反应详情

(4-Morpholin-4-yl-phenyl)-(8-pyridin-3-yl-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-amine and phenyl-(8-pyridin-3-yl-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-amine were prepared from 8-pyridin-3-yl-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine (70.0 mg, 0.331 mmol) and 4-(4-bromo-phenyl)-morpholine (100.0 mg, 0.4130 mmol) in a manner analogous to Example 2d. (4-Morpholin-4-yl-phenyl)-(8-pyridin-3-yl-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-amine was isolated as a yellow solid (0.025 g, 20%). MP=226-228° C. 1H NMR (400 MHz, CDCl3, δ, ppm): 9.16 (d, J=1.9 Hz, 1H), 8.66 (dd, J=4.8, 1.4 Hz, 1H), 8.46-8.41 (m, 2H), 7.61 (dd, J=7.4, 1.1 Hz, 1H), 7.54-7.49 (m, 2H), 7.45 (dd, J=7.9, 4.8 Hz, 1H), 7.00-6.93 (m, 3H), 6.69 (s, 1H), 3.90-3.86 (m, 4H), 3.14-3.09 (m, 4H). MS=373 (MH)+. Example 7, Phenyl-(8-pyridin-3-yl-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-amine, was a byproduct of the above reaction and was isolated as a yellow solid (0.007 g, 7%). MP=211-212° C. 1H NMR (400 MHz, CDCl3, δ, ppm): 9.16 (d, J=2.1 Hz, 1H), 8.67 (dd, J=4.7, 1.4 Hz, 1H), 8.48 (d, J=6.8 Hz, 1H), 8.44 (ddd, J=7.8, 1.8, 1.8 Hz, 1H), 7.65-7.58 (m, 3H), 7.46 (dd, J=8.0, 4.8 Hz, 1H), 7.39-7.34 (m, 2H), 7.04-6.98 (m, 2H), 6.87 (s, 1H). MS=288 (MH)+.