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4,7-Dichloroquinoline → 7-chloro-4-(5-fluoro-2-methyl-1H-indol-3-yl)-quinoline
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4,7-Dichloroquinoline | HCID 6866 | — |
| 反応物 | 5-Fluoro-2-methylindole | HCID 2778715 | — |
| 溶媒 | Hydrochloric Acid | HCID 313 | — |
| 溶媒 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 7-chloro-4-(5-fluoro-2-methyl-1H-indol-3-yl)-quinoline | HCID 68458195 | 80.5% |
反応手順
A solution of 5-fluoro-2-methylindole (149 mg) and 4,7-dichloroquinoline (198 mg) in NMP (2 ml) and 4M hydrogen chloride in dioxan (0.2 ml) was stirred at 140° C. overnight and then at 150° C. for 1 h. and evaporated. The residue was taken up in ethyl acetate, washed with brine (3×), dried (MgSO4) and evaporated in vacuo. The residue was purified by silica chromatography using acetone/isohexane (2:8) as eluent to give the sub-title compound (250 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08093278B2 |
| 出典データセット | uspto-grants-2012_01 |
| ORD ID | ord-fb62c8b020ba418e8f05ec14c5a0d741 |
| 出典メモ | uspto-grants-2012_01 |