Transition Metal-Free, Methoxide-Catalyzed Synthesis of Pyridoindolones

A simple transition metal-free strategy
for the synthesis of pyrido­[1,2-a]­indolone derivatives
has been devised through sodium
methoxide-catalyzed intramolecular cyclization of 2-alkenylated N-pyrimidyl indoles. The reactions involved a Smiles rearrangement/cyclization
cascade, which resulted in a new series of N-fused
indoles, potentially applicable skeletons in medicinal chemistry.
This reaction presents simple eco-friendly reaction conditions, a
high atom- and cost-economy, a short reaction time, and a broad range
of substrate scope with high reaction efficiency.