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  Application of Palladium-Mediated 18F-Fluorination to PET Radiotracer Development: Overcoming Hurdles to Translation

Kamlet, A. S., Neumann, C. N., Lee, E., Carlin, S. M., Moseley, C. K., Stephenson, N., et al. (2013). Application of Palladium-Mediated 18F-Fluorination to PET Radiotracer Development: Overcoming Hurdles to Translation. PLoS One, 8(3): e59187. doi:10.1371/journal.pone.0059187.

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 Creators:
Kamlet, Adam S.1, Author
Neumann, Constanze N.1, Author              
Lee, Eunsung1, Author
Carlin, Stephen M.2, Author
Moseley, Christian K.2, Author
Stephenson, Nickeisha1, Author
Hooker, Jacob M.2, 3, Author
Ritter, Tobias1, 3, Author              
Affiliations:
1Department for Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA, ou_persistent22              
2 Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts, United States of America, ou_persistent22              
3 Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Massachusetts General Hospital, Boston, Massachusetts, United States of America , ou_persistent22              

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 Abstract: New chemistry methods for the synthesis of radiolabeled small molecules have the potential to impact clinical positron emission tomography (PET) imaging, if they can be successfully translated. However, progression of modern reactions from the stage of synthetic chemistry development to the preparation of radiotracer doses ready for use in human PET imaging is challenging and rare. Here we describe the process of and the successful translation of a modern palladium-mediated fluorination reaction to non-human primate (NHP) baboon PET imaging–an important milestone on the path to human PET imaging. The method, which transforms [18F]fluoride into an electrophilic fluorination reagent, provides access to aryl–18F bonds that would be challenging to synthesize via conventional radiochemistry methods.

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Language(s): eng - English
 Dates: 2012-11-282013-02-122013-03-12
 Publication Status: Published online
 Pages: 10
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: DOI: 10.1371/journal.pone.0059187
 Degree: -

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Title: PLoS One
Source Genre: Journal
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Publ. Info: San Francisco, CA : Public Library of Science
Pages: - Volume / Issue: 8 (3) Sequence Number: e59187 Start / End Page: - Identifier: ISSN: 1932-6203
CoNE: https://pure.mpg.de/cone/journals/resource/1000000000277850