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

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.