反应详情

To a solution of [4-(3-amino-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester (30 mg, 0.079 mmol) and benzoyl chloride (16.4 mg, 0.119 mmol) in tetrahydrofuran (3 mL) was added triethylamine (16 mg, 0.158 mmol) at 0° C. After being stirred at room temperature overnight, the mixture was concentrated in vacuo. The residue was purified by flash column (gradient elution, 0-5% methanol in dichloromethane) to afford [4-(3-benzoylamino-benzenesulfonylamino)-4,5,6,7-tetrahydro-indazol-1-yl]-acetic acid ethyl ester (27.4 mg, 72%) as a white solid. MS cald. for C24H26N4O5S 482, obsd. (ESI+) [(M+H)+] 483.

1. concentrationthe mixture was concentrated in vacuo
2. customThe residue was purified by flash column (gradient elution, 0-5% methanol in dichloromethane)