関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1-(Benzyloxy)-4-bromo-2-fluorobenzene | HCID 18757491 | — |
| 反応物 | (R)-2-(tert-butyldimethylsilyloxy)propan-1-amine | HCID 59302513 | — |
| 試薬 | Cesium carbonate | HCID 10796 | — |
| 触媒 | Palladium (II) acetate | HCID 4144353 | — |
| 触媒 | 2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl | HCID 11155794 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | (R)-4-(benzyloxy)-N-(2-(tert-butyldimethylsilyloxy)propyl)-3-fluoroaniline | HCID 58464435 | 0% |
反応手順
PdOAc2 (0.080 g, 0.36 mmol) and dicyclohexyl(2',4',6'-triisopropylbiphenyl-2-yl)phosphine (0.170 g, 0.36 mmol) were added in one portion to a degassed solution of 1-(benzyloxy)-4-bromo-2-fluorobenzene (1 g, 3.56 mmol), (R)-2-(tert- butyldimethylsilyloxy)propan-1-amine (0.808 g, 4.27 mmol) and cesium carbonate (1.739 g, 5.34 mmol) in anhydrous dioxane (20 mL) at 20°C in a microwave vial. The microwave vial was sealed and the reaction was heated to 120 °C for 10 hours in the microwave reactor and cooled to RT. LCMS indicates mainly starting material **** No further action was taken.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-1df10534bfeb467c9df72e530f4b3ab2 |
|---|
| 出典メモ | 750 AstraZeneca ELN dataset |
|---|
