反应详情

温度

80 °C

(2-aminothiazol-4-yl)methanol (70.0 mg, 0.54 mmol) and K2CO3 (148.6 mg, 1.08 mmol) were added to a solution of 5,7-dichloro-3-methylpyrido[4,3-d]pyrimidin-4(3H)-one (123.7 mg, 0.54 mmol) in 1,4-dioxane (2.7 mL). The reaction mixture was heated at 80° C. overnight, cooled down, quenched with H2O (20 mL) and extracted with ethyl acetate (3×5 mL). The combined organic layers were washed with brine, dried over MgSO4, filtered, concentrated, and purified by silica gel chromatography (10% methanol/dichloromethane) to give 7-chloro-5-(4-(hydroxymethyl)thiazol-2-ylamino)-3-methylpyrido[4,3-d]pyrimidin-4(3H)-one as a white solid product.

1. temperaturecooled down
2. customquenched with H2O (20 mL)
3. extractionextracted with ethyl acetate (3×5 mL)
4. washThe combined organic layers were washed with brine
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated
8. custompurified by silica gel chromatography (10% methanol/dichloromethane)