反应详情

A mixture of 3-bromo-6-fluoro-1-(phenylsulfonyl)-1H-indole (Intermediate 2; 317 mg; 0.9 mmol) and 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)pyridine (Intermediate 9; 485 mg; 1.80 mmol), Pd2 dba3 (48 mg; 0.05 mmol) and X-phos (96 mg; 0.20 mmol), and K3PO4 (954 mg; 4.5 mmol) in 1,4-dioxane (8 mL) and water (1 mL) was flushed with argonand reacted at 125° C. for 25 minutes in a microwave reactor. The reaction mixture was filtered through Celite, washed with EtOAc (50 mL), concentrated, and purified by a silica gel chromatography (petroleum ether/EtOAc=1/1) to afford 363 mg (96%) of the title compound as a yellow solid.

1. customwas flushed with argonand
2. customreacted at 125° C. for 25 minutes in a microwave reactor
3. filtrationThe reaction mixture was filtered through Celite
4. washwashed with EtOAc (50 mL)
5. concentrationconcentrated
6. custompurified by a silica gel chromatography (petroleum ether/EtOAc=1/1)