反应详情

To a solution of the N-(4-chlorophenyl)piperidine-4-amine (400.0 mg, 1.9 mmol) obtained in step 2 in acetonitrile were added lithium perchlorate (134.1 mg, 1.3 mmol) and 1-(((2R,3R)-2-(2,4-difluorophenyl)-3-methyloxiran-2-yl)methyl)-1H-1,2,4-triazole (158.9 mg, 0.6 mmol), followed by irradiating microwaves onto the solution at 150° C. for 30 min. After removal of the solvent, the reaction mixture was diluted in ethyl acetate and washed with distilled water and saline to separate an organic solvent layer. The organic solvent layer was dried over anhydrous magnesium sulfate and concentrated in a vacuum. Isolation and purification of the concentrate through silica gel chromatography afforded the title compound (yield 31%).

1. customby irradiating microwaves onto the solution at 150° C. for 30 min
2. customAfter removal of the solvent
3. additionthe reaction mixture was diluted in ethyl acetate
4. washwashed with distilled water and saline
5. customto separate an organic solvent layer
6. dry with materialThe organic solvent layer was dried over anhydrous magnesium sulfate
7. concentrationconcentrated in a vacuum
8. customIsolation and purification of the
9. concentrationconcentrate through silica gel chromatography