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利奈唑酮合成新工艺 被引量:8

New synthetic method of linezolid
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摘要 目的寻找合成利奈唑酮的新工艺。方法以(R) 环氧氯丙烷和间氟苯基异氰酸酯为起始原料,经环化、叠氮化、还原、酰化、溴代、缩合反应得到利奈唑酮。结果与结论成功地合成出利奈唑酮,总收率由文献的11 .3%提高到4 3. 2 % ,而且操作简单,成本低廉。 Aim To find a new synthetic method of linezolid.Methods Starting with 3-fluorophenyl isocyanate and(R)-epichlorohydrin,linezolid was synthesized through cyclization,substitution,acylation,bromination,and condensation.Results and conclusion Linezolid was successfully synthesized in a total yield of 43.2% with the advantages of low cost and simple processing in comparison with the reported yield of 11.3%.
出处 《中国药物化学杂志》 CAS CSCD 2005年第2期89-90,93,共3页 Chinese Journal of Medicinal Chemistry
关键词 药物化学 化学合成 利奈唑酮 medicinal chemistry chemical synthesis linezolid
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  • 1Brickners SJ, Hutchinson DK, Barbachyn MR, et al.Synthesis and antibacterial activity of U-100766 and U-100592[J] .J Med Chem, 1996, 39(3):673 - 679.
  • 2孟庆国,刘浚.利奈唑酮的合成工艺改进[J].中国药物化学杂志,2003,13(1):28-30. 被引量:13

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同被引文献63

  • 1Guang Yu XU Yi ZHOU Man Cai XU.A Convenient Synthesis of Antibacterial Linezolid from (S)-Glyceraldehyde Acetonide[J].Chinese Chemical Letters,2006,17(3):302-304. 被引量:1
  • 2邹翠,周鲁.新型噁唑烷酮类抗菌药的研究进展[J].国外医药(抗生素分册),2006,27(4):187-192. 被引量:4
  • 3Swaney SM, Aoki H, Ganoza C, et al. The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria [J]. Antimicrob Agents Chemother, 1998, 42 (12) : 3251-3255.
  • 4Aoki H, Ke LZ, Poppe SM, et al. Oxazolidinone antibiotics target the P site on Escherichia coli ribosomes [J]. Antimicrob Agents Chemother, 2002, 46 (4): 1080-1085.
  • 5Brickner S J, Hutchinson DK, Barbachyn MR, et al. Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections [J]. JMed Chem, 1996, 39 (3) : 673-679.
  • 6徐广宇,吴希罕,谢毓元.N-[4(R)-(1,3-二噁烷基)甲基]苯胺、制备方法和用途:中国,100369909[P].2008-02-20.(CA2006,145:188857).
  • 7Lohray BB, Baskaran S, Rao BS, et al. A short synthesis of oxazolidinone derivatives linezolid and eperezolid : A new class of antibacteriais [J]. Tetrahedron Lett, 1999, 40(26) : 4855-4856.
  • 8Lohray BB, Chatterjee M, Jayamma Y. A practical approach.to the synthesis of dianhydro sugars [J]. Synth Commun, 1997, 27(10): 1711-1724.
  • 9黄强,李华,牛柏林,等.(R)-N-(3-氟-4-吗啉苯基)-噁唑酮-5-甲基醇制备工艺:中国,1772750[P].2006-05-17.(CA2006,145:62909).
  • 10Moran-Ramallal R, Liz R, Gotor V. Regioselective and stereospecific synthesis of enantiopure 1,3-oxazolidin- 2-ones by intramolecular ring opening of 2- (Bocarninomethyl) aziridines, preparation of the antibiotic linezolid [J]. Org Lett, 2008, 10 (10) : 1935-1938.

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