头孢他美酯的合成实验研究An Experimental Study on Synthesis of Cefetamet Pivoxil
罗喜荣,蒋翠兰,罗小美
LUO Xi-rong1,JIANG Cui-lan2,LUO Xiao-mei3(1.Department of Organic Chemistry
摘要(Abstract):
目的:探讨以头孢他美与特戊酸碘甲酯为原料,合成头孢他美特戊酰氧甲酯路线的可行性,研究原料配比、催化剂、反应温度、反应时间等因素对实验结果的影响。方法:在极性非质子性溶剂N,N-二甲基甲酰胺溶液中,在一定反应温度和反应时间下,用碱作催化剂,以头孢他美与特戊酸碘甲酯为原料,合成头孢他美特戊酰氧甲酯,并优化反应条件。结果:在极性非质子性溶剂N,N-二甲基甲酰胺溶液中,在三乙胺催化下,反应温度20~23℃,以头孢他美与特戊酸碘甲酯为原料,合成头孢他美特戊酰氧甲酯的路线是最佳合成路线,收率可达84%。结论:原料配比、碱、反应温度、反应时间等因素对产品质量、色泽、收率有很大影响。
Objective:To investigate the synthesis route of cefetamet pivoxil from iodomethyl pivalate and cefetamet and affecting factors.Methods:Cefetamet pivoxil was synthesized from iodomethyl pivalate and cefetamet in the N,N-dimethylformamide solution,with the presence of base and at 0-40 ℃.Results:Optimum conditions for cefetamet pivoxil synthesis was summarized that the ratio of iodomethyl pivalate to cefetamet was 0.5∶1 in the N,N-dimethylformamide solution,with the presence of Et3N,and the reaction temperature was 20-23 ℃.The objective compound was obtained by 84% of the total yield.Conclusion:Quality,color and yield of cefetamet pivoxil are affected by material ratio,catalyst,temperature and reaction time.
关键词(KeyWords):
抗生素类;温度;时间;碱类;特戊酸碘甲酯;头孢他美酯
antibiotics;temperature;time;alkalies;iodometyl pivalate;cefetamet pivoxil
基金项目(Foundation):
作者(Author):
罗喜荣,蒋翠兰,罗小美
LUO Xi-rong1,JIANG Cui-lan2,LUO Xiao-mei3(1.Department of Organic Chemistry
DOI: 10.19367/j.cnki.1000-2707.2006.05.007
参考文献(References):
- [1]StoeckelK,TamYK,KneerJ.Pharmacokineticesoforalcefe-tametpivoxil(Ro-15-8075)andintravenouscefetamet(Ro-15-8074)inhumansareview[J].Curr Med Res Opin,1989,11(7):432.
- [2]Heymes Rene,Lutz Andre.Alkyloximes of7-amino-thia-zolyl-acetamido-cephalosporanic acids[P].US4396618,1983-08-02.
- [3]Ochiai Michihi Ro,Morimoto Akira,Matsuchita Yoshihiro.7[-2-(2-Aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporins[P].US4278671,1981-07-14.
- [4]宫平,王钝,邹鹏,等.头孢他美特戊酰氧甲酯的合成[J].中国药物化学杂志,1998,8(2):139-140.
- [5]刘家健,刘敦弗,曾晓辉,等.国产盐酸头孢他美酯的制备[J].中国抗生素杂志,2001,26(2):151-152.
- [6]Mitsuo Numata,Minamida,Masayoshi Yamaka,et al.New cephalosporins with7-acyl groups derived fromβ-ketoacids[J].J Antiobiot,1978(31):1252-1262.
- [7]Ishizuka Kenzo.Antibiotic composition[P].JP53029936,1978-03-20.
- [8]Naito Kenzo.Cephalosporin derivatives and their prepara-tion[P].JP53029913,1978-03-20.
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