反应详情

4-(4-Morpholinyl)benzyl alcohol (150 mg, 0.78 mmol) was added to a solution of phosgene in toluene (1.93 M, 1.2 mL). After 4 h, the mixture was treated with a solution of N1-(4-methoxybenzoyl)-1,2-benzenediamine (188 mg, 0.78 mmol) and pyridine (2 mL) in methylene chloride (3 mL). After 16 h, the mixture was concentrated and the residue was dissolved in EtOAc. The organic layer was washed with water (4×), brine (1×), dried with potassium carbonate, and concentrated. The residue was purified by chromatography (SiO2, 5 to 15% EtOAc in CH2Cl2), yielding 45 mg (14%) of the title compound.

1. waitAfter 16 h
2. concentrationthe mixture was concentrated
3. dissolutionthe residue was dissolved in EtOAc
4. washThe organic layer was washed with water (4×), brine (1×)
5. dry with materialdried with potassium carbonate
6. concentrationconcentrated
7. customThe residue was purified by chromatography (SiO2, 5 to 15% EtOAc in CH2Cl2)