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Issue 17, 2016
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11C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals

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Abstract

The positron-emitting radionuclide carbon-11 (11C, t1/2 = 20.3 min) possesses the unique potential for radiolabeling of any biological, naturally occurring, or synthetic organic molecule for in vivo positron emission tomography (PET) imaging. Carbon-11 is most often incorporated into small molecules by methylation of alcohol, thiol, amine or carboxylic acid precursors using [11C]methyl iodide or [11C]methyl triflate (generated from [11C]carbon dioxide or [11C]methane). Consequently, small molecules that lack an easily substituted 11C-methyl group are often considered to have non-obvious strategies for radiolabeling and require a more customized approach. [11C]Carbon dioxide itself, [11C]carbon monoxide, [11C]cyanide, and [11C]phosgene represent alternative reactants to enable 11C-carbonylation. Methodologies developed for preparation of 11C-carbonyl groups have had a tremendous impact on the development of novel PET tracers and provided key tools for clinical research. 11C-Carbonyl radiopharmaceuticals based on labeled carboxylic acids, amides, carbamates and ureas now account for a substantial number of important imaging agents that have seen translation to higher species and clinical research of previously inaccessible targets, which is a testament to the creativity, utility and practicality of the underlying radiochemistry.

Graphical abstract: 11C [[double bond, length as m-dash]] O bonds made easily for positron emission tomography radiopharmaceuticals

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Publication details

The article was received on 13 Apr 2016 and first published on 08 Jun 2016


Article type: Review Article
DOI: 10.1039/C6CS00310A
Citation: Chem. Soc. Rev., 2016,45, 4708-4726
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    11C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals

    B. H. Rotstein, S. H. Liang, M. S. Placzek, J. M. Hooker, A. D. Gee, F. Dollé, A. A. Wilson and N. Vasdev, Chem. Soc. Rev., 2016, 45, 4708
    DOI: 10.1039/C6CS00310A

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