jo0c01583_si_002.cif (385.4 kB)

TfOH-Catalyzed Cascade C–H Activation/Lactonization of Phenols with α‑Aryl-α-diazoesters: Rapid Access to α‑Aryl Benzofuranones

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posted on 01.10.2020, 11:34 by Sha Hu, Zuolin Lu, Minjie Liu, Hanlin Xu, Jiale Wu, Fener Chen
Aryl benzofuranones are privileged structural units present in natural products and pharmaceutically relevant compounds with high bioactivity and therapeutic value; synthetic access to these scaffolds remains an area of intensive interest. A new and efficient TfOH-catalyzed cascade ortho C–H activation/lactonization of phenols with α-aryl-α-diazoacetates is reported. This metal-free protocol provides an operationally simple and rapid method for the one-pot assembly of diverse α-aryl benzofuranones in high yields with broad substrate scope, a readily starting material, good chemo-regioselectivity, and excellent functional group compatibility.