(R)-N-(5-(2-amino-1-hydroxyethyl)-2-hydroxyphenyl)methanesulfonamide → Ethyl {[(4-{4-[((2R)-2-hydroxy-2-{4-hydroxy-3-[(methylsulfonyl)amino]phenyl}-ethyl)amino]-1-piperidineyl}anilino)carbonyl]amino}acetate

Participants

Reaction Steps

The title compound was prepared from {3-[4-(4-oxo-piperidine-1-yl)-phenyl]-ureido}-acetic acid ethyl ester (which was obtained in Example 366) 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 278 as a white solid; 1H NMR (300 MHz, DMSO-d6) δ 1.20 (t, J=7.1 Hz, 3H), 1.20-1.40 (m, 2H), 1.80-1.95 (m, 2H), 2.50-2.70 (m, 5H), 2.92 (s, 3H), 3.40-3.50 (m, 2H), 3.83 (d, J=5.9 Hz, 2H), 4.10 (q, J=7.1 Hz, 2H), 4.47 (dd, J=8.0, 4.3 Hz, 1H), 6.28 (t, J=5.9 Hz, 1H), 6.75-6.85 (m, 3H), 7.00 (dd, J=8.3, 2.0 Hz, 1H), 7.15-7.25 (m, 3H), 8.45 (s, 1H); MS (ES) m/z: 550.5 (MH+); HRMS Calcd. for C25H36N5O7S(MH+): 550.2330. Found: 550.2319.

Provenance & Evidence