This work describes acylation reactions facilitated by a type of heterocycle‐based acyl transfer agent, 2‐acyloxypyridazinone. Reactions of 2‐acyloxypyridazinone with carboxylic acids yield mixed carbonic anhydride intermediates, which are reactive and could be coupled with a wide range of substrates including acids, amines, alcohols, and thiols. The wide substrate scope, ease of operation (no additive
Breakthrough: A novel catalyzed direct highly selective CCsp bond functionalization of alkynes to amides has been developed. Nitrogenation is achieved by the highly selective CCsp bondcleavage of aryl‐substituted alkynes. The oxidant‐free and mild conditions and wide substrate scope make this method very practical.