反应详情

温度

120 °C

A mixture of 2-methoxy-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol (90 mg), 5-bromo-3-oxazolo[4,5-b]pyridin-2-yl-pyridin-2-amine (100 mg), caesium fluoride (0.038 g) and bis(triphenylphosphine) palladium chloride (12.06 mg) were suspended in methanol (2 ml) and sealed into a microwave tube. The reaction was degassed, purged with nitrogen and heated to 120° C. over a period of 20 minutes in the microwave reactor. The solvent was removed; the residue was diluted with water (20 ml) and stirred for 30 min. The mixture was filtered, washed with water (3×10 ml), dried; and washed with diethyl ether (4×15 ml) and dichloromethane/diethyl ether (10 ml) and dried overnight to give 4-(6-amino-5-(oxazolo[4,5-b]pyridin-2-yl)pyridin-3-yl)-2-methoxyphenol (100 mg); NMR Spectrum: (DMSOd6) 3.88 (s, 3H), 6.87 (d, 1H), 7.09 (dd, 1H), 7.24 (d, 1H), 7.48 (dd, 1H), 7.73 (bs, 2H), 8.25 (dd, 1H), 8.46 (d, 1H), 8.55 (dd, 1H), 8.60 (d, 1H), 9.09 (s, 1H); Mass spectrum: M+H+ 335.

1. customsealed into a microwave tube
2. customThe reaction was degassed
3. custompurged with nitrogen
4. customThe solvent was removed
5. additionthe residue was diluted with water (20 ml)
6. filtrationThe mixture was filtered
7. washwashed with water (3×10 ml)
8. customdried
9. washand washed with diethyl ether (4×15 ml) and dichloromethane/diethyl ether (10 ml)
10. customdried overnight