Rhodium-catalyzed redox-neutral coupling of phenidones with alkynes
Zhoulong Fan1, Heng Lu2, Wei Li3
1CAS Key Laboratory of Receptor Research, and the State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China. aozhang@simm.ac.cn and University of Chinese Academy of Sciences, Beijing 100049, China.
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.
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