4-((2S)-3-Amino-2-hydroxy-propoxy)-phenol → N-[4-(4-{[(2S)-2-Hydroxy-3-(4-hydroxyphenoxy)propyl]amino}-1-piperidineyl)phenyl]-5-(2-pyridinyl)-2-thiophenesulfonamide

Participants

Reaction Steps

The title compound was prepared from 5-pyridin-2-yl-thiophene-2-sulfonic acid [4-(4-oxo-piperidin-1-yl)-phenyl]-amide (which was obtained in Example 227) and 4-((2S)-3-amino-2-hydroxy-propoxy)-phenol (which was obtained in Example 5) according to the procedure of Example 278 as an off-white solid; 1H NMR (300 MHz, DMSO-d6) δ 1.20–1.40 (m, 2 H), 1.80–1.90 (m, 2 H), 2.40–2.80 (m, 5 H), 3.50–3.60 (m, 2 H), 3.70–3.90 (m, 3 H), 4.99 (brs, 1 H), 6.66 (d, J=8.0 Hz, 2 H), 6.75 (d, J=8.0 Hz, 2 H), 6.83 (d, J=9.0 Hz, 2 H), 6.96 (d, J=9.0 Hz, 1 H), 7.36 (dd, J=4.4, 1.7 Hz, 1 H), 7.41 (d, J=4.0 Hz, 1 H), 7.76 (d, J=4.0 Hz, 1 H), 7.88 (dd, J=8.0, 1.7 Hz, 1 H), 8.00(d, J=8.0 Hz, 1 H), 8.54 (d, J=4.4 Hz, 1 H), 8.89 (s, 1 H); MS (ES) m/z: 580.9 (MH+); HRMS Calcd. for C29H33N4O5S2 (MH+): 581.1892. Found: 581.1910.

Provenance & Evidence