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 tert-butyl (5-(5-chloro-2-(4-(N-(2,4-dimethoxybenzyl)-N-(1,2,4-thiadiazol-5-yl)sulfamoyl)-2,5-difluorophenoxy)phenyl)benzo[d]isoxazol-3-yl)(methyl)carbamate, 4-(4-chloro-2-(3-(methylamino)benzo[d]isoxazol-5-yl)phenoxy)-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide was obtained as an off-white solid in 75% yield over two steps (0.21 g): 1H NMR (300 MHz, DMSO-d6) δ8.52 (s, 1H), 7.95 (d, J=1.1 Hz, 1H), 7.72 (dd, J=9.9, 6.5 Hz, 1H), 7.65 (dd, J=8.7, 1.6 Hz, 1H), 7.61 (d, J=2.6 Hz, 1H), 7.52-7.46 (m, 2H), 7.28 (d, J=8.7 Hz, 1H), 7.14 (dd, J=10.4, 6.5 Hz, 1H), 7.04-6.97 (m, 1H), 2.86 (s, 3H), (NH not observed); MS (ES+) m/z 549.6 (M+1), 551.6 (M+1).