反应详情

Into a round bottom flask 4-trimethylsilanylethynyl-1H-pyrrolo[2,3-b]pyridine (7, 0.250 g, 1.17 mmol), N-(2,4-difluoro-3-formyl-phenyl)-4-trifluoromethyl-benzenesulfonamide (4, 0.498 g, 1.36 mmol), and 2.0 mL of methanol were added and the suspension was stirred for 10 minutes. Potassium hydroxide (0.213 g, 3.79 mmol) was added and the reaction was stirred at room temperature for 6 hours. The reaction was poured into 25 mL of water and 25 mL of saturated ammonium chloride, then extracted with 50 mL or ethyl acetate. The organic layer was isolated and concentrated under vacuum. The residue was purified by silica gel column chromatography, eluting with a gradient of 5 to 60% ethyl acetate in hexanes. The appropriate fractions were combined and the solvents removed under vacuum to provide the desired compound (8, 0.146 g).

1. stirringthe reaction was stirred at room temperature for 6 hours
2. extractionextracted with 50 mL or ethyl acetate
3. customThe organic layer was isolated
4. concentrationconcentrated under vacuum
5. customThe residue was purified by silica gel column chromatography
6. washeluting with a gradient of 5 to 60% ethyl acetate in hexanes
7. customthe solvents removed under vacuum