CuI/TEMPO-mediated aerobic oxidative sp3 C-H functionalization affording pyrrol-2-one derivatives
Aritra Mondal1, Sunanda Mandal1, Saikat Khamarui2
1Department of Chemistry, Presidency University, 86/1 College Street, Kolkata 700073, India. sumanray48@gmail.com.
None:
5-Hydroxy-1H-pyrrol-2-ones represent a very important class of compounds. However, their syntheses rely on precursors that are exotic and commercially unavailable, or on multistep operations. A cascade reaction can evade multistep syntheses, but most substrates are not amenable to cascade strategies. We thoughtfully designed a cascade strategy, choosing the Knoevenagel product of a ketone and malononitrile as a very trivial starting material. This strategy afforded 5-hydroxy-1H-pyrrol-2-ones via a cascade of C(sp3)-H functionalization, directed nitrile hydrolysis and C-N bond-forming reactions.
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