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 di-tert-butyl (5-{5-chloro-2-[2-chloro-5-fluoro-4-(1,3-thiazol-4-ylsulfamoyl)phenoxy]phenyl}-1,2-benzoxazol-3-yl)imidodicarbonate, 4-(2-(3-aminobenzo[d]isoxazol-5-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide was obtained as an off-white solid in 83% yield (0.230 g) after trituration in diethyl ether (10 mL): 1H NMR (300 MHz, DMSO-d6) δ11.36 (s, 1H), 8.86-8.84 (m, 1H), 7.97 (s, 1H), 7.81 (d, J=7.1 Hz, 1H), 7.65-7.59 (m, 2H), 7.54 (dd, J=8.6, 2.0 Hz, 1H), 7.42 (d, J=8.7 Hz, 1H), 7.31 (d, J=8.7 Hz, 1H), 7.03-7.00 (m, 1H), 6.95 (d, J=10.8 Hz, 1H), 6.45 (br s, 2H); MS (ES+) m/z 550.7 (M+1), 552.7 (M+1).