反应详情

An analogous sulfonylurea coupling and de-protection procedure to that described in Example 29 was performed on [2-(4-Amino-phenyl)-7-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl]-methyl-carbamic acid tert-butyl ester (Example 9) and 3-methyl-thiophene-2-sulfonamide to give N-({[4-(6-amino-7-fluoro-1-oxoisoquinolin-2(1H)-yl)phenyl]amino}carbonyl)-3-methylthiophene-2-sulfonamide. ES-MS (M+H)+=487.1; 1H-NMR (DMSO-d6) δ (ppm): 8.96-8.92 (bs, 1H), 7.86-7.82 (d, J=5.1 Hz, 1H), 7.66-7.60 (d, J=12.4 Hz, 1H), 7.46-7.40 (m, 2H), 7.32-7.26 (m, 2H), 7.24-7.20 (d, J=7.3 Hz, 1H), 7.03-7.00 (d, J=5.1 Hz, 1H), 6.72-6.68 (d, J=8.8 Hz, 1H), 6.56-6.48 (bs, 1H), 6.50-6.46 (d, J=7.7 Hz, 1H), 2.82-2.78 (bd, J=4.8 Hz, 3H), 2.45-2.43 (s, 3H).