| 引用本文: | 曹志凌,姚国伟,刘玮炜,孟涛.特利霉素前体化合物的新型合成工艺[J].中国现代应用药学,2010,27(12):1107-1109. |
| .Novel Synthesis Route for the Precursor of Telithromycin[J].Chin J Mod Appl Pharm(中国现代应用药学),2010,27(12):1107-1109. |
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| 摘要: |
| 目的 研究特利霉素前体化合物的新合成工艺。方法 以3-羟基-6-O-甲基红霉素肟为原料，经乙酰化，氧化，脱肟，10,11-脱水、12-O-咪唑酰基化反应得到特利霉素前体化合物2’-O-乙酰基-3-酮基-10,11-脱水-12-O-咪唑酰基-6-O-甲基红霉素。结果 目标物收率为60.8%，经质谱、核磁共振氢谱确证结构。结论 新工艺副反应少，原料易得，操作简便。 |
| 关键词: 2’-O-乙酰基-3-酮基-10,11-脱水-12-O-咪唑酰基-6-O-甲基红霉素 特利霉素 合成 |
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| Novel Synthesis Route for the Precursor of Telithromycin |
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CAO Zhiling1 2 YAO Guowei3 LIU Weiwei1 2 MENG Tao3
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| Abstract: |
| OBJECTIVE To study a new synthetic route of the precursor of telithromycin. METHODS 2’-O-acetate-3- keto-10,11-anhydro-12-O-acylimidazole-6-O-methyl-erythromycin, the precursor of telithromycin, was synthesized from 3-hydroxy-6-O-methyl-erythromycin by acetylation, oxidation, deoximation, followed by 10,11-dehydration and acylation with N-acylimidazole. RESULTS The total yield was up to 60.8%. The chemical structures of target compound were confirmed by 1H-NMR and MS. CONCLUSION The novel synthetic route was facile and characterized by less side-effects. |
| Key words: 2’-O-acetate-3-keto-10,11-anhydro-12-O-acylimidazole-6-O-methylerythromycin telithromycin synthesis |
