反应详情

Using the method described in Example 17, 3-cyclopentyl-2-[6-oxo-4-(2-piperidin-1-yl-phenoxy)-6H-pyridazin-1-yl]-propionic acid (Intermediate 52) and 1-(3-amino-pyrazol-1-yl)-2-methyl-propan-2-ol (Intermediate 1) afforded 3-cyclopentyl-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-2-[6-oxo-4-(2-piperidin-1-yl-phenoxy)-6H-pyridazin-1-yl]-propionamide as a white solid (0.79 g, 55%); ES+-HRMS m/e calcd for C30H40N6O4 [M+H+] 549.3184 found 549.3186. 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.05 (s, 3H), 1.06 (s, 3H), 1.08 (m, 1H), 1.32 (m, 1H), 1.40 (br.s., 8H), 1.49-1.71 (m, 5H), 1.93 (m, 1H), 2.31 (m, 1H), 2.89 (m, 4H), 3.89 (s, 2H), 4.67 (s, 1H), 5.52 (dd, J=3.9, J=11.4 Hz, 1H), 5.71 (d, J=2.8 Hz, 1H), 6.39 (d, J=2.3 Hz, 1H), 7.09 (m, 1H), 7.13 (dd, Jo=8.1 Hz, Jm=1.3 Hz, 1H), 7.21 (dd, Jo=7.9 Hz, Jm=1.5 Hz, 1H), 7.28 (m, 1H), 7.52 (d, J=2.3 Hz, 1H), 8.01 (d, J=2.8 Hz, 1H), 10.73 (s, 1H).