反应详情

To a solution of 1,5-dichloro-9-fluorobenzo[c]-2,6-naphthytidine (Example 1, Step 5) (500 mg, 1.87 mmol) and methyl 3-amino-4-methylbenzoate (340 mg, 2.06 mmol) in THF (9.3 mL) was added sodium tert-butoxide (396 mg, 4.12 mmol). The reaction stirred at room temperature for ten minutes and was then quenched by the addition of sat. aq. NaHCO3 solution. The mixture was extracted with EtOAc and the extracts were washed with brine, dried over MgSO4 and concentrated in vacuo. Purification by silica gel column chromatography (0-30% EtOAc/heptane) afforded the title compound.

1. customwas then quenched by the addition of sat. aq. NaHCO3 solution
2. extractionThe mixture was extracted with EtOAc
3. washthe extracts were washed with brine
4. dry with materialdried over MgSO4
5. concentrationconcentrated in vacuo
6. customPurification by silica gel column chromatography (0-30% EtOAc/heptane)