反应详情

温度

120 °C

7-Iodo-2-(4-methoxybenzyl)-2H-pyrazolo[4,3-b]pyridine (198 mg, 0.541 mmol), Tris(dibenzylideneacetone)dipalladium(0) (12.39 mg, 0.014 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (78 mg, 0.135 mmol), 3′-fluoro-6′-methyl-2,2′-bipyridin-4-amine (110 mg, 0.541 mmol) and sodium 2-methylpropan-2-olate (156 mg, 1.624 mmol) were combined in dioxane (5 mL). The mixture was heated at 120° C. for 2 hours then cooled and purified by preparative HPLC using a Sunfire Prep 5 μm C18, 75×30 mm column eluting with a gradient of 10-50% acetonitrile (containing 0.035% TFA) in water (containing 0.05% TFA) to afford N-(3′-fluoro-6′-methyl-2,2′-bipyridin-4-yl)-2-(4-methoxybenzyl)-2H-pyrazolo[4,3-b]pyridin-7-amine (120 mg, 50.3% yield) as a yellow solid. MS [M+H] found 441.4.

1. temperaturethen cooled
2. custompurified by preparative HPLC
3. washeluting with a gradient of 10-50% acetonitrile (containing 0.035% TFA) in water (containing 0.05% TFA)