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HRID 527032作成日:2026年10月27日

Diisopropylethylamine → 2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-((1S,3R)-3-isocyanato-3-methylcyclohexyl)pyrimidin-4-amine

https://huagongshe.com/reaction/527032

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物Diphenylphosphoryl azideHCID 123414—
反応物(1R,3S)-3-(2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)-1-methylcyclohexanecarboxylic acidHCID 68007671—
溶媒TolueneHCID 1140—
生成物2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-N-((1S,3R)-3-isocyanato-3-methylcyclohexyl)pyrimidin-4-amineHCID 86667437—

反応手順

To a solution of (1R,3S)-3-[[2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoro-pyrimidin-4-yl]amino]-1-methyl-cyclohexanecarboxylic acid, 826, (0.100 g, 0.216 mmol) and (azido(phenoxy)phosphoryl)oxybenzene (0.093 mL, 0.432 mmol) in 10 mL of toluene was added 1 mL of N-ethyl-N-isopropyl-propan-2-amine. The reaction was warmed to reflux overnight. The mixture was concentrated to dryness and the residue was purified by silica gel chromatography (EtOAc), yielding 40 mg of desired product as a white foam.

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-949e1de99e9941baaec4e4045766dfaa
出典メモuspto-grants-2016_05