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Updated: Jan 10, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Copper-Catalyzed (5+1) Annulation of Imidazolidines with Cyclopropenes: Synthesis of Functionalized
Xiaoai Liu1, Yu Xiong1, Haiyang Wang1
1School of Pharmacy and Food Engineering, Wuyi University, Jiangmen 529020, China.
Abstract:
Herein, we report a copper-catalyzed (5+1) annulation between imidazolidines and cyclopropenes, providing a modular, atom-economical, and efficient strategy for the synthesis of diverse functionalized 2-vinylpiperazines in moderate to good yields. This method features good geometric and regioselectivity for unsymmetrical cyclopropene and imidazolidine substrates, mild reaction conditions, and a broad substrate scope. Notably, this work represents the first (5+1) annulation of cyclopropenes as vinylmetal carbene precursors.
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