反应详情

(S)-tert-Butyl 4-(1-amino-3-(4-(2-methoxypyridin-4-yl)phenyl)-1-oxopropan-2-ylcarbamoyl)tetrahydro-2H-pyran-4-ylcarbamate (Example 26, step (i), 214 mg) in dichloromethane (10 mL) was treated with Burgess' reagent (205 mg) and the mixture was stirred at room temperature for 18 h. The solvent was evaporated to give a residue that was dissolved in formic acid (2 mL) which was heated at 50° C. for 15 min. The mixture was evaporated and then methanol was added and the solvent was evaporated. The product was purified by reversed phase HPLC using methanol in 0.1% aqueous TFA as eluent. The residue was converted to the free base by elution through a PL-HCO3 MP cartridge in dichloromethane/methanol to afford the titled compound (95 mg).

1. customThe solvent was evaporated
2. customto give a residue that
3. temperaturewas heated at 50° C. for 15 min
4. customThe mixture was evaporated
5. additionmethanol was added
6. customthe solvent was evaporated
7. customThe product was purified by reversed phase
8. washThe residue was converted to the free base by elution through a PL-HCO3 MP cartridge in dichloromethane/methanol