反应详情

To a solution of 1-[5-hydroxymethyl-1-(3-methyl-butyl)-1H-benzoimidazol-2-ylmethyl]-3-isopropyl-1,3-dihydro-benzoimidazol-2-one (41 mg, 0.10 mmol) in DCM (1 mL) was added DAST (32 mg, 0.20 mmol) at 0° C. The final solution was stirred at ambient temperature for 12 h then washed with sat. NaHCO3 and brine. The organic layer was dried over MgSO4 and evaporated. The residue was purified by slash chromatography (hexanes:EtOAc 2:1 to 1:1) to give 32 mg (78%) of 1-[5-fluoromethyl-1-(3-methyl-butyl)-1H-benzoimidazol-2-ylmethyl]-3-isopropyl-1,3-dihydro-benzoimidazol-2-one as a white solid.

1. washthen washed with sat. NaHCO3 and brine
2. dry with materialThe organic layer was dried over MgSO4
3. customevaporated
4. customThe residue was purified by slash chromatography (hexanes:EtOAc 2:1 to 1:1)