Ligand‐Controlled Chemoselective and Enantioselective Cyclization of Enynes With Aroyl Chlorides

Angewandte Chemie International Edition 2026

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Authors: Zhen‐Yu Wang, Ling-Xia Zhang, Yuqing Jiang, Yun‐Qian Zhang, Tian-Qi Gao, Genping Huang, Hui Xu, Hui‐Xiong Dai
DOI: 10.1002/anie.2250866
Cited by: 1
References: 74

Abstract

Herein, we report a palladium-catalyzed, ligand-controlled approach for the switchable construction of cyclopropane-fused heterocycles and seven-membered N-heterocyclic compounds via the chemoselective cyclization of enynes with aroyl chlorides. Furthermore, enantioselective synthesis of cyclopropane-fused heterocycles was achieved using a chiral ligand. To highlight the synthetic utility, late-stage modifications of acid chlorides derived from natural products and pharmaceuticals were demonstrated. DFT calculations reveal that the ligands play an important role in the chemoselective cyclization process by favoring either β-H or β-C elimination of the alkyl-Pd(II) intermediate.

Fields of Study & Subjects

Catalytic C–H Functionalization Methods Catalytic Alkyne Reactions Cyclopropane Reaction Mechanisms

Publication details

Journal / source
Angewandte Chemie International Edition
Publisher
Wiley
Volume
65
Issue
27
Pages
e2250866–e2250866
Publication date
14 May 2026
Language
EN