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Updated: Jul 7, 2026

Efficient Synthesis of Polyfunctionalized Benzenes in Water via Persulfate-promoted Benzannulation of α,β-Unsaturated Compounds and Alkynes
Published on: December 16, 2019
Recent Advances in Benzannulation Approaches to Aromatic Frameworks
Heeeun Kim1, Yonghoon Kwon1,2
1Department of Agricultural Biotechnology, Seoul National University, Seoul, Republic of Korea.
Abstract:
Substituted arenes underpin pharmaceuticals, agrochemicals, and functional materials, yet conventional arene functionalization is often constrained by the substitution pattern of the starting ring. Benzannulation addresses this limitation by assembling aromatic cores from acyclic or nonaromatic precursors via metalcatalyzed cascades, pericyclic processes, radical cyclizations, and benzyne-based manifolds. This review highlights developments reported over the last 5 years and compares transition-metal-catalyzed and metal-free strategies in terms of bond-forming logic, regioselectivity, the functional-group tolerance, and mechanism. Design principles that enable step economy and improved sustainability are discussed, providing practical guidance for selecting and designing benzannulation routes to access complex substituted arenes.
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