反应详情

温度

100 °C

2-amino-5-bromo-pyridine-3-carboxylic acid (797 mg) and 2-amino-5-fluoro-pyridin-3-ol, hydrochloride (400 mg) powders were mixed together and the resulting mixture was portionwise added in trimethylsilyl polyphosphate (4.5 g) stirred at 100° C. The mixture was stirred at 140° C. overnight. After cooling, water (20 ml) was added. The resulting precipitate was collected by filtration, washed with a 2N aqueous solution of HCl and water. The resulting solid was triturated in Ethyl acetate, collected by filtration to afford 5-bromo-3-(6-fluorooxazolo[4,5-b]pyridin-2-yl)pyridin-2-amine (150 mg). NMR Spectrum: (DMSO-d6) 7.10 (bs, 2H), 7.66 (dd, 1H), 8.31 (d, 1H), 8.39 (d, 1H), 8.49 (dd, 1H); Mass spectrum: M+H+ 309-311.

1. stirringThe mixture was stirred at 140° C. overnight
2. temperatureAfter cooling
3. filtrationThe resulting precipitate was collected by filtration
4. washwashed with a 2N aqueous solution of HCl and water
5. customThe resulting solid was triturated in Ethyl acetate
6. filtrationcollected by filtration