Herein, we report a nickel-catalyzed intramolecular denitrogenative dual annulation reaction of aryl nitrile-containing 1,2,3-benzotriazine-4(3)-ones to synthesize polycyclic pyrroloquinazolinones with a tolerance of a wide diversity of substituents. This catalytic reaction is the first denitrogenative transannulation of 1,2,3-benzotriazine-4(3)-one with nitrile, which can be applied as the critical step to synthesize luotonin A with a high step economy.

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http://dx.doi.org/10.1021/acs.orglett.3c03142DOI Listing

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