Oligosaccharides are the ubiquitous molecules of life. In order to translate human bioglycosylation into clinical applications, homogeneous samples of oligosaccharides and glycoconjugates can be obtained by chemical, enzymatic or other biological methods for systematic studies. However, the structural complexity and diversity of glycans and their conjugates present a major challenge for the synthesis of such molecules. This review summarizes the chemical synthesis methods of oligosaccharides, the application of oligosaccharides in the field of medicinal chemistry according to their related biological activities, and shows the great prospect of oligosaccharides in the field of pharmaceutical chemistry.

低聚糖是生命中无处不在的分子。为了将人类生物糖基化转化为临床应用，可以通过化学、酶促或其他生物学方法获得寡糖和糖缀合物的均质样品，以进行系统研究。然而，聚糖及其缀合物的结构复杂性和多样性对此类分子的合成提出了重大挑战。本文综述了低聚糖的化学合成方法、低聚糖在药物化学领域的应用以及低聚糖在药物化学领域的应用，展示了低聚糖在药物化学领域的广阔前景。