Synthesis of Azepino[4,5-b]indole via Ring Expansion of Tetrahydro-β-carbolines Ammonium Ylide

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Abstract
The formal cyclization strategy was generally used to construct azepino[4,5-b]indole. Herein, we reported a novel and expeditious protocol for the synthesis of quaternary carbon azepino[4,5-b]indole via ring expansion of ammonium ylide, which was formed by the reaction of tetrahydro-β-carbolines with the diazo compound. The easily available substrates, mild reaction conditions, and broad functional tolerance rendered this method a practical strategy that may significantly afford an efficient method of scaffold hopping in drug discovery.
Funding Information
  • Natural Science Foundation of Hainan Province (222RC557, 221CXTD434, 221QN170)
  • National Natural Science Foundation of China (82160664)
  • Anhui Laboratory of Molecule Based Materials (fzj21006)

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