反应详情

Sodium hydride (60% wt in mineral oil, 26.8 mg, 0.671 mmol) was added to a solution of 4-bromo-N-((10-(5-chlorofuran-2-yl)-1,3-dimethyl-5-(4-methylthiazol-2-yl)-2,4-dioxo-2,3,4,7,8,10-hexahydro-1H-pyrimido[4′,5′:3,4]pyrrolo[2,1-c][1,4]oxazin-8-yl)methyl)butanamide (82 mg, 0.134 mmol) in THF (6711 μl). The mixture was heated at reflux for 1 hour, then cooled to room temperature and quenched with water (30 ml). The mixture was extracted with ethyl acetate (2×30 ml). The combined organic extracts were washed with brine, passed through a hydrophobic frit and evaporated under vacuum to afford the title compound as a mixture of diastereomers.

1. temperatureThe mixture was heated
2. temperatureat reflux for 1 hour
3. customquenched with water (30 ml)
4. extractionThe mixture was extracted with ethyl acetate (2×30 ml)
5. washThe combined organic extracts were washed with brine
6. customevaporated under vacuum