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Updated: Dec 9, 2025

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Iron-Catalyzed Amination of Strong Aliphatic C(sp3)-H Bonds
Sandip Kumar Das1, Satyajit Roy1, Hillol Khatua1
1Center of Bio-Medical Research, Division of Molecular Synthesis & Drug Discovery, SGPGIMS Campus, Raebareli Road, Lucknow 226014, Uttar Pradesh, India.
Abstract:
A concept for intramolecular denitrogenative C(sp3)-H amination of 1,2,3,4-tetrazoles bearing unactivated primary, secondary, and tertiary C-H bonds is discovered. This catalytic amination follows an unprecedented metalloradical activation mechanism. The utility of the method is showcased with the short synthesis of a bioactive molecule. Moreover, an initial effort has been embarked on for the enantioselective C(sp3)-H amination through the catalyst design. Collectively, this study underlines the development of C(sp3)-H bond functionalization chemistry that should find wide application in the context of drug discovery and natural product synthesis.
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