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Updated: Jun 26, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Enamine Catalytic Annulation of Azonaphthalenes: An Access to Indole Derivatives
Hanhui Zhao1, Huijun Yuan1, Yanru Zhang1
1Department of Medicinal Chemistry, School of Pharmacy , Qingdao University , Qingdao 266021 , P. R. China.
Abstract:
The secondary-amine mediated [3 + 2] annulation of azonaphthalenes with aldehydes and ketones is described for the first time, which provides an alternative protocol for the synthesis of indole derivatives. It features a cheap and readily available catalyst, a broad scope of reactants, very mild reaction conditions, and high efficiency. Significantly different from the transition-metal-mediated processes, the enamine activation represents the first organic base-catalytic protocol for indole synthesis.
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