反应详情

温度

100 °C

To a solution of N-(6-bromo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)cyclo-propanecarboxamide (41 mg, 0.1 mmol) in t-BuOH (1.5 mL) were added 3-amino-4-methyl-N-(3-(trifluoromethyl)-phenyl)benzamide (29 mg, 0.1 mmol) and K2CO3 (42 mg, 0.3 mmol). The reaction mixture was degassed for 10 minutes. To a mixture were added Pd2(dba)3 (6.0 mg) and t-Bu-X-phos (4 mg). The reaction mixture was heated at 100° C. until it was complete as monitored by LC-MS. Then the resulting mixture was filtered through a pad of celite and eluted with dichloromethane. The to solvent was removed by rotavapor and the crude residue was purified by flash chromatography with methylene chloride-methanol to afford the title product (25 mg, 40%), MS (ESI) m/z 624 (M+H)+.

1. customThe reaction mixture was degassed for 10 minutes
2. additionTo a mixture were added Pd2(dba)3 (6.0 mg) and t-Bu-X-phos (4 mg)
3. filtrationThen the resulting mixture was filtered through a pad of celite
4. washeluted with dichloromethane
5. customThe to solvent was removed by rotavapor
6. customthe crude residue was purified by flash chromatography with methylene chloride-methanol