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Updated: May 22, 2025

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Divergent Synthesis of Diaza-oxabicyclo[3.2.1]octanes and Dioxa-azabicyclo[3.2.1]octanes via Cascade Cyclizations
Yu Jin1, Jialing Fu1, Cheng Jiang1
1Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Abstract:
Bicyclo[3.2.1]octanes widely exist in natural products and bioactive compounds. However, the efficient construction of these skeletons remains a challenge. Herein, we reported a convenient synthesis of diaza-oxabicyclo[3.2.1]octanes and dioxa-azabicyclo[3.2.1]octanes by intramolecular cascade cyclizations. The reaction was performed under transition metal-free conditions and with good functional group tolerance. This work provides divergent approaches to bicyclo[3.2.1]octane frameworks.
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