RSC Adv. 2023 Mar 1;13(10):6993-6999. doi: 10.1039/d3ra00088e. eCollection 2023 Feb 21.
ABSTRACT
A simple and effective method for the copper-catalyzed selective C5-H bromination and difluoromethylation of 8-aminoquinoline amides with ethyl bromodifluoroacetate as the bifunctional reagent was developed. The combination of cupric catalyst and alkaline additive results in a C5-bromination reaction, whereas cuprous catalyst combined with silver additive results in the C5-difluoromethylation reaction. This method has a broad substrate scope and allows for easy and convenient access to desired C5-functionalized quinolones with good to excellent yields.
PMID:36874938 | PMC:PMC9977446 | DOI:10.1039/d3ra00088e