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青霉烯类抗生素Men-10700的合成 被引量：1

Synthesis of Men-10700
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摘要 目的:合成新型青霉烯类抗生素Men-10700。方法:以4-乙酰氧基氮杂环丁-2-酮为起始原料,经取代、关环、生成目标侧链、脱保护基等8步合成目标化合物。结果与讨论:经1H-NMR,MS证明得到了Men-10700;其中改用对硝基苄基保护羧基,简化了后处理过程,对引入侧链和脱硅氧保护基2个步骤作了改进。 Objective： To synthesize the new Penem Men-10700. Methods： Starting from Azetidinone, the Men-10700 was synthesized via 8-step reactions, including substitution, cyclization, side chain coupling and hydrolysis. Results： The chemical structure of the Men-10700 was confirmed by ^1 H- NMR and MS. Conclusion： The modified synthetic pathway for MEN-10700 was achievable. The refined procedure is simplified by using p-nitrobenzyl as protecting group of carboxyl, the post processing was simplified. We improved the processes of substitution and hydroxysis.
作者 陈晓芳 韩红娜 李浩 刘浚
机构地区 中国医学科学院中国协和医科大学医药生物技术研究所
出处 《中国新药杂志》 CAS CSCD 北大核心 2007年第5期385-387,共3页 Chinese Journal of New Drugs
关键词 青霉烯类抗生素 Men-10700 药物合成 penem Men-10700 synthesis
分类号 R978.11 [医药卫生—药品] R914.5 [医药卫生—药物化学]
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参考文献7

  • 1FONTANA R,ALTAMURA M,ARCAMONE F,et al.Men10700,a new penem antibiotic:in-vitro activity and its correlation with beta-lactamase stability,PBP affinity and diffusion through the bacterial cell wall[J].J Antimicrob Chemother,1998,41 (5):513 -525.
  • 2HAMILTON-MILLER JM,SHAH S.Comparative anti-anaerobic activity of Men 10700,a penem antibiotic[J].Int J Antimicrob Agents,1998,10(4):321 -324.
  • 3VAROTTO F,PARRAVIDINI E,DE-LUCA M,et al.In vitro antibacterial activity of Men 10700,a new penem antibiotic[J].Chemotherapy,1999,45 (6):405-410.
  • 4HAMILTON-MILLER JM,SHAH S.In-vitro microbiological assessment of a new penem,Men 10700[J].J Antimicrob Chemother,1997,39(5):575 -584.
  • 5ALTAMURA M,PERROTTA E,SBRACI P,et al.2-substituted penems with amino acid-related side chains:synthesis and antibacterial activity of a new series of β-lactam antibiotics[J].J Med Chem,1995,38 (21):4244-4256.
  • 6陈晓芳,韩红娜,李浩,刘浚.2-羟甲基-青霉烯-3-羧酸对硝基苄酯的制备[J].中国药物化学杂志,2004,14(6):354-356. 被引量：2
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二级参考文献6

  • 1Saito A,Kawakami Y,Yamaguchi E,et al.Comparative study on the efficacy of ritipenem acoxil and cefotialhexetil in chronic lower respiratory tract infections by the double blind method[J].Jpn J Antibiot,1996,49(3):219-249.
  • 2Varotto F,Parravidini E,De Luca M,et al.In vitro antibacterial activity of men 10700,a new penem antibiotic[J].Chemotherapy,1999,45(6):405-410.
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  • 4Kawamoto I,Endo R,Suzuki K,et al.Efficient syntheses of a new penem antibiotic,sodium(5R,6S)-2-(2-fluoroethylthio)-6-[(1R)-1-hydroxyethyl]penem-3-carboxylate[J].Heterocycles,1987,25:123-128.
  • 5Corraz AJ,Dax SL,Dunlap NK,et al.Dual-action penems and carbapenems[J].J Med Chem,1992,35:1828-1839.
  • 6Cabri W,Candiani H,Zarini F,et al.Zinc halides-mediated nucleophilic attack of thioacid salts in non protic media.A key step in the total synthesis of penems[J].Tetra Lett,1994,35(20):3379-3382.

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中国新药杂志
2007年 第5期

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