Dimethylformamide → N-[1-amino-1-(4-{[[2-fluoro-3-(2-hydroxyethoxy)-5-methoxyphenyl]-(5-oxo-1-pyrimidin-2-yl-4,5-dihydro-1H-[1,2,4]triazol-3-yl)methyl]amino}phenyl)methylidene]-4-methylbenzamide

Participants

Reaction Steps

To a mixture of 4-({[2-fluoro-3-(2-hydroxyethoxy)-5-methoxyphenyl]-(5-oxo-1-pyrimidin-2-yl-4,5-dihydro-1H-[1,2,4]triazol-3-yl)methyl}amino)benzamidine acetic acid salt (1.6 g) and DMF (120 mL), 4-methylbenzoic acid 4-nitrophenyl ester [CAS No. 15023-67-3] (815 mg) and triethylamine (1.21 mL) were added, and the resulting mixture was stirred overnight at room temperature. The solvent in the reaction solution was distilled off under reduced pressure. The residue obtained was purified by NAM silica gel column chromatography (mixed solvent of methanol-ethyl acetate) to obtain the captioned compound (1.01 g).

Provenance & Evidence