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目的合成加雷沙星。方法1(R)-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。
Objective Synthesis of galefloxacin. Method 1 (R) -methyl-5-bromo-1H-isoindoline was prepared via N-alkylation, borylation, condensation and deprotection. Results The galefloxacin was synthesized by optimizing the conditions. The total yield was 51.0%. The structure of target compound was confirmed by IR, MS, 1H NMR and elemental analysis. Conclusion The process steps less raw materials cheap and easy, suitable for industrial production.