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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

反応式

関与物質

役割名称HCID仕込み量
反応物EthanolHCID 702—
反応物PiperidineHCID 8082—
反応物Methyl (3r,4s)-1-[(z)-1-(methylthio)-2-nitrovinyl]-4-[(3r)-3-phenylpyrrolidin-1-yl]carbonylpiperidine-3-carboxylateHCID 67304566—
生成物methyl(3R,4S)-1-[(E)-2-nitro-1-piperidin-1-ylvinyl]-4-[(3R)-3-phenylpyrrolidin-1-yl]carbonylpiperidine-3-carboxylateHCID 6730465771%

反応条件

温度85 °C

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

DOI10.6084/m9.figshare.5104873.v1
特許番号US09440958B2
出典データセットuspto-grants-2016_09
ORD IDord-303e2880180242558dc50668e5bf6d3e
出典メモuspto-grants-2016_09