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HRID 74935作成日:2026年10月26日

Methyl iodide → 2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-((1S)-3-methoxycyclohexyl)pyrimidin-4-amine

https://huagongshe.com/reaction/74935

反応式

関与物質

役割名称HCID仕込み量
反応物Methyl iodideHCID 6328—
反応物Calcium SulfateHCID 24497—
反応物3-[[2-[5-Chloro-1-(p-tolylsulfonyl)pyrrolo[2,3-b]pyridin-3-yl]-5-fluoro-pyrimidin-4-yl]amino]-cyclohexanolHCID 67285187—
反応物(2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)cyclohexanolHCID 86762726—
触媒Silver(II) oxideHCID 92152—
生成物2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-((1S)-3-methoxycyclohexyl)pyrimidin-4-amineHCID 68007568—

反応手順

To a suspension of methyl iodide (0.20 g, 0.41 mmol) and 3-[[2-[5-chloro-1-(p-tolylsulfonyl)pyrrolo[2,3-b]pyridin-3-yl]-5-fluoro-pyrimidin-4-yl]amino]-cyclohexanol, 27a, (0.47 g, 2.04 mmol) was added silver oxide (0.578 g, 4.07 mmol and calcium sulfate (0.28 g, 2.04 (mmol). The reaction mixture was stirred at room temperature for 18 h. The mixture was filtered through celite and the resulting filtrate was concentrated in vacuo. The resulting crude mixture was purified by silica gel chromatography to afford 120 mg of the desired product, 27b.

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-7fd53e0bb1d34e3f91645872df2f8333
出典メモuspto-grants-2014_09