関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Dimethyl Carbonate | HCID 12021 | — |
| 反応物 | 2-Methylpiperazine | HCID 66057 | — |
| 反応物 | 1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid | HCID 7019465 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 生成物 | Gatifloxacin | HCID 5379 | 70% |
反応手順
Forty grams of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid and 28.4 g (2.1 eq) of 2-methyl piperazine were suspended in DMSO (800 mL) under nitrogen atmosphere. The mixture was heated to 55° C. during 24 hours. Thereafter, dimethylcarbonate (200 mL) was added, the reaction mixture was cooled to 5° C., and held at this temperature overnight. The mixture was then filtered under vacuum and the compound was then dried under vacuum to obtain 35.5 g after assay (70% yield) of gatifloxacin.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07531656B2 |
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| 出典データセット | uspto-grants-2009_05 |
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| ORD ID | ord-350cc5153f134dcb99f8ee9500ed34e2 |
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| 出典メモ | uspto-grants-2009_05 |
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