反应详情

A solution of N-(tert-butoxycarbonyl)-L-aspartic acid 1-benzyl ester (1 g) and piperidine (0.32 mL) in acetonitrile (15 mL) was allowed to react with N-methylmorpholine (0.42 mL) and TBTU (1.2 g) for 6 hr at room temperature. The solvent was removed and the residue, dissolved in EtOAc, was sequentially washed with 2% aqueous hydrochloric acid, saturated aq. NaHCO3 and brine. After drying (Na2SO4) and rotoevaporation, the resulting yellowish oil was purified by flash chromatography over silica to obtain N-(tert-butoxycarbonyl)-L-aspartic acid 1-benzyl ester-4-piperidinamide (900 mg) as a colorless oil.

1. customThe solvent was removed
2. dissolutionthe residue, dissolved in EtOAc
3. washwas sequentially washed with 2% aqueous hydrochloric acid, saturated aq. NaHCO3 and brine
4. dry with materialAfter drying (Na2SO4) and rotoevaporation
5. customthe resulting yellowish oil was purified by flash chromatography over silica