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Synlett
DOI: 10.1055/a-2600-4673
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Synthesis of Dibenzothiophenium Salts and Observations in Radiofluorination

Juntian Zhang
1   Imaging R&D, Eli Lilly and Company, Philadelphia, United States (Ringgold ID: RIN1539)
,
Wei Zhang
2   Discovery and Diagnostic Radiochemistry, Eli Lilly and Company, Philadelphia, United States (Ringgold ID: RIN1539)
,
Adam T. Hoye
1   Imaging R&D, Eli Lilly and Company, Philadelphia, United States (Ringgold ID: RIN1539)
,
Nathaniel C. Lim
2   Discovery and Diagnostic Radiochemistry, Eli Lilly and Company, Philadelphia, United States (Ringgold ID: RIN1539)
,
Hui Xiong
1   Imaging R&D, Eli Lilly and Company, Philadelphia, United States (Ringgold ID: RIN1539)
› InstitutsangabenGefördert durch: Eli Lilly and Company
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We demonstrate an alternative synthesis of dibenzothiophenium (DBT) salts through a 3-step Pd-catalyzed arylation, oxidation, and cyclization sequence. This approach is operationally straightforward and compatible with a variety of common functional groups. We observed that radiofluorination of a set of related DBT salt precursors gave higher radiochemical incorporation (RCI) with substrates bearing ortho-substituents to the DBT leaving group suggestive of an ortho-effect.



Publikationsverlauf

Eingereicht: 04. April 2025

Angenommen nach Revision: 05. Mai 2025

Accepted Manuscript online:
05. Mai 2025

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