Abstract: There exist significant changes in glycosyltransferase expression during tumorigenesis, which leads to the unique sugar chain structural characteristics of glycoproteins on the surface of tumor cells compared to normal cells, namely highly truncated sugar chains. These aberrant glycosylated products are called tumor-associated carbohydrate antigens (tumor-associated carbone antigens, TACAs). As an important molecular marker of malignant tumors, TACAs not only participate in the regulation of tumor occurrence, development, invasion and metastasis of tumors, but also play a key role in tumor immune escape. Thus, targeting abnormally glycosylated proteins or peptides on tumors have become one of most important anti-tumor drug development strategies. However, it is difficult to isolate glycoproteins from natural sources, and it is still challenging to synthesize complex glycoproteins or glycopeptides by chemical methods. This review summarizes the progress of glycopeptide anti-tumor vaccine synthesized by chemical methods in recent years, in order to provide theoretical basis and technical reference for the research and development of glycopeptide anti-tumor vaccine in the future.