A novel ^(18)F labeling strategy was developed to directly construct aryl-SO(2)-^(18)F from arenediazonium tosylates with a SO(2) source and [^(18)F]fluoride. This approach is compatible with a wide range of substrates and enabled the production of ^(18)F-labeled drug-like derivatives through late-stage ^(18)F fluorination, representing a significant advance in the radiosynthesis of ^(18)F-labeled arenesulfonyl fluorides. A reactive ^(18)F labeling synthon, bearing a maleimide-based prosthetic…
Org Lett. 2023 Mar 15. doi: 10.1021/acs.orglett.3c00516. Online ahead of print.
ABSTRACT
A novel 18F labeling strategy was developed to directly construct aryl-SO2-18F from arenediazonium tosylates with a SO2 source and [18F]fluoride. This approach is compatible with a wide range of substrates and enabled the production of 18F-labeled drug-like derivatives through late-stage 18F fluorination, representing a significant advance in the radiosynthesis of 18F-labeled arenesulfonyl fluorides. A reactive 18F labeling synthon, bearing a maleimide-based prosthetic group, allowed for the generation of 18F-labeled temperature-sensitive biomolecules containing cysteine residues via maleimide-cysteine chemistry.
PMID:36920257 | DOI:10.1021/acs.orglett.3c00516
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