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Ugi四组分缩合反应合成肽核酸单体

王文浩, 张婷, 徐萍*   

  1. 北京大学药学院药物化学系, 北京 100083
  • 收稿日期:2003-01-05 修回日期:2003-05-10 出版日期:2003-06-15 发布日期:2003-06-15
  • 通讯作者: 徐萍*

Synthesis of PNA Monomer by Ugi Four-Component Condensation Reaction

WANG Wen-hao, ZHANG Ting, XU Ping*   

  1. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China
  • Received:2003-01-05 Revised:2003-05-10 Online:2003-06-15 Published:2003-06-15
  • Contact: XU Ping*

摘要: 目的 为了改善肽核酸的理化和生物学性质, 对经典肽核酸的结构进行衍生化和修饰. 方法 采用Ugi四组分缩合反应进行PNA单体的合成并采用Fmoc的保护策略. 结果 合成了Fmoc保护的PNA单体和关键组分异腈. 结论 建立了一种简单, 灵活多变的合成PNA单体的方法.

关键词: 肽核酸, Ugi反应, 单体, 异腈

Abstract: Aim To improve the physico-chemical and biological properties, original PNAs were derivatized and modified; Methods Ugi four-component condensation reaction (Ugi 4-CC) was used to synthesize PNAs, in which the Fmocprotecting strategy was adopted; Results The Fmoc-protected PNA monomer and the key component isocyanide were synthesized; Conclusion A simple and changeable method for synthesis of PNA monomer has been developed.

Key words: peptide nucleic acids PNAs, peptide nucleic acids PNAs, Ugi reaction, Ugi reaction, monomer, monomer, isocyanide, isocyanide

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Supporting: Foundation item: National Major Program for Basic Research Development (973 Projects) from the Ministry of Science and Technology of China (G1998051114).
*Corresponding author. Tel.: 010-62091505