Issue 10, 2012
From the journal:

MedChemComm

Synthesis and PET imaging studies of [18F]2-fluoroquinolin-8-ol ([18F]CABS13) in transgenic mouse models of Alzheimer's disease†

Neil Vasdev,*abc   Pengpeng Cao,cd   Erik M. van Oosten,cd   Alan A. Wilson,bc   Sylvain Houle,bc   Guiyang Hao,e   Xiankai Sun,e   Nikolai Slavine,e   Mustafa Alhasan,e   Peter P. Antich,e   Frederick J. Bontee  and  Padmakar Kulkarnie  

* Corresponding authors

a Division of Nuclear Medicine and Molecular Imaging/Radiology, Massachusetts General Hospital and Harvard Medical School, 55 Fruit St White 427, Boston, Massachusetts, USA
E-mail: vasdev.neil@mgh.harvard.edu
Fax: +1 (617) 726-6165
Tel: +1 (617) 643-4736

b Department of Psychiatry, University of Toronto, 250 College St, Toronto, Ontario, Canada

c PET Centre, Centre for Addiction and Mental Health, 250 College St, Toronto, Ontario, Canada

d Department of Chemistry, University of Toronto, 80 St George St, Toronto, Ontario, Canada

e Department of Radiology, University of Texas, Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, Texas, USA

Abstract

Benzyloxy-2-chloroquinoline was reacted with fluorine-18 labelled potassium cryptand fluoride, followed by catalytic hydrogenation to prepare [18F]2-fluoroquinolin-8-ol in high radiochemical yields (30%; uncorrected and relative to [18F]-fluoride), specific activities (>1 Ci μmol−1) and radiochemical purities (>99%) within 70 min; PET-CT imaging with this new radiotracer in double transgenic mice shows excellent promise for imaging Alzheimer's disease.

Graphical abstract: Synthesis and PET imaging studies of [18F]2-fluoroquinolin-8-ol ([18F]CABS13) in transgenic mouse models of Alzheimer's disease

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Article information

DOI
https://doi.org/10.1039/C2MD20075A
Article type
Concise Article
Submitted
22 Mar 2012
Accepted
22 Mar 2012
First published
23 Mar 2012

Med. Chem. Commun., 2012,3, 1228-1230

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Synthesis and PET imaging studies of [18F]2-fluoroquinolin-8-ol ([18F]CABS13) in transgenic mouse models of Alzheimer's disease

N. Vasdev, P. Cao, E. M. van Oosten, A. A. Wilson, S. Houle, G. Hao, X. Sun, N. Slavine, M. Alhasan, P. P. Antich, F. J. Bonte and P. Kulkarni, Med. Chem. Commun., 2012, 3, 1228 DOI: 10.1039/C2MD20075A

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