反应详情

4-benzyl-N-(4-(2-methyl-1H-imidazol-1-yl)phenyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-amine (75 mg, 0.19 mmol, Example 41a) was dissolved in methanol (2 mL). Acetic acid (10.83 μL, 0.19 mmol) was added followed by formaldehyde (0.014 mL, 0.19 mmol). The reaction mixture was stirred at room temperature for 15 minutes and MP-CNBH3 was added. The reaction was stirred for 1 h, the MP-CNBH3 was filtered off and the solvent was evaporated under reduced pressure. The crude was dissolved in methanol, filtered and purified by preparative HPLC yielding 4-benzyl-6-methyl-N-(4-(2-methyl-1H-imidazol-1-yl)phenyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-amine (23.00 mg, 27%).

1. additionMP-CNBH3 was added
2. stirringThe reaction was stirred for 1 h
3. filtrationthe MP-CNBH3 was filtered off
4. customthe solvent was evaporated under reduced pressure
5. dissolutionThe crude was dissolved in methanol
6. filtrationfiltered
7. custompurified by preparative HPLC