反应详情

To a mixed solvent of dimethylformamide (8 mL) and pyridine (0.47 mL) were added 3-amino-5-tert-butylpyrazole (810 mg), N-methylindol-5-boronic acid (780 mg), copper (II) acetate (790 mg) and molecular sieves (400 mg). The reaction mixture was stirred overnight at room temperature. The reaction mixture was added with 10% aqueous ammonia and filtered through Celite®. The filtrate was added with ethyl acetate and separated. The obtained organic layer was washed with a saturated sodium chloride aqueous solution and dried over anhydrous sodium sulfate. The obtained residue was purified on silica gel column chromatography (hexane:ethyl acetate=7:3→1:1→1:4) to give the titled compound (577 mg) having the following physical data.

1. filtrationfiltered through Celite®
2. additionThe filtrate was added with ethyl acetate
3. customseparated
4. washThe obtained organic layer was washed with a saturated sodium chloride aqueous solution
5. dry with materialdried over anhydrous sodium sulfate
6. customThe obtained residue was purified on silica gel column chromatography (hexane:ethyl acetate=7:3→1:1→1:4)