The Rh(III)-catalyzed C-H functionalization and subsequent oxidative annulation between 5-aryl pyrazinones and internal alkynes are reported. This protocol provides facile access to a wide range of pyrazinone-linked naphthalenes via the C(sp)-H alkenylation and subsequent annulation. This transformation is characterized by mild conditions, simplicity, and excellent functional group compatibility. Notably, it is a first report of the utilization of pyrazinones as directing groups in C-H functionalization.
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