Synthesis of 2-Quinolinones through Direct Annulation: A Tandem Suzuki Coupling-Cyclization Strategy

A convenient and general method for the synthesis of 2quinolinones has been developed. Modular β-borylacrylates are validated as programmable, ambiphilic C3 synthons in the cascade annulation of 2-bromoaniline derivatives, enabling the formation of structurally and electronically diverse 2-quinolinones. The transformation is operationally simple and demonstrates broad functional group tolerance, including synthetically valuable substituents such as Cl, CN, NO 2 , and CO 2 Me, which remain intact and allow for late-stage functionalization. The combination of high efficiency, wide substrate scope, and readily available starting materials makes this methodology highly attractive for the streamlined synthesis of 2-quinolinones.

Publication History

Received: 11 October 2025

Accepted after revision: 27 January 2026

Accepted Manuscript online:
20 February 2026