Efficient ruthenium-catalyzed α-alkylation of ketones using pyridyl methanols

By employing an easily available [Ru(p-cymene)Cl2]2/Xantphos/t-BuOK catalyst system, the α-alkylation of ketones was demonstrated by using pyridyl methanol as the alkylating reagents. The synthetic protocol allows synthesizing a wide range of α-pyridyl methylated ketones in reasonable to excellent isolated yields with high atom-efficiency. The transformation is operationally simple, the substrate scope is wide, and the starting materials are readily-available. There is no need for addition of alkenes as the hydrogen receptors or the use of stoichiometric amount of base.