Palladium‐Catalyzed Suzuki–Miyaura Cross‐Coupling of Heteroaryl‐2‐Boronic Acids with Nitroaryl Halides

Heteroaryl‐2‐boronic acids are challenging substrates in the Suzuki–Miyaura cross‐coupling reaction. Here, we report the efficient cross‐coupling of heteroaryl‐2‐boronic acids enabled by using nitro‐substituted aryl halides as the coupling partner under palladium catalysis. The nitro group not only boosts the reactivity of the reaction but also serves as a versatile handle for further functionalization. This method features a broad scope, excellent functional group tolerance, as well as high yields with a low catalyst loading under mild reaction conditions. The utility of the methods is demonstrated by the derivatization of the product and the efficient synthesis of pharmaceutical drug dantrolene.