The precursor dipeptides of RGD (Arg-Gly-Asp), N-CBZ-Arg-Gly-NH2 and CBZ-Gly-Asp-NH2 were synthesized in reverse micellar system and organic solvent using several proteases in different forms under kinetical control. The synthesis reaction conditions for CBZ-Arg-Gly-NH2 and CBZ-Gly-Asp-NH2 catalyzed by chymotrypsin in AOT/isooctane reverse micelles were optimized by examining the effects of several factors including water content, temperature, pH, and reaction time on the dipeptide yields. The best yields for the syntheses of CBZ-Arg-Gly-NH2 and CBZ-Gly-Asp-NH2 were 87.3% and 80.8%, respectively. The dipeptide products were separated from the reverse micelles by using a silica gel column.