(R)-N-(5-(2-amino-1-hydroxyethyl)-2-hydroxyphenyl)methanesulfonamide → Ethyl3-[(4-{4-[((2R)-2-hydroxy-2-[4-hydroxy-3-[(methylsulfonyl)amino]phenyl}-ethyl)amino]-1-piperidinyl}benzoyl)amino]propanoate

Participants

Reaction Steps

The title compound was prepared from 3-[4-(4-oxo-piperidin-1-yl)-benzoylamino]-propionic acid ethyl ester (which was obtained in Example 158) and N-[5-((1R)-2-amino-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methanesulfonamide (which was obtained in Example 10) according to the procedure of Example 179 as a white solid; mp>95° C. (decomposed); 1H NMR (300 MHz, DMSO-d6) δ 1.17 (t, J=7.1 Hz, 3 H), 1.40–1.60 (m, 2 H), 1.90–2.10 (m, 2 H), 2.54 (t, J=7.0 Hz, 2 H), 2.70–2.95 (m, 5 H), 2.94 (s, 3 H), 3.35–3.50 (m, 2 H), 3.80–3.95 (m, 2 H), 4.05 (q, J=7.1 Hz, 2 H), 4.65–4.75 (m, 1 H), 6.88 (d, J=8.2 Hz, 1 H), 6.95 (d, J=8.9 Hz, 2 H), 7.05 (dd, J=8.2, 1.9 Hz, 1 H), 7.22 (d, J=1.9 Hz, 1 H), 7.69 (d, J=8.9 Hz, 2 H), 8.26 (t, J=5.2 Hz, 1 H); MS (ES) m/z: 549.2 (MH+); HRMS Calcd. for C26H37N4O7S (MH+): 549.2377. Found: 549.2369.

Provenance & Evidence