関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 3-Bromopyridine | HCID 12286 | — |
| 反応物 | (R)-1-Boc-3-methylpiperazine | HCID 2756811 | — |
| 試薬 | Sodium t-butoxide | HCID 23676156 | — |
| 触媒 | 1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) | HCID 636044 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | tert-butyl (3R)-3-methyl-4-pyridin-3-ylpiperazine-1-carboxylate | HCID 89555981 | 0% |
反応手順
TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (0.145 g, 0.16 mmol) and 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene (0.183 g, 0.32 mmol) were added to a mixture of Sodium tert-butoxide (0.912 g, 9.49 mmol), 3-bromopyridine (0.610 mL, 6.33 mmol),(R)-tert-butyl 3-methylpiperazine-1-carboxylate (1.901 g, 9.49 mmol) and toluene (20 mL) under nitrogen. The mixture was heated at 85 °C for 16 hours before being cooled to RT and filtered through celite. The filtrate was concentrated and the reaction mixture was seperated by flash silica chromatography, elution gradient 20 to 40% EtOAc in heptane. No product was isolated. .
情報源と証拠
| 出典データセット | 750 AstraZeneca ELN dataset |
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| ORD ID | ord-d7d7e0dc4c0741f08ecfdb907acad13f |
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| 出典メモ | 750 AstraZeneca ELN dataset |
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