反应详情

Following the procedure as described in EXAMPLE 44, making non-critical variations to replace di-tert-butyl [5-(5-chloro-2-{4-[(2,4-dimethoxybenzyl)(1,2,4-thiadiazol-5-yl)sulfamoyl]-2,5-difluorophenoxy}phenyl)-1,2-benzoxazol-3-yl]imidodicarbonate with 4-(4-chloro-2-(3-(dimethylamino)benzo[d]isoxazol-5-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide, 4-(4-chloro-2-(3-(dimethylamino)benzo[d]isoxazol-5-yl)phenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide was obtained as a colorless solid in 31% yield (0.06 g): 1H NMR (300 MHz, DMSO-d6) δ8.53 (s, 1H), 8.03 (d, J=1.1 Hz, 1H), 7.74-7.68 (m, 2H), 7.66 (dd, J=8.7, 1.6 Hz, 1H), 7.56 (d, J=8.9 Hz, 1H), 7.52 (dd, J=8.8, 2.7 Hz, 1H), 7.32 (d, J=8.7 Hz, 1H), 7.13 (dd, J=10.5, 6.5 Hz, 1H), 3.08 (s, 6H); MS (ES+) m/z 563.6 (M+1), 565.6 (M+1).