新产品编号:1818227
Chemical Name: 2(S)-Hydroxy-4-oxo-4-(paclitaxel-2'-O-yl)butyric acid sodium salt; [2aR,4S,4aS,6R,9S(2R,3S),11S,12S,12aR,12bS]-3-Benzamido-2-[4-carboxy-3(S)-hydroxypropanoyloxy]-3-phenylpropionic acid 6,12b-diacetoxy-12-(benzoyloxy)-4,11-dihydroxy-4a,8,13,13-tetramethyl-
项目整合开发状态: Preclinical
项目研究机构: Pharmachemie (Originator)
合成路线:Malic acid (I) was protected as the 1,2-O-isopropylidene derivative (II) upon treatment with acetone in the presence of acid catalyst.Condensation of (II) with paclitaxel (III) using diisopropylcarbodiimide and DMAP produced the 2'-ester (IV).After hydrolytic cleavage of the isopropylidene protecting group of (IV),conversion to the corresponding sodium carboxylate salt furnished the title compound.
📌 参考资料/链接：
参考文献标题:Water soluble analogs and prodrugs of paclitaxel
文献作者:Wiegerinck,P.H.G.; Scheeren,J.W.; Damen,E.W.P.; Sperling,D.; Braamer,L.; De Vos,D.(Pharmachemie BV)
参考来源:WO 0010988
📄 详细内容
合成路线:Malic acid (I) was protected as the 1,2-O-isopropylidene derivative (II) upon treatment with acetone in the presence of acid catalyst.Condensation of (II) with paclitaxel (III) using diisopropylcarbodiimide and DMAP produced the 2'-ester (IV).After hydrolytic cleavage of the isopropylidene protecting group of (IV),conversion to the corresponding sodium carboxylate salt furnished the title compound.
参考文献标题:Paclitaxel esters of malic acid as prodrugs with improved water solubility
文献作者:Damen,E.W.P.; Wiegerinck,P.H.G.; Braamer,L.; Sperling,D.; de Vos,D.; Scheren,H.W.
参考来源:Bioorg Med Chem 2000,8(2),427