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A novel gold-catalyzed tandem alkyne amination/intramolecular O–H insertion has been developed. A variety of [1,4]oxazino[3,2-c]isoquinolines are readily accessed under mild reaction conditions by utilizing this strategy, thereby providing an efficient and practical route for the construction of synthetically useful fused isoquinolines.

Graphical abstract: Synthesis of fused isoquinolines via gold-catalyzed tandem alkyne amination/intramolecular O–H insertion

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