関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Bromopyridine | HCID 14268 | — |
| 反応物 | 4-Hydroxypyrrolidine | HCID 98210 | — |
| 試薬 | Lithium Hexamethyldisilazide | HCID 2733832 | — |
| 触媒 | 2-(Dicyclohexylphosphino)-2'-(dimethylamino)biphenyl | HCID 2734217 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 1-(Pyridin-4-yl)pyrrolidin-3-ol | HCID 21906198 | 43.01% |
反応手順
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.
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-15613520ef9b4d099659a0a3ac545228 |
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| 出典メモ | 750 AstraZeneca ELN dataset |
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