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12 results on '"Meyer, Claudio F."'

1. [18F]Difluorocarbene for positron emission tomography

Author

Sap, Jeroen B. I., Meyer, Claudio F., Ford, Joseph, Straathof, Natan J. W., Dürr, Alexander B., Lelos, Mariah J., Paisey, Stephen J., Mollner, Tim A., Hell, Sandrine M., Trabanco, Andrés A., Genicot, Christophe, am Ende, Christopher W., Paton, Robert S., Tredwell, Matthew, and Gouverneur, Véronique

Published
2022
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4. [18F]Difluorocarbene for positron emission tomography.

Author

Sap, Jeroen B. I., Meyer, Claudio F., Ford, Joseph, Straathof, Natan J. W., Dürr, Alexander B., Lelos, Mariah J., Paisey, Stephen J., Mollner, Tim A., Hell, Sandrine M., Trabanco, Andrés A., Genicot, Christophe, am Ende, Christopher W., Paton, Robert S., Tredwell, Matthew, and Gouverneur, Véronique

Abstract

The advent of total-body positron emission tomography (PET) has vastly broadened the range of research and clinical applications of this powerful molecular imaging technology1. Such possibilities have accelerated progress in fluorine-18 (18F) radiochemistry with numerous methods available to 18F-label (hetero)arenes and alkanes2. However, access to 18F-difluoromethylated molecules in high molar activity is mostly an unsolved problem, despite the indispensability of the difluoromethyl group for pharmaceutical drug discovery3. Here we report a general solution by introducing carbene chemistry to the field of nuclear imaging with a [18F]difluorocarbene reagent capable of a myriad of 18F-difluoromethylation processes. In contrast to the tens of known difluorocarbene reagents, this 18F-reagent is carefully designed for facile accessibility, high molar activity and versatility. The issue of molar activity is solved using an assay examining the likelihood of isotopic dilution on variation of the electronics of the difluorocarbene precursor. Versatility is demonstrated with multiple [18F]difluorocarbene-based reactions including O–H, S–H and N–H insertions, and cross-couplings that harness the reactivity of ubiquitous functional groups such as (thio)phenols, N-heteroarenes and aryl boronic acids that are easy to install. The impact is illustrated with the labelling of highly complex and functionalized biologically relevant molecules and radiotracers.Carbene chemistry is used to introduce difluoromethyl groups labelled with fluorine-18 into compounds for positron emission tomography imaging, using a reagent designed for high molar activity and versatility. [ABSTRACT FROM AUTHOR]

Published
2022
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9. Organophotoredox Hydrodefluorination of Trifluoromethylarenes with Translational Applicability to Drug Discovery

Author

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

Published
2020
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12. Silyl Radical-Mediated Activation of Sulfamoyl Chlorides Enables Direct Access to Aliphatic Sulfonamides from Alkenes

Author

Hell, Sandrine M., Meyer, Claudio F., Laudadio, Gabriele, Misale, Antonio, Willis, Michael C., Noël, Timothy, Trabanco, Andrés A., and Gouverneur, Véronique

Abstract

Single electron reduction is more challenging for sulfamoyl chlorides than sulfonyl chlorides. However, sulfamoyl and sulfonyl chlorides can be easily activated by Cl-atom abstraction by a silyl radical with similar rates. This latter mode of activation was therefore selected to access aliphatic sulfonamides, applying a single-step hydrosulfamoylation using inexpensive olefins, tris(trimethylsilyl)silane, and photocatalyst Eosin Y. This late-stage functionalization protocol generates molecules as complex as sulfonamide-containing cyclobutyl-spirooxindoles for direct use in medicinal chemistry.

Published
2020
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