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Moxifloxacin difluoro methoxy ethyl ester → 1-Cyclopropyl-6,7-difluoro-8-hydroxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Moxifloxacin difluoro methoxy ethyl ester | HCID 10758239 | — |
| 溶媒 | Acetic Acid | HCID 176 | — |
| 溶媒 | Hydrogen Bromide | HCID 260 | — |
| 生成物 | 1-Cyclopropyl-6,7-difluoro-8-hydroxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | HCID 11680737 | 89.8% |
反応手順
The preparation comprises dissolving Ethyl 1-cyclopropyl-6,7-difluoro-8-methoxy-1,4-dihydro-4-oxoquinoline-3-carboxylate (10.0 g, 30.9 mmol) in 40% HBr aqueous solution (20 mL) and acetic acid (20 mL) to react at 100° C., charging reaction mixture into ice water (500 mL) under fast stirring after the reaction finishes, going on with the stirring for 0.5 h, filtering, and drying obtained filter cake to give 1-cyclopropyl-6,7-difluoro-8-hydroxy-1,4-dihydro-oxoquinoline-3-carboxylic acid (7.8 g, 89.6%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07759362B2 |
| 出典データセット | uspto-grants-2010_07 |
| ORD ID | ord-41eeed3c861a4e169441e5ed565efd7a |
| 出典メモ | uspto-grants-2010_07 |