反应详情

To a solution of [(R)-2-benzyloxy-1-(6-fluoro-1-phenyl-1H-benzoimidazol-2-yl)ethyl]carbamic acid tert-butyl ester (0.797 g, 1.7 mmol) in DCM (9 mL) was added TFA (5 mL) and the mixture was stirred at RT for 2 h. The volatiles were removed under reduced pressure and the resulting residue partitioned between DCM and a saturated aqueous solution of NaHCO3. The two phase system was stirred for 10 min, then the organic fraction was dried (MgSO4) and concentrated in vacuo. The resulting residue was purified by column chromatography (Si—PCC, gradient 0-10% MeOH in DCM) to afford the title compound (298 mg, 49%). LCMS (Method J): RT 2.02 min [M+H]+ 362.2.

1. customThe volatiles were removed under reduced pressure
2. customthe resulting residue partitioned between DCM
3. stirringThe two phase system was stirred for 10 min
4. dry with materialthe organic fraction was dried (MgSO4)
5. concentrationconcentrated in vacuo
6. customThe resulting residue was purified by column chromatography (Si—PCC, gradient 0-10% MeOH in DCM)