Fc-PIP Catalyzed Asymmetric Synthesis of cis-2,3-Dihydrobenzofurans

Authors

  • Shanshan Jiang,

    1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
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  • Bin Hu,

    1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
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  • Xingxin Yu,

    Corresponding author
    1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
    • Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China, Tel.: 0086-021-64252431; Fax: 0086-021-64252431

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  • Weiping Deng

    Corresponding author
    1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
    • Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China, Tel.: 0086-021-64252431; Fax: 0086-021-64252431

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Abstract

A highly enantioselective intramolecular Michael addition-Lactonization domino reaction of a range of enon acids catalyzed by nuleophilic organocatalyst (Fc-PIP) was developed, furnishing cis-2,3-dihydrobenzofuran derivatives with excellent enantioselecitivities (94%–98% ee) and good diastereoselectivities (up to 99/1).

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