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Updated: Sep 24, 2025

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Rhodium-Catalyzed Atroposelective Click Cycloaddition of Azides and Alkynes
Linwei Zeng1, Jiaming Li1, Sunliang Cui1
1Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang road, Hangzhou, 310058, China.
Abstract:
The cycloaddition of azides and alkynes is the leading click chemistry technology and has been widely used in drug discovery, biology and material sciences. However, the development of a modular and scalable enantioselective click cycloaddition remains a long-standing challenge. Herein, we report a rhodium-catalyzed enantioselective click cycloaddition of azides and alkynes for rapid and modular access to atropisomeric triazoles in excellent yields and enantioselectivities. The process is mild, efficient and scalable, and features broad substrate scope.
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