Patel, Chandresh K.Gujjarappa, RaghuramKant, KamalGhanta, SusantaSingh, VirenderKabi, Arup K.Al-Zaqri, NabilMalakar, Chandi C.2024-01-212024-08-132024-01-212024-08-132023-06-091615415010.1002/adsc.202300217https://kr.cup.edu.in/handle/32116/3277The established process proceeds through copper (II)-catalyzed C(sp3)? functionalization of ?-diketones/?-ketoesters with 2-bromobenzaldehyde oximes followed by the intramolecular cyclization of in situ generated acylated intermediates to deliver isoquinoline N-oxides. The copper(II) acetate catalyzed C?H functionalization showed maximum efficacy at 60 �C in methanol/toluene as solvent. The described reaction conditions were applicable over a wide range of substrates with a variety of functional groups to yield isoquinoline N-oxides in yields up to 85%. The developed approach was further elucidated by means of control experiments and DFT calculations. � 2023 Wiley-VCH GmbH.en-USActive methylene compoundsC(sp³)? activationCopper catalysisIsoquinoline N-oxidetrans-esterificationArticlehttps://onlinelibrary.wiley.com/doi/10.1002/adsc.202300217