The Renaissance and Bright Future of Synthetic Aryne Chemistry

Recent developments in aryne chemistry are reviewed with a particular focus on synthetic methods. This includes an overview of the precursors of arynes and their activators; the generation of arynes with functional groups and their ensuing reactivities; and the novel transformations achieved via aryne intermediates. These newly developed methods have enabled the synthesis of a variety of previously inaccessible aromatic compounds, allowing the construction of a diversity-enriched chemical library that will further facilitate future drug discoveries.