Synthesis of Indeno-Quinolones and Their Functionalization toward 5-HT3 Receptor.

Abstract

A practical and sustainable approach for the synthesis of bioactive indeno-quinolinones has been developed via tert-butyl hydroperoxide-mediated cross-dehydrogenative coupling. This metal and photocatalyst-free protocol proceeds under mild conditions and demonstrates broad substrate scope and operational simplicity. The potential for late-stage functionalization underscores the utility of this method in the efficient synthesis of bioactive compounds such as 5-HT3 receptor and TAS-103 analogues.