期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 26, 页码 7475-7478出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201703833
关键词
alkynes; asymmetric catalysis; dearomatization; heterocycles; palladium
资金
- National Natural Science Foundation of China [21372202, 21502169, 21522207]
- Natural Science Foundation of Zhejiang Province [LR14B020001, LQ15B020003]
Palladium-catalyzed enantioselective dearomative arylalkynylation of N-substituted indoles, through a Heck/Sonogashira sequence, was established using a new BINOL-based phosphoramidite as the chiral ligand. A wide range of 2,3-disubstituted indolines, bearing vicinal quaternary and tertiary stereocenters, were efficiently constructed in one step with excellent enantioselectivities (up to 97% ee) and diastereoselectivities (> 20:1).
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