A Platform for the Liebeskind-Srogl Coupling of Heteroaromatic Thioethers for Medicinal-Chemistry-Relevant Transformations

Victor Koolma, Roman Staiger, Martin Schuhle, Achim Bixenmann, Elmar Bauschatz, Matthias Schmid, Fedor Miloserdov*, Bart Herle*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

General and robust conditions for the Liebeskind–Srogl coupling were developed and used in functionalization of medicinal-chemistry-relevant heterocyclic substrates. Applicability in HTE and library synthesis, combined with its orthogonality to other cross-coupling reactions, make it highly attractive for discovery chemistry workflows. Additionally, the results suggest that the nature of the Cu(I)-carboxylate plays a more prominent role in the reaction performance than the nature of Pd-catalysts, which is rather uncommon for Pd-catalysis and can be used in further optimization of Liebeskind–Srogl coupling.
Original languageEnglish
Pages (from-to)2852-2856
JournalOrganic Letters
Volume26
Issue number14
Early online date15 Dec 2023
DOIs
Publication statusPublished - 2024

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