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HRID 25175作成日:2026年10月26日
Diisopropyl Ether → 1-(6-Amino-3,5-difluoropyridin-2-yl)-8-bromo-7-(3-ethylaminoazetidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
https://huagongshe.com/reaction/25175
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Diisopropyl Ether | HCID 7914 | — |
| 反応物 | 1-Methylpyrrolidine | HCID 8454 | — |
| 反応物 | N-ethylazetidin-3-amine | HCID 10336591 | — |
| 反応物 | 1-(6-Amino-3,5-difluoropyridin-2-yl)-8-bromo-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 15486977 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 生成物 | 1-(6-Amino-3,5-difluoropyridin-2-yl)-8-bromo-7-(3-ethylaminoazetidin-1-yl)-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 9958049 | 77.6% |
反応手順
3-Ethylaminoazetidine (700 mg), 1-(6-amino-3,5-difluoropyridin-2-yl)-8-bromo-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (1.5 g), N-methyl-pyrrolidine (2.0 g)and dimethylsulfoxide (4.5 g) were combined, and the mixture was heated under stirring at 40° C. for 24 hours. After the mixture was allowed to cool down, isopropyl ether (10 mL) was added, the mixture was stirred, and a clear layer at the top of the mixture was removed. The same procedure was repeated once more, and the residue was concentrated under reduced pressure. Ethanol (5 mL) was added, and the mixture was heated under stirring at 70° C. for 30 minutes. The precipitated solid was collected by filtration. The title compound (1.38 g) was obtained.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06858625B1 |
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| 出典データセット | uspto-grants-2005_02 |
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| ORD ID | ord-f1b6525d2c034223888dbf7e1495eaa4 |
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| 出典メモ | uspto-grants-2005_02 |
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