申请人:Deutsches Krebsforschungszentrum Stiftung des offentlichen Rechts
公开号:US05622936A1
公开(公告)日:1997-04-22
The invention relates to a method for the preparation of glycoconjugates of phosphorus amides with the general formula ##STR1## where the connection of the sugar with the phosphoric acid amide mustard residue, and the ifosfamide mustard residue, respectively, occurs preferably in the 1-position, and where R.sub.1 and R.sub.2 ; which can be the same or different, denote hydrogen, lower C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.6 haloalkyl and where as sugar there can be present mono-, di-, or polysaccharides in all existing isomeric and enantiomeric forms, wherein in a known way protected brominated sugars are conjugated with the respective phosphorus compounds, and freed of the protective residues, and to the use of said compounds as anti-tumour drugs.
本发明涉及一种制备磷酰胺糖结合物的方法,其通式为##STR1##其中糖与磷酸酰氮芥残基和伊福沙胺酰氮芥残基的连接,分别优选在1位发生,其中R.sub.1和R.sub.2;可以相同也可以不同,表示氢、较低的C.sub.1-C.sub.4烷基或C.sub.1-C.sub.6卤代烷基,而作为糖的单糖、双糖或多糖可以存在于所有已知的异构体和对映体形式中。在已知的方法中,保护溴化糖与相应的磷化合物结合,并去除保护基残基,以及将所述化合物用作抗肿瘤药物。