Access to Sultams by Rhodium(III)-Catalyzed Directed C[BOND]H Activation


  • This work is supported by the EPFL and the European Research Council under the European Community’s Seventh Framework Program (FP7 2007–2013)/ERC Grant agreement no 257891. We thank Dr. R. Scopelliti for X-ray crystallographic analysis.


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Director's cut: The pharmaceutically relevant sulfonamide group is shown to be a competent directing group for [Cp*Rh(OAc)2]-catalyzed C[BOND]H functionalizations. Reactions of the cyclometalated intermediate with internal alkynes provide access to a wide range of sultam derivatives. The reaction is high yielding and works best under aerobic conditions with catalytic amounts of CuOAc as an oxidation mediator. Cp*=C5Me5.