Facile construction of diverse polyheterocyclic scaffolds: Via gold-catalysed dearomative spirocyclization/1,6-addition cascade

A gold-catalysed post-Ugi chemo-and diastereoselective cascade dearomative spirocyclization/1,6-addition sequence is disclosed for the synthesis of diverse fused polyheterocyclic scaffolds bearing indole, pyrrole, benzothiophene, furan or electron-rich arene moieties from easily available building blocks. The effectiveness and efficiency of this diversity-oriented approach has been proved in the rapid construction of 28 fused polyheterocyclic scaffolds with a good building-block variability and structural complexity in two operational steps. This journal is © The Royal Society of Chemistry.