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HRID 289作成日:2026年10月23日

2-amino-N,6-dimethoxybenzamide → 2-[[2-[(2,5-dimethylpyrazol-3-yl)amino]-5-(trifluoromethyl)pyridin-4-yl]amino]-N,6-dimethoxybenzamide

https://huagongshe.com/ja/reaction/289

反応式

関与物質

役割名称HCID仕込み量
反応物2-amino-N,6-dimethoxybenzamideHCID 56951659—
反応物N-(1,3-dimethylpyrazol-5-yl)-4-iodo-5-(trifluoromethyl)pyridin-2-amineHCID 67075489—
試薬Potassium CarbonateHCID 11430—
触媒1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
触媒Palladium (II) acetateHCID 4144353—
溶媒1,4-DioxaneHCID 31275—
生成物2-[[2-[(2,5-dimethylpyrazol-3-yl)amino]-5-(trifluoromethyl)pyridin-4-yl]amino]-N,6-dimethoxybenzamideHCID 569515500%

反応条件

温度90 °C

反応手順

N-(1,3-dimethyl-1H-pyrazol-5-yl)-4-iodo-5-(trifluoromethyl)pyridin-2-amine (50 mg, 0.13 mmol), 2-amino-N,6-dimethoxybenzamide (43.6 mg, 0.22 mmol), diacetoxypalladium (1.469 mg, 6.54 µmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (7.57 mg, 0.01 mmol) and potassium carbonate (36.2 mg, 0.26 mmol) were suspended in 1,4-dioxane (423 µl) and sealed into a microwave tube. The reaction was degased, purged with nitrogen and heated to 90 °C overnight => _not complete but seemed to be clean, no des-iodo by-product formed, both SM left_ Same reaction was performed in toluene (423 µl) => _reaction complete, LCMS profile similar to the conception document reference_ **_NOT ISOLATED_**

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-067f9706b99f4ac98e07f49d63946447
出典メモ750 AstraZeneca ELN dataset