neumaier, Bernd ;

Krasikova, Raisa N. ;

Zlatopolskiy, Boris D. .

MOLECULES, 2021, 26 (18)

[28] Module-assisted one-pot synthesis of [18F]SFB for radiolabeling proteins [J].

Wang, Ming-Wei ;

Zhang, Yong-Ping ;

Zhang, Ying-Jian ;

Shen, Clifton Kwang-Fu .

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, 2011, 289 (01) :191-196

[29] Fully automated synthesis of 4-[18F]fluorobenzylamine based on borohydride/NiCl2 reduction [J].

Way, Jenilee ;

Wuest, Frank .

NUCLEAR MEDICINE AND BIOLOGY, 2013, 40 (03) :430-436

[30] [18F] FBB cortical uptake is not related to the age of onset of Alzheimer's disease [J].

Chiaravalloti, Agostino ;

Barbagallo, Gaetano ;

Castellano, Anna Elisa ;

Ricci, Maria ;

Ciccariello, Gabriele ;

Ursini, Francesco ;

D'Ascenzo, Nicola ;

Xie, Quingguo ;

Schillaci, Orazio .

NUCLEAR MEDICINE COMMUNICATIONS, 2020, 41 (02) :175-180

← 1 2 3 4 5 →