反应详情

Crude methyl 2-{2-[benzyl(tert-butoxycarbonyl)amino]ethyl}-5,6-dihydroxypyrimidine-4-carboxylate (prepared as described in Step 2) was dissolved in methanol and treated with p-fluorobenzylamine (2.5 equivalents) at 80° C. for 12 hours. The mixture was then cooled to room temperature, volatiles were evaporated and the residue was poured in EtOAc and washed 0.5 N HCl and brine. The organic phase was dried (Na2SO4), filtered and concentrated to a brown solid residue. MS (ES) C26H29FN4O5 requires 496. Found: 497 (M+H+).

1. customvolatiles were evaporated
2. additionthe residue was poured in EtOAc
3. washwashed 0.5 N HCl and brine
4. dry with materialThe organic phase was dried (Na2SO4)
5. filtrationfiltered
6. concentrationconcentrated to a brown solid residue