反应详情

To a solution of (S)-3-[4-carbamoyl-2-(2-quinolin-5-yl-ethoxy)-benzenesulfonylamino]-4-oxo-butyric acid tert-butyl ester (0.08 g, 0.15 mmol) in dichloromethane (10 mL) and water (0.1 ml) was added trifluoroacetic acid (1 mL). The reaction was stirred for 1 h at room temperature. The reaction was then concentrated under reduced pressure to yield a clear oil. The residue was purified by reverse phase high-pressure liquid chromatograph using a gradient of 0% to 30% acetonitrile containing 0.1% TFA and water containing 0.1% TFA over 140 minutes to yield 3-[4-carbamoyl-2-(2-quinolin-5-yl-ethoxy)-benzenesulfonylamino]-4-oxo-butyric acid as a white solid (0.01 g, 14%). MS(APCI) m/z 472.1 (M+1)

1. concentrationThe reaction was then concentrated under reduced pressure
2. customto yield a clear oil
3. customThe residue was purified by reverse phase high-pressure liquid chromatograph
4. customover 140 minutes