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HRID 529652作成日:2026年10月24日

Triethylamine → 2-Chloro-5-(pyridin-4-yl)-N-(tetrahydro-2H-pyran-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

https://huagongshe.com/ja/reaction/529652

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物4-Aminotetrahydropyran hydrochlorideHCID 44118693—
反応物2,4-Dichloro-5-(pyridin-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidineHCID 86726429—
溶媒1,4-DioxaneHCID 31275—
生成物2-Chloro-5-(pyridin-4-yl)-N-(tetrahydro-2H-pyran-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineHCID 8672643034%

反応条件

温度120 °C

反応手順

To a solution of 2,4-dichloro-5-(pyridin-4-yl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (1 equiv) in 1,4-dioxane (0.4 M) in a sealable vessel was added tetrahydro-2H-pyran-4-amine hydrochloride (1.5 equiv) and triethylamine (3 equiv). The resulting mixture was heated at 120° C. for 2 h under nitrogen atmosphere. After the reaction was complete, the reaction mixture was cooled to room temperature and concentrated. The residue was purified by silica gel chromatography (0-30% ethyl acetate in petroleum ether) to afford the desired product (34% yield) as a yellow solid. MS (ESI) m/z 460.2 [M+1]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09346812B2
出典データセットuspto-grants-2016_05
ORD IDord-6995f1ae4de84246a3838bd68debcd1b
出典メモuspto-grants-2016_05