有机化学 ›› 2001, Vol. 21 ›› Issue (11): 862-868. 上一篇    下一篇

研究论文

具生物活性有机磷化合物的设计与合成

袁承业   

  1. 中国科学院上海有机化学研究所.上海(200032)
  • 发布日期:2001-11-25

Design and synthesis of biologically active organophosphorus compounds

Yuan Chengye   

  1. Shanghai Inst Organ Chem., CAS.Shanghai(200032)
  • Published:2001-11-25

对氨基膦酸及磷肽的合成作了研究,同时考察了引入二氟次甲基及三氟甲基的方法。在此基础上研究成功基于[1,2]不对称诱导及[1,3]质子转移反应的手性合成方法。对多官能团的氨基膦酸及磷肽也作了研究。此外还制备了具1,1-双膦酸基的多种碳环化合物,对含磷酰基,特别对既含磷酰基又含三氟甲基的多种杂环化合物的合成方法与反应机理进行了报导。

关键词: 氨基膦酸, 不对称反应, 三氟甲基, 磷酰化合物, 杂环化合物, 磷肽, 生物活性, 有机磷化合物, 分子设计, 合成

Synthetic study of biologically active organophosphorus compounds including aminophosphonic acids, phosphonopeptides, carbocyclic and hetereocyclic compounds bearing phosphonate moiety was reported. Based on [1, 2] asymmetric induced reaction or [1, 3] proton shift, a series of chiral aminophosphonic acids and their fluorinated derivations were resulted. Introduction of methylene 1, 1- bisphosphonic acid grouping to cyclopropane, cyclopentane as well as cyclic hexadiene usually creates powerful chelating ability of the parent molecule towarding metal ions. Thus, a group of new compounds with medicinal potentiality was reported.

Key words: PHOSPHOAMIDIC ACID, TRIFLUOMETHYL, PHOSPHORYL COMPOUNDS, HETEROCYCLIC COMPOUNDS, BIOLOGICAL ACTIVITY, ORGANO PHOSPHORUS COMPOUNDS, MOLECULAR DESIGN, SYNTHESIS

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