3,4-Dimethoxy-N-[4-(4-oxo-piperidin-1-yl)-phenyl]-benzenesulfonamide → N-{4-[4-({(2S)-2-Hydroxy-3-[(8-hydroxy-2-oxo-1,2,3,4-tetrahydro-5-quinolinyl)oxy]-propyl}amino)-1-piperidineyl]phenyl}-3,4-dimethoxybenzenesulfonamide

Participants

Reaction Steps

The title compound was prepared from 3,4-dimethoxy-N-[4-(4-oxo-piperidine-1-yl)-phenyl]-benzenesulfonamide (which was obtained in Example 242) 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), 1.80-1.95 (m, 2H), 2.39 (t, J=7.2 Hz, 2H), 2.50-2.75 (m, 5H), 2.82 (t, J=7.2 Hz, 2H), 3.45-3.55 (m, 2H), 3.63 (s, 3H), 3.72 (s, 3H), 3.70-3.85 (m, 3H), 4.91 (brs, 1H), 6.44 (d, J=8.8 Hz, 1H), 6.60 (d, J=8.8 Hz, 1H), 6.78 (d, J=9.1 Hz, 1H), 6.88 (d, J=9.1 Hz, 1H), 7.02 (d, J=8.5 Hz, 1H), 7.18 (dd, J=8.5, 2.1 Hz, 1H), 7.36 (d, J=2.1 Hz, 1H),8.72 (s, 1H), 9.17 (brs, 1H); MS (ES) m/z: 627.1 (MH+); HRMS Calcd. for C31H39N4O8S(MH+): 627.2489. Found: 627.2458.

Provenance & Evidence