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Triethylamine → 4-amino-N-(1-ethyl-piperidin-4-yl)-benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1-Ethylpiperidin-4-amine | HCID 3734990 | — |
| 反応物 | 4-Amino-benzoic acid benzotriazol-1-yl ester | HCID 53844583 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 4-amino-N-(1-ethyl-piperidin-4-yl)-benzamide | HCID 54915895 | 84% |
反応手順
To a mixture of 1.0424 g (4.1 mmole) of 4-amino-benzoic acid benzotriazol-1-yl ester and 8 mL of dry tetrahydrofuran at 0 degrees was added 0.5257 g (4.1 mmole) of 4-amino-1-ethylpiperidine followed by 1.0372 g (10.3 mmole) of triethylamine. The cooling bath was removed and the mixture stirred at room temperature for 65 minutes. Volatiles were removed under reduced pressure and the residue taken up in ethyl acetate, and the organic layer washed twice with 50 mL of 0.5 M sodium carbonate, 50 mL water, and then 50 mL brine, dried over anhydrous sodium sulfate and concentrated under reduced pressure to give 0.8522 g 4-amino-N-(1-ethyl-piperidin-4-yl)-benzamide, as a white solid which was used without further purification.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08003785B2 |
| 出典データセット | uspto-grants-2011_08 |
| ORD ID | ord-6618e55103764c5285ec53a92e237d85 |
| 出典メモ | uspto-grants-2011_08 |