Esters Of Glucuronide Prodrugs Of Anthracyclines And Method Of Preparation And Use In Tumor-Selective Chemotherapy
申请人:Aben Rene Wilhelmus Marie
公开号:US20090227617A1
公开(公告)日:2009-09-10
The invention relates to novel esters and in particular to some novel esters of glucuronide prodrugs of anthracyclines having tunable water-solubility, their synthesis and use in tumor-selective chemotherapy. It appeared that in the final step in the synthesis of these prodrugs, i.e. the coupling of the glucuronide spacer moiety to the parent drug molecule, protection of the sugar hydroxyls is, surprisingly, no longer required. A process for the preparation of these unprotected sugar spacer moieties is also disclosed.
该发明涉及新型酯类化合物,特别是一些新型葡萄糖醛酸盐前药的酯类化合物,其具有可调节的水溶性,以及它们在肿瘤选择性化疗中的合成和应用。在这些前药的合成的最后一步中,即将葡萄糖醛酸盐间隔基与母药分子偶联时,令人惊讶的是,不再需要保护糖羟基。还公开了一种制备这些未保护糖间隔基的过程。