Enantioselective Dearomative Difunctionalization of Indoles by Palladium-Catalyzed Heck/Sonogashira Sequence |
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| Authors: | Dr. Ren-Rong Liu Yong-Gang Wang Ying-Long Li Bing-Bing Huang Dr. Ren-Xiao Liang Prof. Dr. Yi-Xia Jia |
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| Affiliation: | College of Chemical Engineering, Zhejiang University of Technology, Chaowang Road 18, Hangzhou, 310014 China |
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| Abstract: | 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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| Keywords: | alkynes asymmetric catalysis dearomatization heterocycles palladium |
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