Potassium Phosphate, Tribasic → HCID 71295625, compound

Participants

Reaction Conditions

Reaction Steps

To a degassed solution of 2-(3-(benzyloxy)-6-chloropyridin-2-yl)-4-fluoro-1H-pyrrolo[2,3-c]pyridine (300 mg, 0.85 mmol) and 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide (387 mg, 0.77 mmol) in 1,4-dioxane (5.0 mL) was added Pd2(dba)3 (10 mg), X-Phos (10 mg) and K3PO4 (452 mg, 1.70 mmol) under N2. The mixture was heated at 100° C. for 3 hours. The reaction mixture was cooled to room temperature and filtered. The filtrate was washed with H2O, brine, dried over Na2SO4. After it was concentrated, the resulting residue was purified using column (petroleum ether:EtOAc=2:1) to provide 5-(5-(benzyloxy)-6-(4-fluoro-1H-pyrrolo[2,3-c]pyridin-2-yl)pyridin-2-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (165 mg, yield: 31%). 1H-NMR (CDCl3, 400 MHz) δ 10.73 (s, 1H), 8.49 (s, 1H), 7.99 (d, J=8.0 Hz, 2H), 7.92 (dd, J=8.0, 8.0 Hz, 2H), 7.50˜7.45 (m, 3H), 7.43˜7.40 (m, 5H), 7.16 (t, J=8.0 Hz, 2H), 6.56 (s, 1H), 5.32 (s, 12H), 3.10 (s, 3H), 2.91 (d, J=4.0 Hz, 3H), 2.80 (s, 3H). MS (M+H)+: 694.

Provenance & Evidence