Herein we report a chiral phosphoric acid-catalyzed intermolecular C2 Friedel-Crafts alkylation reaction between -alkynylnaphthols and various 3-substituted indoles, affording axially chiral alkenes with up to 93% yields ( > 20:1) and up to 98% ee under mild reaction condition. Other substituted indole derivatives could be also tolerated in this system, giving the corresponding axially chiral alkenes with high yields and in excellent enantioselectivity.
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| http://dx.doi.org/10.1021/acs.joc.1c02750 | DOI Listing |
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