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Asymmetric N-Alkylation of 1H-Indoles via Carbene Insertion Reaction
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2023-10-11 , DOI: 10.1002/anie.202313091
Quanxin Peng 1 , Meirong Huang 2 , Guangyang Xu 1 , Yan Zhu 1 , Ying Shao 1 , Shengbiao Tang 1 , Xinhao Zhang 2 , Jiangtao Sun 1
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An intermolecular enantioselective N-alkylation reaction of 1H-indoles has been developed enabled by cooperative rhodium and chiral phosphoric acid catalyzed N−H bond insertion reaction. The reaction provides the N-alkyl indoles with a newly formed stereocenter adjacent to the indole nitrogen atom in good yields (up to 95 %) with excellent enantioselectivities (up to >99 % ee).

中文翻译:

通过卡宾插入反应进行 1H-吲哚的不对称 N-烷基化

通过铑和手性磷酸协同催化的N −H键插入反应,开发了1 H -吲哚的分子间对映选择性 N - 烷基化反应。该反应以良好的收率(高达 95%)和优异的对映选择性(高达 >99% ee)提供了具有与吲哚氮原子相邻的新形成的立构中心的 N-烷基吲哚
更新日期:2023-10-11
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