反应详情

0.3 g (8.2 mmol) of 5-bromo-6-ethyl-4-[2-(2,4-dimethylphenoxy)-propylamino]pyrimidine (according to EP-A-57 440), 0.17 g (9.8 mmol) of chloromethyl benzoate and 0.12 g (8.2 mmol) of sodium iodide in 25 ml of acetone were heated under reflux for 8 hours. After cooling, the precipitated sodium chloride was filtered off and the filtrate was concentrated. The residue was taken up in dichloromethane and washed by stirring with water. The organic phase was dried and concentrated. The residue was digested with ethyl acetate. Filtration with suction gave 0.97 g (53.3% of theory) of light-yellow crystals. mp.: 159-161° C.

1. temperatureunder reflux for 8 hours
2. temperatureAfter cooling
3. filtrationthe precipitated sodium chloride was filtered off
4. concentrationthe filtrate was concentrated
5. washwashed
6. customThe organic phase was dried
7. concentrationconcentrated
8. filtrationFiltration with suction
9. customgave 0.97 g (53.3% of theory) of light-yellow crystals