ABSTRACT Herein, we present a highly efficient method for the late‐stage introduction of “clickable” alkyne moieties into different (hetero)arene scaffolds. A highly efficient dual ligand‐based palladium catalyst combining an N‐acylsulfonamide (NASA) ligand with an N‐heterocycle enables the introduction of acrylate moiety bearing a terminal alkyne via nondirected C─H activation, providing a versatile platform for subsequent bioconjugation or activity‐based protein profiling (ABPP) applications. The utility of the method is demonstrated through a broad substrate scope and the subsequent use of the obtained products in representative click reactions.
Braga et al. (Thu,) studied this question.