関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Pyridine | HCID 1049 | — |
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Sulfuryl chloride | HCID 24648 | — |
| 反応物 | Benzenesulfonyl chloride, 2,4-dinitro- | HCID 74255 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 2,4-Dinitrobenzenesulfonamide | HCID 10911854 | — |
反応手順
A solution of Part A compound (1.01 g, 2.37 mmol) and TFA (8 mL) in CH2Cl2 (30 mL) was stirred at RT for 4.5 h. The solution was concentrated in vacuo, and the residue was dissolved in CH2Cl2 and filtered through a pad of solid K2CO3. The filtrate was concentrated in vacuo to give the corresponding crude amine. To a solution of the crude amine in THF (11.9 mL) were added pyridine (0.383 mL, 4.74 mmol) and 2,4-dinitrobenzenesulfonyl chloride (0.85 g, 3.19 mmol) and the solution was stirred at RT for 15 h. Since some starting material still remained at this point, more sulfonyl chloride (0.32 g, 1.2 mmol) was then added. After a further 4 h, HPLC analysis indicated that all starting material had been consumed. The reaction mixture was diluted with Et2O, washed with 1N aq HCl, saturated aq NaHCO3 and brine, dried (MgSO4), filtered and concentrated in vacuo to provide the crude 2,4-dinitrobenzenesulfonamide
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06919358B2 |
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| 出典データセット | uspto-grants-2005_07 |
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| ORD ID | ord-df7ba9deda284f9f9b24cb3b28f7059a |
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| 出典メモ | uspto-grants-2005_07 |
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