反应详情

To the mixture of 5-(5-bromo-4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrimidin-2-yl)-N-(2-(dimethylamino)ethyl)thiophene-2-sulfonamide (200 mg, 0.39 mmol) in THF/H2O (2 mL/2 mL), Ac2O (0.2 mL, 1.95 mmol, 5.0 eq) was added dropwise. The reaction mixture was stirred at room temperature for 14 h. The reaction mixture was filtered, and the solid was concentrated with ethanol to bring residual water off to afford crude 5-(4-(1-acetyl-5-cyclopropyl-1H-pyrazol-3-ylamino)-5-bromopyrimidin-2-yl)-N-(2-(dimethylamino)ethyl)thiophene-2-sulfonamide (used for the next step without further purification). LC-MS (m/z)=556.0, 558.0 [M+H]+

1. additionwas added dropwise
2. filtrationThe reaction mixture was filtered
3. concentrationthe solid was concentrated with ethanol