Palladium-Catalyzed Coupling of ortho-Alkynylanilines with Terminal Alkynes Under Aerobic Conditions: Efficient Synthesis of 2,3-Disubstituted 3-Alkynylindoles

摘要

The indole nucleus is an ubiquitous heterocycle found in many bioactive natural products, pharmaceuticals, and agro-chemicals. The synthesis and functionalization of indoles have attracted chemists for over a century and remain an active research area. In this context, transition-metal-catalyzed transformations, notably the indole synthesis by Cacchi and co-workers and the heteroannulation by Larock et al. , among others, have had a major impact on the field.