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头孢他美酯的合成实验研究 被引量:1

An Experimental Study on Synthesis of Cefetamet Pivoxil
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摘要 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.
出处 《贵阳医学院学报》 CAS 2006年第5期403-405,共3页 Journal of Guiyang Medical College
关键词 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
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  • 1StoeckelK, TamYK, KneerJ. Pharmacokineticesoforalcefetametpivoxil ( Ro-15-8075 ) andintravenouscefetamet ( Ro- 15-8074) inhmnansareview [ J]. Curr Med Res Opin, 1989,11(7) :432. 被引量:1
  • 2Heymes Rene, Lutz Andre. Alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids [ P ]. US4396618, 1983 - 08 - 02. 被引量:1
  • 3Ochiai Michlhi Ro, Morimoto Akira, Matsuchlta Yoshihiro. 7 [-2- (2-Aminothiazol-4-yl)-2- (syn) -methoxyiminoacetamido ] cephalosporins[P]. US4278671, 1981 -07 - 14. 被引量:1
  • 4宫平,王钝,邹鹏,王燕鹏.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. 被引量:9
  • 5刘家健,刘敦茀,曾晓辉,游莉.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. 被引量:9
  • 6Mitsuo Numata, Minamida, Masayoshi Yamaka, et al. New cephalosporins with 7-acyl groups derived from β-ketoacids [J]. J Antiobiot,1978 (31) :1252 - 1262. 被引量:1
  • 7Ishizuka Kenzo. Antibiotic composition [ P ]. JP53029936, 1978 - 03 - 20. 被引量:1
  • 8Naito Kenzo. Cephalosporin derivatives and their preparation[ P]. JP53029913,1978 - 03 - 20. 被引量:1

二级参考文献6

  • 1Stoeckel K, Tam Y K, Kneer J.Pharmacokinetices of oral cefetamet pivoxil (Ro-15-8075) and intravenous cefetamet(Ro-15-8074) in humans a review [J]. Curr Med Res Opin,1989;11(7):432 被引量:1
  • 2Michihiko O, Akira M, Yoshihiro M. Cephalosporin-derivate, verfahren Zu ihrerHerstellung und sie enthaltende Arzneimittel [P]. DT 2715385 A1,1977 被引量:1
  • 3Andr′e F, Urs W. Verfahren zur Herstellung von Carbonsureamiden [P]. EP,0231845,A2,1987 被引量:1
  • 4Yoshimura Y, Hamaguchi N. Yashiki T. Synthesis and relationship betweenphysicochemical properties and oral absorption ofpivaloyloxymethyl esters of parenteralcepha-losporins [P]. Int J Pharm,1985;23:117 被引量:1
  • 5Iyer R P, Phillips L R, Biddle J A et al. Synthesis of acyloxyalkylacylphosphonates as potential prodrugs of the antiviral trisodium phosphonoformate [J].Tetrahedron Lett,1989;30(51):7141 被引量:1
  • 6Iyer R P, Yu D, Ho N H, et al. Synthesis of iodoalkylacylates and their use in thepreparation of S-alkyl phosphorothiolates [J]. Synthetic Commun,1995;25(18):2739 被引量:1

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