反应详情

To a solution of 300 mg (1.1 mmol) 3,5-bis(trifluoromethyl)-phenylacetic acid in 7 ml N,N-dimethylformamide were added 185 mg (1.14 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 over night at 90° C. 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 506 mg (94%) of the title compound as a light brown foam.

1. customfor the preparation of Example 23), the reaction mixture
2. temperaturewas heated over night at 90° C
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