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抗病毒药物普来可那利的合成 被引量：1

Synthesis of Antiviral Agent Pleconaril
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摘要 Starting from 2,6-dimethyl phenol,antiviral agent pleconaril was synthesized via bromination,cyanidation and etherification followed by reaction with acetaldehyde oxime,hydroxylamine hydrochloride and trifluoroacetic anhydride respectively.Its structure was confirmed by IR,MS, 1 HNMR and elemental analysis. Starting from 2,6-dimethyl phenol,antiviral agent pleconaril was synthesized via bromination,cyanidation and etherification followed by reaction with acetaldehyde oxime,hydroxylamine hydrochloride and trifluoroacetic anhydride respectively.Its structure was confirmed by IR,MS, 1 HNMR and elemental analysis.
作者 吴艳俊 朱崇泉 张奕华 王巍
机构地区 中国药科大学新药研究中心 江苏吴中苏药医药开发有限责任公司 中国药科大学
出处 《中国药科大学学报》 CAS CSCD 北大核心 2004年第5期478-480,共3页 Journal of China Pharmaceutical University
关键词 抗病毒药物 鼻病毒 治疗 鼻分泌物 病毒衣壳 肠病毒 药物口服 发生 药物浓度 诱导 Pleconaril Antiviral agents Synthesis
分类号 TQ463 [化学工程—制药化工]
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参考文献4

  • 1Romero JR.Pleconaril:a novel antipicornaviral drug[J].Expert Opin Investig Drugs, 2001,10(2):369-379.
  • 2Diana GD,Nitz TJ.EP 566199,1993,10,20.
  • 3Friedman L,Shechter H.Dimethylformamide as a useful solvent in preparing nitriles from aryl halides and cuprous cyanide;improved isolation techniques[J].J Org Chem, 1961,26(7):2522-2524.
  • 4Bruice TC,Kharasch N,Winzler RJ,et al.The synthesis of some new thyroxine analogs[J].J Org Chem,1953,18(1):83-91.

同被引文献11

  • 1Whiteman SC, Spiteri MA. IFN-gamma regulation of ICAM - 1 receptors in bronchial epithelial cells: soluble ICAM- 1 release inhibits human rhinovirus infection [ J ]. J Inflamm ( Lond ), 2008,5(8) :1 -16.
  • 2Schiff GM, Sherwood JR. Clinical activity of pleconaril in an experimentally induced coxsackievirus A21 respiratory infection [J]. J Infect Dis ,2000,181( 1 ) :20 -26.
  • 3Shih SR, Chen SJ, Hakimelahi GH,et al. Selective human entero- virus and rhinovirus inhibitors : an overview of capsid-binding and protease-inhibiting molecules [ J ]. Med Res Rev, 2004,24 ( 4 ) : 449 - 474.
  • 4Zhang Y, Simpson AA, Ledford RM, et al. Structural and virologi- cal studies of the stages of virus replication that are affected by antirhinovirus compounds [ J ]. J Virol, 2004,78 ( 20 ) : 11 061 - 11 069.
  • 5Rotbart HA. Pleconaril treatment of enterovirus and rhinovirus infections[ J]. Infect Med,2000,17(7 ) :488 -494.
  • 6Kearns GL, Abdel-Rahman SM, James LP, et al. Single-dose pharmacokinetics of a pleconaril ( VP63843 ) oral solution in children and adolescents [ J ]. Antimicrob Agents Chemother, 1999,43 (3) :634 - 638.
  • 7McKinlay MA, Pevear DC, Rossmann MG. Treatment of the picor- navirus common cold by inhibitors of viral uncoating and attach- ment[ J ]. Annu Rev Microbiol, 1992,46:635 - 654.
  • 8Bruice TC, Kharasch N, Winzler R J, et al. The synthesis of some new thyroxine analogs [ J ]. J Org Chem, 1953,18 ( 1 ) : 83 - 91.
  • 9Friedman L, Shechter H. Dimethylformamide as a useful solvent in preparing nitriles from aryl halides and cuprous cyanide; improved isolation techniques [ J ]. J Org Chem, 1961,26 ( 7 ) : 2 522-2 524.
  • 10Diana GD, Volkots DL, Nitz TJ, et al. Oxadiazoles as ester bioisosteric replacements in compounds related to disoxaril. Antirhinovirus activity [ J ]. J Med Chem, 1994,37 ( 15 ) :2 421 - 2 436.

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中国药科大学学报
2004年 第5期

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