3-Hydroxyazetidine → 1-(4-{5-[1-(2-fluorophenyl)-5-pyridin-4-yl-1H-1,2,3-triazol-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)azetidin-3-ol

関与物質

反応手順

The title compound was prepared following the procedure described for Example 94, but starting from 4-(5-(1-(2-fluorophenyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-3-yl)benzaldehyde, obtained as described in Example 113, Step 1, (100 mg; 0.24 mmol) and 3-azetidinol (35.4 mg; 0.48 mmol) to give Example 135 as a white solid. 1H NMR: (DMSO-d6, 400 MHz) δ 8.75 (2H, dd, J=4.7, 1.5 Hz), 7.97-7.87 (3H, m), 7.76-7.69 (1H, m), 7.61 (2H, dd, J=4.7, 1.6 Hz), 7.57-7.47 (4H, m), 5.35 (1H, d, J=6.4 Hz), 4.27-4.19 (1H, m), 3.67 (2H, s), 3.55 (2H, dd, J=7.4, 5.8 Hz), 2.83 (2H, t, J=6.6 Hz). LC/MS (Method C): 470 (M+H)+. HPLC (Method E) Rt 2.13 min (Purity: 98.2%).

情報源と証拠