関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Glycine ethyl ester, hydrochloride | HCID 2723640 | — |
| 反応物 | 2-Bromo-5-fluoropyridin-3-amine | HCID 40427367 | — |
| 試薬 | Cesium carbonate | HCID 10796 | — |
| 触媒 | Binap, (A+-)- | HCID 634876 | — |
| 触媒 | Palladium (II) acetate | HCID 4144353 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | Ethyl 2-[(3-amino-5-fluoro-2-pyridinyl)amino]acetate | HCID 132224848 | 0% |
反応手順
In a 50 mL round-bottomed flask 2-bromo-5-fluoropyridin-3-amine (500 mg, 2.62 mmol) ethyl 2-aminoacetate hydrochloride (731 mg, 5.24 mmol) BINAP (163 mg, 0.26 mmol) palladium(II) acetate (58.8 mg, 0.26 mmol) CESIUM CARBONATE (2559 mg, 7.85 mmol) were taken.The solids were mixed well and degassed.The toluene was taken in another RB and degassed using Nitrogen.The degassed toluene was then added to the solids.The resulting RM was heated to reflux for 16 hrs. The reaction was monitored by LCMS, which indicated starting material only and no required product. Therefore, the batch was discarded.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-a7df51f0be0a4af98f3bfe87d6600255 |
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| 出典メモ | 750 AstraZeneca ELN dataset |
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