Quinolones represent an important class of compounds in medicinal chemistry e.g. as substructures in antibacterial agents. Here, we present a mild and efficient protocol for the synthesis of functionalised quinolones. A carbonylative Sonogashira cross-coupling reaction using Mo(CO)6 as a solid source of carbon monoxide provides the non-cyclised precursor. By the addition of diethylamine to the reaction mixture the cyclised compound can be obtained.The quinolone scaffold can be used in the synthesis of potent inhibitors of Mycobacterium tuberculosis.

Mild and efficient protocol for the synthesis of functionalised quinolones via a carbonylative Sonogashira cross-coupling

244th National Meeting (2012)

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