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

Participants

Reaction Steps

The title compound was prepared from 5-(5-trifluoromethyl-pyridine-2-sulfonyl)-thiophene-2-sulfonic acid [4-(4-oxo-piperidin-1-yl)-phenyl]-amide (which was obtained in Example 229) and 4-((2S)-3-amino-2-hydroxy-propoxyl)-phenol (which was obtained in Example 5) according to the procedure of Example 278 as a grey solid; 1H NMR (300 MHz, DMSO-d6) δ 1.25–1.45 (m, 2 H), 1.70–1.95 (m, 2 H), 2.50–2.85 (m, 5 H), 3.54 (brd, J=12.4 Hz, 2 H), 3.65–3.95 (m, 3 H), 6.60–6.90 (m, 8 H), 7.92 (d, J=1.6 Hz, 1 H), 8.41 (d, J=8.3 Hz, 1 H), 8.48 (d, J=1.6 Hz, 1 H), 8.61 (dd, J=8.3, 2.0 Hz, 1 H), 8.89 (s, 1 H), 9.23 (s, 1 H); MS (ES) m/z: 713.1 (MH+); HRMS Calcd. for C30H32F3N4O7S3 (MH+): 713.1385. Found: 713.1407.

Provenance & Evidence