1-Sulfonylurea → HCID 69434770, compound

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) using 3-chloro-thiophene-2-sulfonic acid amide as the coupling partner to give N-({[4-(6-amino-7-fluoro-1-oxoisoquinolin-2(1H)-yl)phenyl]amino}carbonyl)-3-chlorothiophene-2-sulfonamide. ES-MS (M+H)+=507.0, 509.0 (Cl); 1H-NMR (DMSO-d6) δ (ppm): 8.98-8.91 (bs, 1H), 8.06-7.98 (m, 1H), 7.66-7.60 (d, J=12.8 Hz, 1H), 7.48-7.40 (d, J=8.8 Hz, 2H), 7.30-7.25 (d, J=8.8 Hz, 2H), 7.24-7.20 (m, 1H), 7.24-7.18 (d, J=7.3 Hz, 1H), 6.72-6.66 (d, J=8.4 Hz, 1H), 6.56-6.48 (bs, 1H), 6.50-6.46 (d, J=7.3 Hz, 1H), 2.82-2.75 (s, 3H).

Provenance & Evidence