反应详情

A solution of 4-amino-5-fluoro-1-(3-hydroxy-cyclopentyl)-1H-pyrimidin-2-one (0.346 g, 1.62 mmol) in anhydrous dimethylformamide (3 mL) was treated with dimethylformamide dimethyl acetal (3 mL). The mixture was stirred at room temperature under nitrogen for 12 hours, concentrated in vacuo, loaded on silica gel, and chromatographed on silica gel (3×7 cm SiO2, 4:1 ethyl acetate/methanol) to afford N′-[5-Fluoro-1-(3-hydroxy-cyclopentyl)-2-oxo-1,2-dihydro-pyrimidin-4-yl]-N,N-dimethyl-formamidine 30 as a milky white oil (0.361 g, 83%).

1. concentrationconcentrated in vacuo
2. customchromatographed on silica gel (3×7 cm SiO2, 4:1 ethyl acetate/methanol)