To improve the biological activities of rupestonic acid, 21 new rupestonic acid fatty ester derivatives (2a-2h) and aromatic ester derivatives (2i-2u) were synthesized and preliminarily evaluated for their anti-influenza activity in vitro by the national center for drug screening of China, using the Oseltamivir and Ribavirin as reference drugs. The results showed that 2l ($IC_{50}=0.5{mu}mol/L$) exhibited potent anti-influenza $A_3$ viral activity among the synthesized compounds and was 10-fold more potent than that of the reference drug Oseltamivir ($IC_{50}=5.1{mu}mol/L$).