Solvent-free ruthenium-catalysed triflate coupling as a convenient method for selective azole-o-C–H monoarylation

Abstract

Metal-catalysed ortho-directed C–H functionalization usually faces selectivity issues in the competition between mono- and disubstitution processes. We report herein the ruthenium-catalysed N-directed C–H monoarylation of arylpyrazoles with a selectivity of up to 96% or that generally reaches values above 80%. This selectivity is an effect of solvent-free conditions associated with sulfonate reagents, in the absence of frequently used acidic additives.