反应详情

In an analogous manner to the stepwise sequence outlined in Intermediate 70, starting from 5-iodo-2-(tetrahydro-pyran-2-yl)-2H-pyridazin-3-one (Intermediate 70, step 2) and 2-methyl-5-trifluoromethyl-2,4-dihydro-pyrazol-3-one and alkylating with 2-bromo-3-cyclopentyl-propionic acid methyl ester (Intermediate 10) afforded 3-cyclopentyl-2-[4-(2-methyl-5-trifluoromethyl-2H-pyrazol-3-yloxy)-6-oxo-6H-pyridazin-1-yl]-propionic acid as a white solid (4.3 g, 64% for the final step); LC-MS: 401.1 (M+1)+, tR=4.39 min. Purity on HPLC: 97.0% (214 nm), 99.8% (254 nm), tR=9.36 min. 1H NMR (300 MHz, CDCl3): δ 9.00 (s, 1H), 7.91 (d, 1H), 6.46 (d, 1H, J=2.1 Hz), 6.27 (s, 1H), 5.55 (dd, 1H, J1=7.8 Hz, J2=4.2 Hz,), 3.81 (s, 3H), 2.36˜2.20 (m, 1H), 2.20˜2.05 (m, 1H), 1.78˜1.47 (m, 7H), 1.28˜1.10 (m, 2H).