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利奈唑胺合成工艺的优化 被引量：6

Optimization of synthetic process of Linezolid
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摘要 利奈唑胺是新型化学全合成噁唑烷酮类抗菌药,本文通过研究对比,首先合成(S)-N-[2-(乙酰氧基)-3-氯丙基]乙酰胺和N-羰基苄氧-3-氟-4-吗啉基苯胺,利用缩合反应制备利奈唑胺的方法,经过一系列地优化,发现了适合工业化生产的工艺路线。 Linezolid is a novel chemical synthesis of oxazolidinone antibacterial drugs. This paper compared these reported literature and optimized its synthetic route. First, synthesis of （S）-N-[2 - （acetylaminooxy） -3 - chloropropyl] acetamide and N-carbonyl-benzyloxycarbonyl -3 - fluoro-4 - morpholinyl aniline, then by using the condensation reaction method of the above key intermediates to get high quality linezolid, after a series of optimization, a promising industrialization production process route was established.
作者 徐辉 汤有坚 魏丹
机构地区 浙江永宁药业股份有限公司
出处 《浙江化工》 CAS 2013年第2期10-13,共4页 Zhejiang Chemical Industry
关键词 噁唑烷酮 利奈唑胺 缩合 工艺优化 oxazolidnone linezolid condensation optimization
分类号 R914 [医药卫生—药物化学]
作者简介 徐辉（1981-），男，湖北荆门人，工程师，大学本科，毕业于武汉大学药学专业，研究方向：化学药物及中间体的合成。
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参考文献12

  • 1Aoki H, Ke L Z, Poppe S M, et al. Oxazolidinone antibiotics targe the P site on Escherichia coli ribosomes [J]. Antimicrob Agents Chemother,2002,46(4):1080-1085.
  • 2王鲁燕,陈代杰.噁唑烷酮类抗菌药物的研究[J].药学进展,2002,26(1):16-22. 被引量：9
  • 3何飚,张乐.噁唑烷酮类抗菌药物的合成[J].国外医药（抗生素分册）,2009,30(2):82-88. 被引量：8
  • 4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
  • 5张慧,杜鲲,桑志培,邓勇.利奈唑胺的合成[J].中国医药工业杂志,2011,42(4):245-247. 被引量：12
  • 6Junzo O, Yoshiro F, Hiroshi Y. Preparation of oxazolidin- 2-ones:JP,2003206282 [P].2003-07-22.
  • 7王萍,潘强彪,李杨州,等.一种利奈唑胺的制备方法及其中间体:中国,101774978[P].2010-07-14.
  • 8Brickner S J, Hutchinson D K, Barbachyn M R, et al. Synthesis and antibacterial activity of U-100592 and U- 100766, two oxazolidinone antibacterial agents for the potential treatment of muhidrug-resistant gram-positive bacterial infections [J].J Med Chem,1996,39(3):673-679.
  • 9Ramallal R M, Liz R, Gotor V. Regioselective and stereospecific synthesis of enantiopure 1,3-oxazolidin-2- ones by intramolecular ring opening of 2-(Boc- aminomethyl)aziridines. Preparation of the antibiotic linezolid [J]. Org Lett,2008,10(10):1935-1938.
  • 10黄强,李华,牛柏林,等.(rt)-N-(3-氟-4-吗啉苯基)-嗯唑酮-5-甲基醇制备工艺:中同,1772750[P].2006-05-17.

二级参考文献56

  • 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
  • 2Gregory W A. P-oxooxazolidinyl benzene compounds as antibacyerial agents: US 4461773[P]. 1984-07-24
  • 3Gregory W A, Brittelli D R, Wang C L, et al. Antibacterial. synthesis and structure-activity studies of 3-aryl-2-oxazolidinones. 1. the "B"group[J]. J Med Chem, 1989, 32(8): 1673
  • 4Barbachyn M R, Brickner S J, Hutchinson D K, et al. Substituted oxazine and thiazine oxazolidinone antimicrobials: US 5688792[P]. 1997-11-18
  • 5Brickner S J, Hutchinson D K, Barbachyn M R, et al. Synthesis and antibacterial aciticity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections[J]. J Med Chem, 1996, 39(3): 673
  • 6Stevens D L, Dotter B, Madaras-Kelly K. A review of linezolid: the first oxazolidinone Antibiotic[J]. Expert Rev Anti Infect Ther, 2004, 2(1): 51
  • 7Herweh J E, Kauffmann W J. 2-oxazolidones via The lithium bromide catalyzed reaction of isocyanates with epoxides in hydrocarbon solvents[J]. Tetra Lett, 1971, 12:809
  • 8Barbachyn M R, Brickner S J. Substituted aryl and heteroary-phenyl-oxazolidinones: US 5565571[P]. 1996- 10-15
  • 9Gregory W A, Brittelli D R, Wang C L, et al. Antibacterial synthesis and structure -activity studies of 3-aryl-2- oxazolidinones. 2. the "A"group[J]. J Med Chem, 1990, 33(9): 2569
  • 10Yu D, Huiyuan G. Synthesis and antibacterial activity of linezolid analogues[J]. Bioorg Med Chem Lett, 2002, 12(6): 857

共引文献34

同被引文献46

  • 1赵肖玉,马燕如,徐正.利奈唑胺合成工艺的改进[J].华西药学杂志,2007,22(2):179-181. 被引量：9
  • 2Lizondo L, Rabasseda X, Castaner J. Linezolid [J]. Drugs Future,1996,21(11):1116-1123.
  • 3Briekners S J, Hutchinson D K, Barbaehyn M R, et al. Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treament of multidrug-resistant gram-positive bacterial infectionsl-J]. Journal of Medicinal Chemistry, 1996,39 (3) : 673-679.
  • 4Ford C W, Hamel J C, Wilson D M, et al. In vitro activities of U-100592 and U-100766, noveloxazolidinone antimicrobial agents, against experimental bacterial infections [J]. Antimierobial Agents and Chemotherapy,1996,40 (6) : 1508-1513.
  • 5Jorgensen J H, McElmeen M L, Trippy C W. Invitroactivities of the oxazolidinone antibiotics U-100592 and U- 100766 against staphylococcus aureus and coagulase-negative staphylococcus speeies[-J]. Antimierobial Agents and Chemotherapy, 1997,41 (2) : 465-467.
  • 6Perrault W R, Pearlman B A, Godrej D B, et al. The synthesis of N-aryl-5-(S)-aminomethyl-2-oxazolidinoneantibacterials and derivatives in one step from arylcarbamates[J]. Organic Process Research - Development,2003,7(4):533-546.
  • 7Ross J E,Anderegg T R,Sader H,et al.Trends in linezolid susceptibility patterns in 2002:report from the worldwide Zyvox annual appraisal of potency and spectrum program[J].Diagostic Microbiology and Infection Disease,2005,52:53-58.
  • 8Aoki H,Ke L Z,Poppe S M,et al.Oxazolidinone antibiotics targe the P site on Escherichia coli ribosomes[J].Antimicrob Agents Chemother,2002,46(4):1080- 1085.
  • 9法玛西雅厄普约翰美国公司.取代的噁嗪和噻嗪噁唑烷酮抗微生物剂:CN,20001130379[P].2000-10-04.
  • 10Mohan R,Dodda.Novel intermediates for linezolid and related compounds:WO,2006 008754[P].2006-01-26.

引证文献6

二级引证文献6

浙江化工
2013年 第2期

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