関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Pyridine | HCID 1049 | — |
| 反応物 | 2-Propanesulfonyl chloride | HCID 82408 | — |
| 反応物 | 5-(4-amino-2-fluorophenyl)-1-methyl-1H-pyrrole-2-carbonitrile | HCID 16050432 | — |
| 溶媒 | Water | HCID 962 | — |
| 生成物 | N-[4-(5-cyano-1-methyl-1H-pyrrol-2-yl)-3-fluorophenyl]propane-2-sulfonamide | HCID 16051008 | 19.4% |
反応手順
5-(4-amino-2-fluorophenyl)-1-methyl-1H-pyrrole-2-carbonitrile (200 mg, 0.93 mmol) was dissolved in isopropyl sulfonyl chloride (0.50 mL, 2.8 mmol), pyridine (0.2 mL) was added and the mixture was heated to 100° C. for 6 hours. The mixture was then cooled and diluted with water and extracted with ethyl acetate. The organics were combined, washed with water, brine, dried over MgSO4, and concentrated. Flash chromatography (0%-100% ethyl acetate in hexane) afforded N-[4-(5-cyano-1-methyl-1H-pyrrol-2-yl)-3-fluorophenyl]propane-2-sulfonamide (58 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07291643B2 |
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| 出典データセット | uspto-grants-2007_11 |
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| ORD ID | ord-e17024f1d65a4795b31d6b1814552010 |
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| 出典メモ | uspto-grants-2007_11 |
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