참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | 2-Methylpiperazine | HCID 66057 | — |
| 반응물 | 1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid | HCID 7019465 | — |
| 용매 | Dimethyl Sulfoxide | HCID 679 | — |
| 생성물 | Gatifloxacin | HCID 5379 | 75% |
반응 단계
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 put in suspension in DMSO (800 mL) under nitrogen atmosphere. The mixture was heated to 55° C. during 24 hours. Subsequently, the mixture was heated to 70° C. and half of the amount of DMSO was distilled-off at reduced pressure (1-5 mm Hg). At the end of the distillation, toluene (200 mL) was added, the reaction mixture was cooled to 5° C., and held at this temperature overnight. The solution was filtered and dried under vacuum to obtain 38 g after assay (75% yield) of gatifloxacin.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US07531656B2 |
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| 출처 데이터셋 | uspto-grants-2009_05 |
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| ORD ID | ord-67e8ed0ba11d4a1cb5562f304898781a |
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| 출처 메모 | uspto-grants-2009_05 |
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