The Design And Synthesis Of Water-soluble Prodrug Of Taxanes

Objective:The design and synthesis of water-soluble prodrug oftaxanes;Methods: Paclitaxel and docetaxel were esterified withN,N-dimethyl-2-methoxyl-aminobutanoyl chloride hydrochloride in thepresence of DMAP to get the target products;Results:The target products were identified by mass spectrum andNMR;Conclusion:The target compounds showed a good water-solubility,the initial experiments in serum indicated that the metabolites of targetproducts contained active compounds and the target products were betterthan previous products on decomposition ratio.