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HRID 220842作成日：2026年10月25日
Triphenylphosphine → 4-[2-(4-Methoxycarbonyl-2-methyl-phenoxy)-ethyl]-piperazine-1-carboxylic Acid Tert-butyl Ester
https://huagongshe.com/reaction/220842
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | Tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate | HCID 735736 | — |
| 反応物 | Diethyl azodicarboxylate | HCID 5462977 | — |
| 反応物 | Methyl 4-hydroxy-3-methylbenzoate | HCID 11240684 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 4-[2-(4-Methoxycarbonyl-2-methyl-phenoxy)-ethyl]-piperazine-1-carboxylic Acid Tert-butyl Ester | HCID 57555264 | 60% |
反応手順
4-(2-Hydroxy-ethyl)-piperazine-1-carboxylic acid tert-butyl ester (500 mg, 2.2 mmol) was dissolved in THF (30 ml) and cooled down to 0° C. Polymer-supported triphenylphosphine (2.2 g, 2.2 mmol), DEAD (378 mg, 2.2 mmol) and 4-hydroxy-3-methyl-benzoic acid methyl ester from Example E29 (361 mg, 2.2 mmol) were added and the mixture was stirred for 20 h at room temperature. The resin was filtered off and the filtrate concentrated in vacuo. The residue was purified by flash chromatography on silica gel (eluant; EtOAc) to yield the title compound (495 mg, 60%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08202858B2 |
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| 出典データセット | uspto-grants-2012_06 |
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| ORD ID | ord-b4e2e9c5d231412787ececaf7ea10150 |
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| 出典メモ | uspto-grants-2012_06 |
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