N-{4-[4-(4-Oxo-piperidin-1-yl)-phenylsulfamoyl]-phenyl}-acetamide → N-[4-({4-[4-({(2S)-2-Hydroxy-3-[(8-hydroxy-2-oxo-1,2,3,4-tetrahydro-5-quinolinyl)oxy]propyl}amino)-1-piperidineyl]anilino}sulfonyl)phenyl]acetamide

Participants

Reaction Steps

The title compound was prepared from N-{4-[4-(4-oxo-piperidine-1-yl)-phenylsulfamoyl]-phenyl}-acetamide (which was obtained in Example 216) and 5-(3-amino-(2S)-2-hydroxy-propoxy)-8-hydroxy-3,4-dihydro-1H-quinolin-2-one (which was obtained in Example 12) according to the procedure of Example 278 as a white solid; 1H NMR (300 MHz, DMSO-d6) δ 1.20-1.40 (m, 2H), 1.75-1.90 (m, 2H), 2.05 (s, 3H), 2.39 (t, J=7.5 Hz, 2H), 2.50-2.80 (m, 5H), 2.83 (t, J=7.5 Hz, 2H), 3.40-3.55 (m, 2H), 3.70-3.85 (m, 3H), 6.44 (d, J=8.7 Hz, 1H), 6.60 (d, J=8.7 Hz, 1H), 6.76 (d, J=9.0 Hz, 2H), 6.85 (d, J=9.0 Hz, 2H), 7.58 (d, J=9.0 Hz, 2H), 7.67 (d, J=9.0 Hz, 2H), 8.72 (s, 1H), 10.27 (s, 1H); MS (ES) m/z: 623.9 (MH+); HRMS Calcd. for C31H38N5O7S(MH+): 624.2492. Found: 624.2469.

Provenance & Evidence