反应详情

N4-Ethyl-N2-(4-(2-methyl-1H-imidazol-1-yl)phenyl)-N4-((tetrahydrofuran-2-yl)methyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-2,4-diamine (95 mg, 0.22 mmol) was dissolved in methanol (3 mL). Acetic acid (0.013 mL, 0.22 mmol) was added followed by glycoaldehyde (13.16 mg, 0.22 mmol). The reaction was stirred at room temperature for 15 minutes and sodium cyanoborohydride (13.77 mg, 0.22 mmol) was added. The reaction was stirred for 1 h, the solvent was evaporated under reduced pressure, the crude redissolved in methanol, filtered and purified twice by preparative HPLC yielding 2-(4-(ethyl((tetrahydrofuran-2-yl)methyl)amino)-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanol (7.10 mg, 6.6%).

1. stirringThe reaction was stirred for 1 h
2. customthe solvent was evaporated under reduced pressure
3. dissolutionthe crude redissolved in methanol
4. filtrationfiltered
5. custompurified twice by preparative HPLC