Light‐Induced Chiral Aldehyde/Palladium Catalysis‐Enabled Asymmetric Allylic C─H Alkylation of Alkenes With NH <sub>2</sub> ‐Unprotected Amino Acid Derivatives

H Hong‐Lin Guan (Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft‐Matter Material Chemistry and Function Manufacturing School of Chemistry and Chemical Engineering Southwest University Chongqing China) B Bo‐Xuan Yao (College of Chemistry &amp; Chemical Engineering and Key Laboratory For Preparation and Application of Ordered Structural Materials of Guangdong Province Shantou University Shantou China) W Wei Wen (Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft-Matter Material Chemistry and Function Manufacturing, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China) Z Zhu‐Lian Wu (Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft‐Matter Material Chemistry and Function Manufacturing School of Chemistry and Chemical Engineering Southwest University Chongqing China) T Tian Cai (Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft-Matter Material Chemistry and Function Manufacturing, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China) S Shao‐Fei Ni (College of Chemistry &amp; Chemical Engineering and Key Laboratory For Preparation and Application of Ordered Structural Materials of Guangdong Province Shantou University Shantou China) Q Qi‐Xiang Guo (Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft‐Matter Material Chemistry and Function Manufacturing School of Chemistry and Chemical Engineering Southwest University Chongqing China)

Abstract

ABSTRACT The catalytic asymmetric allylic C–H alkylation of alkenes with the α‐carbon of readily available amino acid derivatives represents an ideal strategy for constructing chiral nonproteinogenic α,α‐disubstituted amino acids. However, such synthetic methodologies remain unexplored. Herein, we report a light‐induced, chiral aldehyde/palladium catalysis‐enabled direct allylic C–H alkylation of allyl arenes and 1,4‐enynes using NH 2 ‐unprotected amino acid esters. The results demonstrate that competing allylic C–H amination is completely suppressed, and the desired alkylation products—bearing either allyl or conjugated enyne moieties—are obtained in 32%–93% yields with 80%–98% ee values. Mechanistic studies reveal that enantiocontrol is achieved through the cooperative action of the chiral aldehyde and the chiral ligand, and the latter primarily dictates the absolute configuration of the product by forming noncovalent C–H···π and C–H···O interactions with the chiral aldehyde‐involved Zn complex.

Article Details

Volume / Issue Vol. 65, Issue 23
Published June 01, 2026
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (7)

H

Hong‐Lin Guan

Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft‐Matter Material Chemistry and Function Manufacturing School of Chemistry and Chemical Engineering Southwest University Chongqing China

B

Bo‐Xuan Yao

College of Chemistry &amp; Chemical Engineering and Key Laboratory For Preparation and Application of Ordered Structural Materials of Guangdong Province Shantou University Shantou China

W

Wei Wen

Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft-Matter Material Chemistry and Function Manufacturing, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China

Z

Zhu‐Lian Wu

Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft‐Matter Material Chemistry and Function Manufacturing School of Chemistry and Chemical Engineering Southwest University Chongqing China

T

Tian Cai

Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft-Matter Material Chemistry and Function Manufacturing, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China

S

Shao‐Fei Ni

College of Chemistry &amp; Chemical Engineering and Key Laboratory For Preparation and Application of Ordered Structural Materials of Guangdong Province Shantou University Shantou China

Q

Qi‐Xiang Guo

Key Laboratory of Applied Chemistry of Chongqing Municipality and Chongqing Key Laboratory of Soft‐Matter Material Chemistry and Function Manufacturing School of Chemistry and Chemical Engineering Southwest University Chongqing China