Cesium fluoride → (S)-4-Amino-N-(3,5-dimethoxyphenyl)-6-((1-(5-methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)pyrimidine-5-carboxamide

Participants

Reaction Conditions

Reaction Steps

(S)-2-(1-Aminoethyl)-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one (200 mg, 0.75 mmol), 4-amino-6-chloro-N-(3,5-dimethoxyphenyl)pyrimidine-5-carboxamide (575 mg, 1.23 mmol), DIEA (650 μl, 3.73 mmol) and cesium fluoride (227 mg, 1.49 mmol) were suspended in tert-butanol (7 ml) and the mixture was heated overnight at 120° C. in a sealed tube. The reaction mixture was diluted with ethyl acetate and washed with water and brine. After evaporation of the solvent, the residue (720 mg, 33% purity, 58% yield) was used in the next synthetic step without further purification.

Provenance & Evidence