Enantioselective S‐Alkylation of Sulfenamides With Copper‐Catalyzed Amino‐Radical‐Transfer Deboronation

K Ke Wang (Tianjin Medical University Cancer Institute and Hospital Tianjin China) Y Yu Qi M Menghui Ding (Department of Medicinal Chemistry, State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, School of Pharmaceutical Sciences Shandong University Jinan Shandong China) Q Qi Tang (State Key Laboratory of Genetics and Development of Complex Phenotypes, School of Life Sciences, Fudan University, Shanghai, China.) X Xiaodong Shi X Xiaohan Ye (Department of Medicinal Chemistry, State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, School of Pharmaceutical Sciences Shandong University Jinan Shandong China)

Abstract

ABSTRACT This work reports a copper‐catalyzed enantioselective S‐alkylation of sulfenamides enabled by an amino‐radical‐transfer deboronation pathway. Chiral sulfilimines are obtained in high yields (up to 95%) and enantioselectivities (up to 98% ee) under mild conditions. An isomerizable bis(oxazoline) ligand bearing a bridging CH 2 unit is identified as the key factor for both reactivity and stereoselectivity in the copper‐catalyzed radical‐relay coupling with sulfenamides. The method offers a general platform for accessing enantioenriched S(IV) architectures with aliphatic substituents and demonstrates strong potential for applications in medicinal chemistry.

Article Details

Volume / Issue Vol. 65, Issue 13
Published March 23, 2026
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (6)

K

Ke Wang

Tianjin Medical University Cancer Institute and Hospital Tianjin China

Y

Yu Qi

M

Menghui Ding

Department of Medicinal Chemistry, State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, School of Pharmaceutical Sciences Shandong University Jinan Shandong China

Q

Qi Tang

State Key Laboratory of Genetics and Development of Complex Phenotypes, School of Life Sciences, Fudan University, Shanghai, China.

X

Xiaodong Shi

X

Xiaohan Ye

Department of Medicinal Chemistry, State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, School of Pharmaceutical Sciences Shandong University Jinan Shandong China