反应详情

To a solution of 266 mg (1.2 mmol) 3-fluoro-5-trifluoromethyl-phenylacetic acid in 7 ml N,N-dimethylformamide were added 195 mg (1.2 mmol) 1,1′-carbonyl-diimidazole and the solution was stirred for 30 min at room temperature. After addition of 283 mg (1 mmol) of methyl-(6-morpholin-4-yl-4-tolyl-pyridin-3-yl)-amine (as described in step f) for the preparation of Example 23), the reaction mixture was heated at 90° C. for 6 h. After cooling to room temperature, the solvent was removed in vacuo and the residue was re-dissolved in 30 ml ethyl acetate. The organic phase was washed with water (2×30 ml), brine, dried (magnesium sulfate) and evaporated. Flash chromatography gave 432 mg (88%) of the title compound as a light yellow foam.

1. customfor the preparation of Example 23), the reaction mixture
2. temperaturewas heated at 90° C. for 6 h
3. temperatureAfter cooling to room temperature
4. customthe solvent was removed in vacuo
5. dissolutionthe residue was re-dissolved in 30 ml ethyl acetate
6. washThe organic phase was washed with water (2×30 ml), brine
7. dry with materialdried (magnesium sulfate)
8. customevaporated