1,2-Dichloroethane → N-[4-(3-Hydroxy-propyl)-phenyl]-2-[3-oxo-1-(toluene-4-sulfonyl)-1,2,3,4-tetrahydro-pyrazin-2-yl]-acetamide

関与物質

反応手順

To a 20 mL vial was added [3-oxo-1-(toluene-4-sulfonyl)-1,2,3,4-tetrahydro-pyrazin-2-yl]-acetic acid (500 mg, 1.61 mmol), EDC (Aldrich, 464 mg, 2.42 mmol), HOBt (Aldrich, 195 mg, 1.45 mmol), CH2Cl2 (5 mL), 3-(4-amino-phenyl)-propan-1-ol (731 mg, 4.84 mmol) and (iPr)2NEt (Aldrich, 0.56 mL, 3.22 mmol). The reaction mixture was stirred at room temperature overnight and diluted with CH2Cl2 (60 mL). The organic phase was washed with saturated NaHCO3, water and brine, dried over Na2SO4, filtered and concentrated in vacuo. The crude was purified by silica gel chomatography (6%-8% MeOH—CH2Cl2) to afford the title compound. MS (ESI): 444 (M+H)+.

情報源と証拠