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Issue 27, 2017
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Rhodium-catalyzed redox-neutral coupling of phenidones with alkynes

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Abstract

A switchable synthesis of N-substituted indole derivatives from phenidones via rhodium-catalyzed redox-neutral C–H activation has been achieved. In this protocol, we firstly disclosed that the reactivity of Rh(III) catalysis could be enhanced through employing palladium acetate as an additive. Some representative features include external oxidant-free, applicable to terminal alkynes, short reaction time and operational simplicity. The utility of this method is further showcased by the economical synthesis of potent anticancer PARP-1 inhibitors.

Graphical abstract: Rhodium-catalyzed redox-neutral coupling of phenidones with alkynes

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Publication details

The article was received on 24 May 2017, accepted on 16 Jun 2017 and first published on 16 Jun 2017


Article type: Paper
DOI: 10.1039/C7OB01271C
Citation: Org. Biomol. Chem., 2017,15, 5701-5708
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    Rhodium-catalyzed redox-neutral coupling of phenidones with alkynes

    Z. Fan, H. Lu, W. Li, K. Geng and A. Zhang, Org. Biomol. Chem., 2017, 15, 5701
    DOI: 10.1039/C7OB01271C

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