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HRID 61482作成日:2026年10月25日
Ethanol → methyl(3R,4S)-1-[(E)-2-nitro-1-piperidin-1-ylvinyl]-4-[(3R)-3-phenylpyrrolidin-1-yl]carbonylpiperidine-3-carboxylate
https://huagongshe.com/reaction/61482
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Ethanol | HCID 702 | — |
| 反応物 | Piperidine | HCID 8082 | — |
| 反応物 | Methyl (3r,4s)-1-[(z)-1-(methylthio)-2-nitrovinyl]-4-[(3r)-3-phenylpyrrolidin-1-yl]carbonylpiperidine-3-carboxylate | HCID 67304566 | — |
| 生成物 | methyl(3R,4S)-1-[(E)-2-nitro-1-piperidin-1-ylvinyl]-4-[(3R)-3-phenylpyrrolidin-1-yl]carbonylpiperidine-3-carboxylate | HCID 67304657 | 71% |
反応手順
To a stirred solution of methyl(3R,4S)-1-[(Z)-1-(methylthio)-2-nitrovinyl]-4-[(3R)-3-phenylpyrrolidin-1-yl]carbonylpiperidine-3-carboxylate (81.0 mg, 0.000187 mol) in ethanol (3.0 mL, 0.051 mol) was added piperidine (92.8 uL, 0.000934 mol). The reaction mixture was heated to reflux (oil bath temperature: 85° C.) for 17 h 45 min. The reaction mixture was concentrated in vacuo. The residue was purified by Combiflash with 0-8% MeOH/CH2Cl2 to give the product as a yellow solid (62 mg, 71% in yield). MS (ESI): (M+H)+=471.1.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09440958B2 |
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| 出典データセット | uspto-grants-2016_09 |
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| ORD ID | ord-303e2880180242558dc50668e5bf6d3e |
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| 出典メモ | uspto-grants-2016_09 |
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