Objective:To explore an economical and effective method to synthesize 2,6-dimethyl-L-tyrosine. Methods: 2,6-dimethyl-L-tyrosine was stereoselectively synthesized by coupling of O-carbethoxy-3,5-dimethyl-4-chloromethyl phenol with (S)-2-[N-(N’-benzylprolyl)-amino] benzophenone-Ni-glycine[(S)-BPB-Ni-Gly] Schiff base. Results: The target compound was successfully synthesized starting from 3,5-dimethylphenol by 4 steps with a total yield of 34.3%. Conclusion: This method has the characteristics of cheap starting material,practicable,and reproducible.