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Chloride → 1-[1-(4-Fluorophenethyl)piperidin-4-yl]-6-(1-methylpyrrol-2-yl)indole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Chloride | HCID 312 | — |
| 反応物 | 1-Methylpyrrole | HCID 7304 | — |
| 反応物 | 1-methyl-2-(tributylstannyl)-1H-pyrrole | HCID 2769397 | — |
| 反応物 | 1-[1-(4-Fluorophenethyl)piperidin-4-yl]-6-bromoindole | HCID 22038188 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 1-[1-(4-Fluorophenethyl)piperidin-4-yl]-6-(1-methylpyrrol-2-yl)indole | HCID 22037951 | 57.5% |
反応手順
1-[1-(4-Fluorophenethyl)piperidin-4-yl]-6-bromoindole (0.2 g) was dissolved in toluene (2.50 ml). Next, 1-methyl-2-tributylstannylpyrrole (1.44 g) synthesized in accordance with the method described in Tetrahedron Lett., 4407 (1986). with the use of 1-methylpyrrole and tributylthin chloride was added thereto and the resultant mixture was heated under reflux for 3 hr under nitrogen atmosphere. After adding ethyl acetate, the mixture was washed with brine, dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane/ethyl acetate system) to give the title compound (0.115 g) as a yellow oil (yield: 57.28%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07071201B2 |
| 出典データセット | uspto-grants-2006_07 |
| ORD ID | ord-9dc8408c89a94e299be6d35e8736e5aa |
| 出典メモ | uspto-grants-2006_07 |