関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 2-Methoxy-5-nitroaniline | HCID 7447 | — |
| 反応物 | 3-(2,5-Dichloropyrimidin-4-yl)-1H-indole | HCID 56655376 | — |
| 試薬 | Cesium carbonate | HCID 10796 | — |
| 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 | 5-chloro-4-(1H-indol-3-yl)-N-(2-methoxy-5-nitrophenyl)pyrimidin-2-amine | HCID 73292546 | 0% |
反応手順
To a stirred solution of 3-(2,5-dichloropyrimidin-4-yl)-1H-indole (100 mg, 0.38 mmol) in dioxane (10 mL) was added 2-methoxy-5-nitroaniline (63.7 mg, 0.38 mmol), cesium carbonate (247 mg, 0.76 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (26.3 mg, 0.05 mmol). The resulting suspension was purged with nitrogen for 5 minutes. diacetoxypalladium (5.10 mg, 0.02 mmol) was added and the mixture was purged with nitrogen for a further 5 minutes, and then heated at 80 °C overnight. UPLC shows di-Cl SM almost completely consumed but no evidence of desired product. Reaction stopped
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-95b63e9e9ac540bc8fc7f0ffbc5bc6a7 |
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| 出典メモ | 750 AstraZeneca ELN dataset |
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