Nickel‐Catalyzed Boron‐Mediated Saturative Trifunctionalization of Alkynes

S Shanglin Chen (Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources) Y Yaru Peng (Key Laboratory of Molecule Synthesis and Function Discovery Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources Fuzhou University Fuzhou China) J Junmei Lin (Key Laboratory of Molecule Synthesis and Function Discovery Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources Fuzhou University Fuzhou China) P Puhui Li (Key Laboratory of Molecule Synthesis and Function Discovery Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources Fuzhou University Fuzhou China) D Daojun Ye (College of Materials Science and Engineering Fuzhou University Fuzhou Fujian China) Y Yuhan Wang X Xingxing Ma (Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources) Q Qiuling Song (Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources)

Abstract

ABSTRACT Converting simple alkynes into fully substituted alkanes—installing three distinct groups via a sequential one‑pot process—remains a formidable challenge. Herein, we report a boron‐mediated, nickel‐catalyzed strategy that achieves this transformation, enabling the modular assembly of valuable 1,1‐diarylalkanes from both simple alkynyl tetracoordinate borons and N ‐acylglutarimides. The reaction proceeds with high regio‐ and chemoselectivity under mild conditions, exhibiting good functional group tolerance across both coupling partners. Mechanistic studies support a unique reaction pathway involving dual 1,2‐metallate shifts, with water serving as the terminal proton source. The synthetic utility is demonstrated through one‐pot synthesis, late‐stage functionalization of drugs, gram‐scale reactions, and versatile downstream transformations of the products. This strategy represents a distinct strategy that differs from stepwise alkyne reduction, offering a useful disconnection for complex alkane synthesis starting from alkynyl tetracoordinate borons or terminal alkynes via one‑pot borylation.

Article Details

Volume / Issue Vol. 65, Issue 28
Published July 06, 2026
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (8)

S

Shanglin Chen

Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources

Y

Yaru Peng

Key Laboratory of Molecule Synthesis and Function Discovery Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources Fuzhou University Fuzhou China

J

Junmei Lin

Key Laboratory of Molecule Synthesis and Function Discovery Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources Fuzhou University Fuzhou China

P

Puhui Li

Key Laboratory of Molecule Synthesis and Function Discovery Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources Fuzhou University Fuzhou China

D

Daojun Ye

College of Materials Science and Engineering Fuzhou University Fuzhou Fujian China

Y

Yuhan Wang

X

Xingxing Ma

Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources

Q

Qiuling Song

Key Laboratory of Molecule Synthesis and Function Discovery, Fujian Province University, College of Chemistry, State Key Laboratory of Green and Efficient Development of Phosphorus Resources