化工社化工社 化学情報印刷レポート · 研究参考用
HRID 226335作成日：2026年10月27日
1-Hydroxybenzotriazole → ethyl (2E)-3-[6-({1-[4-(1H-pyrrol-1-yl)benzoyl]-4-piperidyl}amino)-3-pyridyl]acrylate
https://huagongshe.com/reaction/226335
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 4-(1H-Pyrrol-1-yl)benzoic acid | HCID 2737256 | — |
| 反応物 | ethyl (2E)-3-[6-(4-piperidylamino)-3-pyridyl]acrylate dihydrochloride | HCID 86603643 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Triethylamine | HCID 8471 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | ethyl (2E)-3-[6-({1-[4-(1H-pyrrol-1-yl)benzoyl]-4-piperidyl}amino)-3-pyridyl]acrylate | HCID 86603647 | 107.5% |
反応手順
To a suspension of ethyl (2E)-3-[6-(4-piperidylamino)-3-pyridyl]acrylate dihydrochloride (500 mg) in DMF (5 ml) was added 4-(1H-pyrrol-1-yl)benzoic acid (309 mg), EDCI.HCl (317 mg), HOBt (223 mg), Et3N(0.63 ml), the mixture was stirred at 23° C. for 8 hours. The mixed solution was poured into a mixture of water (20 ml) and AcOEt (20 ml). The organic layer was separated, washed with water twice and brine, dried-over sodium sulfate and concentrated in vacuo. The residue was purified by silica gel column chromatography eluted with 5% MeOH in dichloromethane to give ethyl (2E)-3-[6-({1-[4-(1H-pyrrol-1-yl)benzoyl]-4-piperidyl}amino)-3-pyridyl]acrylate (686 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07557127B2 |
|---|
| 出典データセット | uspto-grants-2009_07 |
|---|
| ORD ID | ord-e59c90f992f942e79eaf2fc990c3f4ce |
|---|
| 出典メモ | uspto-grants-2009_07 |
|---|
