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新型抗菌药利奈唑胺合成的研究 被引量:7

Study on Synthesis of A Novel Chiral Antibacterial Drug Linezolid
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摘要 报道了新型手性抗菌药利奈唑胺的合成研究。以3,4-二氟硝基苯和(S)-环氧氯丙烷为原料,分别合成两个中间体N-苄氧羰基-3-氟-4-吗啉基苯胺和(R/S)-N-(2,3-环氧丙基)乙酰胺,通过汇聚式合成得到利奈唑胺,总收率约29%。目标产物结构经1 HNMR和质谱确证。 This paper deals with the study on the synthesis of a novel chlral antibacterial arug llnezolla. , ne interaediates N-benzyloxycarbonyl-3-fluoro-4-moropholinyl aniline (Ⅲ ) and (R/S)-N-(2,3-epoxypropyl) ac- etamide(Ⅶ) was respectively synthesized from 3,4-difluoronitrobenzene and (S)-epichlorohydrin. Then the typical representative of antibacterial drug linezolid was convergently synthesized by Ⅲ andⅦ with an overall yield of 29%. The structure of target compound was confirmed by 1^HNMR and MS.
出处 《化学与生物工程》 CAS 2013年第1期57-59,共3页 Chemistry & Bioengineering
关键词 利奈唑胺 噁唑烷酮 新型抗菌药 合成 linezolid oxazolidinone novel chiral antibacterial drug synthesis
作者简介 李桂杰(1986-),男。湖北麻城人,硕士研究生,研究方向:药物化学.E—mail:lgjdyxo@163.com; 通讯作者:赵静国,副教授。
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参考文献7

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二级参考文献43

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共引文献18

同被引文献62

  • 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
  • 2BRICKNER S J, HUTCHINSON D K, BAR- BACHYN M R, et al. Synthesis and antibacterial ac- tivity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of mul- tidrug-resistant gram-positive bacterial infections [J]. Journal of Medicinal Chemistry, 1996, 39 (3): 673-679.
  • 3黄强,李华,牛柏林,等.(R)-N-(3-氟-4-吗啉苯基)-嗯唑酮-5-甲基醇制备工艺:中国,1772750[P].2006-05-17.
  • 4MORAN-RAMALLAL R, LIZ R, GOTOR V. Regi- oseleetive 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]. Organic Letters, 2008, 10 (10) : 1935-1938.
  • 5PERRAULT W R, PEARLMAN B A, GODREJ D B. Process to prepare oxazolidinones: WO, 02085849[P]. 2002-10-31.
  • 6中国药典2015年版.四部[S].2015:518.
  • 7朱德妹,张婴元,周乐,吴培澄,胡付品,吴卫红,吴湜,汪复.利奈唑胺的体外抗菌作用研究[J].中国感染与化疗杂志,2008,8(2):81-88. 被引量:62
  • 8崔向丽,赵志刚.新型噁唑烷酮类抗生素利奈唑胺[J].中国新药杂志,2008,17(6):530-533. 被引量:88
  • 9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
  • 10杨曦,朱曼,孙艳,张静.利奈唑胺致血小板减少1例[J].中国药物应用与监测,2009,6(2):128-128. 被引量:15

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