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 (50 mg, 0.12 mmol, Example 1) was dissolved in DMF (3 mL). Cyclopropanecarbonyl chloride (10.59 μL, 0.12 mmol) was added and the reaction was stirred at room temperature for 4 h. An extra equivalent of cyclopropanecarbonyl chloride was added and the reaction was stirred for 2 h. The solvent was evaporated, the crude dissolved in few drops dimethylformamide and acetonitrile, filtered and purified by preparative HPLC yielding cyclopropyl(4-((2-hydroxyethyl)(phenyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)methanone (1.8 mg, 2.96%).

1. stirringthe reaction was stirred for 2 h
2. customThe solvent was evaporated
3. dissolutionthe crude dissolved in few drops dimethylformamide and acetonitrile
4. filtrationfiltered
5. custompurified by preparative HPLC