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C-Carbonylation for PET Imaging and Drug Discovery.
J Labelled Comp Radiopharm
May 2024
PET Science Centre, Precision Medicine and Biosamples, Oncology R&D, AstraZeneca, Stockholm, Sweden.
Light-Driven Radiochemistry with Fluorine-18, Carbon-11 and Zirconium-89.
Angew Chem Int Ed Engl
April 2024
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
This review discusses recent advances in light-driven radiochemistry for three key isotopes: fluorine-18, carbon-11, and zirconium-89, and their applications in positron emission tomography (PET). In the case of fluorine-18, the predominant approach involves the use of cyclotron-produced [F]fluoride or reagents derived thereof. Light serves to activate either the substrate or the fluorine-18 labeled reagent.
View Article and Find Full Text PDFPreliminary PET imaging of [C]evobrutinib in mouse models of colorectal cancer, SARS-CoV-2, and lung damage: Radiosynthesis via base-aided palladium-NiXantphos-mediated C-carbonylation.
J Labelled Comp Radiopharm
May 2024
Azrieli Centre for Neuro-Radiochemistry, Centre for Addiction and Mental Health, Toronto, Ontario, Canada.
Evobrutinib is a second-generation, highly selective, irreversible Bruton's tyrosine kinase (BTK) inhibitor that has shown efficacy in the autoimmune diseases arthritis and multiple sclerosis. Its development as a positron emission tomography (PET) radiotracer has potential for in vivo imaging of BTK in various disease models including several cancers, severe acute respiratory syndrome-coronavirus-2 (SARS-CoV-2), and lipopolysaccharide (LPS)-induced lung damage. Herein, we report the automated radiosynthesis of [C]evobrutinib using a base-aided palladium-NiXantphos-mediated C-carbonylation reaction.
View Article and Find Full Text PDFReactive Palladium-Ligand Complexes for C-Carbonylation at Ambient Pressure: A Breakthrough in Carbon-11 Chemistry.
Pharmaceuticals (Basel)
July 2023
PET Science Centre, Precision Medicine and Biosamples, Oncology R&D, AstraZeneca, Karolinska Institutet, SE-17176 Stockholm, Sweden.
The Pd-Xantphos-mediated C-carbonylation protocol (also known as the "Xantphos- method"), due to its simplistic and convenient nature, has facilitated researchers in meeting a longstanding need for preparing C-carbonyl-labeled radiopharmaceuticals at ambient pressure for positron emission tomography (PET) imaging and drug discovery. This development could be viewed as a breakthrough in carbon-11 chemistry, as evidenced by the rapid global adoption of the method by the pharmaceutical industry and academic laboratories worldwide. The method has been fully automated for the good manufacturing practice (GMP)-compliant production of novel radiopharmaceuticals for human use, and it has been adapted for "in-loop" reactions and microwave technology; an impressive number of C-labeled compounds (>100) have been synthesized.
View Article and Find Full Text PDFSynthesis of Radiopharmaceuticals "In-Loop" C-Carbonylation as Exemplified by the Radiolabeling of Inhibitors of Bruton's Tyrosine Kinase.
Front Nucl Med
January 2022
Department of Radiology, University of Michigan, Ann Arbor, MI, United States.
Article Synopsis
- Positron emission tomography (PET) is a non-invasive imaging technique that helps in drug discovery by providing insights into how drugs distribute in the body and interact with targets.
- Recent advancements involve developing drug candidates with acryloyl functional groups that can form covalent bonds with biological targets, although incorporating a carbon-11 radionuclide into these compounds is technically challenging.
- The study presents a new method for synthesizing carbon-11-acrylamide drug candidates like [C]ibrutinib, [C]tolebrutinib, and [C]evobrutinib, demonstrating reliable production and potential for clinical applications with enhanced efficiency using standard automated systems.
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