Methyl chloroformate → methyl 4-((2-hydroxyethyl)(phenyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate

Participants

Reaction Steps

2-((2-(4-(Oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)(phenyl)amino)ethanol (80 mg, 0.19 mmol, Example 1) was dissolved in DMF (5 mL). Methyl chloroformate (0.014 mL, 0.19 mmol) was added and the reaction was stirred for 2 h. The solvent was evaporated, the crude dissolved in few drops of dimethylformamide and acetonitrile, filtered and purified by HPLC. The fractions containing the title compound were pulled together and freezed-dried overnight, yielding methyl 4-((2-hydroxyethyl)(phenyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (28.0 mg, 30.8%).

Provenance & Evidence