反应详情

2-((2-(4-(Oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)(phenyl)amino)ethanol (85 mg, 0.20 mmol, Example 1) was dissolved in DMF (0.5 mL) and dichloromethane (4 mL). Triethylamine (0.028 mL, 0.20 mmol) was added followed by propionyl chloride (0.021 mL, 0.24 mmol). The reaction mixture was stirred at room temperature for 2 h and the solvent was evaporated under reduced pressure. The crude was dissolved in dimethylformamide and acetonitrile, filtered and purified by preparative HPLC yielding 1-(4-((2-hydroxyethyl)(phenyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)propan-1-one (8.0 mg, 8.32%).

1. customthe solvent was evaporated under reduced pressure
2. dissolutionThe crude was dissolved in dimethylformamide
3. filtrationacetonitrile, filtered
4. custompurified by preparative HPLC