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Synfacts 2010(3): 0313-0313  
DOI: 10.1055/s-0029-1219336
Metal-Catalyzed Asymmetric Synthesis and Stereoselective Reactions
© Georg Thieme Verlag Stuttgart ˙ New York

Copper-Catalyzed Enantioselective Friedel-Crafts Alkylation of Indoles

Contributor(s): Mark Lautens, Chit Tsui
Y.-J. Sun, N. Li, Z.-B. Zheng, L. Liu, Y.-B. Yu, Z.-H. Qin, B. Fu*
China Agricultural University, Beijing, P. R. of China
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Publication History

Publication Date:
18 February 2010 (online)

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Significance

Friedel-Crafts alkylation of indole derivatives with α,β-unsaturated carbonyl compounds has been extensively developed due to the importance of indoles as building blocks in natural products and pharmaceutical agents. Despite the many contributions already in the literature, challenges still remain in developing highly efficient chiral catalysts for the Friedel-Crafts alkylation between indole and alkylidenemalonate. The authors reported the studies of hetero­arylidenemalonate-derived bis(oxazoline) ligands, such as 1, and their copper(II) complexes in the highly efficient and enantioselective Friedel-Crafts alkylation of indoles and alkylidenemalonates.