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Gold‐Catalyzed CH Annulation of Anthranils with Alkynes: A Facile,Flexible, and Atom‐Economical Synthesis of Unprotected 7‐Acylindoles
Authors:Hongming Jin  Long Huang  Jin Xie  Matthias Rudolph  Frank Rominger  A. Stephen K. Hashmi
Affiliation:1. Institut für Organische Chemie, Universit?t Heidelberg, Im Neuenheimer Feld 270, 69120 Heidelberg (Germany);2. Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia
Abstract:The gold‐catalyzed C? H annulation of anthranil derivatives with alkynes offers a facile, flexible, and atom‐economical one‐step route to unprotected 7‐acylindoles. An intermediate α‐imino gold carbene, generated by an intermolecular reaction, promotes ortho‐aryl C? H functionalization to afford the target products. The transformation proceeds with a broad range of substrates under mild conditions. Moreover, the obtained functionalized indole products represent a versatile platform for the construction of diverse indolyl frameworks.
Keywords:alkynes  C  H functionalization  gold carbenoids  gold catalysis  indoles
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