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One-pot synthesis of 2,3-difunctionalized indoles via Rh(III)-catalyzed carbenoid insertion C–H activation/cyclization

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Abstract

Reported herein is the first Rh(III)-catalyzed carbenoid insertion C–H activation/cyclization of N-arylureas and α-diazo β-keto esters. The redox-neutral reaction has the following features: good to excellent yields, broad substrate/functional group tolerance, exclusive regioselectivity, and no need for additional oxidants or additives, which render this methodology as a more efficient and versatile alternative to the existing methods for the synthesis of 2,3-difunctionalized indoles.

Graphical abstract: One-pot synthesis of 2,3-difunctionalized indoles via Rh(iii)-catalyzed carbenoid insertion C–H activation/cyclization

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Publication details

The article was received on 09 Aug 2017, accepted on 05 Sep 2017 and first published on 05 Sep 2017


Article type: Paper
DOI: 10.1039/C7OB01977G
Citation: Org. Biomol. Chem., 2017, Advance Article
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    One-pot synthesis of 2,3-difunctionalized indoles via Rh(III)-catalyzed carbenoid insertion C–H activation/cyclization

    H. Lv, J. Shi, B. Wu, Y. Guo, J. Huang and W. Yi, Org. Biomol. Chem., 2017, Advance Article , DOI: 10.1039/C7OB01977G

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