Advances in α‐Hydroxylation of β‐Dicarbonyl Compounds

Abstract The α ‐hydroxy‐ β ‐dicarbonyl motif is essential in many biologically active compounds, sparking significant interest in their synthesis. This review comprehensively examines the advancements in the α ‐hydroxylation of β ‐dicarbonyl compounds, systematically categorizing the methods based on the types of oxidants employed and highlighting advances in asymmetric α ‐hydroxylation. It evaluates the substrate scope, advantages, and disadvantages of each approach, summarizing the possible intermediates involved and the types of reaction mechanisms.