Recent Advances in Aryne Generation Methods: From Classical Strategies to Cutting-edge Breakthroughs

doi:10.1007/s40242-026-6106-0

Abstract

Abstract: This review summarizes the evolution of aryne generation methodologies, from early harsh approaches to recent mild and practical strategies. It aims to provide a systematic overview of advances over the past decade, with particular emphasis on the last five years. Key methods discussed include activation using bulky bases, cyclic onium salts, photochemical triggers, ringopening of four-membered rings, and transition-metal-assisted processes. These modern techniques enable aryne formation under milder conditions, with improved functional group tolerance, operational safety, and scalability. As a result, arynes have become versatile tools for constructing complex aromatic molecules, modifying pharmaceuticals, and performing bioorthogonal reactions. The review concludes by highlighting future directions, such as developing more accessible precursors, discovering new reaction modes, and expanding applications in drug discovery, materials science, and chemical biology.

Key words: Aryne, Aryne generation, Aryne precursor, Activation condition

YIN Wenhao, QIU Dachuan, LI Yang. Recent Advances in Aryne Generation Methods: From Classical Strategies to Cutting-edge Breakthroughs[J]. Chemical Research in Chinese Universities, 2026, 42(4): 1069-1080.

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