Asymmetric Intramolecular Hydroamination to Construct Diverse N–N/C–N Indole Atropisomers via Cooperative Pd(0) and Chiral Phosphoric Acid Catalysis

作者：Zhi Chen, Xiaojun Wang, Fu Pi, Yufan Li, Shun‐Zhong Tan, Lei Zhu, Qin Ouyang, Wei Du, Ying‐Chun Chen · 发表于：Organic Letters · 年份：2025 · DOI：10.1021/acs.orglett.5c00662 · 被引用次数：8 · 研究领域：Axial and Atropisomeric Chirality Synthesis、Molecular spectroscopy and chirality、Asymmetric Synthesis and Catalysis

-aminophenyl-1,3-enynes via cooperative catalysis of Pd(0) and chiral phosphoric acid. This approach enables the efficient construction of N-N/C-N axially stereogenic indoles with broad skeletal diversity and high levels of enantioselectivity in a completely atom-economic manner. Mechanistic studies indicate that a protonation of the alkyne moiety via Pd(0) π-Lewis base activation is favored, and the chiral phosphate counteranion plays a crucial role in controlling the atroposelectivity in the ring-closure step.