Full text can be accessed at http://www.sciencedirect.com/science/article/pii/S0008621511005714Acacetin-7-O-β-d-galactopyranoside (1), a natural flavonoid isolated from flower heads of Chrysanthemum morifolium, has been reported to inhibit the replication of HIV in H9 cells. We achieved the total synthesis of compound 1 by employing a one-pot synthesis of the aglycon. The key reactions in this approach include the modified Baker–Venkataraman reaction and regio- and stereoselective O-glycosylations.