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18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological PET Imaging Agents

Resource type
Date created
2017-03
Authors/Contributors
Abstract
A mild and selective photocatalytic C-H 18F-fluorination reaction has been developed that provides direct access to 18F-fluorinated amino acids. The biodis-tribution and uptake of three 18F-labelled leucine ana-logues via LAT1 mediated transport in several cancer cell lines is reported. PET imaging of mice bearing PC3 (pros-tate) or U87 (glioma) xenografts using 5-[18F]-fluoro-homoleucine showed high tumor uptake and excellent tumor visualization, highlighting the utility of this strat-egy for rapid tracer discovery for oncology.
Document
Description
This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of the American Chemical Society, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see DOI: 10.1021/jacs.6b11533.
Published as
Nodwell, M.B., Yang, H., Čolović, M., et al. (2017). 18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological Positron Emission Tomography Imaging Agents. Journal of the American Chemical Society 139(10): 3595-3598. DOI: 10.1021/jacs.6b11533
Publication title
Journal of the American Chemical Society
Document title
18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological PET Imaging Agents
Date
2017
Volume
139
Issue
10
First page
3595
Last page
3598
Publisher DOI
10.1021/jacs.6b11533
Copyright statement
Copyright is held by the author(s).
Scholarly level
Peer reviewed?
Yes
Language
English
Member of collection

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