Abstract

AbstractHerein, we report a highly efficient Sonogashira‐type cross‐coupling reaction of heteroaryl halides with terminal alkynes under mild transition‐metal‐free conditions using PPh3 and Cs2CO3/NEt3, A wide range of functional groups was tolerated under optimized conditions. Furthermore, the protocol could be extended to the Suzuki‐type cross‐coupling of heteroaryl halides with phenylboronic acid, achieving the corresponding products in good to excellent yields. A test reaction on gram scale delivered the product in reasonably high yield and thus has the potential of promising applications in drug discovery and functional materials.

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