Tumor-associated carbohydrate antigens (TACAs), important molecular markers on tumor cells, are major targets for the development of anti-cancer vaccines. However, due to the immunotolerance and weak immunogenicity, native TACAs cannot induce powerful immune response. The use of modified TACAs such as N-glycosides could be an alternative strategy to overcome this problem. Herein, the synthesis of N(OMe)-linked analogue of tumor-associated disaccharide antigen Thomsen-Friedenreich (TF) by the glycosylation reaction is described.