乙酰基保护的活性硫酯法制备头孢地尼新工艺

发布时间：2018-06-25 07:00

本文选题：头孢菌素 + 合成工艺　；参考：《中国抗生素杂志》2016年04期

【摘要】：目的优化头孢地尼的生产工艺。方法 (Z)-2-(2-氨基噻唑-4-基)-2-乙酰氧亚氨基乙酸-2巯基苯并噻唑硫酯与7-氨基-3-乙烯基头孢烷酸(7-AVCA)在三乙胺存在下,缩合得到乙酰基地尼;无须分离,用氯化铵和碳酸钾溶液处理,脱除乙酰基保护基,得到头孢地尼粗品。用磷酸处理粗品,制得头孢地尼磷酸复合物,在水溶热中用碳酸钠中和、酸析。结果头孢地尼原料药物质的量收率达70%以上,高效液相色谱测得纯度99%。结论产品质量达到药典标准,并简化了操作步骤提高了收率。
[Abstract]:Objective to optimize the production process of cefdiidyl. Method (Z) -2- (2- aminothiazole -4-) -2- acetothioacetic acid -2 mercaptothiazolyl thiazolide and 7- amino -3- vinyl cephalosporanic acid (7-AVCA) in the presence of three ethylamine, condensation of acetyl benzyl, without separation, treatment with ammonium chloride and potassium carbonate solution, removal of acetyl protection The crude product of cefidii was treated with phosphoric acid to produce the cefidii phosphate compound, and the sodium carbonate was neutralized and acid analyzed in water soluble heat. The yield of the cefidii material was over 70%. The quality of the product was determined by high performance liquid chromatography (99%.), the product quality reached the pharmacopoeia standard, and the operation procedure was simplified to improve the yield.
【作者单位】：河北化工医药职业技术学院制药工程系;
【基金】：河北省科技厅2013年度计划项目(No.13272615) 河北省人才工程培养经费项目(No.A201400346)
【分类号】：R943

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