反应详情

4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzoic acid (500 mg, 1.042 mmol), 2-aminoethanesulfonamide (142 mg, 1.146 mmol), HATU (594 mg, 1.563 mmol), and Hunig's Base (0.910 mL, 5.21 mmol) were stirred in DCM (Volume: 5 mL) for 16 h. The solvent was removed and the crude material was purified by silica gel chromatography using EtOAc to give 4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)-N-(2-sulfamoylethyl)benzamide (150 mg). 1H NMR (400 MHz, MeOD) δ ppm 1.31-1.42 (m, 4H), 3.34-3.40 (m, 2H), 3.79-3.89 (m, 2H), 4.86-4.92 (m, 2H), 7.20-7.33 (m, 4H), 7.58-7.71 (m, 3H), 7.76-7.89 (m, 1H); LC-MS (Condition A), MS m/z (M++H) 585.9.

1. customThe solvent was removed
2. customthe crude material was purified by silica gel chromatography