Schüll Aaron, Grothe Lisa, Rodrigo Eduardo, Erhard Thomas, Waldvogel Siegfried R
Department of Chemistry, Johannes Gutenberg-University Mainz, Duesbergweg 10-14, 55128 Mainz, Germany.
Medicinal Chemistry & Screening Biology, AbbVie Deutschland GmbH & Co. KG, Knollstraße, 67061 Ludwigshafen am Rhein, Germany.
Org Lett. 2024 Apr 12;26(14):2790-2794. doi: 10.1021/acs.orglett.3c02921. Epub 2023 Oct 8.
A novel electrosynthetic approach to aryl dibenzothiophenium salts, including the direct intramolecular formation of a C-S bond in a metal-free, electrochemical key step under ambient conditions, is reported. The broad applicability of this method is demonstrated with 14 examples, including nitrogen-containing heterocycles in isolated yields up to 72%. The resulting sulfonium salts can be used as precursors for fluorine labeling to give [F]fluoroarenes as found in PET tracer ligands.
报道了一种合成芳基二苯并噻吩盐的新型电合成方法,该方法包括在环境条件下的无金属电化学关键步骤中直接分子内形成C-S键。该方法的广泛适用性通过14个实例得到证明,包括分离产率高达72%的含氮杂环。所得的锍盐可用作氟标记的前体,以得到如PET示踪剂配体中的[F]氟芳烃。