1-Sulfonylurea → N-({[4-(6-amino-7-fluoro-1-oxoisoquinolin-2(1H)-yl)phenyl]amino}carbonyl)-5-ethynylthiophene-2-sulfonamide

Participants

Reaction Steps

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 5-ethynylthiophene-2-sulfonamide to give N-({[4-(6-amino-7-fluoro-1-oxoisoquinolin-2(1H)-yl)phenyl]amino}carbonyl)-5-ethynylthiophene-2-sulfonamide. ES-MS (M+H)+=497.1; 1H-NMR (DMSO-d6) δ (ppm): 9.22-9.18 (bs, 1H), 7.70-7.66 (m, 1H), 7.65-7.60 (d, J=12.4 Hz, 1H), 7.48-7.42 (d, J=9.1 Hz, 2H), 7.40-7.36 (m, 1H), 7.32-7.25 (d, J=8.8 Hz, 2H), 7.24-7.18 (d, J=7.7 Hz, 1H), 6.72-6.66 (d, J=8.4 Hz, 1H), 6.58-6.48 (bs, 1H), 6.50-6.46 (d, J=7.3 Hz, 1H), 4.86-4.84 (s, 1H), 2.82-2.76 (s, 3H).

Provenance & Evidence