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HRID 419作成日:2026年10月23日

2-Bromo-4-nitroanisole → 5-chloro-N-(2-methoxy-5-nitrophenyl)-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-amine

https://huagongshe.com/ja/reaction/419

反応式

関与物質

役割名称HCID仕込み量
反応物2-Bromo-4-nitroanisoleHCID 78870—
反応物5-Chloro-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-amineHCID 141474958—
試薬Cesium carbonateHCID 10796—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒1,4-DioxaneHCID 31275—
生成物5-chloro-N-(2-methoxy-5-nitrophenyl)-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-amineHCID 732925484%

反応条件

温度150 °C

反応手順

_Crude SM used_ 2-bromo-1-methoxy-4-nitrobenzene (0.029 g, 0.13 mmol), 5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-amine (0.031 g, 0.125 mmol) and cesium carbonate (0.057 g, 0.18 mmol) were suspended in dry dioxane (2 mL) the mixture degassed with nitrogen for 10 minutes. TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (6.87 mg, 7.50 µmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (5.79 mg, 10.00 µmol) were added and the mixture was sealed into a microwave tube. The reaction was heated to 150 °C for 2 hours in the microwave reactor and cooled to RT. Possibly product - not very much. The reaction was heated to 150 °C for 10 hours in the microwave reactor and cooled to RT. Product now c4%, both starting materials still present. Not continued.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-75e934c9ac8c4736a342c35dfcb5f15c
出典メモ750 AstraZeneca ELN dataset