反应详情

To a mixture of 4-(benzoxazol-2-yl)phenol (0.3 g; 1.4 mmol), N-(2-hydroxyethyl)phthalimide (0.27 g; 1.4 mmol), triphenylphosphine (0.56 g; 2.1 mmol) and THF (5 ml) is added diisopropyl azodicarboxylate (0.42 ml; 2.1 mmol). The reaction is stirred 24 hours, diluted with ethyl acetate, washed with H2O, 2N HCl, NaHCO3 and brine, dried (MgSO4) and concentrated in vacuo to dryness. The residue is purified by gradient elution column chromatography using CH2Cl2 and 1% MeOH/99% CH2Cl2 to yield N-[2-[4-(benzoxazol-2-yl)phenoxy]ethyl]phthalimide which is used directly in Step D.

1. washwashed with H2O, 2N HCl, NaHCO3 and brine
2. dry with materialdried (MgSO4)
3. concentrationconcentrated in vacuo to dryness
4. customThe residue is purified by gradient elution column chromatography