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硫酸头孢匹罗的合成 被引量:12

Synthesis of Cefpirome Sulfate
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摘要 7-ACA与苯并噻唑硫醇活性酯反应得到头孢噻肟,在三甲基碘硅烷的作用下与环戊烷并[b]吡啶进行3-位取代得到头孢匹罗二氢碘酸盐,阴离子交换树脂除去碘离子得到的头孢匹罗游离碱再与硫酸成盐,得到抗菌剂硫酸头孢匹罗,总收率45%。 Acylation of 7-ACA with S-benzothiazol-2-yl2-(2-aminothiazol-4-yl) (methoxyimino) thioacetate (MAEM) afforded cefotaxime, which underwent 3-substitution by cyclopentano [b] pyridine and then salt formation using KI/HCI to obtain cefpirome dihydroiodide followed by salt exchange with sulfuric acid to give cefpirome sulfate in 45% overall yield.
作者 王飞 林善良
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2005年第8期455-456,共2页 Chinese Journal of Pharmaceuticals
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参考文献4

  • 1Schwab W, Duerckheimer W, Rirrstetter R, et al. Process for the preparation of cephem compounds [P]. US: 4667028,1987-05-19; DE: 3316798, 1984-11-08. (CA 1985, 102:113174)
  • 2Lattrell 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) -oxyiminoacetamido]-3-[ (substituted-1-pyridino) methyl]-ceph-3-em-4-carboxylates[J]. JAntibiot, 1988, 41 (10): 1374-1394.
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同被引文献58

  • 1于文博,程冬萍,夏成才,颜继忠.头孢匹罗的合成进展[J].化学与生物工程,2005,22(3):4-6. 被引量:7
  • 2孟红,赵平,刘志友.盐酸头孢吡肟合成方法的改进[J].中国抗生素杂志,2005,30(8):469-472. 被引量:4
  • 3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. 被引量:7
  • 4张致平.合成、半合成抗生素研究的进展[J].中国抗生素杂志,1996,21(A00):47-61. 被引量:16
  • 5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
  • 6段学民,郑鹏武,许艳杰,等.一种头孢匹罗及其类似物的合成新工艺:CN,200510110098.7[P].2006-05-17.
  • 7LATTRELL R, BLUMBACH J, DUERKHEIMER W, et al. Synthesis and structure-activity relationships in the cefpirome series Ⅰ[J]. J Antibiot, 1988, 41(10) : 1374 - 1394.
  • 8Macher I, Widschwenter G. Production of cefotaxime and new sodium salts [P]. US: 5831086, 1998-11-03.
  • 9Schwab W, Duerckheimer W, Rirrstetter R, et al. Process for the preparation of cephem compounds[P] .US: 4667028, 1987-05-19.
  • 10Lattrell 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.

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