参与物
| 角色 | 名称 | HCID | 投料 |
|---|
| 反应物 | 4-溴吡啶 | HCID 14268 | — |
| 反应物 | 3-羟基吡咯烷 | HCID 98210 | — |
| 试剂 | 双三甲基硅基胺基锂 | HCID 2733832 | — |
| 催化剂 | 2-二环己膦基-2'-(N,N-二甲胺)-联苯 | HCID 2734217 | — |
| 催化剂 | 三(二亚苄基丙酮)二钯 | HCID 9811564 | — |
| 溶剂 | 四氢呋喃 | HCID 8028 | — |
| 产物 | 1-(Pyridin-4-yl)pyrrolidin-3-ol | HCID 21906198 | 43.01% |
反应步骤
In a 50 ml round bottomed flask THF (1 mL) was added to a mixture of 4-bromopyridine (1 g, 6.33 mmol), pyrrolidin-3-ol (0.662 g, 7.60 mmol),2-(dimethylamino)-2'-(dicyclohexylphosphino)biphenyl (0.249 g, 0.63 mmol) and Pd2(dba)3 (0.580 g, 0.63 mmol). To the slurry lithium bis(trimethylsilyl)amide (13.92 mL, 13.92 mmol) was added dropwise at 0 °C and the solution was refluxed at 65 °C overnight for 20 hrs. The reaction mixture was passed through celite, concentrated and column purified (0-20%MeOH/DCM) to obtain 0.447 mg of product.
来源与证据
| 来源数据集 | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-15613520ef9b4d099659a0a3ac545228 |
|---|
| 来源说明 | 750 AstraZeneca ELN dataset |
|---|
