関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Indole | HCID 798 | — |
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 3-Bromopyridine-2-carbonitrile | HCID 817694 | — |
| 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 | 3-Indol-1-yl-pyridine-2-carbonitrile | HCID 67271706 | 89% |
反応手順
To a solution of 3-bromo-2-cyanopyridine (Sakamoto, T. et al., Chem. Pharm. Bull. 1985, 33(2), 565-571) (340 mg, 1.86 mmol) and indole (436 mg, 3.72 mmol) in toluene (15 mL) was added Cs2CO3 (737 mg, 2.26 mmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (83 mg, 0.143 mmol) and Pd2(dba)3 (42 mg, 0.046 mmol) and the reaction stirred at 110° C. for 2.5 d. The mixture was concentrated and purified by column chromatography on silica gel (EtOAc/Hexanes, 2:1) to give 3-indol-1-yl-pyridine-2-carbonitrile (362 mg, 89%) as a beige solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07863293B2 |
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| 出典データセット | uspto-grants-2011_01 |
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| ORD ID | ord-c75c30a8e3a5439193376c99a7645a8a |
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| 出典メモ | uspto-grants-2011_01 |
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