Keynote

KN03. T. Ritter – Late-Stage Fluorination for PET Imaging


Effectenbeurszaal, ground floor July 10, 2017 16:00 - 16:30

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Prof. Tobias Ritter, PhD

Prof. Tobias Ritter, PhD
Max Planck Institut für Kohlenforschung
Kaiser-Wilhelm-Platz 1
45470 Mülheim, Germany
ritter@mpi-muelheim.mpg.de

Harvard University
Department for Chemistry and Chemical Biology
12 Oxford Street
Cambridge, MA 02138, USA
Massachusetts General Hospital

Massachusetts General Hospital
Department of Radiology
55 Fruit Street
Boston, MA 02114 USA

The unnatural isotope fluorine–18 (18F) is used as a positron emitter in molecular imaging. Currently, many potentially useful 18F-labeled probe molecules are inaccessible for imaging, because no fluorination chemistry is available to make them. Syntheses must be rapid on account of the 110-minute half-life of 18F and benefit from using [18F]fluoride due to practical access and suitable isotope enrichment. But [18F]fluoride chemistry has been limited in reaction and substrate scope. I will describe the development of novel, modern fluorination reactions and evaluate them based on their utility for 18F and 19F chemistry. In particular, I will describe the mechanism of an unusual deoxyfluorination reaction, and the mechanism-based application of this reaction to a practical method for 18F incorporation into a variety of small molecules.

References
1. T. Furuyam, A. S. Kamlet T. Ritter, Nature 2011, 473, 470-477
2. E. Lee, A. S. Kamlet, D. C. Powers, C. N. Neumann, G. B. Boursalian, T. Furuya, D. C. Choi, J. M. Hooker, T. Ritter, Science 2011, 334, 639–642
3. C. N. Neumann, J. M. Hooker, T. Ritter, Nature 2016, 534, 369–373