反应详情

[5-(7-Amino[1,3]thiazolo[5,4-d]pyrimidin-2-yl)-1-methyl-4-phenyl-1H-imidazol-2-yl](phenyl)methyl dimethylcarbamate (Intermediate 97) (25 mg) was dissolved in THF (4 mL), TFA (0.1 mL) and water (0.1 mL) added then heated at reflux under an inert atmosphere. After 2 hours, cooled to ambient temperature, diluted with EtOAc (10 mL), washed with saturated aqueous NaHCO3 (10 mL), organic layer dried (MgSO4), filtered and concentrated in vacuo. Residue was purified by flash chromatography on silica eluting with 4% MeOH/DCM to give the title compound as a colourless foam (21 mg, 99%);

1. temperaturethen heated
2. temperatureat reflux under an inert atmosphere
3. washwashed with saturated aqueous NaHCO3 (10 mL), organic layer
4. dry with materialdried (MgSO4)
5. filtrationfiltered
6. concentrationconcentrated in vacuo
7. customResidue was purified by flash chromatography on silica eluting with 4% MeOH/DCM