Synthesis of 4‐Cyclobutene‐Isoquinolines From Aryl Imidates by Ru(II)‐Catalyzed Domino C–H Activation/Cyclization

ABSTRACT A highly regioselective approach for constructing 4‐cyclobutene‐isoquinoline derivatives through ruthenium‐catalyzed domino C–H activation/cyclization of aryl imidates has been demonstrated. This new transformation tolerates various substituted functional groups on imidates and propargylic monofluoroalkynes, resulting in the corresponding products being delivered in moderate yields.