2023
DOI: 10.1002/ange.202317104
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One‐Carbon Ring Expansion of Indoles and Pyrroles: A Straightforward Access to 3‐Fluorinated Quinolines and Pyridines

Huaixuan Guo,
Shiqin Qiu,
Peng Xu

Abstract: Abstract3‐Fluorinated quinolines and pyridines are prevalent pharmacophores, yet their synthesis is often challenging. Herein, we demonstrate that dibromofluoromethane as bromofluorocarbene source enables the one‐carbon ring expansion of readily available indoles and pyrroles to structurally diverse 3‐fluorinated quinolines and pyridines. This straightforward protocol requires only a short reaction time of ten minutes and can be performed under air atmosphere. Preliminary investigations reveal that this strate… Show more

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