Cesium carbonate → 2-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-6-(5-(5-(4-hydroxy-4-methylpiperidine-1-carbonyl)pyridin-2-ylamino)-1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)benzyl acetate

Participants

Reaction Conditions

Reaction Steps

To a 10 mL microwave vial was added 6-chloro-4-(5-(4-hydroxy-4-methylpiperidine-1-carbonyl)pyridin-2-ylamino)-2-methylpyridazin-3(2H)-one (33 mg, 87.3 μmol), 2-(6-tert-butyl-8-fluoro-1-oxophthalazin-2(1H)-yl)-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acetate (56.1 mg, 114 μmol) and Cs2CO3 (99.6 mg, 306 μmol) in dioxane (5 ml) and water (0.5 ml). The yellow suspension was purged with argon and PdCl2(DPPF) (7.13 mg, 8.73 μmol) was added. The vial was capped and heated in the microwave at 125° C. for 30 min. The reaction was cooled to 25° C. and diluted with DCM. Na2SO4 was added and the mixture was filtered through celite. The filter cake was washed with DCM until clear and the yellow filtrate was conc. in vacuo to afford the title compound as a brown solid in quantitative yield. (M−H)+=708 m/e.

Provenance & Evidence