Реакция #300

ord-3c36e457f5e64b5b9130db89ea6a541e

Растворители

Условия реакции

Температура
100°CELSIUS

Методика

pyridin-3-amine (95 mg, 1.01 mmol), 2,4-dichloropyridine (0.151 mL, 1.01 mmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (70.4 mg, 0.12 mmol) and cesium carbonate (660 mg, 2.03 mmol) were stirred in dioxane (5 mL). The mixture was purged with nitrogen for 10 minutes. Palladium(II) acetate (22.76 mg, 0.10 mmol) was added and the mixture heated at 100 °C for 2h. The mixture was cooled, filtered and concentrated. The crude product was purified by flash silica chromatography, eluting gradient 5-45% EtOAc in isohexane. Fractions were evaporated to dryness and purified by flash silica chromatography, eluting at 35% EtOAc in isohexane to afford 4-chloro-N-(pyridin-3-yl)pyridin-2-amine (107 mg, 51.5 %) as a cream powder.

Источник

750 AstraZeneca ELN dataset