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

関与物質

反応条件

反応手順

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]benzamide (Example 1a, 150 mg) and DMF (3 mL), potassium hydrogen carbonate (150 mg) and carbonic acid 1-chloroethyl ester (R)-1-methylbutyl ester (150 mg) were sequentially added, and the resulting mixture was stirred at 55° C. for 18 hours. The reaction mixture was purified by reverse phase silica gel column chromatography (mixed solvent of acetonitrile-water) to obtain the captioned compound (130 mg).

情報源と証拠