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利奈唑酮的合成研究 被引量：3

Study on the Synthesis of Linezolid
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摘要 以3,4-二氟硝基苯为原料,(R)-环氧氯丙烷作手性源,经亲核取代、还原、开环、环化、盖布瑞尔反应、胺解、酰化反应合成得到利奈唑酮,总收率29.3%,其结构经1H NMR和MS确证。 Linezolid was synthesized from 3,4-difluoronitrobenzene in an overall yield of 29.3% using（R）-epichlorohydrin as the chiral source. The structure of linezolid was identified with1H NMR and MS spectra.
作者 潘成迟 周晖 钟世华 徐广宇 雷卫平
机构地区 湖南师范大学化学化工学院 湖南康源制药有限公司
出处 《精细化工中间体》 CAS 2013年第5期23-25,29,共4页 Fine Chemical Intermediates
基金 湖南省校企合作人才培养示范基地(湘教通[2012]163号)项目
关键词 噁唑烷酮 利奈唑酮 工艺 合成 oxazolidinone linezolid synthesis!
分类号 TQ463.5 [化学工程—制药化工]
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参考文献10

  • 1Meagher A K, Forrest A, Rayner C A, et al. Population pharmacokinetics of linezolid in patients treated in a compassionate use program [J ]. Antimicrob Agents Chemother, 2003, 47 (2): 548-553.
  • 2Barbachyn M R. Bicyclic oxazine and thiazine oxazolidinone antibacterials: WO, 9615130[P]. 1996-06-23.
  • 3Fines M, Leclercq R. Activity of linezolid against grampositive cocci possessing genes conferring resistance to protein synthesis inhibitors[J].JAntimicrobChemother, 2000, 45 (4): 797-802.
  • 4Lin A H, Murray R W, Vidmar T J, et aL The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin [J ]. Antimicrob Agents Chemother, 1997, 41 (10): 2 127-2 131.
  • 5Shinabarger D L, Marotti K R, Murray R W, et al. Mechanism of action of oxazolidinones : effects of linezolid and eperezolid on translation reactions[J]. Antimicrob Agents Chemother, 1997, 41 (10): 2 132-2 136.
  • 6陈炜,胡建良,张兴贤.利奈唑胺合成路线图解[J].中国医药工业杂志,2010,41(1):62-63. 被引量：17
  • 7Mohan D D. Novel process for the preparation of linezolid and related compounds: US, 20080027219[P]. 2008-01-31.
  • 8Alla R M. Novel process for preparation of linezolid arid novel intermediates: WO, 2012114355[P].2012-02-21.
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  • 10Basoglu S, Yolal M, Demirbas A, etal. Synthesis of linezolid- like molecules and evaluation of their antimicrobial activities [J] Turkish Journal of Chemistry, 2012, 36 (1) : 37-53.

二级参考文献11

  • 1余德胜,王志谦,熊莺,赵燕芳,宫平.利奈唑酮合成新工艺[J].中国药物化学杂志,2005,15(2):89-90. 被引量：8
  • 2Swaney 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.
  • 3Aoki 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.
  • 4Brickner 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.
  • 5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).
  • 6Lohray 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.
  • 7Lohray BB, Chatterjee M, Jayamma Y. A practical approach.to the synthesis of dianhydro sugars [J]. Synth Commun, 1997, 27(10): 1711-1724.
  • 8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).
  • 9Moran-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.
  • 10Immordino RJ, Perrault WR, Reeder MR. Process for preparing linezolid: WO, 2007116284 [P]. 2007-10-18. (CA 2007, 147: 469356).

共引文献16

同被引文献30

引证文献3

二级引证文献5

精细化工中间体
2013年 第5期

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