反应详情

The title compound was synthesized from N-((1R,2R)-2-(hydroxymethyl)cyclohexyl)-6-(trifluoromethyl)pyridine-3-sulfonamide (50 mg, 0.15 mmol), cesium carbonate (72 mg, 0.22 mmol), and 3-(4-(bromomethyl)-2,5-difluorophenyl)-1,2,4-oxadiazole (50 mg, 0.18 mmol) according to the procedure described for 4-chloro-N-(2,3-difluoro-4-(oxazol-2-yl)benzyl)-N-((1R,2R)-2-(hydroxymethyl)cyclohexyl)benzenesulfonamide (Example 20) to give N-(2,5-difluoro-4-(1,2,4-oxadiazol-3-yl)benzyl)-N-(1R,2R)-2-(hydroxymethyl)cyclohexyl)-6-(trifluoromethyl)pyridine-3-sulfonamide (28 mg, 35%). 1H NMR (400 MHz, CDCl3) δ ppm 9.08 (d, J=2.01 Hz, 1H), 8.82 (s, 1H), 8.25 (dd, J=8.31, 2.01 Hz, 1H), 7.81 (d, J=8.31 Hz, 1H), 7.74 (dd, J=9.82, 5.54 Hz, 1H), 7.55 (dd, J=10.20, 5.92 Hz, 1H), 4.53 (d, J=15.50 Hz, 1H), 4.47 (d, J=15.60 Hz, 1H), 3.70-3.84 (m, 1H), 3.57 (dd, J=11.71, 2.90 Hz, 1H), 321 (d, J=11.58 Hz, 1H), 1.63-1.81 (m, 3H), 1.43-1.56 (m, 2H), 1.33-1.41 (m, 1H), 1.16-1.31 (m, 2H), 1.05-1.14 (m, 1H). Analytical HPLC R.T=21.66. HRMS [M+H]+ calc'd 533.1282, found 533.1277.