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A Robust and Efficient Catalyst Possessing an Electron-Deficient Ligand for the Palladium-Catalyzed Direct Arylation of Heteroarenes
The exploration of the direct arylation capacity of a unique, thermally stable, and air-stable Pd0–phosphine catalyst is reported. Besides decisively contributing to catalyst robustness, the electron-deficient trifluoromethyl-substituted triphenylphosphine ligands make the palladium center more electron-deficient and accelerate the direct arylation step. The combination of only 0.5–2 mol-% of the catalyst and a substoichiometric quantity of pivalic acid generates an efficient system to promote biaryl-forming reactions of a broad range of electronically varied hetarenes and aryl bromides. The observed regioselective arylations suggest that a concerted metalation–deprotonation pathway is involved in the C–H activation step…
(read more in “European Journal of Organic Chemistry”)
EDAC – Water Soluble Carbodiimide (WSC) … is used as a versatile coupling agent to cross-link proteins, nucleic acids or to bind molecules to surfaces in aqueous or organic media … or as water scavenger … or as a reagent for heterocyclic ring formation … (read more)