反应详情

Using the method described in Example 49, 3-cyclopentyl-2-(6-oxo-4-phenylsulfanyl-6H-pyridazin-1-yl)-propionic acid (Intermediate 95) 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-phenylsulfanyl-6H-pyridazin-1-yl)-propionamide was obtained as an off-white solid (83.5 mg, 61%); ES+-HRMS m/e calcd for C25H31N5O3S [M+H+] 482.2221 found 482.2221. 1H NMR (300 MHz, DMSO-d6) δ ppm 1.04 (br. s., 3H), 1.05 (br. s., 3H), 1.19-1.78 (m, 9H), 1.78-2.00 (m, 1H), 2.10-2.32 (m, 1H), 3.88 (s, 2H), 4.67 (s, 1H), 5.42 (dd, J=10.9, 4.2 Hz, 1H), 5.95 (d, J=2.4 Hz, 1H), 6.38 (d, J=2.4 Hz, 1H), 7.52 (d, J=2.4 Hz, 1H), 7.56-7.70 (m, 5H), 7.94 (d, J=2.4 Hz, 1H), 10.79 (s, 1H).