Cesium carbonate → HCID 66742927, compound

Participants

Reaction Conditions

Reaction Steps

In a 15 mL microwave reaction vial was added a solution of 5-(2-(dimethylamino)ethoxy)pyrazin-2-amine (190 mg, 1.04 mmol, Eq: 1.00) in dioxane (7 ml) under argon. 4-bromo-6-chloro-2-methylpyridazin-3(2H)-one (303 mg, 1.36 mmol, Eq: 1.3), Cs2CO3 (1.02 g, 3.13 mmol, Eq: 3), xantphos (90.5 mg, 156 μmol, Eq: 0.15) and bis(dibenzylideneacetone)palladium (45.0 mg, 78.2 μmol, Eq: 0.075) were added and the reaction tube was heated in an oil bath at 105° C. (bath temp) for 7 hrs followed by stirring at room temperature overnight. The reaction mixture was filtered and the solid was washed with dioxane (20 mL) and DCM (5 mL). The combined filtrate and washes was concentrated. The residue was purified by LC chromatography eluting with 0-10% (10% NH4OH in MeOH) in (1/1) EtOAc/heptane to afford 339 mg (67%) of the title compound.

Provenance & Evidence