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Synlett
DOI: 10.1055/a-2675-4391
DOI: 10.1055/a-2675-4391
Synpacts
Dynamic Kinetic Activation of Aziridines to Access Azepines
G.-W.W acknowledges the funding supports from the National Natural Science Foundation of China (No. 22201114), the Science and Technology Major Program of Gansu Province of China (22ZD6FA006, 23ZDFA015, 24ZD13FA017) and the National Natural Science Fund for Excellent Young Scientists Fund Program (Overseas)-YQHW.
Supported by: Science and Technology Major Program of Gansu Province of China 22ZD6FA006, 23ZDFA015, 24ZD13FA017
Supported by: The National Natural Science Foundation of China 22201114
Abstract
The activation of aziridines is typically a substrate-controlled process, where the regioselectivity of C–N bond cleavage is strongly influenced by the substitution pattern on the aziridine ring. Recently, our group developed a dynamic kinetic protocol that enables a catalyst-controlled activation strategy for aziridines. This article first provides a brief overview of existing methods for aziridine activation and then focuses on the development of a radical–polar crossover (4+3) cycloaddition between aziridines and 2-substituted 1,3-dienes, which is made possible through this dynamic kinetic activation approach.
Keywords
Aziridines ring-opening reaction - Dynamic kinetic activation - Cycloaddition - Radical–polar crossoverPublication History
Received: 08 June 2025
Accepted after revision: 03 August 2025
Article published online:
20 August 2025
© 2025. Thieme. All rights reserved.
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