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HRID 74876作成日:2026年10月25日

Cyclobutanecarbonyl chloride → 3-((2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)piperidin-1-yl)(cyclobutyl)methanone

https://huagongshe.com/reaction/74876

反応式

関与物質

役割名称HCID仕込み量
反応物Cyclobutanecarbonyl chlorideHCID 78705—
反応物DiisopropylethylamineHCID 81531—
反応物(S)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-(piperidin-3-yl)pyrimidin-4-amine hydrochlorideHCID 67287751—
反応物(S)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-(piperidin-3-yl)pyrimidin-4-amineHCID 67287752—
溶媒DimethylformamideHCID 6228—
溶媒DichloromethaneHCID 6344—
生成物3-((2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)piperidin-1-yl)(cyclobutyl)methanoneHCID 86762720—

反応手順

To a solution of (S)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-(piperidin-3-yl)pyrimidin-4-amine hydrochloride, 5b, (0.04 g, 0.11 mmol) in CH2Cl2 (1.40 mL) and DMF (300 g was added N,N-diisopropyl-N-ethylamine (0.30 mL, 1.70 mmol) followed by cyclobutanecarbonyl chloride (0.01 g. 0.12 mmol). The reaction mixture was allowed to stir at room temperature for 17 hours. The mixture was concentrated in vacuo, dissolved in 1 mL of DMSO and purified by preparatory HPLC (0.1% ammonium formate-H2O/acetonitrile) to afford the desired product, 395.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08829007B2
出典データセットuspto-grants-2014_09
ORD IDord-888b41de75714cbcb8d46508d56d04d5
出典メモuspto-grants-2014_09