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Ferulic acid was used as a common drug for cardia-cerebrovascular disease and leukopenia, but the application of ferulic acid was inhibited by the poor absorption and stability. The improvement of these defects can be realized by modifying ferulic acid by amino acids, because the amido bond can increase the bioavailability and therapeutic effect of some drugs based on the peptide transporter system of mammalian which can transport the peptidyl drugs. The peptidyl derivatives of ferulic acid, namely acetyl feruloyl tyrosine and acetyl feruloyl valyl tyrosine, were synthesized using Fmoc solid-phase synthesis method. The synthesized ferulic acid amide derivatives were purified by RP-HPLC, and characterized by IR, 1HNMR and ESI-MS. The results indicated that Fmoc solid phase synthesis was a convenient method for the amide bond modification of ferulic acid and the further property research on ferulic acid derivatives.