Switchable Regiodivergent Reductive Alkyl–Alkyl Coupling by Nickel Catalysis: Sorting Different Alkyl–Nickel Intermediates

Q Quan‐Xing Zi (Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis Guangming Advanced Research Institute Shenzhen Grubbs Institute Department of Chemistry and Guangdong Provincial Key Laboratory of Catalysis Southern University of Science and Technology Shenzhen Guangdong 518055 P.R. China) L Lin Min (Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis Guangming Advanced Research Institute Shenzhen Grubbs Institute Department of Chemistry and Guangdong Provincial Key Laboratory of Catalysis Southern University of Science and Technology Shenzhen Guangdong 518055 P.R. China) H Hai‐Wu Du (Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis Guangming Advanced Research Institute Shenzhen Grubbs Institute Department of Chemistry and Guangdong Provincial Key Laboratory of Catalysis Southern University of Science and Technology Shenzhen Guangdong 518055 P.R. China) Q Qiong Yu (Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Shenzhen Grubbs Institute, Guangming Advanced Research Institute, Department of Chemistry, and Guangdong Provincial Key Laboratory of Catalysis) Y Yu‐Long Li (College of Chemistry and Environmental Engineering Key Laboratory of Green Catalysis of Higher Education Institutes of Sichuan Sichuan University of Science and Engineering Zigong Sichuan 643000 P.R. China) W Wei Shu (Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Shenzhen Grubbs Institute, Guangming Advanced Research Institute, Department of Chemistry, and Guangdong Provincial Key Laboratory of Catalysis)

Abstract

Abstract Site‐selective and divergent functionalizations on saturated alkyl chain at specific unfunctionalized positions is a key challenge in organic chemistry and other related areas and offers unprecedented synthetic opportunities. Herein, a ligand‐controlled Ni‐catalyzed site‐selective and divergent alkyl–alkyl reductive coupling between two different alkyl halides has been developed. Notably, the reaction finely tunes and recognizes thermodynamic favored α‐aminoalkyl radicals over β‐aminoalkyl radicals, and distal ipso ‐alkyl radicals to deliver chemo‐ and position‐selective alkylation of unactivated α‐H and β‐H of amines under reductive conditions. Moreover, the reaction selectively functionalizes one alkyl chain over two migratable alkyl chains. By just switching the catalytic parameters, α‐ and β‐alkylation of saturated C─H bonds, and ipso ‐alkyl‐alkyl coupling allow for rapid access to three types of branched aliphatic amine architectures from identical starting materials.

Article Details

Volume / Issue Vol. 64, Issue 30
Published July 21, 2025
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (6)

Q

Quan‐Xing Zi

Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis Guangming Advanced Research Institute Shenzhen Grubbs Institute Department of Chemistry and Guangdong Provincial Key Laboratory of Catalysis Southern University of Science and Technology Shenzhen Guangdong 518055 P.R. China

L

Lin Min

Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis Guangming Advanced Research Institute Shenzhen Grubbs Institute Department of Chemistry and Guangdong Provincial Key Laboratory of Catalysis Southern University of Science and Technology Shenzhen Guangdong 518055 P.R. China

H

Hai‐Wu Du

Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis Guangming Advanced Research Institute Shenzhen Grubbs Institute Department of Chemistry and Guangdong Provincial Key Laboratory of Catalysis Southern University of Science and Technology Shenzhen Guangdong 518055 P.R. China

Q

Qiong Yu

Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Shenzhen Grubbs Institute, Guangming Advanced Research Institute, Department of Chemistry, and Guangdong Provincial Key Laboratory of Catalysis

Y

Yu‐Long Li

College of Chemistry and Environmental Engineering Key Laboratory of Green Catalysis of Higher Education Institutes of Sichuan Sichuan University of Science and Engineering Zigong Sichuan 643000 P.R. China

W

Wei Shu

Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Shenzhen Grubbs Institute, Guangming Advanced Research Institute, Department of Chemistry, and Guangdong Provincial Key Laboratory of Catalysis