Organocatalytic Enantioselective Synthesis of α-Hydroxyketones through a Friedel−Crafts Reaction of Naphthols and Activated Phenols with Aryl- and Alkylglyoxal Hydrates

Abstract

An efficient organocatalytic asymmetric synthesis of α-hydroxyketones has been developed. Quinine-derived thiourea catalyzed the enantioselective Friedel−Crafts alkylation of naphthols and activated phenols with aryl- and alkylglyoxal hydrates, providing the corresponding chiral α-hydroxyketones with high yields (up to 97%) and excellent enantioselectivities (up to 99% ee)

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