biostudies-literatureXu HJNational Natural Science Foundation of China (National Science Foundation of China)764https://www.ebi.ac.uk/biostudies/studies/S-EPMC12820061biostudies-literatureUnknown17(1)Catalytic enantioselective hydroarylation of alkynes is a concise protocol towards axial, helical, and planar chirality. By using an enantioselective π-acid catalysis strategy, these enantioenriched hydroarylation products could be obtained in a green pathway; however, noble-metal catalysts are unavoidable. Here we report a copper-catalyzed intramolecular atroposelective hydroarylation of 1-alkynylindoles with (hetero)arenes, providing a modular platform for the construction of C─N axially chiral carbazolyl and phenanthryl indoles in excellent yields with good to excellent ee values. Moreover, the constructed C─N axially chiral indoles could be easily diversified to various functional group-containing chiral frameworks, and further applied as a chiral ligand in asymmetric catalysis. Importantly, this reaction represents a rare non-noble metal-catalyzed enantioselective hydroarylation of alkynes by π-acid catalysis.Nature communicationsCopper-catalyzed atroposelective hydroarylation of 1-alkynylindoles.PMC1282006122301250Zhang ZChen CMZhou BXu HJYe LWfalseCopper-catalyzed atroposelective hydroarylation of 1-alkynylindoles.Catalytic enantioselective hydroarylation of alkynes is a concise protocol towards axial, helical, and planar chirality. By using an enantioselective π-acid catalysis strategy, these enantioenriched hydroarylation products could be obtained in a green pathway; however, noble-metal catalysts are unavoidable. Here we report a copper-catalyzed intramolecular atroposelective hydroarylation of 1-alkynylindoles with (hetero)arenes, providing a modular platform for the construction of C─N axially chiral carbazolyl and phenanthryl indoles in excellent yields with good to excellent ee values. Moreover, the constructed C─N axially chiral indoles could be easily diversified to various functional group-containing chiral frameworks, and further applied as a chiral ligand in asymmetric catalysis. Importantly, this reaction represents a rare non-noble metal-catalyzed enantioselective hydroarylation of alkynes by π-acid catalysis.2025-01-01T00:00:00Z2025 Dec2026-06-06T19:46:56.577Z2026-06-04T03:11:28.322ZS-EPMC128200614138155910.1038/s41467-025-67440-x