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

Participants

Reaction Steps

The title compound was prepared from methyl {[4-(4-oxo-1-piperidineyl)benzoyl]amino}acetate (which was obtained in Example 162) 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 180 as a white solid; mp >75° C. (decomposed); 1H NMR (300 MHz, DMSO-d6) δ 1.20-1.35 (m, 2H), 1.75-1.90 (m, 2H), 2.50-2.90 (m, 5H), 2.91 (s, 3H), 3.63 (s, 3H), 3.70-3.85 (m, 2H), 3.95 (d, J=5.7 Hz, 2H), 4.49 (dd, J=8.0, 4.3 Hz, 1H), 6.81 (d, J=8.2 Hz, 1H), 6.96 (d, J=8.9 Hz, 2H), 7.00 (dd, J=8.2, 2.0 Hz, 1H), 7.17 (d, J=2.0 Hz, 1H), 7.71 (d, J=8.9 Hz, 2H), 8.60 (t, J=5.8 Hz, 1H); MS (ES) m/z: 521.3 (MH+); HRMS Calcd. for C25H37N4O7S(M+): 520.2064. Found: 520.2054.

Provenance & Evidence