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.
He, Y., Wu, D., Li, Z., Robeyns, K., Van Meervelt, L., & Van der Eycken, E. V. (2019). Facile construction of diverse polyheterocyclic scaffolds via gold-catalysed dearomative spirocyclization/1,6-addition cascade. Organic & Biomolecular Chemistry, 17(25), 6284-6292. https://doi.org/10.1039/c9ob01299k (Original work published 2019)