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Enantioselective Synthesis of gem-Diaryl Benzofuran-3(2H)-ones via One-Pot Asymmetric Rhodium/Palladium Relay Catalysis

Zong-Feng Zhang, Dong-Xing Zhu, Wen-Wen Chen, Bin Xu* and Ming-Hua Xu*

*State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China, Email:,

Z.-F. Zhang, D.-X. Zhu, W.-W. Chen, B. Xu, M.-H. Xu, Org. Lett., 2017, 19, 2726-2729.

DOI: 10.1021/acs.orglett.7b01070 (free Supporting Information)


An asymmetric dual-metal relay catalysis strategy that combines Rh/chiral sulfur-olefin-catalyzed enantioselective 1,2-addition with a Pd-catalyzed intramolecular C-O coupling enables a rapid and efficient synthesis of quaternary carbon-containing gem-diaryl benzofuran-3(2H)-ones in good yields in a highly enantioselective manner.

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ID: J54-Y2017