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HRID 11718作成日:2026年10月26日

Potassium Iodide → 4-(5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-pyridin-3-ylamino)-butyric acid ethyl ester

https://huagongshe.com/reaction/11718

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium IodideHCID 4875—
反応物Ethyl 4-bromobutyrateHCID 76300—
反応物Butanoic acid, 2-bromo-, ethyl esterHCID 79039—
反応物Sodium BicarbonateHCID 516892—
反応物2-(3-Amino-5-chloro-pyridin-2-yloxy)-1-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-ethanoneHCID 69655590—
溶媒EthanolHCID 702—
生成物4-(5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-pyridin-3-ylamino)-butyric acid ethyl esterHCID 6965597136.3%

反応条件

温度70 °C

反応手順

To a solution of 2-(3-amino-5-chloro-pyridin-2-yloxy)-1-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-ethanone (0.072 g, 0.18 mmol) in ethanol (1 mL) was added 4-bromo-butyric acid ethyl ester (0.030 mL, 0.21 mmol), sodium bicarbonate (0.031 g, 0.37 mmol) and potassium iodide (˜0.030 g). The resulting solution was stirred at 70° C. for 18 hours. Additional bromo-butyric acid ethyl ester (0.030 mL, 0.21 mmol) was added and the reaction was stirred at 70° C. for 18 hours. The reaction was cooled, concentrated in vacuo and purified via flash chromatography on silica gel to give the title compound (0.034 g).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07098212B2
出典データセットuspto-grants-2006_08
ORD IDord-5c62ce052f7a4c5586df582a6416f915
出典メモuspto-grants-2006_08