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Construction of N-C Axial Chirality through Atroposelective C-H Olefination of N-Arylindoles by Palladium/Amino Acid Cooperative Catalysis.

Direct construction of N-C axial chirality via Pd-catalyzed atroposelective C-H olefination of N-arylindoles is reported. The crucial role of chiral amino acid as a cocatalyst in the regio- and stereocontrol has been disclosed. In this reaction, a wide range of arylindoles and functional alkenes could be well tolerated. Moreover, the practicality and synthetic value of this process were demonstrated by the divers and simple transformations of the products.