| 引用本文: | 钟秀文,张蕾,黄友纯,罗峰,陈仁尔,俞永平,陈文腾.塞拉菌素合成新工艺研究[J].中国现代应用药学,2024,41(2):221-227. |
| ZHONG Xiuwen,ZHANG Lei,HUANG Youchun,LUO Feng,CHEN Ren'er,YU Yongping,CHEN Wenteng.Study on New Process for Synthesis of Selamectin[J].Chin J Mod Appl Pharm(中国现代应用药学),2024,41(2):221-227. |
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| 摘要: |
| 目的 改进塞拉菌素的合成工艺。方法 以多拉菌素为起始原料，经二氧化锰氧化、一锅法脱糖肟化反应得到关键中间体25-环己烷基-25-去(1-甲丙基)-5-脱氧-5-(肟基)-阿维菌素B1a单糖，用乙腈和水混合溶剂重结晶，再通过氢化反应制得塞拉菌素。结果 中间体及目标产物结构均经1H-NMR、13C-NMR和HPLC-HRMS确证，总收率达53.2%，产物纯度97.1%。结论 此工艺步骤简化，操作简便，收率高，成本较低，有应用于工业化生产的潜力。 |
| 关键词: 塞拉菌素 合成 新工艺 |
| DOI：10.13748/j.cnki.issn1007-7693.20224245 |
| 分类号:R914.5 |
| 基金项目: |
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| Study on New Process for Synthesis of Selamectin |
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ZHONG Xiuwen1, ZHANG Lei1, HUANG Youchun1, LUO Feng1, CHEN Ren'er2, YU Yongping1, CHEN Wenteng1
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1.Zhejiang University, Hangzhou 310058, China;2.Rongyao Biotech, Taizhou 318000, China
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| Abstract: |
| OBJECTIVE To improve the synthetic process of selamectin. METHODS As the starting material, doramectin was firstly oxidated by manganese dioxide and then the key intermediate 25-cyclohexyl-25-de(1-methypropyl)-5-demethoxy-5-hydroxyimino-avermectin Bla monosaccharide was obtained via deglycosidation and oximation. Selamectin was prepared by hydrogenation after recrystallization with acetonitrile and water. RESULTS The structures of intermediates and product were confirmed by 1H-NMR, 13C-NMR and HPLC-HRMS, the total yield was 53.2% and the purity of the product was 97.1%. CONCLUSION This synthetic process is charactered by simplified step, simple operation, high yield and lower cost, which exhibits the potential to be applied for industrial production. |
| Key words: selamectin synthesis new process |
