摘要
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 To prove synthetic procedure of Garenoxacin. METHODS Garenoxacin was synthesized from 1 （ R）- methyl -5-Bromo-1H-isoindole via N-alkylation, boronation, condensation and deprotection. RESULTS Garenoxacin 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. CONCLUSION The 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.
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2009年第3期218-220,共3页
Chinese Journal of Modern Applied Pharmacy
