反应详情

1-(4-(2-Methyl-1H-imidazol-1-yl)phenyl)guanidine (224 mg, 1.04 mmol), tert-butyl 4-oxo-3-(2-phenylacetyl)piperidine-1-carboxylate (330 mg, 1.04 mmol) and sodium ethoxide (70.8 mg, 1.04 mmol) in ethanol (5 mL) were heated to 110° C. in a microwave reactor for 1 h 20 min. The reaction was allowed to reach room temperature and the solvent was evaporated under reduced pressure. The crude was dissolved in ethyl acetate and washed with water. The organic phase was dried under MgSO4 and the solvent evaporated under reduced pressure yielding tert-butyl 4-benzyl-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (280 mg, 54.2%) which was used in the subsequent step as such.

1. customto reach room temperature
2. customthe solvent was evaporated under reduced pressure
3. dissolutionThe crude was dissolved in ethyl acetate
4. washwashed with water
5. customThe organic phase was dried under MgSO4
6. customthe solvent evaporated under reduced pressure