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头孢唑肟酸合成方法研究
引用本文:付德才,李航,徐成博,蔡娟娟,陈兴贺. 头孢唑肟酸合成方法研究[J]. 中国抗生素杂志, 2011, 36(2)
作者姓名:付德才  李航  徐成博  蔡娟娟  陈兴贺
作者单位:河北科技大学,化学与制药工程学院,石家庄,050018
摘    要:目的 优化头孢唑肟酸合成条件.方法 考察四氢呋喃,乙酸乙酯,二氯甲烷,N,N-二甲基乙酰胺四种溶剂对7-氨基-3-去甲基-3-头孢烷酸(7-ANCA)与2-(2-氨基4-噻唑基-2-甲氧亚胺乙酸苯并噻唑硫酯(AE活性酯)合成头孢唑肟酸收率的影响.结果 确立了较优合成工艺条件:以乙酸乙酯为溶剂,n(7.ANCA):n(AE活酯):n(三乙胺)=1:1.2:2时,产品收率91.8%,纯度99.85%(HPLC),产品质量符合药典标准.结论 此方法简捷、易于产业化.

关 键 词:头孢唑肟酸  7-氨基-3-去甲基-3-头孢烷酸  合成

Studies on the synthesis of ceftizoxime
Fu De-cai,Li Hang,Xu Cheng-bo,Cai Juan-juan,Chen Xing-he. Studies on the synthesis of ceftizoxime[J]. Chinese Journal of Antibiotics, 2011, 36(2)
Authors:Fu De-cai  Li Hang  Xu Cheng-bo  Cai Juan-juan  Chen Xing-he
Affiliation:Fu De-cai,Li Hang,Xu Cheng-bo,Cai Juan-juan and Chen Xing-he(College of Chemical & Pharmaceutical Engineering,Hebei University of Science and Technology,Shijiazhuang 050018)
Abstract:Objective To optimize the manufacturing process of ceftizoxime.Methods It was appreciated that the preparation of ceftizoxime by reaction of 7-amino-3-nor-3-cephem-4-carboxylic acid(7-ANCA) with 2-(2-aminothiazol-4-thiazolyl)-2-[[(Z)-methoxy]imino]acetic acid S-mercapto ben-zothiazolylester(activated ester) in different kind solvents,such as tetrahydrofuran,ethyl acetate,dichlor-omethane,N,N-dimethylacetamide.Results The optimum conditions were as follows: while using ethyl acetate as solvent,the molar rati...
Keywords:Ceftizoxime  7-amino-3-nor-3-cephem-4-carboxylic acid  Synthesis  
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