For efficiently constructing functionalized β-aryl-δ-amino acid derivatives, starting from easily prepared 5-phthalimide-2-pentenoic acid methyl ester and arylboric acids as raw materials, nine kinds of 5-phthalimide-3-arylvalerate methyl ester were obtained via a [Rh(COD)Cl]2 catalyzed Michael reaction. And the yields were more than 95%. The obtained compounds were confirmed by 1HNMR, 13CNMR and HR-MS, respectively. Moreover, the optimum reaction conditions for synthesis of 5-phthalimide-3-arylvalerate methyl ester were as follows: methyl 5-phthalimide-2-pentenoate (0.2 mmol), arylboric acid (0.4 mmol), potassium hydroxide aqueous solution (0.1 mL, 1.0 mol/L), [Rh(COD)Cl]2 (0.005 mmol), 1,4-dioxane (1.0 ml) as solvent，reaction time of 10 hours，at the temperature 100℃. In addition, 5-phthalimide-3-p-chlorophenylvalerate methyl ester can be used for the rapid preparation of the active molecules of homobaclofen hydrochloride.