反应详情

3-(2-{2-[2-(2-Dimethylamino-ethoxy)-naphthalen-1-yl]-ethoxy}-benzenesulfonylamino)-4-oxo-butyric acid tert-butyl ester (190 mg, 0.33 mmol) was stirred with trifluoroacetic acid (0.4 mL) in CH2Cl2 (1.2 mL) at room temperature for 1 h. Analytical HPLC analysis indicated the reaction was complete. The reaction mixture was concentrated. Residual trifluoroacetic acid was azeotroped with toluene. The crude product was purified by preparative HPLC to give 3-(2-{2-[2-(2-Dimethylamino-ethoxy)-naphthalen-1-yl]-ethoxy}-benzenesulfonylamino)-4-oxo-butyric acid (31 mg, 0.060 mmol) as a white solid in 18% yield. MS (APCI) m/z 515.1 (M+1).

1. concentrationThe reaction mixture was concentrated
2. customResidual trifluoroacetic acid was azeotroped with toluene
3. customThe crude product was purified by preparative HPLC