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Diisopropylethylamine → 4-Iodo-3-methoxy-N-(1-methylpiperidin-yl)benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate | HCID 2733207 | — |
| 反応物 | 4-Amino-1-methylpiperidine | HCID 2737531 | — |
| 反応物 | tert-Butyloxy 4-Iodo-3-methoxybenzoate | HCID 86653099 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 4-Iodo-3-methoxy-N-(1-methylpiperidin-yl)benzamide | HCID 66688078 | 74.2% |
反応手順
A solution of tert-butyloxy 4-iodo-3-methoxybenzoate (250 mg, 0.90 mmol) in anhydrous dimethylformamide (8 mL) was treated with N-ethyl-N,N-diisopropylamine (0.63 mL, 3.6 mmol) and TBTU (404 mg, 1.26 mmol). The mixture was then treated with 1-methylpiperidin-4-amine (0.160 mL, 1.26 mmol). The reaction mixture was stirred at room temperature for 24 h. The reaction was diluted with water and the resulting precipitate was collected by filtration to afford the title compound (250 mg, 71% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08846701B2 |
| 出典データセット | uspto-grants-2014_09 |
| ORD ID | ord-0c9e7cf7d3ff4f94af6359c374cf9327 |
| 出典メモ | uspto-grants-2014_09 |