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A convenient CuI/L-proline-catalyzed, two-step one-pot method has been developed for the preparation of indolo[1,2-a]quinazoline derivatives using a sequential Ullmann-type C-C and C-N coupling. This protocol provides an operationally simple and rapid strategy for preparing indolo[1,2-a]quinazoline derivatives and displays good functional group tolerance. All the starting materials are commercial available or can be easily prepared.

A simple copper-catalyzed two-step one-pot synthesis of indolo[1,2-a]quinazoline