期刊
CHEMICAL COMMUNICATIONS
卷 56, 期 16, 页码 2499-2502出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9cc09637j
关键词
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资金
- Youth Innovation Promotion Association CAS [2018402]
- Natural Science Foundation of Sichuan province, China [2017JY0055]
- Innovative Team of Sichuan Province [2017TD0021, 2012SZ0219]
Hydroxyl alkylation of indoles by Friedel-Crafts reaction with a carbonyl compound is a useful strategy. However, the reaction was restricted to ketones due to the easy formation of a bisindole byproduct. Therefore, hydroxyl alkylation of an aldehyde with indole is confronted with great challenges. Here, we report an efficient strategy for asymmetric hydroxyl alkylation of 2-substituted indoles with aldehydes under 0.1 mol% chiral phosphoric acid. A series of alpha-hydroxyl ketones were obtained in high yields (up to 99%) and good enantioselectivities (up to 97%).
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