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Published on: August 8, 2014
Facile construction of diverse polyheterocyclic scaffolds via gold-catalysed dearomative
Yi He1, Danjun Wu, Zhenghua Li
1Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, KU Leuven, Celestijnenlaan 200F, B-3001, Leuven, Belgium. ahlzhchem@gmail.com erik.vandereycken@kuleuven.be.
Abstract:
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.
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