A highly enantioselective intramolecular arylative dearomatization of indoles via palladium-catalyzed reductive Heck reactions was developed. The new strategy led to a series of optically active indolines bearing C2-quaternary stereocenters in modest to good yields with excellent enantioselectivities (up to 99% ee).

Highly enantioselective Friedel-Crafts C2-alkylation reactions of 3-substituted indoles with α,β-unsaturated esters and nitroalkenes were developed using chiral Lewis acids as catalysts, which afforded chiral indole derivatives bearing C2-benzylic stereogenic centers in good to excellent yields (up to 99%) and enantioselectivities (up to 96% ee).

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Enantioselective Arylative Dearomatization of Indoles via Pd-Catalyzed Intramolecular Reductive Heck Reactions. -(SHEN, C.; LIU, R.-R.; FAN, R.-J.; LI, Y.-L.; XU, T.-F.; GAO, J.-R.; JIA*, Y.-X.; J. Am. Chem. Soc. 137 (2015) 15, 4936-4939, http://dx.doi.org/10.1021/jacs.5b01705 ; Coll. Chem. Eng., Zhejiang Univ. Technol.,