反应详情

温度

80 °C

5-(3-fluoro-4-methanesulfonyl-phenyl)-2-isocyanato-4-methyl-thiazole (88a)(0.58 mmol, 0.183 g) is dissolved in dioxane (5 ml) and treated with 2-aminoethanol (0.64 mmol, 0.039 ml) under argon. The reaction mixture is stirred and heated to 80° C. for 1 hour. The solvent is then removed and the residue dissolved in EtOAc and washed with water (2×20 ml) followed by brine (20 ml) and dried over MgSO4. After filtration, the solvent is removed in vacuo and the residue purified by chromatography on silica eluting with ethyl acetate—methanol (9:1) to give the title compound.

1. customThe solvent is then removed
2. dissolutionthe residue dissolved in EtOAc
3. washwashed with water (2×20 ml)
4. dry with materialdried over MgSO4
5. filtrationAfter filtration
6. customthe solvent is removed in vacuo
7. customthe residue purified by chromatography on silica eluting with ethyl acetate—methanol (9:1)