N-benzoyl-O-benzoyl-L-tyrosine(Ⅰ) were synthesized，in the yields of 87 %，by L-tyrosine with benzoyl chloride under the alkaline condition. Ⅱ is formed with L-Phenylglycinol condensation under the IBCF-NMM, Ⅲ was synthesized by alkaline hydrolysis of Ⅱ. 2-Dimethylaminoethyl chloride hydrochloride by n(anhydrous K2CO3)︰n(compound 3)=7︰1 gave Ⅳ with a yield of 79 % at 110 ℃ for 4 h. 11 compounds of derivatives were synthesized by compound Ⅳ in DMF, reacted with an organic acid under conditions of EDC•HCl, and 4-dimethylamino pyridine. Its structure was confirmed by NMR, ESI-MS.