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| 摘要: |
| 目的合成加雷沙星。方法1R-甲基-5-溴-1H-异吲哚啉经N-烷基化、硼酸化、缩合、去保护反应制得加雷沙星。结果通过优化条件合成了加雷沙星,总收率51.0%,目标化合物结构经红外、质谱、核磁共振谱、元素分析确证。结论本工艺步骤少,原材料价廉易得,适合工业化生产。 |
| 关键词: 1R-甲基-5-溴-1H-异吲哚啉 N-烷基化 硼酸化 加雷沙星 |
| DOI： |
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| The Synthesis of Garenoxacin |
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WU Xiaoguo,MAO Yaqin
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| Abstract: |
| OBJECTIVE To prove synthetic procedure of Garenoxacin.METHODSGarenoxacin was synthesized from 1R-methyl -5-Bromo-1H-isoindole via N-alkylation, boronation, condensation and deprotection. RESULTSGarenoxacin was prepared in an overall yield of 51.0%.The structure of the target compound was confirmed by IR spectra, MS, H-NMR and elemental analysis. CONCLUSIONThe procedure avoids the use of expensive reagents and the target compound was synthesized in a few steps, so it benefits to the production of industry. |
| Key words: 1?-methyl-5-bromo-1H-isoindole N-alkylation boronation Garenoxacin |
