Metal-free construction of dihydropyrazino[2,3-]indoles from 2-aminoacetophenones, isocyanates and 1,2-diamines.

A Brønsted acid/iodine co-mediated approach to construct dihydropyrazino[2,3-]indoles in 2-MeTHF as a green solvent at room temperature was established. A wide range of diversely substituted dihydropyrazino[2,3-]indoles (42 examples, 61-85% yields) were synthesized under mild conditions, even on a gram scale. This protocol features organocatalysts, an eco-friendly solvent, mild conditions, readily accessible substrates, broad substrate scope and simple work-up.