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塞拉菌素合成新工艺研究

Study on New Process for Synthesis of Selamectin

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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Bla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.
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(l-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.

selamectinsynthesisnew process

钟秀文、张蕾、黄友纯、罗峰、陈仁尔、俞永平、陈文腾

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浙江大学,杭州 310058

浙江荣耀生物科技股份有限公司,浙江台州 318000

塞拉菌素 合成 新工艺

2024

中国现代应用药学
中国药学会

中国现代应用药学

CSTPCD北大核心
影响因子:0.877
ISSN:1007-7693
年,卷(期):2024.41(2)
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