反应详情

温度

120 °C

A mixture of cis-4-hydroxy-N-benzyloxycarbonyl-D-proline 2-oxo-1,2-diphenylethyl ester (7.0 g) and AcONH4 (11.8 g) in AcOH was stirred at 120° C. for 1 hour. The reaction mixture was evaporated, and the residue was dissolved in EtOAc, washed with water, 3N NaOH solution, water and brine, dried (MgSO4), and evaporated in vacuo. The residue was purified by silica gal column chromatography (hexane-EtOAc, 1:1˜2:3 elution) to give first benzyl (2R, 4R)-4-acetoxy-2-(4,5-diphenyloxazol-2-yl)pyrrolidine-1-carboxylate (972.6 mg), then benzyl (2R, 4R)-2-(4,5-diphenyloxazol-2-yl)-4-hydroxypyrrolidine-1-carboxylate (5.12 g).

1. customThe reaction mixture was evaporated
2. dissolutionthe residue was dissolved in EtOAc
3. washwashed with water, 3N NaOH solution, water and brine
4. dry with materialdried (MgSO4)
5. customevaporated in vacuo
6. customThe residue was purified by silica gal column chromatography (hexane-EtOAc, 1:1˜2:3 elution)