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Triethylamine → Ethyl 4-(1,2,3,4-tetrahydro-2,8-dimethylpyrido[4,3-b]indol-5-yl)butanoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 4-Methylphenylhydrazine monohydrochloride | HCID 12504 | — |
| 反応物 | Ethyl 4-chlorobutyrate | HCID 18474 | — |
| 反応物 | 1-Methylpiperidin-4-one hydrochloride | HCID 12210057 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | Ethyl 4-(1,2,3,4-tetrahydro-2,8-dimethylpyrido[4,3-b]indol-5-yl)butanoate | HCID 44159096 | 11.2% |
反応手順
Preparation of the title compound was carried out according to General Method 1 by using p-Tolylhydrazine hydrochloride (600 mg, 3.7 mmol), ethyl-4-chlorobutyrate (0.54 ml, 3.7 mmol), triethylamine (1.5 ml, 11.3 mmol) and N-methyl-4-piperidone hydrochloride (0.563 g, 3.7 mmol) in ethanol (10 ml) to obtain 130 mg of ethyl 4-(1,2,3,4-tetrahydro-2,8-dimethylpyrido[4,3-b]indol-5-yl)butanoate after purification on silica gel (230-400 mesh) chromatography eluting with methanol-dichloromethane gradient. The free base was converted into its oxalate salt by treatment of oxalic acid (1 equiv) in anhydrous THF.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09115137B2 |
| 出典データセット | uspto-grants-2015_08 |
| ORD ID | ord-b17996800eb1421faf6af1e04bf13769 |
| 出典メモ | uspto-grants-2015_08 |