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Updated: Mar 21, 2026

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Published on: May 27, 2015
Ag(I)-Catalyzed Indolization/C3-Functionalization Cascade of 2-Ethynylanilines via Ring Opening of Donor-Acceptor
Raju Karmakar1, Arun Suneja1, Vinod K Singh1,2
1Department of Chemistry, Indian Institute of Science Education and Research Bhopal , Bhopal Bypass Road, Bhauri, Bhopal, Madhya Pradesh 462 066, India.
Abstract:
A AgSbF6-catalyzed cascade involving the ring opening of donor-acceptor cyclopropanes (DACs) preceded by the cyclization of N-protected 2-ethynylaniline is described. The method discloses a step-economy route to 2,3-disubstituted indole, where a Ag catalyst is found to trigger the cascade by activating both alkyne and DACs. Various functionalities at different ends of both substrates offer rapid access to 2,3-disubstituted indole derivatives in one pot in good to excellent yields. Elaboration of the cascade product to useful intermediates is also depicted.
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