Potassium Phosphate, Tribasic → HCID 118116489, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of N-(2-(6-(5-bromo-1-methyl-2-oxo-1,2-dihydropyridin-3-ylamino)pyridin-2-yloxy)ethyl)-N-methylacrylamide 112e (100 mg, 0.25 mmol), (4-fluoro-2-{6-oxo-8-thia-4,5-diazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3-triene-5-yl}-6-(tetra-methyl-1,3,2-dioxaborolan-2-yl)phenyl)methyl acetate 108c (187 mg, 0.375 mmol), Pd(dppf)Cl2 (19 mg, 0.025 mmol) and K3PO4 (133 mg, 0.625 mmol) in acetonitrile (5 mL) and water (0.5 mL) was stirred at 90° C. for 6 h under N2. The mixture was filtered and the filtrate was concentrated. The residue was purified by prep-TLC (PE/EA=1/4) to give N-[2-[[6-[[5-[5-fluoro-2-(acetoxymethyl)-3-(4-oxo-6,7,8,9-tetrahydrobenzothiopheno[2,3-d]pyridazin-3-yl)phenyl]-1-methyl-2-oxo-3-pyridyl]amino]-2-pyridyl]oxy]ethyl]-N-methyl-prop-2-enamide 113a (100 mg, 57%) as light yellow solid. MS-ESI: [M+H]+ 699.2

Provenance & Evidence