利奈唑酮的合成
金洁，孟庆国，刘浚，武燕彬
[摘要] 利奈唑酮为化学全合成噁唑烷酮类抗菌剂，对G+具有很强的抑制作用，与其他抗生素无交叉耐药。该类抗菌剂作用机理独特，抑制细菌蛋白质合成的最早阶段，而其他抗生素抑制蛋白质合成的最后阶段。本研究对文献合成方法中的三步反应进行了改进，成功合成出利奈唑酮。
[关键词] 噁唑烷酮，利奈唑酮，全合成
Synthesis of Linezolid
JIN Jie，MENG Qingguo，LIU Jun，WU Yanbin
(Institute of Medicinal Biotechnology, Chinese Academy of Medicinal Sciences,Peking Union Medical College, Beijing 100050 China)
[Abstract] Linezolid is synthetic oxazolidinone multi-drug resistant antibacterial agent that mainly inhibits gram-positive bacteria. It inhibit synthesis of bacteria protein in early stage, on the country other antibiotics inhibit in last stage. Three reactions of the method reported by literature have been modified and Linezolid has been successfully synthesized.
[Key words] oxazolidinone; Linezolid; total synthesis
[参考文献]
[1] Ford C W,Hamel J C,Wilson D W, et al.In vitro activities of U-100592 and U-100766,noval oxazolidinone antimicrobial agents ,against experimental bacterial infections [J]. Antimicrob Agents Chemther 1993,37(2): 377-9
[2] Jorgensen J H,McElmeen M L,Trippy C W. In vitro activities of the oxazolidinone antibiotics U-100592 and U-100766 agaainst Staphylococcus aureus and Coagulase-negative Staphylococcus species [J]. Antimicrob Agents Chemther， 1997,41(2): 465-7
[3] Brickners S J, Hutchinson D K, Barbachyn M R, et al. Synthesis and antibacterial activity of U-100766 and U-100592 [J]. J Med Chem 1996,39(3): 673-9
[4] Lizondo L,Rabasseda X,Castaner J. Lizezolid[J].Drugs of the Future1996,21(11): 1116-23, http://www.100md.com
[摘要] 利奈唑酮为化学全合成噁唑烷酮类抗菌剂，对G+具有很强的抑制作用，与其他抗生素无交叉耐药。该类抗菌剂作用机理独特，抑制细菌蛋白质合成的最早阶段，而其他抗生素抑制蛋白质合成的最后阶段。本研究对文献合成方法中的三步反应进行了改进，成功合成出利奈唑酮。
[关键词] 噁唑烷酮，利奈唑酮，全合成
Synthesis of Linezolid
JIN Jie，MENG Qingguo，LIU Jun，WU Yanbin
(Institute of Medicinal Biotechnology, Chinese Academy of Medicinal Sciences,Peking Union Medical College, Beijing 100050 China)
[Abstract] Linezolid is synthetic oxazolidinone multi-drug resistant antibacterial agent that mainly inhibits gram-positive bacteria. It inhibit synthesis of bacteria protein in early stage, on the country other antibiotics inhibit in last stage. Three reactions of the method reported by literature have been modified and Linezolid has been successfully synthesized.
[Key words] oxazolidinone; Linezolid; total synthesis
[参考文献]
[1] Ford C W,Hamel J C,Wilson D W, et al.In vitro activities of U-100592 and U-100766,noval oxazolidinone antimicrobial agents ,against experimental bacterial infections [J]. Antimicrob Agents Chemther 1993,37(2): 377-9
[2] Jorgensen J H,McElmeen M L,Trippy C W. In vitro activities of the oxazolidinone antibiotics U-100592 and U-100766 agaainst Staphylococcus aureus and Coagulase-negative Staphylococcus species [J]. Antimicrob Agents Chemther， 1997,41(2): 465-7
[3] Brickners S J, Hutchinson D K, Barbachyn M R, et al. Synthesis and antibacterial activity of U-100766 and U-100592 [J]. J Med Chem 1996,39(3): 673-9
[4] Lizondo L,Rabasseda X,Castaner J. Lizezolid[J].Drugs of the Future1996,21(11): 1116-23, http://www.100md.com