multi-patient dose synthesis of [18F]Flumazenil via a copper-mediated 18F-fluorination

Autor: Thibault Gendron, Gianluca Destro, Natan J. W. Straathof, Jeroen B. I. Sap, Florian Guibbal, Charles Vriamont, Claire Caygill, John R. Atack, Andrew J. Watkins, Christopher Marshall, Rebekka Hueting, Corentin Warnier, Véronique Gouverneur, Matthew Tredwell

Publikováno v: EJNMMI Radiopharmacy and Chemistry, Vol 7, Iss 1, Pp 1-11 (2022)

Abstract Background Flumazenil (FMZ) is a functionally silent imidazobenzodiazepine which binds to the benzodiazepine binding site of approximately 75% of the brain γ-aminobutyric acid-A receptors (GABAARs). Positron Emission Tomography (PET) imagin

Externí odkaz: https://doaj.org/article/5341d4ac0ec2446bab32fb0383e7b523

Late-stage difluoromethylation: concepts, developments and perspective

Autor: Andrés A. Trabanco, Jeroen B. I. Sap, Christopher W. am Ende, Claudio F. Meyer, Ndidi Iwumene, Natan J. W. Straathof, Véronique Gouverneur

Publikováno v: Chemical Society Reviews. 50:8214-8247

This review describes the recent advances made in difluoromethylation processes based on X–CF2H bond formation where X is C(sp), C(sp2), C(sp3), O, N or S, a field of research that has benefited from the invention of multiple difluoromethylation re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bceb28dc5b9371989b69605705ba240
https://doi.org/10.1039/d1cs00360g

Organophotoredox Hydrodefluorination of Trifluoromethylarenes with Translational Applicability to Drug Discovery

Autor: Natan J. W. Straathof, Thomas Knauber, Laura Buglioni, Véronique Gouverneur, Christopher W. am Ende, Claudio F. Meyer, Andrés A. Trabanco, Jeroen B. I. Sap, Timothy Noël, Christophe Genicot, Maurice Médebielle

Publikováno v: Journal of the American Chemical Society
Journal of the American Chemical Society, American Chemical Society, 2020, 142 (20), pp.9181-9187. ⟨10.1021/jacs.0c03881⟩
Journal of the American Chemical Society, 142(20), 9181-9187. American Chemical Society

Molecular editing such as insertion, deletion, and single atom exchange in highly functionalized compounds is an aspirational goal for all chemists. Here, we disclose a photoredox protocol for the replacement of a single fluorine atom with hydrogen i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b50cda0eabdf7a5b3e85f17bf72e0a2
http://europepmc.org/articles/PMC7304874

Manual and automated Cu-mediated radiosynthesis of the PARP inhibitor [18F]olaparib

Autor: Damien Mahaut, Patrick G. Isenegger, Thomas C. Wilson, Véronique Gouverneur, Jeroen B. I. Sap, Rebekka Hueting, Nicholas J. Taylor, Florian Guibbal, Sean Preshlock, Bart Cornelissen, Stefan Verhoog, Anna Pacelli

Positron emission tomography (PET) is a diagnostic nuclear imaging modality that relies on automated protocols to prepare agents labeled with a positron-emitting radionuclide (e.g., 18F). In recent years, new reactions have appeared for the 18F-label

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cafac54e928f569bf5dc415170a7a4f1
https://doi.org/10.1038/s41596-020-0295-7

Synthesis of 18F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [18F]fluoride

Autor: Natan J. W. Straathof, Christopher W. am Ende, Choon Wee Kee, Christophe Genicot, Véronique Gouverneur, Lei Zhang, Paramita Mukherjee, Jeroen B. I. Sap, Thomas C. Wilson

Herein, we report the radiosynthesis of 18F-difluoromethylarenes via the assembly of three components, a boron reagent, ethyl bromofluoroacetate, and cyclotron-produced non-carrier added [18F]fluoride. The two key steps are a copper-catalysed cross-c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c08e65ed2e38e459121333baf9d52bc
https://doi.org/10.1039/c8sc05096a