Polycyclic indole frameworks are more important scaffolds that can be found in a large number of pharmaceutical and bioactive natural products. Therefore, efficient and selective reactions allowing the construction of fused cyclic systems could be useful methods. Past few decades intramolecular C–H activation of indole has been developed using the different strategies with transition metal catalysts. Using efficient catalysts and the suitable directing group would be enhanced reactivity, structural diversity, atom, and step economy of the C–H activation. Herein, we report intramolecular C–H activation using 1-napthylamine as a transient directing group by incorporating [RuCl2(p-cymene)]2 as a catalyst with high yields.

Synthesis of polycyclic indoles via Ru(II)-catalyzed C–H activation

ACS Spring 2022

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