Abstract
Quinazolinones are common substructures in molecules of medicinal importance. We report an enantioselective copper‐catalyzed borylative cyclization for the assembly of privileged pyrroloquinazolinone motifs. The reaction proceeds with high enantio‐ and diastereocontrol, and can deliver products containing quaternary stereocenters. The utility of the products is demonstrated through further manipulations.
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