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

Participants

Reaction Steps

The title compound was prepared from {4-[4-(4-oxo-piperidine-1-yl)-phenylsulfamoyl]-phenoxy}-acetic acid methyl ester (which was obtained in Example 232) 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 an off-white solid; 1H NMR (300 MHz, DMSO-d6) δ 1.20-1.40 (m, 2H), 1.75-1.90 (m, 2H), 2.50-2.80 (m, 5H), 2.92 (s, 3H), 3.65-3.75 (m, 2H), 3.67 (s, 3H), 4.47 (dd, J=8.0, 4.1 Hz, 1H), 4.87 (s, 2H), 6.50-6.90 (m, 8H), 7.17 (d, J=1.8 Hz, 1H), 7.59 (d, J=8.9 Hz, 2H); MS (ES) m/z: 649.0 (MH+); HRMS Calcd. for C29H37N4O9S2 (MH+): 649.2004. Found: 649.2014.

Provenance & Evidence