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

Abstract

Abstractγ‐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.