Esters of glucuronide prodrugs of anthracyclines and method...

C - Chemistry – Metallurgy – 07 – H

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C07H 15/252 (2006.01) A61K 31/704 (2006.01) A61P 35/00 (2006.01) C07H 13/12 (2006.01)

Patent

CA 2657526

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.

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