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HRID 2089629作成日:2026年10月27日

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 cyclohexyl ester

https://huagongshe.com/reaction/2089629

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium BicarbonateHCID 516893—
反応物1-Chloroethyl Cyclohexyl CarbonateHCID 11229529—
反応物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]benzamideHCID 136334022—
溶媒DimethylformamideHCID 6228—
生成物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 cyclohexyl esterHCID 6747116852.9%

反応条件

温度55 °C

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, 1.0 g) and DMF (20 mL), potassium hydrogen carbonate (1.67 g) and 1-chloroethyl cyclohexyl carbonate (2.76 g) were added, and the resulting mixture was stirred at 55° C. for 26 hours. The reaction solution was filtered, and the filtrate obtained was concentrated 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 (680 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08436009B2
出典データセットuspto-grants-2013_05
ORD IDord-2b6ad9cf33da400599b25bbc2a97d622
出典メモuspto-grants-2013_05