反应详情

Tyramine (5.52 g, 0.040 mol) in 40 ml of anhydrous DMF was treated with diisopropylethylamine (6.1 ml, 0.035 mol). After stirring at rt for 15 minutes, 2-chloro-5-ethylpyrimidine (4.25 ml, 0.035 mol) was added and the mixture heated at 80° C. for 14 hours. The solution was allowed to cool to room temperature and was partitioned between equal volumes of water and ethyl acetate. The aqueous phase was washed with ethyl acetate and the combined organic phases were dried over MgSO4 and concentrated. The residue was purified by flash chromatography eluting with 40% ethyl acetate-hexane to afford the title compound as a colorless solid (4.94 g; 58% yield).

1. temperaturethe mixture heated at 80° C. for 14 hours
2. temperatureto cool to room temperature
3. customwas partitioned between equal volumes of water and ethyl acetate
4. washThe aqueous phase was washed with ethyl acetate
5. dry with materialthe combined organic phases were dried over MgSO4
6. concentrationconcentrated
7. customThe residue was purified by flash chromatography
8. washeluting with 40% ethyl acetate-hexane