Synthesis of 4-quinolones via a palladium-catalyzed carbonylative cyclization of o-iodoanilines and alkynes

Abstract

4-Quinolones are widely utilized in pharmaceutical chemistry as a versatile scaffold, exhibiting a broad spectrum of biological activities. However, the development of general and step-economical methods for their direct synthesis from simple starting materials remains a significant challenge. Herein, we report a highly efficient one-pot synthesis of 4-quinolones. This strategy employs a ppm-level palladium-catalyzed carbonylative coupling of 2-iodoanilines with terminal alkynes, followed by a piperazinemediated cyclization. The protocol features a broad substrate scope and proceeds under mild reaction conditions, delivering the desired products in yields of up to 96%.