Privileged scaffolds on demand: a Passerini-based strategy toward α-ketoamides
Abstract
We report a scalable Passerini-based method for synthesizing α-ketoamides, key medicinal motifs. Using p-hydroxybenzoic acid and ethanol, Mumm rearrangement was interrupted to yield α-hydroxyamides and then oxidized in one pot. The method tolerates diverse substrates, enables gram-scale synthesis and affords inhibitors of human 15-LOX-1, highlighting its biological and synthetic potential.

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