4-((2S)-3-Amino-2-hydroxy-propoxy)-1,3-dihydrobenzoimidazol-2-one → 4-{[(Hexylamino)carbonyl]amino}-N-{4-[4-({(2S)-2-hydroxy-3-[(2-oxo-2,3-dihydro-1H-benzimidazol-4-yl)oxy]propyl}amino)-1-piperidineyl]phenyl}benzenesulfonamide

Participants

Reaction Steps

The title compound was prepared from 4-(3-hexyl-ureido)-N-[4-(4-oxo-piperidin-1-yl)-phenyl]-benzenesulfonamide (which was obtained in Example 225) and (S)-4-[2-hydroxy-3-aminopropoxy]-1,3-dihydro-2H-benzimidazol-2-one (U.S. Pat. No. 5,786,356/1998) according to the procedure of Example 255 as a white solid; 1H NMR (300 MHz, DMSO-d6) δ 0.86 (t, J=6.8 Hz, 3 H), 1.20–1.60 (m, 10 H), 1.90–2.05 (m, 2 H), 2.50–3.50 (m, 9 H), 3.50–3.65 (m, 1 H), 3.95–4.05 (m, 2 H), 6.43 (t, J=5.6 Hz, 1 H), 6.58 (d, J=7.8 Hz, 1 H), 6.61 (d, J=8.2 Hz, 1 H), 6.70–6.89 (m, 5 H), 7.46(d, J=9.0 Hz, 2 H), 7.51(d, J=9.0 Hz, 2 H), 9.06 (s, 1 H), 9.60 (brs, 1 H), 10.60 (s, 1 H), 10.75 (s, 1 H); MS (ES) m/z: 680.3 (MH+); HRMS Calcd. for C34H46N7O6S (MH+): 680.3230. Found: 680.3221.

Provenance & Evidence