反应详情

温度

200 °C

To a solution of 2-amino-N-(2-hydroxy-4-methoxy-phenyl)-5-[1-(1-methyl-4-piperidyl)pyrazol-4-yl]pyridine-3-carboxamide (110 mg) in acetic acid (1.8 ml) was added TFA (1.8 ml). The clear mixture was sealed into a microwave tube. The reaction was heated to 200° C. a 300 W microwave for 20 minutes. The solvents were evaporated. The residue was trituratred in diethyl ether, dried to give a yellow solid. The solid was dissolved in DMF (1.5 ml) and two drops of a 30% aqueous ammonia solution. The precipitate was filtered, washed with Ether and dried at 50° C. for 48 h to afford 3-(6-methoxy-1,3-benzoxazol-2-yl)-5-[1-(1-methyl-4-piperidyl)pyrazol-4-yl]pyridin-2-amine (25.00 mg). NMR Spectrum: (DMSOd6) 1.93-2.12 (m, 6H), 2.22 (s, 3H), 2.94-2.91 (m, 2H), 3.86 (s, 3H), 4.07-4.16 (m, 1H), 7.03 (dd, 1H), 7.40 (d, 1H), 7.57 (bs, 2H), 7.72 (d, 1H), 7.89 (d, 1H), 8.30 (s, 1H), 8.36 (d, 1H), 8.49 (d, 1H). Mass spectrum: M+H+ 405.

1. customThe clear mixture was sealed into a microwave tube
2. customThe solvents were evaporated
3. customdried
4. customto give a yellow solid
5. filtrationThe precipitate was filtered
6. washwashed with Ether
7. customdried at 50° C. for 48 h