関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 2-amino-N,6-dimethoxybenzamide | HCID 56951659 | — |
| 反応物 | N-(1,3-dimethylpyrazol-5-yl)-4-iodo-5-(trifluoromethyl)pyridin-2-amine | HCID 67075489 | — |
| 試薬 | Potassium Carbonate | HCID 11430 | — |
| 触媒 | 1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) | HCID 636044 | — |
| 触媒 | Palladium (II) acetate | HCID 4144353 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 2-[[2-[(2,5-dimethylpyrazol-3-yl)amino]-5-(trifluoromethyl)pyridin-4-yl]amino]-N,6-dimethoxybenzamide | HCID 56951550 | 0% |
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 |
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| ORD ID | ord-067f9706b99f4ac98e07f49d63946447 |
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| 出典メモ | 750 AstraZeneca ELN dataset |
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