Sodium Iodide → Carbonic acid 1-(5-{(R)-(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 (1S,2S)-2-fluorocyclohexyl ester

Participants

Reaction Conditions

Reaction Steps

To a mixture of N-[1-amino-1-(4-{[(R)-[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 (200 mg) and DMF (3 mL), potassium hydrogen carbonate (200 mg), carbonic acid 1-chloroethyl ester (1S,2S)-2-fluorocyclohexyl ester (200 mg), and sodium iodide (100 mg) were sequentially added, and the resulting mixture was stirred at 55° C. for 24 hours. The reaction mixture was crudely purified by NAM silica gel column chromatography (mixed solvent of ethyl acetate-methanol) to obtain the captioned compound (110 mg) as a crudely purified product.

Provenance & Evidence