Iridium-Catalyzed Borylation of 6-Fluoroquinolines: Access to 6-Fluoroquinolones

The Ir-catalyzed C-H borylation of fluoroquino-lines has been realized. The quinoline boronic ester formed undergoes a range of important transformations of relevance to medicinal chemistry. Judicious choice of the substituent at C4 on the quinoline facilitated the unmasking of a fluoroquinolone?the core structure of many antibiotics.

Automated summary

The Ir-catalyzed C-H borylation of fluoroquinolines has been achieved, leading to the formation of quinoline boronic esters that can undergo important transformations relevant to medicinal chemistry. The strategic choice of the substituent at C4 on the quinoline enables the unmasking of fluoroquinolone, which serves as the core structure for many antibiotics.