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-(2-oxoindolin-5-yl)phenoxy)-N-(2,4-dimethoxybenzyl)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide, 4-(4-chloro-2-(2-oxoindolin-5-yl)phenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide was obtained as an off-white solid in 53% yield over two steps (0.03 g): 1H NMR (300 MHz, DMSO-d6) δ10.48 (s, 1H), 8.52 (s, 1H), 7.74 (dd, J=9.9, J=6.4 Hz, 1H), 7.52 (d, J=2.6 Hz, 1H), 7.43 (dd, J=8.7, 2.6 Hz, 1H), 7.35 (br s, 1H), 7.31 (dd, J=8.1, 1.4 Hz, 1H), 7.23 (d, J=8.7 Hz, 1H), 7.09 (dd, J=10.5, 6.5 Hz, 1H), 6.83 (d, J=8.0 Hz, 1H), 3.47 (s, 2H), (NH not observed); MS (ES+) m/z 534.8 (M+1), 536.8 (M+1).