Copper-Catalyzed,\nIntramolecular Amination of Unactivated\nC(sp<sup>3</sup>)–H Bonds through Radical Relay

Although copper-catalyzed amination of activated C­(sp<sup>3</sup>)–H bonds through radical relay has been developed,\namination\nof unactivated C­(sp<sup>3</sup>)–H bonds is rare. Herein, copper-catalyzed\nintramolecular amination of remote unactivated C­(sp<sup>3</sup>)–H\nbonds is reported. The reaction is conducted in a mild and effective\nmanner with moderate to good yields, demonstrating broad tolerance\ntoward various functional groups and exhibiting complete regio- and\nchemoselectivities. This innovation supplies novel synthetic pathways\nfor the construction of saturated nitrogenated heterocycles.

Publication Details

Journal
Figshare
Published
2024-08-29
DOI
https://doi.org/10.1021/acs.joc.4c01163.s001
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Copper-Catalyzed,\nIntramolecular Amination of Unactivated\nC(sp3)–H Bonds through Radical Relay

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Catalytic C–H Functionalization Methods
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Copper-Catalyzed,\nIntramolecular Amination of Unactivated\nC(sp3)–H Bonds through Radical Relay

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Abstract

Although copper-catalyzed amination of activated C­(sp<sup>3</sup>)–H bonds through radical relay has been developed,\namination\nof unactivated C­(sp<sup>3</sup>)–H bonds is rare. Herein, copper-catalyzed\nintramolecular amination of remote unactivated C­(sp<sup>3</sup>)–H\nbonds is reported. The reaction is conducted in a mild and effective\nmanner with moderate to good yields, demonstrating broad tolerance\ntoward various functional groups and exhibiting complete regio- and\nchemoselectivities. This innovation supplies novel synthetic pathways\nfor the construction of saturated nitrogenated heterocycles.

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Catalytic C–H Functionalization Methods
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Copper-Catalyzed,\nIntramolecular Amination of Unactivated\nC(sp<sup>3</sup>)–H Bonds through Radical Relay · Figshare (2024) | TGRS Research Map | TGRS