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2’-乙酰基-3-酮基-10,11-脱水-6-O-甲氧基红霉素的合成 被引量：1

Synthesis of 2'-acetyl-3-oxo-10,11-dehydro-6-O-methoxyerythromycin
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摘要 目的:合成泰利霉素中间体2’-乙酰基-3-酮基-10,11-脱水-6-O-甲氧基红霉素。方法:以6-O-甲氧基红霉素为起始原料,经脱水、酸水解、乙酰化和氧化得到目标产物。结果:以6-O-甲氧基红霉素计,总收率79.9%。目标产物的光谱数据与文献报道一致。结论:该方法合成操作简单,反应条件温和。 Objective: To synthesize 2'-acetyl-3-oxo-10, 11-dehydro-6-O-methoxyerythromycin, an intermediate of telithromycin. Methods: Starting from 6-O-methoxyerythromycin, 2'-acetyl-3-oxo-10, 11-dehydro-6-O-methoxyerythromycin was synthesized via dehydration,acidic hydrolysis, acetylation and oxidation. Results: A total yield of the target product was 79.9%. The structure of the target product was confirmed by the spectral analyses. Conclusion: A simple and easily manipulated way to synthesize the intermediate was attainable.
作者 易红 许先栋
机构地区 中国医学科学院中国协和医科大学医药生物技术研究所
出处 《中国新药杂志》 CAS CSCD 北大核心 2005年第5期581-582,共2页 Chinese Journal of New Drugs
关键词 2’-乙酰基-3-酮基-11 12-脱水-6-O-甲氧基红霉素 泰利霉素 合成 2'-acetyl-3-oxo-10,11-dehydro-6-O-methoxyerythromycin telithromycin synthesis
分类号 R914.3 [医药卫生—药物化学] R978.1 [医药卫生—药品]
  • 相关文献

参考文献6

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二级参考文献8

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共引文献17

同被引文献31

  • 1王翀,郑忠辉.3-脱克拉定糖-3-酮基-6-O-甲基-10,11-脱氢-12-O-咪唑酰基-2′-苯甲酰基红霉素A的合成[J].齐鲁药事,2006,25(10):617-618. 被引量：1
  • 2尤启冬,魏新,赵英.泰利霉素的合成改进[J].中国医药工业杂志,2007,38(4):318-320. 被引量：9
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  • 7George R C, Thomas H, Grace C L. The synthesis of phenyl and phridyl-glyoxalines[J]. J Chem Soc, 1938,753 -755.
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  • 10Ghilsoo N, Tae Won Kang, Jung Hyu Shin, et al. Design, synthesis, and anti-helicobacter pylori activity of erythromycin A(E) -9-oxime ether derivatives[J]. Bioorg Med Chem Lett, 2006,16 ( 3 ) :569 - 572.

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中国新药杂志
2005年 第5期

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