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HRID 407928作成日：2026年10月25日
Sodium Carbonate → (S)-tert-butyl 3-(2,5-difluoro-4-(methylsulfonyl)phenylamino)-2-oxo-1,4'-bipiperidine-1'-carboxylate
https://huagongshe.com/reaction/407928
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | 1,2,4-Trifluoro-5-(methylsulfonyl)benzene | HCID 46739396 | — |
| 反応物 | (S)-tert-butyl 3-amino-2-oxo-1,4'-bipiperidine-1'-carboxylate | HCID 66802275 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (S)-tert-butyl 3-(2,5-difluoro-4-(methylsulfonyl)phenylamino)-2-oxo-1,4'-bipiperidine-1'-carboxylate | HCID 67470435 | 72.3% |
反応手順
(S)-tert-butyl 3-amino-2-oxo-1,4′-bipiperidine-1′-carboxylate (4.0 g, 13 mmol), 1,2,4-trifluoro-5-(methylsulfonyl)benzene (Preparation C, 4.2 g, 20 mmol) and Na2CO3 (2.9 g, 27 mmol) were dissolved in DMF (30 mL) and heated at 130° C. overnight. The reaction was concentrated and purified over silica gel (25-75% EtOAc in hexanes) to afford (S)-tert-butyl 3-(2,5-difluoro-4-(methylsulfonyl)phenylamino)-2-oxo-1,4′-bipiperidine-1′-carboxylate (4.6 g, 9.4 mmol, 70% yield) as yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08754226B2 |
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| 出典データセット | uspto-grants-2014_06 |
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| ORD ID | ord-f53e1b5d05224dcdaa472d4935f18b81 |
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| 出典メモ | uspto-grants-2014_06 |
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