1-(2-methoxyphenyl)piperazine (500 mg, 2.60 mmol) was dissolved in DMF (15 mL). To this solution was added N-benzyloxycarbonyl-L-phenylalanine (770 mg, 2.60 mmol) and 1-hydroxybenzotriazole monohydrate (414 mg, 2.71 mmol). The reaction mixture was cooled to 0 °C, then 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (515 mg, 2.71 mmol) was added. Reaction was allowed to warm to room temperature, then stirred for 20 h at room temperature. Complete of the reaction was confirmed by TLC. Reaction was quenched by adding H₂O (20 mL). Reaction mixture was extracted by EtOAc (30 mL). Organic phase was washed with H₂O (20 mL, twice) and brine (20 mL), dried over Na₂SO₄, concentrated under reduced pressure to afford the crude product (1.2 g) as pale yellow oil. Crude product was purified by column chromatography on silica-gel (EtOAc: Hexane = 60: 40) to afford the product as white powder (1.10 g, 2.32 mmol, 90%).

¹H NMR (400 MHz, CD₂Cl₂) δ 7.39-7.16 (m, 10H), 6.99 (m, 1H), 6.91-6.84 (m, 2H), 6.78 (m, 1H), 5.73 (d, J = 8,2 Hz, 1H), 5.12-5.01 (m, 2H), 4.91 (dd, J = 7.7, 7.3 Hz, 1H), 3.82 (s, 3H), 3.71-3.63 (m, 2H), 3.51 (m, 1H), 3.31 (m, 1H), 3.07-2.78 (m, 5H), 2.51 (m, 1H).