Palladium‐Catalyzed C−H Arylation of Aliphatic and Aromatic Ketones using Dipeptide Transient Directing Groups

Abstract

Abstract Ketones are ubiquitous structural motifs in chemical materials and medicinally active pharmaceutical ingredients. Transition metal‐catalyzed C−H bond functionalization is one of the most efficient tactics for diversification of ketones. Palladium‐catalyzed C−H arylation of aliphatic and aromatic ketones has been achieved utilizing an inexpensive dipeptide as a transient directing group. The tridentate coordination used in this reaction enhances the reactivity of the substrates and allows reduction of the loading of the directing group compounds to 20%. This approach allows rapid arylation of complex natural products, medicinal‐chemistry‐related scaffolds, and even remote C(sp 2 )−H bonds.