Potassium Phosphate, Tribasic → HCID 87054905, compound

Participants

Reaction Conditions

Reaction Steps

To a degassed mixture of 6-bromo-3-(2-fluorophenyl)pyrido[2,3-d]pyrimidin-4(3H)-one (75 mg, 0.234 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 (100 mg, 0.199 mmol) in N, N-dimethyl-formamide (5 mL) were added Pd(dppf)Cl2 (15 mg) and K3PO4 (127 mg, 0.468 mmol) under N2. The mixture was heated to 80° C. overnight. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated, and the residue was purified by prep-HPLC to give 2-(4-fluorophenyl)-5-(3-(2-fluorophenyl)-4-oxo-3,4-dihydropyrido[3,2-d]pyrimidin-6-yl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (30 mg, yield: 30%). 1H-NMR (CDCl3, 400 MHz) δ 8.22 (d, J=8.8 Hz, 1H), 8.08˜8.14 (m, 3H), 7.96˜7.99 (m, 2H), 7.65 (s, 1H), 7.47˜7.57 (m, 2H), 7.32˜7.38 (m, 2H), 7.19 (t, J=8.8 Hz, 2H), 6.47 (br s, 1H), 3.27 (s, 3H), 2.98 (d, J=4.8 Hz, 3H), 2.93 (s, 3H). MS (M+H)+: 616.

Provenance & Evidence