American Chemical Society
ol2c00962_si_001.pdf (14.96 MB)

Palladium-Catalyzed Asymmetric Dearomative Carbonylation of Indoles

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journal contribution
posted on 2022-04-18, 21:05 authored by Qiuyu Li, Yunchu Zhang, Yuye Zeng, Yujing Fan, Aijun Lin, Hequan Yao
Herein, we disclose a strategy for the asymmetric dearomatization of N-arylacyl indoles via a palladium-catalyzed tandem Heck/carbonylation, leading to an array of indoline-3-carboxylates bearing vicinal C2-aza-quaternary and C3 tertiary stereocenters in high yields and excellent enantio- and diastereoselectivities. This study is an important advance in the field of asymmetric carbonylation and enantioselective dearomatization reactions.