目前,α-羟基羰基化合物存在于多种天然产物和药物分子中,并都具有生物活性。羰基化合物的直接α-官能化是构建C-C键和C-X键最有效、最直接的方法之一;合成α-羟基羰基化合物可通过羰基化合物的α-羟基化来实现。分子氧丰富、廉价、易得、对环境友好,可以作为羰基化合物α-羟基的理想氧源。因此,以氧气为氧源的羰基化合物的直接α-羟基受到了广泛的关注。本文从金属有机催化和有机小分子催化两个角度出发,主要阐述了近年来羰基化合物的不对称有氧α-羟基化反应的研究进展。Currently, α-hydroxycarbonyl compounds exist in a variety of natural products and drug molecules, and all of them are biologically active. Direct α-functionalization of carbonyl compounds is one of the most effective and direct methods to construct C-C and C-X bonds;the synthesis of α-hydroxycarbonyl compounds can be achieved by α-hydroxylation of carbonyl compounds. Molecular oxygen is abundant, cheap, easy to obtain, and environmentally friendly, and can be used as an ideal oxygen source for the α-hydroxylation of carbonyl compounds. Therefore, the direct α-hydroxylation of carbonyl compounds using oxygen as an oxygen source has received extensive attention. This paper focuses on the research progress of asymmetric aerobic α-hydroxylation reactions of carbonyl compounds in recent years from the perspectives of both metal-organic catalysis and organic small molecule catalysis.