The method of synthesizing the active peptide RGD was adopted with the combinational strategies of chemistry and enzyme. DCC was used to produce GD dipeptide (HCl·Gly-Asp(oBzl)_2) , and then RGD tripeptide (Z-Arg-Gly-Asp(oBzl)_2) was enzymatically synthesized by trypsin. The results showed that the yield of GD dipeptide is 77.7% after 10 hours with the mole ratio of G and D is 1.5∶1, and under the low-water 1,4-butanediol solvents condition the yield of RGD is 41.9%.