反应详情

Using the method described in Example 17, 3-cyclopentyl-2-[4-(2-methanesulfonyl-phenoxy)-6-oxo-6H-pyridazin-1-yl]-propionic acid (Intermediate 48) 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-[4-(2-methanesulfonyl-phenoxy)-6-oxo-6H-pyridazin-1-yl]-propionamide as a white solid (0.74 g, 54%); ES+-HRMS m/e calcd for C26H33N5O6S [M+Na+] 566.2044 found 566.2045. 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.05 (s, 3H), 1.06 (s, 3H), 1.10 (m, 1H), 1.28-1.76 (m, 8H), 1.92 (m, 1H), 2.28 (m, 1H), 3.36 (s, 3H), 3.89 (s, 2H), 4.67 (s, 1H), 5.48 (dd, J=4.4, J=10.9 Hz, 1H), 5.96 (d, J=2.8 Hz, 1H), 6.41 (d, J=2.2 Hz, 1H), 7.53 (d, J=2.2 Hz, 1H), 7.56-7.66 (m, 2H), 7.87 (m, 1H), 8.00 (dd, Jo=8.0 Hz, Jm=1.6 Hz, 1H), 8.21 (d, J=2.8 Hz, 1H), 10.83 (s, 1H).