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) and methanesulfonyl chloride (7.23 μL, 0.09 mmol) were added and the reaction mixture was stirred at room temperature, under nitrogen atmosphere, for 3 h. The solvent was evaporated under reduced pressure, the crude dissolved in few drops of dimethylformamide and acetonitrile, filtered and purified by preparative HPLC yielding 2-((6-(methylsulfonyl)-2-(4-(oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)(phenyl)amino)ethanol (5.2 mg, 10.15%).

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