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 (40 mg, 0.09 mmol, Example 1) was dissolved in methanol (0.5 mL) and dichloromethane (3 mL). Triethylamine (0.013 mL, 0.09 mmol) was added followed by methoxyacetyl chloride (8.55 μL, 0.09 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 few drops of 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)-2-methoxyethanone (8.4 mg, 16.96%). HPLC, ms detection: (ESI) (M+1) m/z 501;

1. customthe solvent was evaporated under reduced pressure
2. dissolutionThe crude was dissolved in few drops of dimethylformamide and acetonitrile
3. filtrationfiltered
4. custompurified by preparative HPLC