反应详情

温度

120 °C

A mixture of 5-bromo-3-oxazolo[5,4-b]pyridin-2-yl-pyridin-2-amine (1 g, Example 9 starting material), 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol (0.794 g), bis(triphenylphosphine) palladium(II) chloride (0.121 g) and caesium fluoride (1.56 g) in methanol (17 ml) was heated at 120° C. for 20 min in a microwave oven. The reaction was repeated and the reaction mixtures were combined. The resulting mixture was concentrated, then diluted with water (400 ml) and stirred for 30 min. The resulting solid was filtered, washed with water (4×150 ml), dried, washed with diethyl ether (4×150 ml) and dried overnight to give 4-(6-amino-5-oxazolo[5,4-b]pyridin-2-yl-3-pyridyl)phenol (12.3 g) as a solid. NMR Spectrum: (DMSOd6) 6.88 (d, 2H), 7.50-7.57 (m, 3H), 7.72 (bs, 2H), 8.28 (dd, 1H), 8.37-8.42 (m, 2H), 8.53 (d, 1H), 8.55 (bs, 1H); Mass spectrum: M+H+ 355

1. customthe reaction mixtures
2. concentrationThe resulting mixture was concentrated
3. additiondiluted with water (400 ml)
4. filtrationThe resulting solid was filtered
5. washwashed with water (4×150 ml)
6. customdried
7. washwashed with diethyl ether (4×150 ml)
8. customdried overnight