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HRID 526879作成日:2026年10月26日

Lithium Hydroxide → (S)-N-(1-((1H-imidazol-2-yl)methyl)piperidin-3-yl)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-amine

https://huagongshe.com/reaction/526879

反応式

関与物質

役割名称HCID仕込み量
反応物Lithium HydroxideHCID 3939—
反応物2-[5-chloro-1-(p-tolylsulfonyl)pyrrolo[2,3-b]pyridin-3-yl]-5-fluoro-N-[(3S)-1-(1H-imidazol-2-ylmethyl)-3-piperidyl]pyrimidin-4-amineHCID 67287763—
溶媒TetrahydrofuranHCID 8028—
溶媒Sodium chloride; waterHCID 57417360—
生成物(S)-N-(1-((1H-imidazol-2-yl)methyl)piperidin-3-yl)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-amineHCID 68007120—

反応条件

温度120 °C

反応手順

To a solution of 2-[5-chloro-1-(p-tolylsulfonyl)pyrrolo[2,3-b]pyridin-3-yl]-5-fluoro-N-[(3S)-1-(1H-imidazol-2-ylmethyl)-3-piperidyl]pyrimidin-4-amine, 4a, (0.08 g, 0.13 mmol) in THF (2.5 mL) was added 1M LiOH (0.67 mL, 0.65 mmol) solution. The reaction mixture was heated in microwave at 120° C. for 10 minutes. The mixture was cooled to room temperature and diluted with brine. The aqueous phase was extracted with CH2Cl2, then twice with 20% isopropanol/CH2Cl2. The combined organic phases were dried (MgSO4), filtered and concentrated in vacuo to afford the desired product, 589, as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09345708B2
出典データセットuspto-grants-2016_05
ORD IDord-154068b842c14c7b86930b57eed137e1
出典メモuspto-grants-2016_05