2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-3-phenyl-propionic acid → 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-3-phenyl-propionamide

Participants

Reaction Steps

Using the method described in Example 17 from 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-3-phenyl-propionic acid (Intermediate 30) and 1-(3-amino-pyrazol-1-yl)-2-methyl-propan-2-ol (Intermediate 1) afforded 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-3-phenyl-propionamide was obtained as a white solid (0.26 g, 34%); ES+-HRMS m/e calcd for C26H25N5O4F2 [M+H+] 510.1948 found 510.1949. 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.06 (s, 3H) 1.07 (s, 3H) 3.35-3.56 (m, 2H) 3.91 (s, 2H) 4.67 (s, 1H) 5.81 (dd, J=10.7, 4.9 Hz, 1H) 5.92 (d, J=3.0 Hz, 1H) 6.44 (d, J=2.3 Hz, 1H) 7.10-7.20 (m, 1H) 7.24 (t, J=7.1 Hz, 2H) 7.29 (d, J=7.1 Hz, 2H) 7.32-7.40 (m, 2H) 7.40-7.50 (m, 1H) 7.55 (d, J=2.3 Hz, 1H) 8.24 (d, J=3.0 Hz, 1H) 11.00 (s, 1H).

Provenance & Evidence