反应详情

N2-(4-(Oxazol-5-yl)phenyl)-N4-((tetrahydro-2H-pyran-4-yl)methyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-2,4-diamine (134 mg, 0.33 mmol, example 85a) was dissolved in methanol (3 mL). Acetic acid (0.019 mL, 0.33 mmol) was added followed by glycoaldehyde (19.80 mg, 0.33 mmol). The reaction mixture was stirred at room temperature for 15 minutes and MP—CNBH3 was added. The reaction mixture was stirred overnight, the MP—CNBH3 was filtered off, the solvent was evaporated under reduced pressure, the crude was purified twice by HPLC yielding 2-(2-(4-(oxazol-5-yl)phenylamino)-4-((tetrahydro-2H-pyran-4-yl)methylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanol (38.0 mg, 22.58%) as acetate salt. MS (ES+) m/z 451.3 (M+H)+

1. additionMP—CNBH3 was added
2. stirringThe reaction mixture was stirred overnight
3. filtrationthe MP—CNBH3 was filtered off
4. customthe solvent was evaporated under reduced pressure
5. customthe crude was purified twice by HPLC