Asymmetric amination of alkyl radicals with two minimally different alkyl substituents DOI

Yu‐Feng Zhang,

Biao Wang,

Chen Zheng

et al.

Science, Journal Year: 2025, Volume and Issue: 388(6744), P. 283 - 291

Published: April 17, 2025

Differentiating between similar alkyl groups is a major challenge in asymmetric catalysis. Achieving enantiocontrol over unactivated prochiral radicals even more difficult owing to their high reactivity and limited interactions with chiral catalysts. In this study, we report copper-catalyzed amination of secondary radicals, using specifically designed anionic multidentate ligands radical substitution reaction. This approach efficiently produces highly enantioenriched α-chiral amines facilitates the enantioselective formal synthesis series important drug molecules. Mechanistic studies reveal that bulky peripheral modifications on help create truncated cone-shaped pocket, enabling precise enantiodiscrimination through steric hindrance noncovalent interactions. strategy holds broad potential for transformations involving diverse nucleophiles.

Language: Английский

Asymmetric amination of alkyl radicals with two minimally different alkyl substituents DOI

Yu‐Feng Zhang,

Biao Wang,

Chen Zheng

et al.

Science, Journal Year: 2025, Volume and Issue: 388(6744), P. 283 - 291

Published: April 17, 2025

Differentiating between similar alkyl groups is a major challenge in asymmetric catalysis. Achieving enantiocontrol over unactivated prochiral radicals even more difficult owing to their high reactivity and limited interactions with chiral catalysts. In this study, we report copper-catalyzed amination of secondary radicals, using specifically designed anionic multidentate ligands radical substitution reaction. This approach efficiently produces highly enantioenriched α-chiral amines facilitates the enantioselective formal synthesis series important drug molecules. Mechanistic studies reveal that bulky peripheral modifications on help create truncated cone-shaped pocket, enabling precise enantiodiscrimination through steric hindrance noncovalent interactions. strategy holds broad potential for transformations involving diverse nucleophiles.

Language: Английский

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