Potassium Phosphate, Tribasic → (4-(5-(6-(2-acrylamidoethoxyl)pyridin-2-ylamino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)pyridin-3-yl)methyl acetate

Participants

Reaction Conditions

Reaction Steps

A mixture of 104c (256 mg, 0.62 mmol), 3-(6-(2-aminoethoxyl)pyridin-2-ylamino)-5-bromo-1-methylpyridin-2(1H)-one hydrochloride 103b (120 mg, 0.31 mmol), Pd(dppf)Cl2 (47 mg, 0.062 mmol) and K3PO4 (131 mg, 0.62 mmol) in acetonitrile (2 mL) and water (0.2 mL) was stirred at 90° C. for 3 h under N2. The mixture was filtered and the filtrate was concentrated. The residue was washed with petroleum ether, PE to give 104d (160 mg) as brown solid. This material was used for the next step directly.

Provenance & Evidence