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头孢匹罗的合成
引用本文:程冬萍,于文博,夏成才,颜继忠. 头孢匹罗的合成[J]. 应用化工, 2006, 35(3): 183-184
作者姓名:程冬萍  于文博  夏成才  颜继忠
作者单位:浙江工业大学,药学院,浙江,杭州,310014
摘    要:丙炔胺和环戊酮在无水乙醇中回流反应5 h生成2,3-环戊烯并吡啶,收率55%。7-氨基头孢烷酸和2-甲氧亚氨基-2-(2-氨基-4-噻唑基)-(z)-硫代乙酸苯胼噻唑酯(AE活性酯)发生酰化反应生成头孢噻肟酸,收率90%。在三甲基碘硅烷作用下,头孢噻肟酸与2,3-环戊烯并吡啶反应,生成头孢匹罗,收率65%1。H NMR对产物及中间体进行了鉴定。

关 键 词:头孢匹罗  丙炔胺  2,3-环戊烯并吡啶  AE活性酯  合成
文章编号:1671-3206(2006)03-0183-02
收稿时间:2006-02-15
修稿时间:2006-02-15

Synthesis of cefpirome
CHENG Dong-ping,YU Wen-bo,XIA Cheng-cai,YAN Ji-zhong. Synthesis of cefpirome[J]. Applied chemical industry, 2006, 35(3): 183-184
Authors:CHENG Dong-ping  YU Wen-bo  XIA Cheng-cai  YAN Ji-zhong
Affiliation:College of Pharmaceutical, Zhejiang University of Technology, Htmgzhou 310014, China
Abstract:2,3-Cyclopentenopyridine was prepared by reaction of cyclopentanone and propargylamine in absolute ethanol,refluxing 5 h,the yield was 55%.Cefotaxime acid was synthesized by 7-ACA and AE active ester,the yield was 90%.Then,in the presence of trimethyliodosiliane,cefpirome was obtained through the reaction of cefotaxime acid and 2,3-cyclopentenopyridine,the yield was 65%.The structure of target substance and intermediate were determined by ~1H NMR.
Keywords:cefpirome  propargylamine  2  3-cyclopentenopyridine  AE active ester  synthesis
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