具生物活性有机磷化合物的设计与合成  

Design and Synthesis of Biologically Active Organophosphorus Compounds

作　　者：袁承业[1] 

机构地区：[1]中国科学院上海有机化学研究所，上海200032

出　　处：《有机化学》2001年第11期862-868,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金

摘　　要：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.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.

关 键 词：氨基膦酸 磷肽 手性合成 磷酰基 生物活性 有机磷化合物 杂环化合物 设计 

分 类 号：O627.51[理学—有机化学]