Cesium fluoride → (S)-4-Amino-N-(3-hydroxy-4-(oxazol-5-yl)phenyl)-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 (100 mg, 0.37 mmol), 4-amino-6-bromo-N-(3-hydroxy-4-(oxazol-5-yl)phenyl)pyrimidine-5-carboxamide (220 mg, 0.58 mmol), DIEA (325 μl, 1.87 mmol) and cesium fluoride (113 mg, 0.74 mmol) were suspended in tert-butanol (10 ml) and the mixture was stirred 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 was purified by reverse phase using SP1® Purification System to give 3 mg (1% yield) of the title compound as a solid. Purity 97%.

Provenance & Evidence