Ligand-Enabled Double γ-C(sp3)−H Functionalization of Aliphatic Acids: One-Step Synthesis of γ-Arylated γ-Lactones

Abstract

γ-methylene C(sp3)−H functionalization of linear free carboxylic acids remains a significant challenge. Here in we report a Pd(II)-catalyzed tandem γ-arylation and γ-lactonization of aliphatic acids enabled by a L,X-type CarboxPyridone ligand. A wide range of γ-arylated γ-lactones are synthesized in a single step from aliphatic acids in moderate to good yield. Arylated lactones can readily be converted into disubstituted tetrahydrofurans, a prominent scaffold amongst bioactive molecules.