An efficient phosphoric acid-catalyzed cycloaddition reaction between pyrazolones and 2-indolyldimethanols for the construction of indole-fused seven-membered oxepane skeletons was developed. This protocol featured excellent functional group tolerance, broad substrate generality, and high reaction yields. Moreover, the scalable gram-scale synthesis and facile product derivatization further demonstrated its synthetic practicability. This work provided a reliable strategy for the assembly of complex oxepane heterocyclic frameworks.
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Tao et al. (2026) studied this question.
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