反应详情

Compound i (445 mg, 1.18 mmol) was dissolved in DMF (7 mL) and solution of CDI (577 mg, 3.56 mmol) in DMF (3 mL) was added drop-wise at 0° C. with stirring under argon. The mixture was warmed to RT and stirred for 16 h. A solution of ethanolamine (710 μL, 11.85 mmol) in DMF (2 mL) was then added and the mixture stirred at RT for 4 h. The mixture was diluted with EtOAc, washed with H2O, brine. The organic fraction was dried (Na2SO4) and concentrated in vacuo. The residue was washed with MeOH and Et2O to afford ii (253 mg, 46%). MS: 463.00 [M+H]+.

1. stirringstirred for 16 h
2. stirringthe mixture stirred at RT for 4 h
3. washwashed with H2O, brine
4. dry with materialThe organic fraction was dried (Na2SO4)
5. concentrationconcentrated in vacuo
6. washThe residue was washed with MeOH and Et2O