C4-arylation via Pd(i)–Pd(ii) catalysis and domino C4-arylation/3,2-carbonyl migration of indoles via Pd(ii) catalysis tuning by acids have been developed.

No abstract

Ketones are ubiquitous structural motifs in chemical materials and medicinally active pharmaceutical ingredients. Transition metal-catalyzed CÀ H bond functionalization is one of the most efficient tactics for diversification of ketones. Palladium-catalyzed CÀ 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 )À H bonds.