期刊文献+

头孢匹胺的合成工艺研究 被引量:2

Studies on Synthetic Process of Cefpiramide
原文传递
导出
摘要 目的:探讨第3代头孢类抗菌药物——头孢匹胺的合成工艺。方法:以4-羟基-6-甲基-2-吡喃酮为原料合成(2R)-2-[(4-羟基-6-甲基-3-吡啶)甲酰胺基]-2-(4-羟基苯基)乙酸,再与侧链(6R,7R)-3-[(-甲基-1H-四唑-5-基)硫基]-7-氨基-8氧代-5-硫杂-1-氮杂双环[4,2,0]辛-2-烯-2-羧酸(7-ACA-MMT)反应合成得最终产品头孢匹胺。结果:反应总收率为19.42%,化合物经过核共振氢谱(1H-NMR)、红外图谱(IR)确证结构为头孢匹胺。结论:头孢匹胺的合成工艺确定增强了产率,提高了效率。 Objective:To study the synthetic process of cefpiramide in the 3 rd generation cephalosporin antibiotic drugs.Methods:Using 4-hydroxyl-6-methyl-2-pyrone as raw materials,(2R)-2-[4(-hydroxyl-6-methyl-3-pyridine)carboxamide]-2-(4-hydroxyl phenyl)acetic acid was produced,then condensation was conducted with(6 R,7 R)-3-[(methyl-1H-tetrazole-5)sulfenyl]-7-amino-8-oxo-5-thio-1-azabicyclo-[4,2,0]-2-octylene-2-carboxylic acid,and cefpiramide was synthesized.Results:The total yield of reactants was 19.42%,and structure of product was characterized by 1H-NMR,and IR.Conclusion:The synthesis process 1 of cefpiramide described here has advantages of high yield and efficiency.
作者 周艺海
出处 《抗感染药学》 2010年第3期194-196,共3页 Anti-infection Pharmacy
关键词 头孢匹胺 抗菌药物 核磁共振氢谱 红外图谱 合成工艺 cefpiramide antibacterial agents H-NMR IR synthetic process
  • 相关文献

参考文献4

二级参考文献52

  • 1王飞,林善良.硫酸头孢匹罗的合成[J].中国医药工业杂志,2005,36(8):455-456. 被引量:12
  • 2赵美法.头孢中间体GCLE的生产与发展前景[J].精细化工原料及中间体,2005(11):26-30. 被引量:3
  • 3邵意阳,屈一新,任慧.硫酸头孢喹肟的合成[J].中国医药工业杂志,2007,38(6):405-406. 被引量:10
  • 4Macher I, Widschwenter G. Production of cefotaxime and new sodium salts [P]. US: 5831086, 1998-11-03.
  • 5Schwab W, Duerckheimer W, Rirrstetter R, et al. Process for the preparation of cephem compounds[P] .US: 4667028, 1987-05-19.
  • 6Lattrell R, Blumbach J, Duerckheimer W, et al. Synthesis and structure-activity relationships in the cefpirome series. Ⅰ.7- [ 2- (2-Aminothiazol-4-yl) -2- (Z) -oxyimino-aeetamido ] -3- [ (substituted-l-pyridino) methyl] -ceph-3-em-4-carboxylates [J]. JAntibiot, 1988, 41(10): 1374 - 1394.
  • 7Walker D G, Brodfuehrer P R, Brundidge S P, et al. Use of bistrimethylsilylate intermediates in the preparation of semisynthetic 7-amino-3-substituted cephems. Expedient syntheses of a new 3 - [ ( 1 -methyl- 1 -pyrrolidinio) methyl ] cephalosporin [ J ]. J Org Chem, 1988,53(5): 983 N991.
  • 8Duerckheimer W, Lattrell R. Crystalline cephem-acid addition salts and processes for their preparation[P]. US: 4609653, 1986-09-02; DE: 3248281, 1982-12-28. (CA 1984, 101:198194).
  • 9Takaya T, Takasugi H, Masugi T, et al. 7 - Acylamino - 3 -vinyl cephalosporanic acid derivatives and processes for the preparation thereof: US, 4409214 [ P ]. 1983 - 08 - 11.
  • 10Ascher G. Process for the production of known 2 - oximinoacetamido - 3 - cephem - 4 - carboxylic derivatives comprising acylation of 7 - amino - 3 - cephem -4 -carboxylic acid derivatives with novel 2 - oximinoacetic acid thio esters, as well as such thioesters and their production: US,4767852 [ P ]. 1988 - 08 - 30.

共引文献11

同被引文献9

引证文献2

二级引证文献6

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部