参与物
| 角色 | 名称 | HCID | 投料 |
|---|
| 反应物 | 5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine | HCID 16665498 | — |
| 反应物 | 4-(4-Bromo-3-fluorobenzyl)morpholine | HCID 53417818 | — |
| 试剂 | 叔戊醇钠 | HCID 2733478 | — |
| 催化剂 | 钯 | HCID 23938 | — |
| 催化剂 | 2-双环己基膦-2',6'-二甲氧基联苯 | HCID 11269872 | — |
| 溶剂 | 甲苯 | HCID 1140 | — |
| 产物 | 5-Fluoro-N-(2-fluoro-4-(morpholinomethyl)phenyl)-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine | HCID 49782013 | 85% |
反应步骤
The aim of the reaction is test/optimization: 5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidin-2-amine (100 mg, 0.36 mmol), 4-(4-bromo-3-fluorobenzyl)morpholine (109 mg, 0.40 mmol), Palladium, 10% On Charcoal (115 mg, 0.11 mmol), 2-Dicyclohexylphosphino-2',6'-dimethoxy-1,1'-biphenyl (66.6 mg, 0.16 mmol) and Sodium tert-pentoxide (79 mg, 0.72 mmol) were dissolved in toluene (1.5 mL) and heated to 110 °C under argon. The reaction was monitorred by HPLC. After 16 h 85 % conversion was achieved. The reaction was stopped and the mixture was discarded.
来源与证据
| 来源数据集 | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-28a0ca5c779744199b5c278aec8fa826 |
|---|
| 来源说明 | 750 AstraZeneca ELN dataset |
|---|
