反应详情

温度

50 °C

To a solution of 8 g of 1-tert-butoxycarbonyl-4-methyl-5-nitrobenzimidazole in 40 mL of methanol and 400 mL of ethyl acetate are added 500 mg of palladium-on-carbon (10%) and 7.27 g of ammonium formate. The mixture is stirred at 50° C. for 2 hours, then filtered on Celite, with a methanol wash of the solids. The filtrate is rotary evaporated and the residue partitioned between water and ethyl acetate. The organic layer is washed with saturated ammonium chloride, dried over magnesium sulfate, filtered and rotary evaporated to afford pure 5-amino-1-tert-butoxycarbonyl-4-methylbenzimidazole as an off-white solid.

1. filtrationfiltered on Celite, with a methanol
2. washwash of the solids
3. customThe filtrate is rotary evaporated
4. customthe residue partitioned between water and ethyl acetate
5. washThe organic layer is washed with saturated ammonium chloride
6. dry with materialdried over magnesium sulfate
7. filtrationfiltered
8. customrotary evaporated