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塞拉菌素合成新工艺研究

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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.
Study on New Process for Synthesis of Selamectin
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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