Potassium Bicarbonate → Carbonic acid 1-(5-{(4-{amino[4-methylbenzoylimino]methyl}phenylamino)-[2-fluoro-3-(2-hydroxyethoxy)-5-methoxyphenyl]methyl}-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxy)ethyl ester (1R,2R)-2-methylcyclohexyl ester

Participants

Reaction Conditions

Reaction Steps

To a mixture of 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 (230 mg) and DMF (3 mL), potassium hydrogen carbonate (113 mg) and carbonic acid 1-chloroethyl ester (1R,2R)-2-methylcyclohexyl ester (250 mg) were sequentially added, and the resulting mixture was stirred at 55° C. for 24 hours and at room temperature for another 2 days. The reaction solution was purified by reverse phase silica gel column chromatography (mixed solvent of acetonitrile-water) to obtain the captioned compound (129.2 mg).

Provenance & Evidence