反应详情

Using general procedure E, 3-{[[1-(3-amino-1-methyl-propyl)-piperidin-4-yl]-(1H-indol-5-yl)-amino]-methyl}-4-fluoro-benzonitrile (see EXAMPLE 244) (45 mg, 0.11 mmol) and 4,6-dimethyl-pyrimidine-5-carboxylic acid (20 mg, 0.13 mmol) afforded COMPOUND 245 as a white solid (35 mg, 60%). 1H NMR (CDCl3) δ 0.88-1.25 (m, 5H), 1.54-1.64 (m, 1H), 1.76-1.92 (m, 3H), 2.13-2.20 (m, 1H), 2.51 (s, 6H), 2.51-2.57 (m, 1H), 2.69-2.84 (m, 3H), 3.31-3.37 (m, 2H), 3.82-3.85 (m, 1H), 3.98 (s, 2H), 6.39 (s, 1H), 6.72 (d, 1H, J=8.6 Hz), 7.00 (s, 1H), 7.08-7.14 (m, 2H), 7.21 (d, 1H, J=8.6 Hz), 7.43-7.45 (m, 1H), 7.65 (d, 1H, J=6.4 Hz), 8.02 (s, 1H), 8.50 (br s, 1H), 8.83 (s, 1H). 13C NMR (CDCl3) δ 13.74, 22.36, 29.89, 30.88, 31.26, 40.33, 43.81, 44.17, 52.34, 60.54, 60.81, 102.63, 108.63, 110.70, 111.94, 116.61, 116.72, 116.92, 118.91, 125.26, 128.77, 131.10, 132.79, 134.50, 157.98, 163.38. ES-MS m/z 554 (M+H). Anal. Calcd. for C32H36N7OF.0.2CH2Cl2: C, 67.77; H, 6.43; N, 17.18; F, 3.33. Found: C, 68.16; H, 6.64; N, 16.86; F, 3.05.